Hoa Duoc 46

n thi l thuyt tng hp -T 3 lp C4K46 2015
Chuyn 1: THUC IU TR LAO
I I CNG V BNH :
1/ nh ngha.
- Lao l mt bnh truyn nhim do vi khun lao gy ra.
- Bnh c th biu hin cp tnh hay mn tnh.
2/ Nguyn nhn.
- Vi khun lao ngi (Mycobacterium tuberculosis) l chng ch yu gy ra bnh lao trn ton th gii,
cc vi khun khc thuc h Mycobacteria cng c th gy bnh lao nhng him gp
o Vi khun Mycobacterium tuberculosis c c im:
- Trc khun hnh que
- L vi khun hiu kh
- Khng cn khng acid, bt mu (gram dng) khi nhum Ziehl-Neelsen.
- Sinh sn chm, thi gian phn i l 15 22h, tn ti mi trng t 3-4 thng.
3/ C ch bnh sinh.
- trc khun ly truyn ch yu qua ng h hp do th, ht phi TK lao c trong nhng git nc nh
bn ra t ming, mi bnh nhn b bnh lao phi. Ngoi ra c th ly qua ng da, tiu ha.
- Bnh lao din bin qua 2 giai on:
+ Giai on nhim lao (lao s nhim)
+ Giai on lao th pht (bnh lao)
- Khong 10% lao s nhim chuyn thnh bnh lao do h thng min dch km, 90% cn li thng
khng c biu hin lm sng hoc c th t khi hon ton.
4/ Triu chng lao phi
4.1/ Triu chng lm sng:
- Bnh nhn gy st, mt mi, chn n.
- Ra m hi v m, st nh ko di v chiu.
- Ho ko di > 2 tun, c th ho khan hoc ho c m
- au ngc m
- Khm phi: khng c g c bit hoc c t ran n ri rc.
4.2/ Triu chng cn lm sng:
a/ Xt nghim tm VK lao trong m: l phng php c hiu nht
- Nhum soi trc tip theo phng php Ziehl-Neelsen, kt qa AFB (+)
- Nui cy trong mi trng Loeweinstein sau 8 tun c khun lc mc.
b/ Xt nghim mu:
- S lng v t l bch cu lympho tng.
- Tc mu lng tng cao
c/ Phn ng da vi tuberculin: Mantoux (+)
d/ X quang phi:
Cc tn thng a dng, thng gp cc m m nh v h n 1 hoc 2 bn phi.
Cc dng tn thng:
- Nt m - m thm nhim
- Hang lao - U lao
- Nt vi ha - Cc di x phi
5/ iu tr
5.1 Nguyn tc iu tr ( son theo HD v iu tr ca BYT)
a- Phi phi hp cc thuc chng lao:
Mi loi thuc chng lao c tc dng khc nhau trn vi khun lao (dit khun, km khun), do vy phi
phi hp t nht 3 loi thuc chng lao trong giai on tn cng v t nht 2 loi trong giai on duy tr.
b- Phi dng thuc ng liu v thi gian quy nh:
Cc thuc chng lao tc dng hp ng, mi thuc c mt nng tc dng nht nh. Nu dng liu
thp s khng hiu qu v d to ra cc chng vi khun khng thuc, nu dng liu cao d gy tai bin.
c- Phi dng thuc lin tc, u n:
Cc thuc chng lao phi c ung cng mt ln vo thi gian nht nh trong ngy v xa ba n
t hp thu thuc ti a.
d- Phi dng thuc thi gian quy nh - iu tr thng chia 2 giai on : giai on tn cng v
giai on duy tr
1
TI LIU THAM KHO
Giai on tn cng ko di 2, 3 thng nhm tiu dit nhanh s lng ln vi khun c trong cc vng
tn thng ngn chn cc t bin khng thuc. Giai on duy tr ko di 4 n 6 thng nhm tiu
dit trit cc vi khun lao trong vng tn thng trnh ti pht.
e- iu tr c kim sot:
Kim sot vic tun th iu tr ca ngi bnh, theo di kt qu xt nghim m, theo di din bin
lm sng, x tr kp thi cc bin chng ca bnh v tc dng ph ca thuc.
f- Ci thin ch dinh dng:
5.2 Phc iu tr
a) 5 thuc chng lao thit yu : Isoniazid (H), Rifampicin (R), Pyrazinamid (Z), Streptomycin (S) v
Ethambutol (E).
b) Ch nh v phc iu tr
Phc I: 2S (E)HRZ/6HE hoc 2S(E)RHZ/4RH (Ch p dng khi thc hin kim sot trc tip c giai
on duy tr).
- Hng dn:
+ Giai on tn cng ko di 2 thng, gm 4 loi thuc dng hng ngy, E c th thay th cho S.
+ Giai on duy tr ko di 6 thng gm 2 loi thuc l H v E dng hng ngy hoc 4 thng gm 2 loi
thuc R v H dng hng ngy.
- Ch nh: Cho cc trng hp ngi bnh lao mi (cha iu tr lao bao gi hoc tng iu tr lao
nhng di 1 thng).
Phc II: 2SHRZE/1HRZE/5H3 R3 E3
- Hng dn: Giai on tn cng ko di 3 thng, 2 thng u tin vi c 5 loi thuc chng lao thit yu
(SHRZE) dng hng ngy, 1 thng tip theo vi 4 loi thuc (HRZE) dng hng ngy. Giai on duy tr
ko di 5 thng vi 3 loi thuc H, R v E dng 3 ln mt tun.
- Ch nh: Cho cc trng hp ngi bnh lao ti pht, tht bi phc I, iu tr li sau b tr, mt s
th lao nng v phn loi khc (phn phn loi theo tin s iu tr).
Phc III: 2HRZE/4HR hoc 2HRZ/4HR
- Hng dn: Giai on tn cng ko di 2 thng, gm 4 loi thuc (HRZE) hoc 3 loi thuc (HRZ)
dng hng ngy, iu tr cho tt c cc th lao tr em. Giai on duy tr ko di 4 thng gm 2 loi thuc
l H v R dng hng ngy.
- Ch nh: Cho tt c cc th lao tr em. Trong trng hp lao tr em th nng c th cn nhc dng
phi hp vi S.
6/ Phng bnh
Phng bnh lao l p dng cc bin php nhm:
Gim nguy c nhim vi khun lao:
- Kim sot v sinh mi trng:
- S dng phng tin phng h c nhn
- Gim tip xc ngun ly
Gim nguy c chuyn t nhim lao sang bnh lao.
- Tim vc xin BCG nhm gip cho c th hnh thnh min dch chng li bnh lao khi b nhim lao
- iu tr d phng lao bng INH cho bnh nhn nhim HIV.
II A CNG V NHM THUC:

Thuc nhm 1: tc dng mnh, t tc dng ph. Gm: isoniazid, rifampicin, pyrazinamid, ethambutol,
streptomycin.
Thuc nhm 2: tc dng km nhm 1, nhiu tc dng ph. Dng khi bnh nhn khng dung np thuc
nhm 1 hoc khng p ng thuc nhm 1. Gm: kanamycin, amikacin, capreomycin, ethionamid, PAS,
cycloserin.
III- C C THUC C TH:
1. ISONIAZID O
Tn khoa hc: Hydrazid ca acid isonicotinic (Isonicotinohydrazid) NH2

Tn khc: INH N
H
1/ Ngun gc: Tng hp.
2/ iu ch: N
- Cho Hydrazin tc dng vi Methyl isonicotinat isoniazid :
2
TI LIU THAM KHO
O O
CH3 NH2
O N
H2N NH2 H
+
N N
3/ Tnh cht:
a. L tnh:
- Cm quan: Bt kt tinh trng, khng mi.
- tan: + D tan trong nc + t tan trong Bromoform + Rt kh tan trong Ether
- Hp th UV
- IR c trng ???? ( hi thy xem c IR ko?)
b.Ha tnh:
- P/ ca nhn Pyridin: tnh base :
+ un vi Na2CO3 pyridin (mi c bit).
+ DD ch phm trong ethanol T/d vi 1-cloro-2,4-dinitrobenzen trong mi trng kim to mu c
trng: nu
- P/ ca nhm Hydrazin:Tnh kh, acid v ngng t:
+ Tc dng AgNO3 to ta trng, un nng en
H O
INH + 4AgNO3 2 4 Ag+ + N2 + 4 HNO3 +
+ DD ch phm trong nc tc dng vi dd CuSO4 to mu xanh da tri v c ta. un nng dd

chuyn sang mu xanh ngc thch v c bt kh bay ra.
+ DD ch phm trong ethanol tc dng vi vanilin v un nng to ta vng.
4/ im nghim.
a. nh tnh:
+ Cm quan tan : Bt kt tinh trng, khng mi. D tan trong nc, t tan trong Bromoform, Rt kh
tan trong Ether
+ o ph hng ngoi so vi cht chun.
+ nh tnh bng pp sc k lp mng so snh vi INH chun
+ o nng chy Tnc 170 174oC
+ Bng cc phn ng ha hc : ( nh trong phn ha tnh)
To ta vng vi Vanilin: Ho tan 0,1 g ch phm trong 2 ml nc, thm dung dch nng ca 0,10 g
vanilin (TT) trong 10 ml nc, yn v c thnh ng nghim bng mt a thu tinh, s c ta vng
b. nh lng:
+ Bng PP o quang hoc HPLC
+ Bng pp o acid trong mi trng khan : ha tan / CH3COOH; nh lng = 1 acid mnh HClO4 0,1M;
pht hin im tng ng = cch o th or ch th mu.
+ Bng phng php o Iod: nguyn tc:
Kh I2 thnh I-
nh lng I2 d bng dd Na2S2O3 vi ch th h tinh bt. nh lng n khi xut hin mu vng rm
+ Bng pp o Brom : cht chun l dd brom chun hoc dd KBr chun. lng Brom d c xc nh =
pp o Nitrit.
5/ Dc ng hc.
- Hp thu: tt qua ung, tim v trc trng. Thc n lm chm hp thu v gim sinh kh dng isoniazid
- Phn b: vo tt c cc c quan, cc m v dch c th, phn b cao dch mng phi, mng bng,
hot dch, dch no ty, huyt tng. Thuc thm c vo hang lao, d dng qua nhau thai v vo thai
nhi
- Chuyn ha: chuyn ha gan bng phn ng acetyl ha, tc p/ng acetyl ha ph thuc vo yu
t di truyn.
- Thi tr : Xp x 75 - 95% thuc thi tr qua thn trong vng 24 gi di dng cht chuyn ha khng
hot tnh. Mt lng nh thi qua phn. Thuc c th c loi khi mu bng thm phn thn nhn to
hay thm phn mng bng.
6/ Tc dng v c ch tc dng .
a. Tc dng:
+ Tc dng km khun v dit khun
+ Nng /ch ti thiu i vi trc khun lao l 0,025- 0,05 g / ml
+ Thuc tc dng tt vi mi dng lao c trong v ngoi phi, c th cp v mn tnh.
3
TI LIU THAM KHO
b. C ch tc dng:
+ c ch tng hp a. Mycolic l thnh phn ch yu to nn lp v phospholipid ca trc khun lao.
V acid Mycolic ch c VK lao, nn thuc c hiu vi trc khun lao.
+ INH to phc chelat vi ng v c ch cnh tranh vi Nicotinamid v Pyridoxin lm ri lon chuyn
ha ca VK lao.
7/ Ch nh. Phng v iu tr mi th lao trong v ngoi phi, cp v mn tnh.
8/ Tc dng MM.
i vi gan: Vim gan, hoi t t bo gan. c tnh gan tng khi dng ng thi vi cc thuc c
vi gan nh: Rifampicin, Pyrazinamid, ru
Hn ch = cch phi hp vi thuc bo v gan trong time dng thuc, theo di ASAT, ALAT
TKT: co git, RLTT hng cm, mt ng, tng cn ng kinh
TK ngoi bin: vim, au c
Hn ch = cch b sung thm vitamin B6 trong thi gian iu tr.
D ng: st, pht ban, tan huyt, thiu mu, gim BC ht, gim tiu cu
RLTH : Bun nn, nn, a chy, au vng thng v
9/ Chng ch nh.
- ng kinh, ri lon tm thn hng cm.
- Bnh gan, thn nng.
- Mn cm vi thuc.
10/ Ch phm v liu dng.
a. Ch phm: Bit dc: Rimifon, INH, Nydrazid
Vin nn 50, 100, 150mg. Dng ng tim 500mg/ 5ml
b. Liu dng:
+ Liu tn cng: 5mg/ kg/ 24h; ti a 300mg/ 24h.
+ Liu duy tr: 10mg/ kg/ 1ln x 3 ln/ 1 tun.
15mg/ kg/ 1 ln x 2 ln/ 1 tun.
11/ Tng tc thuc.
- INH gy cm ng enzym chuyn ha thuc microsom gan P450 v vy Khi dng kt hp isoniazid vi
cc thuc ny c th lm tng nng trong huyt thanh v lm tng c tnh ca thuc phi hp, nht
l cc thuc cha ng kinh. Cc thuc sau y khi phi hp vi isoniazid phi iu chnh liu: alfentanil,
cc cht chng ng mu dn cht coumarin hoc dn cht indandion, cc benzodiazepin,
carbamazepin, theophylin, phenytoin, enfluran, disulfiram v cycloserin.
- Dng ng thi rifampicin, acetaminophen hoc ru vi isoniazid c th lm tng c tnh vi gan,
c bit ngi c tin s suy gan.
- Dng ng thi isoniazid vi niridazol c th lm tng tc dng khng mong mun i vi h thn
kinh, nh co git v ri lon tm thn.
- Isoniazid lm gim nng ketoconazol trong huyt thanh, v vy lm gim tc dng iu tr nm ca
thuc ny.
- Cc corticoid lm tng thi tr isoniazid, v vy lm gim nng v tc dng ca isoniazid, c bit
nhng ngi bnh chuyn ha isoniazid nhanh.
- Cc thuc khng acid, c bit mui nhm lm gim hp thu isoniazid. V vy 2 thuc ny cn phi
ung cch nhau t nht 1 gi.
12. Bo ch ............??????
2. RIFAMPICIN
Tn KH : 1-methyleamino-4-methylpiperazin
Cng thc: C43H58N4O12 PTL: 822,95
1/ Ngun gc:
L khng sinh bn tng hp t cc KS thin nhin
rifamycin, cc rifamycin thin nhin c chit xut t
Streptomyces mediterranei
2/ Tnh cht l ha:
- Bt kt tinh mu cam hoc nu. Ko bn khi b m
- tan: Rt d tan trong Cloroform, tan/ MeOH, t tan/
H2O, Ether
- Hp th UV, IR c trng
- C gc quay cc
- Dng dd khng bn, d b oxy ha, bin i theo pH v To :
4
TI LIU THAM KHO
+ pH kim: d b oxy ha bi O2 to ra Quinon.

+ pH acid: d b thy phn 3 formyl Rifampicin SV.
+ pH trung tnh: cc chc ester cng b thy phn nhng chm.
3/ im nghim.
a. nh tnh:
- o UV
- o gc quay cc
- o ph hp th t ngoi so vi cht chun.
- nh tnh bng pp sc k lp mng so snh vi rifampycin chun
- Tc dng vi Amonipersulfat trong m pH 7,4 s chuyn sang mu tm.
b. nh lng:
- HPLC
- PP o quang.
4/ Dc ng hc.
a. Hp thu + Hp thu tt qua ng tiu ha, SKD > 90%. Thc n lm gim hp thu thuc
+ t Cmax / mu sau 2-4 h. Duy tr tc dng 8-12 h.
b. Phn b: phn b rng ri vo cc m v dch c th, c bit vo phi v dch ph qun. Thuc qua
c nhau thai, sa m v dch no ty khi mng no b vim
c. Chuyn ha: Chuyn ha gan bng phn ng Acetyl ha
d. Thi tr: 65% qua phn, 30% qua nc tiu, phn cn li tha qua m hi, nc mt. sp thi tr c
mu . T1/2 l 3-5 h.
5/ Tc dng v c ch.
a. Tc dng:
- Tc dng tt i vi chng vi khun M.tuberculosis v M.laprae.
- Tc dng c vi VK c hi: M.bovis, M.avium.
- L KS ph rng: tc dng trn VK Gr (+) v Gr (-) nh lu cu, no m cu, lin cu, k c chng
khng Methicillin (tr cu khun ng rut )
b. C ch:
- Rifampicin gn vo tiu n v ca ARN- polymerase, lm sai lch thng tin ca enzym ny c ch
s khi u ca qu trnh tng hp ARN mi. thuc c t/dng dit khun.
- Trn ngi, ARN- polymerase t nhy cm vi thuc nn t c tr khi dng liu rt cao
- VK khng Rifampicin l do s thay i cu trc tiu n v ca ARN- polymerase.
6/ Ch nh.
- iu tr mi dng lao: s nhim, th pht, cp v mn tnh(phi hp thuc khc theo phc )
- iu tri bnh phong (phi hp thuc khc theo phc )
- Phng v iu tr vim mng no do H. influenzae v N. meningitidis.
- iu tr nhim khun nng do Staphylococcus khng Methicillin.
7/ Tc dng MM:
- Vim gan, nht l trn ngi c tin s bnh gan, ngi nghin ru, cao tui hoc khi phi hp vi
thuc cng gy c vi gan nh INH
- RLTH: nn, bun nn
- Ri lon chuyn ha porphyrin
- Ngoi ra cn : au u, mt mi, thiu mu, ban da, gim tiu cu, hi chng gi cm khi dng ch
ngt qung 2 ln/ tun
8/ Chng ch nh:
- Suy gan nng, ri lon chuyn ha porphyrin, ngi mn cm vi thuc.
- Thn trng vi ngi mang thai, nht l 3 thng cui, v d gy xut huyt.
a. Ch phm:
+ Vin nang 150, 300, 500mg.
+ Hn dch 1% l 120ml ung, l bt pha tim 300, 600mg (tim tnh mch)
b. Liu dng: iu tr lao :
+ Giai on tn cng: 10mg/ kg/ 24h, ti a 600mg/ 24 h dng hng ngy.
+ Giai on duy tr: 10mg/ kg /24h x 2-3ln/ tun.
10/ Tng tc thuc.
- Rifampicin gy cm ng enzym chuyn ha thuc microsom gan P450 nn lm gim tc dng 1 s
thuc khi dng ng thi:
+ Cc thuc khng c dng ng thi: thuc chn knh Calci nh Nifedipin, Nimodipin
+ Cc thuc phi iu chnh liu khi kt hp: vin ung trnh thai, Digoxin, Diazepam, dicoumarin,
macrolid 14 carbon, phenytoin, theophylin
5
TI LIU THAM KHO
- Cc thuc lm gim hp thu Rifampicin nh cc antacid, bentonid, khc phc bng cch ung cch
nhau t nht 2h.
11. Bo ch : ( tham kho thi LTTH 2009)
Nang cng Rifampicin c cng thc sau ;
Rifampicin 300mg
Licatab 120mg
Lactose 70mg
Magnesi stearat 5mg
Talc 5mg
a) Phn tch vai tr cc thnh phn
b) M t trnh t bo ch v nhng lu trong qu trnh bo ch
c) Trnh by nhng ni dung cn thit ca nhn in trc tip trn v 10 vin nang Rifampicin 300mg
v v minh ha
Gii :
a) Phn tch vai tr cc thnh phn
- Rifampicin l dc cht, mu , t tan trong nc, kch ng da v nim mc
- Licatab: l tinh bt bin tnh, ng vai tr l t dc n, r, iu ho s chy
- Lactose l t dc n, to knh khuych tn
- Magnesi stearat-Talc l hn hp t dc trn iu ho s chy
b) M t trnh t bo ch v nhng lu trong qu trnh bo ch
- Trn bt kp Lactose-Licatab
- Thm Rifampicin trn u (trong thit b kn)
- Thm hn hp Magnesi-Stearat-Talc trn u
- ng nang trn my ng nang thch hp
- Ch khi bo ch: Ngi pha ch cn eo gng tay, khu trang trnh kch ng, Trnh m
c) Trnh by nhng ni dung cn thit ca nhn in trc tip trn v 10 vin nang Rifampicin 300mg
v v minh ha
- Tn v a ch c s sn xut: l tn y ca c s sn xut c ghi trong cc vn bn php l
lin quan n vic thnh lp c s sn xut . Tn nh sn xut c th vit tt nhng phi m bo
nhn din c tn nh sn xut, khng c dng tn giao dch thay th.
- Tn thuc km theo hm lng.
- S l sn xut do c s sn xut quy nh. Trng hp cu trc ca s l sn xut khng th hin
c ngy sn xut, c s sn xut phi ghi thm ngy sn xut
- C hn dng.
- V minh ha
CHUYN 2 : THUC H ST GIM AU CHNG VIM

I- I CNG V BNH:
1/ nh ngha:
+ St: - Nhit c th ngi lun hng nh mc 37oC, thn nhit lun gi n nh nh s iu ha
gia qu trnh sinh nhit v mt nhit.
- St l phn ng t nhin bo v c th khi c tc nhn gy bnh ngoi mi trng xm nhp
hoc do nhng bt thng trong c th sinh ra.
- St l trng thi tng thn nhit do trung tm iu ha thn nhit b ri lon bi cc tc nhn gy bnh,
thng gp nht l nhim khun.
+ au: l c ch t v ca c th chng li nhng kch thch c hi, l mt biu hin v cm gic v
cm xc, lin quan n tn thng c tht hoc tn thng tim tng ca c th.
2/ Nguyn tc iu tr: c 4 nguyn tc sau (Thuc gim au ngoi vi )
- La chn thuc ph hp vi ngi bnh.
- Trnh vt qu mc liu gii hn.
- Tn trng nguyn tc phi hp thuc.
- Lu cc bin php h tr khng dng thuc hoc dng thuc gim tc dng KMM
II- I CNG V NHM THUC:
1/ Phn loi thuc h st, gim au, chng vim :
6
TI LIU THAM KHO
DN CHT THUC C TH T C DNG

Acid Salicylic Acid acetylsalicylic, Methylsalicylat
Pyrazolon Phenylbutazol, Noramidopyrin
Indol Indomethacin, Sulindac
Oxicam Piroxicam, Tenoxicam, Meloxicam
Acid Propionic Ibuprofen, Ketoprofen, Naproxen, Fenoprofen
Acid Phenylacetic Diclofenac
Acid Fenamic Acid Mefenamic, Acid Meclofenamic H st, gim au,
chng vim
Nhm Coxib Celecoxib, Rofecoxib, Valdecoxib
Nhm Aminophenol Acetaminophen H st, gim au
(dn cht Anilin)
Acid Floctafenic Floctafenin Gim au.
2/ Tc dng v c ch.
a) Tc dng h st
- Tc dng : thuc h st co bt k nguyn nhn no v ch c tc dng iu tr triu chng, ko h thn
nhit ngi ko st.
- C ch h st : cht gy st ngoi lai kch thch bch cu SX cht gy st ni ti, hot ha
prostaglandin synthetase lm tng tng hp PGE1 v PGE2 t acid arachidonic vng di i gy mt
cn bng c ch iu nhit gy nn st. thuc c ch prostaglandin synthetase lm gim tng hp PGE1
v PGE2, c ch qu trnh sinh nhit, tng cng qu trnh thi nhit lm h st
b) Tc dng gim au
- Tc dng : gim au t nh n va, gim au ngoi vi, tc dng tt vi vi cc loi au do vim.
Khc vi nhm opiate, thuc nhm ny ko c t/dng gim au mnh, ko gim au su trong ni tng, ko
gy c ch h hp, ko gy l thuc thuc khi dng ko di.
- C ch gim au: thuc gim tng hp PGF2 lm gim tnh cm th ca ngc dy thn kinh cm gic
vi cc cht gy au ca phn ng vim nh bradykinin, serotonin
c) Tc dng chng vim
- Tc dng : c 2 loi COX: COX 1 cn cho tc dng sinh l ca 1 s c quan (d dy, tiu cu,
thn), COX 2 c vai tr to prostaglandin gy vim. Mt s thuc c ch chn lc COX 2 t nh
hng ti chc nng sinh l bnh thng , gim tc dng KMM
- C ch chng vim : cc thuc chng vim c ch enzyme cyclooxygenase (COX), ngn cn tng
hp prostaglandin l cht trung gian ha hc gy vim, lm gim qu trnh vim
3/ Tc dng MM.
Trn tiu ha: kch ng, au thng v, nng hn l lot DDTT, xut huyt tiu ha
Trn mu: Ko di thi gian ng mu mt mu ko nhn thy qua phn, tng nguy c chy mu.
Trn thn: Gim lu lng mu qua thn, gim sc lc cu thn, gim thi lm nc, tng kali mu
v vim thn k
Trn h hp: gy co tht ph qun gy cn hen gi trn ngi ko b hen hoc lm tng cn hen
ngi hen ph qun
Cc tc dng MM khc.
- Mn cm: ban, m ay, shock qu mn.
- Gy c vi gan.
- d tt thai nhi nu dng thuc trong 3 thng u, ko di thi k mang thai v chuyn d, d xut huyt
khi sinh..
4/ Ch nh chung.
- Gim au mc nh v trung bnh, nht l au do vim.
- H st do mi nguyn nhn gy st.
- Chng vim cp v mn tnh.
III- THUC C TH :
1 . ASPIRIN
Tn khoa hc: Acid 2 acethoxy benzoic
Tn khc: Aspirin
7
TI LIU THAM KHO
COOH
OCOCH3
1/ iu ch :
Ester ha nhm OH ca acid salicylic bng anhydrid acetic vi xc tc l acid sulfuric c hoc pyridin:
COOH COOH
OH CH3 CO OCOCH3
H2SO4
+ O + CH3COOH
CH3 CO
2/ Tnh cht.
a) L tnh :
- Bt kt tinh mu trng, tinh th khng mu
- tan:
+ Kh tan trong nc
+D tan trong EtOH 96%, Tan trong ether, cloroform, cc dung dch kim
+ tan trong cc dd kim v mui carbonat kim (do c nhm acid)
- Hp th UV
- IR c trng
- Dung dch / H2O lm giy qy xanh v ko cho mu vi thuc th FeCl3 v ko cn nhm OH phenolic
t do
b) Ha tnh :
- Thy phn to acid salycylic v acid cetic
Acid salicylic: tc dng vi FeCl3 tm

Acid acetic:
3/ im nghim.
a. nh tnh:
- Thy phn chc ester bng NaOH, sau ngui, acid ha dd cho ta a.salicylic, lc tch ta v
dch lc.
+ Phn ta ra sch, thm FeCl3 mu tm.
+ Phn dch lc em trung tnh bng CaCO3 sau thm FeCl3 mu hng.
b. tinh khit:
- Ch phm khng c c mi dm.
- Th gii hn a.salicylic t do: ng tc dng mui Fe3+ (thng dng phn st amoni ) mu tm xut
hin trong dung dch th khng c m hn dung dch mu.
c. nh lng:
+ Dng PP o quang hay HPLC
+ Dng phng php acid base.
- Trung ha chc acid bng NaOH 0,1N vi ch th phenolphtalein / EtOH, trong iu kin T o thp v thao
tc nhanh trnh phn hy chc ester.
- cho ch phm tc dng vi 1 lng kim d thy phn chc ester, sau nh lng kim d bng
acid chun. (pp tha tr)
4/ Dc ng hc.
a. Hp thu:
8
TI LIU THAM KHO
- Hp thu tt qua ng tiu ha.

- Ung sau 2h t Cmax , pht huy tc dng sau 30 pht, duy tr tc dng trong 4h.
b. Phn b:
- Lin kt vi protein huyt tng 70 80%
- Phn b ti hu ht cc m, qua c hng ro mu no v rau thai.
c. Chuyn ha v thi tr :
- Chuyn ha qua gan.
- Thi tr qua nc tiu dng chuyn ha.
- Thi gian bn thi T1/2 = 6h.
5/ Tc dng v c ch.
Tc dng: Ph thuc liu dng
- Liu cao > 4g / 24h : chng vim
- Liu trung bnh : h st, gim au.
- Liu thp (70 320mg) : chng kt tp tiu cu v ko di thi gian ng mu dng lm thuc d
phng huyt khi.
- Tc dng thi tr a.uric
+ Liu < 1 2g / 24h: gim thi tr a.uric qua thn.
+ Liu > 2g / 24h: tng thi tr a.uric qua thn.
C ch:
- C ch h st : cht gy st ngoi lai kch thch bch cu SX cht gy st ni ti, hot ha
cn bng c ch iu nhit gy nn st. thuc c ch prostaglandin synthetase lm gim tng hp PGE 1
- C ch gim au: thuc gim tng hp PGF2 lm gim tnh cm th ca ngc dy thn kinh cm gic
- C ch chng vim : cc thuc chng vim c ch enzyme cyclooxygenase (COX), ngn cn tng
hp prostaglandin l cht trung gian ha hc gy vim, lm gim qu trnh vim
6/ Ch nh.
- H st: do mi nguyn nhn, tr st xut huyt v st do virus. Khng dng cho TE di 12 tui v d
gp h chng Reye.
- Chng vim: cc trng hp vim nh nh vim xng khp, vim c, vim khp dng thp
- Gim au: dng trong cc trng hp au nh v va nh au u, au c, au khp..
- D phng th pht nhi mu c tim v t qu
7/ Tc dng MM.
- Mn cm: D ng, m ay, ph Quink, shock phn v
- Gy kch ng ng tiu ha: lot da dy, xut huyt tiu ha
- D gy chy mu nht l ngi c c a chy mu hay ang dng thuc chng ng.
- Co tht ph qun, gy hen.
- tng HA, ph. Khi dng liu cao, ko di gy tai, chng mt.
- Vi ngi c thai: c ch co bp t cung ko di thi gian chuyn d, tng nguy c chy mu c
m v thai nhi
- Liu c gy ri lon kim toan, ri lon h hp.
8/ Chng ch nh.
- Mn cm - Lot d dy t trng, xut huyt tiu ha
- R lon ng mu - Thiu men G6PD
- St do virus - Hen ph qun
- Bnh gan nng - Ph n c thai
a. Ch phm: Vin nn, vin bao tan trong rut 100, 320, 500, 600mg
- Vin si 320, 500mg
- Gi bt 80 300mg
- Dng tim: l 500mg
b. Liu lng:
- Chng vim: 3-6g / 24h
- H st, gim au: 0,5 2g /24h
- D phng huyt khi: 100-150mg /24h dng hng ngy hoc cch ngy.
10/ Tngtc thuc.
Do cnh tranh lin kt vi Protein huyt tng tng tc dng v c tnh ca mt s thuc nh
Warfarin, Phenytoin, Thiopentan iu chnh liu khi kt hp cc thuc ny.
9
TI LIU THAM KHO
Gim thi tr a.uric qua thn gim td ca mt s thuc: Probenecid, Sulfinpyrazon khng dng
cho bnh nhn vim khp do gout.
11/ bo ch : ?????
2. PARACETAMOL
NHCOCH3
OH
- Tn khoa hc: N-(4- hydroxyphenyl ) acetamid
- Tn khc: Acetaminophen
- Bit dc: Panadol, Efferalgan
1/ Ngun gc.
iu ch bng pp tng hp ha hc:
S iu ch :
NO2 NH2 NHCOCH3

CH3 CO
+ O
+ H2 CH3 CO +
CH3COOH
CH3COOH
OH OH OH
P. Nitrophenol P. Aminophenol Paracetamol
2/ Tnh cht.
a. L tnh:
- Bt kt tinh mu trng, ko mi, v ng nh
- tan: hi tan trong nc, tan nhiu hn trong nc si, rt kh tan trong chloroform, ether, tan trong
ethanol v cc dd kim
Dd bo ha trong nc c pH khong 5,3 5,6. pKa = 9,51
- hp th UV, IR c trng
b. Ha tnh:
- Nhm OH phenol : tc dng vi dd mui FeCl3 cho mu tm
- Nhm Acetamid:
Thy phn = dd HCl , thm Kalibicromat c mu tm
Thy phn = dd HCl, dch thy phn cho phn ng to phm mu Nit
- Nhn thm: hp th nh sng t ngoi, ng dng nh tnh, nh lng
- un nng vi acid sulfuric c mi acid acetic
3/ im nghim.
a. nh tnh:
- Nhm OH phenol c tnh acid + FeCl3 cho mu tm.
- Ch phm + HCL To P.aminophenol + K2Cr2O7 ta mu tm.
- Ch phm + H2SO4 To c mi a. acetic.

- o ph hng ngoi, so snh vi cht chun
- SKLM
b. nh lng: ( ch cn nu 1 trong cc pp sau: )
- Phng php o Nit: v c ha gii phng N di dng NH3, cho cht ny tc dng vi H2SO4 d,
nh lng acid d bng NaOH 0,1 N
- Thy phn ch phm bng acid ri nh lng P.aminophenol = php o Nitrit hoc nh lng = ceri IV
10
TI LIU THAM KHO
- PP o quang : o UV trong mi trng MetOH hoc kim

- PP HPLC
4/ Dc ng hc.
Hp thu: Nhanh v gn nh hon ton qua ng tiu ha, t nng ti a sau khi ung 30 - 60 pht.
Phn b: Phn b nhanh ti hu ht cc m trong c th. Lin kt vi protein huyt tng khang 25%
- Chuyn ha gan ( oxy ha bi Cyt P450 to N-acetyl benzoquinonimin l cht trung gian. Cht ny
lin hp vi Glutathion to cht khng cn hot tnh.
- Thi tr qua nc tiu dng chuyn ha. T1/2 l 2,5h.
5/ Tc dng v c ch.
- Gim au, h st, khng c tc dng chng vim.
- H st do mi nguyn nhn gy st, khng h nhit ngi bnh thng.
- liu iu tr, t tc dng ph.
- C ch :
C ch h st : cht gy st ngoi lai kch thch bch cu SX cht gy st ni ti, hot ha
cn bng c ch iu nhit gy nn st. thuc c ch prostaglandin synthetase lm gim tng hp PGE1
C ch gim au: thuc gim tng hp PGF2 lm gim tnh cm th ca ngc dy thn kinh cm gic
6/ Ch nh.
- Gim au do cc cn au ngoi vi t au nh n trung bnh: au u, au rng, au bng kinh
- H st do mi nguyn nhn ( k c trng hp CC vi Aspirin v NSAIDS)
7/ Tc dng MM.
- Mn cm vi thuc: ban da, my ay, bun nn, nn
- c tnh vi gan, thn khi dng liu cao ko di
X tr:
- Cho bnh nhn ung tin cht ca Glutathion l Methionin hoc Acetyl cystein cng sm cng tt.
- Nu x tr chm sau 36h, gan b tn thng v rt kh hi phc.
8/ Chng ch nh.
- Mn cm vi thuc - Thiu men G6PD.
- Bnh gan - Khng phi hp vi thuc gy c gan: INH, Rifampicin
- Khng ung ru khi dng thuc.
- Ch phm: vin nn, vin si, cm, n, gi bt 80 650mg
- Liu: ngi ln v TE > 11 tui 500mg / ln x 3-4 ln / ngy.
TE < 11 tui 80 500mg / ln c 4 6h dng 1 ln.
10/ Bo ch : tham kho thi tt nghip LTTH ln 2 2010
Cho cng thc vin nn ( 1 vin)
Paracetamol 500mg
Tinh bt m 90mg
Avicel (cellulose vi tinh th) 75mg
H tinh bt 10% va
Natri croscarmellose 25mg
Magnesi stearat 4mg
Talc 6mg
a) Nu vai tr cc t dc trong cng thc
b) Trnh by quy trnh bo ch vin nn trn
c) Trnh by nhng ni dung bt buc phi c trn nhn ca v thuc cha 10 vin nn
paracetamol 500mg
Gii :
a) Nu vai tr cc t dc trong cng thc
- Tinh bt m: t dc n, r
- Avicel (cellulose vi tinh th) : t dc r, n, c kh nng chu nn tt
- H tinh bt 10% : t dc dnh lng, t nh hng n thi gian r ca vin
- Natri croscarmellose: t dc siu r
- Magnesi stearat , Talc: t dc trn ( nghin qua ry 180)
b) Trnh by quy trnh bo ch vin nn : vin c bo ch = pp xt ht t:
- Nghin ry dc cht, t dc n qua c ry thch hp (250)
- Nghin ry t dc trn qua ry 180
- Trn dc cht vi tinh bt, avicel theo nguyn tc ng lng
11
TI LIU THAM KHO
- Cho t t H tinh bt vo khi bt kp trn, nho thnh khi m

- Xt ht qua c ry thch hp. c th xt ht 2 ln
- Sy ht nhit 60 700C ti m t yu cu ( 2 4% )
- Sa ht, trn ht kh vi Natri croscarmellose, Magnesi stearat , Talc
- Dp vin vi b chy ci thch hp, iu chnh khi lng trung bnh vin v cng ca vin t yu
cu
- ng gi, dn nhn ng quy nh.
c) Trnh by nhng ni dung bt buc phi c trn nhn ca v thuc cha 10 vin nn
paracetamol 500mg
- Tn v a ch c s sn xut: l tn y ca c s sn xut c ghi trong cc vn bn php l
lin quan n vic thnh lp c s sn xut . Tn nh sn xut c th vit tt nhng phi m bo
nhn din c tn nh sn xut, khng c dng tn giao dch thay th.
- Tn thuc km theo hm lng : (Paracetamol 500mg)
- S l sn xut do c s sn xut quy nh. Trng hp cu trc ca s l sn xut khng th hin
c ngy sn xut, c s sn xut phi ghi thm ngy sn xut
- C hn dng; ghi thng v nm ht hn s dng, thng c th ghi = ch hoc s , nm c ghi = 2
s cui ca nm.
Chuyn 3: THUC GIM AU GY NGHIN
I- AI CNG V BNH:
1/ nh ngha:
- au l c ch t v ca c th chng li nhng kch thch c hi, l mt biu hin v cm gic v cm
xc, lin quan n tn thng c tht hoc tn thng tim tng ca c th.
2/ Nguyn nhn: au c th do nhiu nguyn nhn khc nhau:
- au do cm th : Gy ra do kch thch cc th th cm nhn au cn nguyn vn , do tn thng m,
c quan
- au do bnh l thn kinh: Gy ra do s tn thng cc dy thn kinh
3/ Nguyn tc iu tr:
C 4 nguyn tc s dng thuc gim au TW:
* Ch s dng trong trng hp au mc nng v va, khi nhm gim au ngoi vi khng hiu
lc.
* S dng n c hoc phi hp ty mc au.
* Thuc c dng u n c nng trong mu n nh vi au do ung th
* Lu vic dng cc bin php h tr v thuc gim tc dng khng mong mun.
II- I CNG V THUC:
1/ hi nim:
- Thuc gim au l thuc c tc dng lm gim hoc mt cm gic au m khng tc dng ln nguyn
nhn gy au, khng lm mt cm gic khc v khng lm mt thc.
2/ Tc dng v c ch chung ca thuc gim au TW:
- Tc dng c hiu trn Receptor opioid v b mt tc dng bi cc cht i khng l Naloxon v
Naltrexon.
- Tc dng gim au mnh, chn lc v su trong ni tng.
- C tc dng an thn gy ng.
- Gy c ch h hp.
- Gy sng khoi v gy nghin.
- C ch :
Tc dng trn receptor opioid (Receptor ): Opioid - receptor hot ha Gi c ch
adenylcyclase
Hot ha knh K+ (postsynaptic)
c ch knh Ca++ (presynaptic)
Ngoi ra: c ch gii phng ACh, NE, serotonin, glutamat & cht P
3/ Lin quan gia cu trc v tc dng:
- cc thuc trong nhm u c cu trc Nhn Phenanthren tng t morphin l cu trc quyt nh
tc dng gim au ca cc thuc.
12
TI LIU THAM KHO
- Khi thay i nhm OH C3 ; C6 trong phn t morphin th tc dng dc l v c tnh DH thay i

nh sau:
+ Methyl ha nhm OH C3: tc dng gim au gy nghin gim;tc dng gim ho tng ln; sinh
kh dng qua ng ung cng tng . vd: codein
+ Acetyl ha nhm OH C3 v / hoc C6 : thuc xm nhp qua hng ro mu no tt hn morphin;
t/dng gim au gy nghin tng. Vd: Heroin
+ Kh H ca OH C6 to nhm ceton hoc ester ha th : tc dng gim au v c tnh tng,
nhng thi gian tc dng li ngn. vd: Hydromorphon
- Thay CH3 C17 bng nhm allyl (- CH2-CH=CH2 ) th c Nalorphin tc dng i khng vi Morphin
4/ Phn loi: Da vo c ch tc dng chia thnh 3 nhm:
- Thuc ch vn trn Receptor opioid:
+ Cc Opioid t nhin : Morphin v dn xut: Morphin, Codein
+ Cc Opioid tng hp: Pethidin, Methadon
- Thuc ch vn - i khng hn hp v ch vn tng phn trn Receptor opioid: Pentazocin,
Nalorphin, butorphanol.
- Thuc i khng n thun trn Receptor opioid: Naloxon, Naltrexon.
5/ Tc dng MM:
- Cp: bun nn, nn, to bn, b tiu, c ch h hp, co ng t, hn m, tru tim mch t vong
X tr: Dng thuc i khng: Naloxon, naltrexon, atropin . Tng cng chc nng sng (duy tr h
hp, tun hon)
- Mn : Nghin thuc ; Cai thuc
X tr: Ngng thuc, dng methadon , Cch ly mi trng & tm l liu php
6/ Ch nh:
- Gim au: t au va n au nng: morphin, pethidin, fentanyl, Codein, Pentazocin,
- Lm thuc tin m: Morphin, Fentanyl
- Gim ho: Codein, Dextromethorphan
2
- tiu chy : Loperamid, diphenoxylat
HO 3 1
- Cai nghin : Methadon, Naloxon & naltrexon
4
11
III. THUC C TH : O
12 10 HCl 3H2O
13 9
14
THUC C NGUN GC HO5 DC:
15 17 N CH3
6 16
HO 8
1. MORPHIN
7
HYDROCLORID
Tn khoa hc: 3,6-dihydroxy-4,5-epoxy-7,8-dihydro-17-methyl morphinan HCL.
Bit dc: Epimor, Morphitec
1/ Ngun gc: Chit xut t nha cy thuc phin (Papaver somniferum h thuc phin Papaveraceae)
Phng php chit xut nh sau:
13
TI LIU THAM KHO
2/ Tnh cht.
a. L tnh:
- Bt kt tinh trng hnh kim, ko mu
- D thng hoa, d bin mu ngoi khng kh.
- tan: + Tan trong nc, glycerin, dung dch kim mnh.
+ Kh tan trong EtOH, khng tan trong Ether.
- Hp th UV mnh
- IR c trng, c gc quay cc ring
b. Ha tnh:
- Phn ng ca Nit bc 3 c t/cht ca Alcaloid cho phn ng vi thuc th chung ca alcaloid.
- Phn ng ca nhm - OH phenol c tnh acid
- Tnh kh
- Nhn thm hp th UV.
- Cho Phn ng ca ion Cl-
3/ im nghim.
a. nh tnh:
- o ph hng ngoi, so snh vi cht chun
- o gc quay cc
- Phn ng vi thuc th alcaloid:
+ Dragendoff ta da cam.
+ Marquis ta ta sau chuyn sang mu tm.
+ Frod c mu tm chuyn sang xanh.
- Vi nhm OH phenol:
+ Tc dng vi FeCl3 mu tm.
+ Tc dng vi mui Diazoni / OH- mu ca phm mu nit.
- Tnh kh: d b oxy ha
+ Tc dng vi K3 [ Fe(CN)6] / HCl Dehydrodimorphin + acid Ferocyanic, nu thm FeCl3 mu
xanh lam ph ca Ferocyanid feric (Codein khng cho P/ ny).
+ Tc dng vi KI gii phng Iod.
14
TI LIU THAM KHO
- Nhn thm: hp th UV
- Cho phn ng ca ion Cl- : tc dng vi AgNO3 kt ta trng
b. Th tp: cc tp cht lin quan xc nh bng SKLM.
c. nh Lng:
- nh lng PP o acid trong mi trng khan: ( ha tan / CH3COOH; nh lng = 1 acid mnh HClO4
0,1M; pht hin im tng ng = ch th tm tinh th
- nh lng HCl bng phng php o bc.
- nh lng bng pp o quang
- nh lng = pp HPLC
4/ Dc ng hc.
a. Hp thu:
- Qua ng: ung, tim, h hp trong ng tim hp thu nhanh v mnh hn.
- SKD ng ung thp khong 25%, v chuyn ha qua gan ln u ln.
b. Phn b:
- Lin kt Protein huyt tng khong 30%.
- Tp trung c vn, gan, phi, thn.
- Qua c hng ro mu no, nhau thai, sa m.
c. Chuyn ha v thi tr:
- Chuyn ha gan ch yu l lin hp vi a.glucoronic.
- Thi tr ch yu qua nc tiu, mt phn qua phn ( c chu k gan rut), T1/2 l 2-3h
5/ Tc dng v c ch t/dng.
Tc dng chn lc trn receptor . Liu cao c c t/dng trn cc receptor opioid khc. Tc dng thay i
theo liu, la tui, gii tnh, loituy nhin, tc dng chnh l c ch TKTW
a. Trn thn kinh TW
Tc dng gim au: Gim au mnh, gim au ni tng v chn lc ( chn lc trn trung tm au,
khng nh hng ti cm gic khc v khng mt thc).
+ C ch: Tc dng chn lc trn receptor gim gii phng cc cht dn truyn TK v lm tng
ngng chu au.
Tc dng an thn gy ng: Tc dng ny ch r khi dng liu thp hn liu gim au, v ch r ngi
cao tui. t gy bun ng ngi tr tui.
Tm thn: Gy cm gic sng khoi, m mng, tng tr tng tng. Mt cm gic i kht, bun
phin. Dng lu gy nghin.
b. Trn h hp:
+ Liu iu tr: c ch trung tm h hp, gim hot ng ca h h hp lm nhp th chm v su,
+ Liu cao: c ch mnh h hp ri lon h hp.
+ C ch gy c ch h hp : thuc lm gim p ng ca trung tm h hp i vi CO2 v c ch
trung tm h hp hnh no. Ngoi ra, thuc cn gy co tht c trn ph qun
- c ch trung tm ho v phn x ho gim ho.
c. Trn tun hon:
+ Liu iu tr: t nh hng.
+ Liu cao: chm nhp tim, gin mch, h huyt p.
d. Trn tiu ha:
+ Lm gim nhu ng d dy- rut, gim tit dch tiu ha to bn
+ Co c vng Oddi gy tng p lc ng mt ch.
e. Trn tit niu : thuc gy co c vng bng quang gy b tiu.
f. Tc dng khc:
+ D gy nn do kch thch trung tm nn.
+ H thn nhit do kch thch trung tm ta nhit.
+ Tng tit hormon tuyn yn.
+ Gim chuyn ha, gim oxy ha.
+ Kch thch trung tm dy III co ng t.
+ Gim tit dch, tng tit m hi.
6/ Ch nh:
15
TI LIU THAM KHO
- au nng hoc au khng p ng vi cc thuc gim au khc nh si mt, si thn, ung th

- Ph phi cp th nh hay va.
- Dng lm thuc tin m.
7/ Tc dng MM.
- Bun nn, nn, to bn.
- c ch h hp.
- Co ng t.
- c tnh cp: khi dng liu 0,05-0,06g , liu gy cht 0,1-0,15g
+ Triu chng: hn m, co dng t, suy h hp nng gin mch, suy h hp t vong.
+ X tr: dng cht i khng morphin nh Naloxon kt hp Atropin.
- c tnh mn: - Dng 2-3 tun lin tc quen thuc nghin
- Nu khng tip tc dng hi chng cai thuc.
X tr: + Cch ly vi mi trng gy nghin
+ Kt hp lao ng chn tay v vt l tr liu.
+ Dng cht i khng vi opiat.
8/ Chng ch nh.
- Suy h hp, HPQ.
- Chn thng no hoc tng p lc s no.
- Trng thi co git.
- Nhim c ru cp.
- ang dng cc IMAO.
- Tr em < 30 thng tui.
- Suy gan nng.
- au bng cp khng r nguyn nhn.
- Thn trng vi ngi gi v PNCT.
9/ Tng tc thuc.
- Vi cc thuc c ch TKTW khc : thuc an thn, gim au, gy ng lm tng tc dng c ch
TKTW ca morphin Khng dng kt hp.
- Vi cc IMAO try tim mch, hn m, c th t vong Khng c phi hp.
- Vin nn, vin nang 10-200mg.
- ng tim 10mg/ml ; 20mg/2ml,
Tim di da, tim bp:
- Ngi ln: 5-20mg x 2-4 ln / 24h.
- Tr em > 30 thng: 0,1-0,2mg / kg / ln.
Ung: 10mg/ln x 2-4 ln / 24h.
11/ Lin quan cu trc tc dng : ( nh phn i cng)
- Khi thay i nhm OH C3 ; C6 trong phn t morphin th tc dng dc l v c tnh DH thay i
nh sau:
+ Methyl ha nhm OH C3: tc dng gim au gy nghin gim;tc dng gim ho tng ln; sinh
kh dng qua ng ung cng tng . vd: codein
+ Acetyl ha nhm OH C3 v / hoc C6 : thuc xm nhp qua hng ro mu no tt hn morphin;
t/dng gim au gy nghin tng. Vd: Heroin
+ Kh H ca OH C6 to nhm ceton hoc ester ha th : tc dng gim au v c tnh tng,
nhng thi gian tc dng li ngn. vd: Hydromorphon
- Thay CH3 C17 bng nhm allyl (- CH2-CH=CH2 ) th c Nalorphin tc dng i khng vi Morphin
12/ Quy nh qun l thuc gy nghin: ????????
2. PETHIDIN HYDROCLORID
CH3
N
HCl
H5C6 COOC2H5
Tn khoa hc: N-methyl- 4-phenyl-4-carbethoxypiperidin hydroclorid.
Tn khc: Meperidin, Dolargan, Dolosal, Dolantin.
1/ Ngun gc.
16
TI LIU THAM KHO
- L cht c tng hp ha hc, iu ch t benzyl clorid.

NH( CH2 CH2 OH )2
C6H5 CH2 Cl C6H5 CH2 N( CH2 CH2 OH )2
( diethanolamin )
SOCl2 C2H5OH
C6H5 CH2 N( CH2 CH2 Cl )2
Thionylclorid H2SO4
CH3
N
H2 / Pt
C6H5 CH2 N COOC2H5 HCl
HCHO
C6H5
H5C6 COOC2H5
2/ Tnh cht.
a. L tnh:
- Bt kt tinh trng, khng mi.
- tan: + tan trong EtOH, nc
+ t tan trong ether, benzen
- Vng bn trong khng kh.
b. Ha tnh:
- Nhn piperidin.
- Nhn thm.
- Nhm chc ester v tnh cht ca phn t HCl.
3/ im nghim.
a. nh tnh:
- o IR so snh ph chun
- SKLM.
- un ch phm vi a.acetic v a. Sulfuric Ethyl acetat c mi thm c bit.
- Phn ng ca N bc 3 : p/ng vi cc TT chung ca alcaloid
- Ch phm / nc + a. picric ta ; ta ny c Tn / c 187-189oC.
- V c ha cho phn ng ca ion Cl- : Dd cho kt ta trng vi AgNO3
b. nh lng:
- PP o quang, HPLC
- nh lng bng phng php o acid trong mi trng a.acetic khan: : ( ha tan / CH3COOH; nh
lng = 1 acid mnh HClO4 0,1M; pht hin im tng ng = ch th tm tinh th
- nh lng HCl bng phng php o bc hoc pp trung ha
Phng php trung ha: ta alkaloid bng NaOH. Ha tan ta vo HCl 0,1N d. nh lng HCl d
bng NaOH 0,1N vi ch th phenolphtalein.
4/ Dc ng hc.
a. Hp thu:
- hp thu qua ng tiu ha tt hn Morphin, SKD 50%.
- Ung sau 1-2h t Cmax, duy tr tc dng trong 2 - 4h.
b. Phn b:
- Lin kt vi Protein huyt tng khong 60%.
c. Chuyn ha v thi tr:
- Chuyn ha gan to thnh Normeperidin c t1/2 ko di hn cht m.
- Thi tr qua nc tiu di dng chuyn ha, T1 / 2 = 3h.
5/ Tc dng v c ch.
- Trn thn kinh TW: Gim au km morphin 10 ln. liu gim au cng c tc dng gy sng khoi,
gy nghin v c ch trung tm h hp, nhng khng c tc dng gim ho.
- Trn tim mch: lm h huyt p do gim sc cn ngoi vi, gin mch theo c ch trung ng nhng
lm tng lu lng tim, tng nhp tim.
- Trn tiu ha: Gy to bn. Tng p lc ng mt.
6/ Ch nh.
- au nng hoc au khng p ng vi cc thuc gim au khc nh si mt, si thn, ung th
- Ph phi cp th nh hay va.
- Dng lm thuc tin m.
7/ Tc dng MM.
- Bun nn, nn,
17
TI LIU THAM KHO
- Gy to bn v b tiu nhng t hn morphin .

- c ch h hp.
- Co ng t.
- c tnh: khc vi morphin, c biu hin tng t ng c Atropin nh nhp tim nhanh, gin ng t,
kh ming, gy o gic, co git.
- Dng ko di s gy nghin.
8/ Chng ch nh.
- Nhp tim nhanh.
- Suy h hp, HPQ.
- Chn thng no hoc tng p lc s no.
- Trng thi co git.
- Nhim c ru cp.
- ang dng cc IMAO.
- Tr em < 30 thng tui.
- Suy gan nng.
- au bng cp khng r nguyn nhn.
- Thn trng vi ngi gi v PNCT.
9/ Ch phm, liu dng.
- Ch phm: vin nn 25mg, ng tim 100mg / 2ml
- Liu dng: 75 100mg / 24h.
CHUYN 4 : THUC LI TIU

I/ i cng nhm thuc
1/ nh ngha.
Thuc li tiu lm tng khi lng nc tiu ch yu bng cch lm tng thi tr Na+ v nc dch
ngoi bo gy li niu.
2/ Phn loi: Theo mc ch iu tr, phn thnh 2 nhm ln:
- Li niu gim Kali :
+ Thuc c ch Carbonic anhydrase ( CA ): Acetazolamid.
+ Li niu quai: Furosemid.
+ Li niu Thiazid: Hydroclorothiazid.
- Li niu gi K+ : Spironolacton, amilorid
- Ngoi ra cn c thuc Li niu thm thu: Manitol v ko gy ri lon ion
3/ C ch tc dng ca tng nhm :
a) Thuc li niu gim Kali mu :
Thuc c ch Carbonic anhydrase ( CA ):
- Trong t bo ng thn, enzyme CA xc tc cho vic gii phng ion H+ theo phn ng sau:
- Sau khi c gii phng, H+ s bi xut vo long ng thn v trao i vi Na+ c ti hp thu
- Khi enzyme CA b phong ta, lng H+ gim hoc ko c gii phng. V vy, Na+ gim or ko c
ti hp thu , thi tr ra ngoi nc tiu, ko theo nc nn li tiu
- Mt khc do s tranh chp bi xut gia H+ v K+ , khi thiu H+ th K+ tng thi tr v hn ch chuyn
NH3 thnh NH4+ . nh vy, thuc phong ta CA lm tng thi tr Na+ , K+, HCO3- , gim Kali mu v
gy nhim acid chuyn ha nu dng ko di
Thuc li tiu quai: v tr t/dng quai henle. t/dng li tiu nhanh mnh nhng thi gian t/dng
ngn
- Tc dng li tiu theo cc c ch sau:
+ - +
+ Phong ta c ch ng vn chuyn nhnh ln of quai Henle, lm tng thi tr Na , Cl , K ko theo
nc nn li tiu
+ Gin mch thn, tng lu lng mu qua thn, tng sc lc cu thn, phn phi li mu c li cho
cc vng su v thn. Khng ADH ti ng ln xa
+ Gin TM, gim mu phi, gim p sut tht tri
++ ++ ++ ++
+ Tng o thi Ca , Mg lm gim Ca , Mg mu
Thuc li niu thiazid :
- c ch ti hp thu Na+ v Cl- on pha long ca ng ln xa, theo c ch ng vn chuyn nh
nhnh ln of quai Henle
- Liu cao gy c ch enzym carbonic anhydrase (CA)
18
TI LIU THAM KHO
- Tng thi tr K+ theo 2 c ch :

o Thuc c ch CA, H+ gim thi tr nn K+ tng thi
o Do c ch ti hp thu Na+ nn nng Na+ tng cao ng ln xa, gy phn ng b tr tng thi K+
ko Na+ li.
b) Thuc li niu gi ali: c ch ti hp thu Na+ = c ch trao i vi K+ v th gim thi tr K+ . tng
thi Na+ ko theo nc nn li tiu. hiu lc li tiu yu v gy tng K + nn thng phi hp vi
thuc li tiu gim Kali mu gi c t/dng ca thuc v khc phc tng K+ mu.
c) Thuc li niu thm thu: cc thuc trong nhm ny c lc t do qua cu thn, t hp thu qua ng
thn do phn t lng ln, lm tng p lc thm thu ng thn nn ko theo nc trong lng ng
gy li tiu
II/ THUC C TH:
1. FUROSEMID
H
Cl N CH2
O
H2NO2S COOH
Tn khoa hc: Acid-4-chloro-5-sulfamoyl-2-[ (2-furanylmethyl )amino] benzoic.

Tn khc: Frusemid,
1/ Ngun gc.
- Tng hp ha hc: un acid 2,4 diclorobenzoic + a. clorosulfonic cho tc dng vi NH3 un
hi lu vi Furfurylamin ( d nhiu ) / NaHCO3 Furosemid th kt tinh li t EtOH long Furosemid
( xem pt iu ch sgk ha dc 1 trang 221)
2/ Tnh cht.
a. L tnh:
- Bt kt tinh trng hoc hu nh trng, khng mi, khng v.
- Ko bn vi nh sng, nhng bn vng ngoi khng kh.
- Ton/c = 210oC
- tan: + Khng tan trong nc, kh tan trong ether, hi tan trong EtOH.
+ Tan trong aceton, MeOH, dd kim long.
+ Rt d tan trong dimethylformamid.
b. Ha tnh:
- Nhm Carboxylic
- Nhm sulfonamid
- Nhm amin thm.
- Nhn thm.
- Ion Cl-
3/ im nghim.
a. nh tnh:
- o ph t ngoi, so snh ph chun
- SKLM
- Nhm acid carboxylic:
+ Furosemid tan/cc dd kim do to mui vi KL kim.
+ Thy phn furosemid = acid, thm Natri nitrit ri thm amoni sulfamat v N-(1-naphtyl) ethylendiamin
dihydroclorid th to mu t n mu tm.
- Nhm sulfonamide : c tnh acid:
- Nhm amin thm: (tnh base)

Tnh kh: lm mt mu TT c tnh oxi ha ( KMnO4..)
Phn ng to phm mu Nit:
Ar- NH2 + dd NaNO2/ HCl Ar [ N+ = N ] Cl ( mui diazoni) + NaCl + 2H2O
19
TI LIU THAM KHO
Ar [ N+ = N ] Cl ( mui diazoni) + naphtol Ar N = N - naphtol ( mu )

b. nh lng:
- Phng php o kim trong mi trng khan: ha tan / DMF ( dimethyl formamid) ; nh lng = dd
chun NaOH; tm im tng ng = ch th xanh Bromothymol.
- PP o quang, HPLC
4/ Dc ng hc:
a. Hp thu:
- Hp thu tt qua ng tiu ha, SKD theo ng ung l 60%. t Cmax sau 1,5h
- Xut hin tc dng nhanh: 3-5 pht sau tim tnh mch, 10-20 pht sau khi ung.
b. Phn b:
- Lin kt vi protein huyt tng cao > 90%.
- Thi gian tc dng 4-6h.
c. Chuyn ha, thi tr:
- Thi tr ch yu qua thn, mt phn qua mt. T1/2 = 1-1,5h.
5/ Tc dng v c ch. ( nh phn i cng thuc li tiu quai)
v tr t/dng quai henle. t/dng li tiu nhanh mnh nhng thi gian t/dng ngn. Tc dng li tiu theo
c ch sau:
+ - +
+ Phong ta c ch ng vn chuyn nhnh ln of quai Henle, lm tng thi tr Na , Cl , K ko theo
nc nn li tiu
+ Gin mch thn, tng lu lng mu qua thn, tng sc lc cu thn, phn phi li mu c li cho
cc vng su v thn. Khng ADH ti ng ln xa
+ Gin TM, gim mu phi, gim p sut tht tri
++ ++ ++ ++
+ Tng o thi Ca , Mg lm gim Ca , Mg mu
6/ Ch nh.
- Cp cu: ph phi cp, ph nng (x gan c chng) ; cn tng huyt p.
- Ph do bnh gan, phi, thn v phng sn git.
- Suy tim tri cp; suy tim mn tnh khng cc thuc li niu khc.
- iu tr chng Ca++ mu cao.
- Thuc t hiu qu cao trong Suy thn ur huyt cao.
7/ Tc dng MM.
- Ri lon in gii do tc dng nhanh, mnh nn thuc thi nhanh nc v in gii c th mt mi,
chut rt, c th h huyt p t th ng.
- Nhim base: do gim Cl- , K+, Ca++ , H+ trong mu.
- R lon chuyn ha: tng a. uric mu , tng glucose mu, tng cholesteron
- R lon chc nng gan, thn.
- R lon tiu ha, ri lon to mu ( gim tiu cu, bch cu).
- c vi dy TK VIII: chng mt, tai ( c th gy ic)
- D ng: ni mn, au c, au khp
8/ Chng ch nh.
- Mn cm vi thuc.
- X gan, gout.
- Gim K+ mu, gim th tch mu h HA.
- Ch phm: vin 20, 40, 80mg hoc ng tim 20mg / 2ml.
- Liu dng: ung 20-80 mg / ngy. Tim bp, TM 1-2 ng/ln/ngy.
10/ Tng tc.
- Phi hp vi khng sinh aminosid: tng c tnh dy VIII ic.
- Phi hp cc thuc gy xon nh : Quinidin, Aminodaron, Astemisol, erythromycin tim tnh mch
lm tng nguy c ri lon nhp tim.
- Phi hp vi thuc c ch men chuyn h HA t ngt.
- Phenytoin lm gim tc dng li tiu ca thuc.
- Dng ng thi vi Glycosid tr tim loi Digitalis tng c tnh ca cc thuc ny.
O O
H2NO2S 8 S
1
7 2NH
6 3
5 4
Cl N
H
2. HYDROCHLOROTHIAZID:
Tn khoa hc: 6-cloro-3,4 dihydro-2H-1,2,4 benzothiadiazin-7-sulfonamid-1,1- dioxyd.
20
TI LIU THAM KHO
Bit dc: Apo- hydro, Hypothiazid, Hydro-chlor.

1/ Ngun gc.
Tng hp ha hc:
Acyl ha 3 chloroanilin bng a. chlorosulfonic 4,6 disulfonylchlorid + NH3
4,6 disulfonamid + Formaldehyd (un nng) Hydrochlorothiazid.
2/ Tnh cht.
a. L tnh:
- Bt kt tinh trng, khng mi.
- tan: t tan trong nc, tan tt trong mt s dung mi hu c
b. Ha tnh:
- Tnh acid yu (sulfonamid), base yu (amin thm), d b thy phn.
- Nhn thm hp th mnh bc x t ngoi.
- tan trong cc dd kim
- cho phn ng vi cc TT chung ca alkaloid
- thy phn = kim, gii phng amoniac
- thy phn = acid gii phng amin thm bc 1
- v c ha trog s c mt ca cht oxy ha
3/ im nghim.
a. nh tnh:
- Hydrochlorothiazid d tan trong cc dd kim, T/d vi mt s mui mui mi hoc dd c mu.
- Hydrochlorothiazid tan trong HCL, DD cho P/ng dng tnh vi TT chung ca alkaloid
- Phn ng ca nhm sulfonamide
- un vi dd kim gii phng NH3 lm xanh giy qu .

- T/d vi hydroperoxyd hoc HNO3 ion sulfat, pht hin ion sulfat bng BaCl2:
- Thy phn hydroclorothiazid gii phng nhm amin thm t do , pht hin amin ny = p/ng to phm
mu azo.
- nh tnh = o ph t ngoi so snh ph chun
- nh tnh = SKLM, qut ph UV
b. nh lng:
- Phng php o kim trong mi trng khan, dm dimethylsulfoxyd, cht chun tetrabutylamino
hydroxyd, ch th o th (ly im un th 2). Trong trng hp ny, c 2 chc acid u tham gia p/.
- PP o quang, HPLC
4/ Dc ng hc.
a. Hp thu:
- Hp thu tt qua ng ung, thi gian tc dng di 6-12h.
b. Phn b:
- Thuc qua c rau thai v sa m.
c. Chuyn ha, thi tr.
- Thi tr qua thn.
- Cnh tranh bi tit vi a.uric lm gim bi xut a.uric qua thn.
5/ Tc dng v c ch.
a. C ch:
- c ch ti hp thu Na+ v Cl- on pha long ca ng ln xa, theo c ch ng vn chuyn nh
nhnh ln of quai Henle
- Liu cao gy c ch enzym carbonic anhydrase (CA)
- Tng thi tr K+ theo 2 c ch :
o Thuc c ch CA, H+ gim thi tr nn K+ tng thi
o Do c ch ti hp thu Na+ nn nng Na+ tng cao ng ln xa, gy phn ng b tr tng thi K+
ko Na+ li.
21
TI LIU THAM KHO
- Khng tng thi tr HCO3- khngnhim acid mu.

b. Tc dng:
- Td li niu trung bnh, tc dng c trong mi trng acid v base.
- t lm RL thnh phn dch ngoi bo.
- Lm gim tit a.uric qua ng thn tng a.uric mu.
- Dng lu: lm gim Ca++ niu , tng thi tr Mg++ gim Mg++ mu.
- Lm h huyt p trn bnh nhn tng HA do thi mui v c ch ti ch tc dng ca cc cht co
mch nh Vasopressin, No-adrenalin.
6/ Ch nh.
- Ph cc loi bnh v gan, thn, tim mch v nhim c thai nghn .
- Tng HA. Thng phi hp vi cc thuc h HA khc
- Tng Ca++ niu ko r ng/ nhn gy si thn.
7/ Tc dng MM.
- RL in gii: dng lu gy gim Na+, gim K+, gim Mg++ v tng Ca++ mu mt mi, nhc u,
bun nn, nhim base chuyn ha.
- RL chuyn ha:
+ Tng a.uric mu lm bnh gout nng thm v pht trin.
+ Lm nng thm bnh i ng ty do / c gii phng Insulin v tng bi xut Catecholamin
tng Glucose mu v cholesteron huyt.
- Gy d ng.
8/ Chng ch nh.
- Trng thi gim K+ mu trn bnh nhn x gan.
- ang iu tr bng ch phm Digitalis.
- Bnh nhn gout, hay suy gan, thn.
- Mn cm vi thuc.
- D ng vi sulfamid
- Ch phm vin nn 25mg, 100mg
- Liu dng 0,025-1g / ln x 2 ln / ngy.
10/ Bo ch : thi tt nghip LTTH nm 2013
a) Trnh by vai tr cc t dc trong cng thc vin nn sau :
Hydroclorothiazid 25mg
Avicel PH 101 30mg
Latose 45mg
PVP K-30 4mg
Talc 4mg
Magnesi stearat 2mg
Aerosil 200 1mg
Natrilaurylsulfat 0,5mg
Nc tinh khit va
b) Trnh by nhn ca l thuc, mi l cha 500g bt hydroclorothiazid
- Nu nhng ni dung bt buc cn phi c trn nhn
- V nhn ca l thuc trn
Gii :
a. Nu vai tr cc t dc trong cng thc
- Dc cht t tan trong nc, cn s dng c t dc lm tng r v ha tan
- Avicel PH 101 (cellulose vi tinh th) : t dc r, n, c kh nng chu nn tt, t dc dnh kh
- Lactose : t dc n
- Natri croscarmellose: t dc siu r, r theo c ch trng n
- PVP K30: t dc dnh thn nc
- Magnesi stearat , Talc: t dc trn ( nghin qua ry 180) iu ha s chy
- Aerosil 200: t dc trn iu ha s chy
- Natrilaurylsulfat: t dc trn, cht din hot, ci thin ha tan cho dc cht
- Nc tinh khit
b. Trnh by nhng ni dung bt buc phi c trn nhn ca l thuc cha 500g bt
hydroclorothiazid
Nhn nguyn liu
- Tn nguyn liu
- Khi lng tnh/ th tich
22
TI LIU THAM KHO
- S ng k (nu c)
- Hm lng, nng
- S l SX, ngy SX
- Tn v a ch c s sn xut, xut x
- Tiu chun ca nguyn liu
- Hn dng, iu kin bo qun
- Tn, a ch c s nhp khu
CHUYN 5 : THUC IU TR TNG HUYT P

I- I CNG V BNH:
1/ nh ngha:
- Tng huyt p (THA) l tnh trng tng HA tm thu v/hoc HA tm trng c hoc khng c nguyn
nhn.
- Nguyn nhn:
+ 90-95% khng r nguyn nhn.
+ 5-10%: do bnh l tim, thn hoc do di truyn
2/ Chn on:
chn on xc nh bnh THA phi da vo ch s HA ca bnh nhn. HA c s bin thin t nhin
rt nhiu phi o nhiu ln v nhiu thi im khc nhau.
- HA bnh thng: 80 120mmHg.
- THA nh: 90 150mmHg.
- THA trung bnh: 100 170mmHg.
- THA nng: 110 180mmHg.
* Cc c quan b nh hng nhiu do THA:
- Tim: ph i tm tht, cn au tht ngc, nhi mu c tim, suy tim.
- No: xut huyt no t qu, thiu mu no cc b thong qua.
- Thn: suy thn, THA do thn.
- Mt: xut huyt vng mc, ph gai th.
3/ Nguyn tc iu tr.
- iu tr sm v lu di.
- a HA v mc ti u: mc thp nht m b/n c th sinh hot c bnh thng.
- Kt hp iu tr thuc vi ch sinh hot hp l.
- Chn thuc t tc dng ph, ph hp vi i tng bnh
- iu tr cc yu t nguy c v bnh mc km nu c.
5/ iu tr c th:
a. Bin php khng dng thuc:
iu chnh cch sinh hot ph hp vi bnh nhn:
- Ngng ht thuc l.
- Gim cn nng (nu tha cn)
- Hn ch ung ru, hn ch n mn.
- Tng hot ng th lc.
b. Bin php dng thuc: dng thuc h HA tc ng vo c ch gy tng HA: tng thi ion Na + ,
chng co mch.:
- Thuc li tiu tng thi Na+ v nc.
- Thuc chn , giao cm v giao cm TW ngn c tc ng ca TK giao cm.
- Thuc /c men chuyn, thuc i khng th th angiotensin, thuc chn knh Ca++ , thuc gin mch
trc tip chng co mch.
II- I CNG V NHM THUC.
1/ Phn loi:
Theo c ch iu ha HA, chia thnh 5 nhm:
- Nhm 1: Thuc li tiu.
- Nhm 2: Thuc gim hot ng h giao cm v hy receptor adrenergic
+ Tc ng ln giao cm TW.
+ Lit hch.
+ Tc dng ln TK hu hch giao cm.
+ Hy adrenergic
+ Hy adrenergic.
- Nhm 3: Thuc gin mch trc tip.
- Nhm 4: Thuc chn knh Ca++ tc dng trn tim mch.
23
TI LIU THAM KHO
- Nhm 5: Thuc c ch h RAA

+ c ch enzym chuyn dng angiotensin (ECA Angiotensin Coverting Enzym)
+ c ch receptor AT1 ca angiotensin II.
2/ C ch iu ha HA:
- HA ph thuc 2 yu t chnh: Cung lng tim v sc cn ngoi vi.
- 2 yu t ny li ph thuc vo nhiu yu t khc: hot dng ca h TKTW, h TK th c vt ca v v
ty thng thn, ADH, h RAA, tnh trng c tim.
- 2 thng s ca HA l tin gnh v hu gnh ph thuc vo s co hp lng mch.
Thuc iu tr THA phi tc ng ln cc khu ca c ch iu ha lm gin mch, gim lu lng
tim h HA.
S c ch hnh 1.5 : sgk dc l 2 trang 55
LU : xem thm c ch tc dng ca cc nhm thuc trong sgk dc l 2 trang 55
III / THUC C TH :
1. NIFEDIPIN
( Chn knh Ca++ )
Tn khoa hc: dimethyl 1,4- dihydro- 2,6- dimethyl-4-(2- nitrophenyl) pyridin-
3,5- dicarboxylat.
Bit dc: Adalat, Cordicant.
1/ Ngun gc: Tng hp. + NH3

Acetylacetat methyl + 2- nitrobenzaldehyd Nifedipin
- H2O
2/ Tnh cht l ha :
- Bt kt tinh mu vng nht, d b bin mu khi tip xc vi nh sng.
- Tn / c = 171 175oC.
- tan:
+ Khng tan trong nc
+ Tan trong MeOH, EtOH.
+ D tan trong ether, cloroform.
- Hp th UV mnh, IR c trng.
- Nhm Nitro thm Ar-NO2 kh ha to amin thm phn ng to mu:
Tnh kh: lm mt mu TT c tnh oxi ha ( KMnO4..)
Phn ng to phm mu Nit:
Ar- NH2 + dd NaNO2/ HCl Ar [ N+ = N ] Cl ( mui diazoni) + NaCl + 2H2O
Ar [ N+ = N ] Cl ( mui diazoni) + naphtol Ar N = N - naphtol ( mu )
-
3/ Kim nghim
a. nh tnh:
- o ph hp th t ngoi
- o ph hng ngoi so snh vi ph ca cht chun, SKLM
- To phm mu nit: Kh ha nhm nitro thnh amin thm bc I to mui diazoni vi HNO 2, sau
ngng t vi mt phenol phm mu nit (mu )
b. nh lng:
- PP o acid trong mi trng khan: ( ha tan / CH3COOH; nh lng = 1 acid mnh HClO4 0,1M; pht
hin im tng ng = cch o th
- = PP o ceri : dng dd chun l ceri amoni sulfat 0,1M (cht oxh). Trong p/, phn dihydropyridin b
oxy ha thnh pyrodin.
- PP HPCL.
- PP o quang
4/ Dc ng hc.
- t nng ti a trong huyt tng sau 0,5 1 gi
- Dng gii phng ko di t nng ti a sau 6 8 gi
- Thi tr ch yu qua thn. thi gian bn thi : 16 18 gi
5/ Tc dng v c ch.
a. Tc dng:
- Gin mch ngoi vi nhiu gim hu gnh h HA.
- Khng tc dng n nt nh tht khng nh hng n dn truyn TK tim, nhng gy phn x
giaocm tng nhp tim.
- Ci thin chc nng thn do: Tng lng mu vo thn. Khng nh hng ti h RAA.
24
TI LIU THAM KHO
- Khc vi thuc chn knh Ca++ khc: ngoi gin mch, cn gin PQ, c trn tiu ha v t cung.
b. C ch:
- Gn c hiu vo knh Ca++ c t bo c tim v c trn thnh mch phong ta khng cho Ca ++ i
vo t bo lm gin c.
- c ch nucleotid phosphodiesterase vng trong t bo c trn tng nucletid vng gin c trn
mch mu h HA.
- lu lng mu ti cu thn sc lc cu thn li tiu h HA.
6/ Ch nh.
- iu tr tng HA.
- Cn au tht ngc th n nh v Prizmetal, th khng n nh.
7/ Tc dng MM.
- RLTH
- Tng enzym gan, tng sn li, au c, ri lon th gic.
8/ Chng ch nh.
- Mn cm vi thuc.
- Thn trng trong suy gan, PNCT v cho con b.
- Adalat vin bc ng 10mg, vin nn 20mg tc dng nhanh, ngn.
- Adalat LA 30mg, Adalat LP 20mg tc dng ko di, liu 20 - 60mg/ngy
10/ Bo ch : thi LTTH nm 2009
a) Vin nn nifedipin c cng thc sau:
Niedipin 10mg
Tinh bt m 30mg
Lactose 60mg
DD PVP 10% trong ethanol 900C va
natri starch glycobat
Magnesi stearat 2mg
Talc 5mg
Aerosil 3mg
- Nu vai tr cc thnh phn trong cng thc
- Trnh by vn tt cc bc trong quy trnh bo ch
b. Trnh by ni dung t HDSD thuc nifedipin vin nn 10mg
Gii :
a.
- Nu vai tr cc thnh phn trong cng thc
+ Niedipin : dc cht
+ Tinh bt m : t dc n, r
+ Lactose : t dc n
0
+ DD PVP 10% trong ethanol 90 C : t dc dnh
+ Natri croscarmellose, natri starch glycobat: t dc siu r
+ Magnesi stearat , Talc , Aerosil: t dc n, trn chng dnh, iu ha s chy
- Trnh by vn tt cc bc trong quy trnh bo ch
+ Nghin v ry nguyn liu
+ Trn bt kp tinh bt, nifedipin, lactose, natri starch glycobat theo nguyn tc ng lng
+ Nho m vi dd PVP
+ Xt ht qua ry (0,6 0,8 mm) c th dng pp th cng hoc thit b ph hp
+ Sy cm ti m thch hp ( 2- 3%)
+ Sa cm qua ry
+ Trn t dc trn, natri croscarmellose ( ry qua ry 180 hoc 125)
+ Dp vin, ng gi
b. Trnh by ni dung t HDSD thuc nifedipin vin nn 10mg ( phn Php ch dc)
- tn thuc : tn quc t, tn bit c nu c
- cng thc 1 vin nifedipin 10mg ( trong cng thc phi ghi hm lng nifedipin v hm lng t
dc)
- Dng bo ch: vin nn
- Quy cch ng gi: (v d hp 10 v x 10 vin nn)
- Ch nh
25
TI LIU THAM KHO
- Chng ch nh
- Thn trng khi dng
- Tng tc thuc
- Tc dng KMM
- Liu dng : 1 ln, 24h
- Cch dng
- Khuyn co (c k HDSD trc khi dng)
- Hn dng (HSD)
- Tiu chun p dng
- iu kin bo qun ( bo qun nhit phng 250C)
- Tn, a ch c s SX, in thoi, Fax, e-mail nu c
2. CAPTOPRIL
(Thuc c ch enzym chuyn dng angiotensin ECA)
CH3
N CO C CH2SH
H
COOH
Tn khoa hc: Acid 1-(3-mercapto-2-methylpropanoyl) pyrolidin-2-carboxylic.
Bit dc: Acepril, Capoten, Lopril.
1/ Ngun gc. Tng hp ha hc.
2/ Tnh cht.
- Bt kt tinh mu trng ng., bin mu trong khng kh, nh sng.
- tan: + D tan trong nc, MeOH, methylenclorid
+ tan trong dung dch NaOH long.
- Tn/c = 105 108oC.
- IR c trng.UV km; C gc quay cc ring
- Ha tnh :
+ Tnh base yu ca N bc 3
+ Tnh acid
+ Phn ng ca nhm thiol
3/ im nghim.
nh tnh:
- o ph hp th t ngoi
- o ph hng ngoi so snh vi ph ca cht chun, S LM
- Phn ng ca N bc 3: c tnh base yu: Dd cho kt ta vi cc thuc th chung ca alkaloid
- Phn ng ca nhm thiol : R- SH: tnh kh: -> d b oxh -> chc acid SO3H lm mt mu iod
T/dng vi TT Natri Nitro prussiat tm m
T/dng vi TT Fehling gch
T/dng vi AgNO3 trng
- Tnh acid: to mui tan trong dd kim, tc dng vi mui to mui mi (c th to ta hay mu)
nh lng:
- PP o quang hoc HPLC ( hi li thy ??????? )
- Bng php do iod: dd chun Iod 0,05M, ch th o in th.
4/ Dc ng hc.
a. Hp thu:
- Hp thu nhanh qua ng tiu ha, thc n lm chm hp thu.
- SKD 75%, xut hin tc dng sau 1h, ko di td 6-8h.
- Thuc qua c nhau thai v sa m
b. Chuyn ha, thi tr:
- Khng chuyn ha qua gan ln u.
- Thi tr qua thn dng chuyn ha khong 40-45%. T1/2 = 4h.
5/ Tc dng v c ch.
a. Tc dng.
* Trn mch:
- Gin mch: do c ch enzym ECA nn angiotensin II b gim v lm gim vasopressin huyt tng lm
gim sc cn tun han ngoi vi.
26
TI LIU THAM KHO
- Gin mch chn lc cc m quan trng (vnh, thn, no, thng thn) nn ti phn phi lu lng
tun hon ti cc khu vc khc nhau lm gim c tin gnh v hu gnh.
- Gim ph i thnh mch, tng tnh n hi ca ng mch ci thin chc nng mch mu.
* Trn tim:
- Khng tc dng trc tip trn nt xoang , khng thay i nhp tim.
- Gim s ph i v x ha tm tht, vch ln tht.
* Trn thn:
- Tng thi Na+, gi K+ do lm gim tc dng ca aldosteron h huyt p.
- Tng thi a. uric
- Tng tun hon n thn tng sc lc cu thn.
* Chuyn ha:
- Tng nhy cm vi Insulin v Tng hp thu glucose.
b. C ch:
- ECA c nhiu trong huyt tng v cc m nh thnh mch, tim, thn, tuyn thng thn, no.
- ECA xc tc cho qu trnh to angiotensin II l cht c t/dng gy co mch, tng gi Na+ v lm ging
ha Bradykinin tng hut p. Khi dng Thuc c ch ECA, angiotensin II ko c hnh thnh v
Bradykinin b ngn ging ha gin mch, tng thi Na+ lm h HA.
6/ Ch nh.
- iu tr tng huyt p do tn thng thn, do tiu ng.
- iu tr suy tim xung huyt mn tnh do thuc lm gim tin gnh v hu gnh.
- Dng sau nhi mu c tim.
7/ Tc dng MM.
- H HA hay gp liu u tin.
- Ho khan do tch ly Bradykinin v Prostaglandin trong phi.
- Tng K+ mu khi chc nng thn km, hoc dng phi hp vi thuc li niu gi K +, NSAID, c ch
adrenergic.
- Suy thn cp hay gp bnh nhn hp ng mch thn.
- D ng , pht ban, st, albumin niu
- Ph mch thn kinh do thot nc qua mao mch. Ph nim mc ni, hng, thanh qun
- Thay i v gic.
8/ Chng ch nh.
- Mn cm vi thuc. - PNCT v cho con b.
- Thn trng vi ngi suy thn. - Thn trng vi ngi suy thn.
- Hp ng mch thn - H HA.
- Vin nn 25mg v 50mg.
- Liu THA: 25-50mg x 2-3 ln / ngy.
- Liu suy tim: khi u 6,25mg/ln ; duy tr 50mg x 3 ln / ngy.
10/ bo ch - Php ch: ????
27
TI LIU THAM KHO
Chuyn 6: THUC CHNG VIM NSAIDs V DC LIU CHA

THP HP
I. I CNG V THUC:
1. Tc dng v c ch:
- Tc dng h st: C ch h st: cht gy st ngoi lai kch thch bch cu sn xut cht gy st ni
ti, hot ha prostaglandin synthetase lm tng tng hp PGE1 v PGE2 t acid arachidonic vng di
i gy mt cn bng c ch iu nhit gy nn st. Thuc c ch Prostaglandin synthetase, lm gim
tng hp PGE1 v PGE2, c ch qu trnh sinh nhit, tng cng qu trnh thi nhit, lm h st.
+ Tc dng h st: thuc h st do bt k nguyn nhn no v ch c tc dng iu tr triu chng, khng
h thn nhit ngi khng st
- Tc dng gim au: C ch gim au: thuc gim tng hp PGE2, lm gim tnh cm th ca ngn
dy thn kinh cm gic vi cc cht gy au ca phn ng vim nh bradykinin, serotonin
+ Tc dng gim au: gim au t nh n va, gim au ngoi vi, tc dng tt vi cc loi au do vim.
Khc vi nhm opiat, thuc nhm ny khng c tc dng gim au mnh, khng gim au su trong ni
tng, khng gy c ch h hp, khng gy l thuc thuc khi dng ko di.
- Tc dng chng vim: C ch chng vim: thuc c ch enzym cyclooxygenase (COX), ngn cn
tng hp prostaglandin l cht trung gian ha hc gy vim, lm gim qu trnh vim.
+ C 2 loi COX: COX-1 cn cho tc dng sinh l ca mt s c quan (d dy, tiu cu, thn); COX-2
c vai tr to PG gy vim. Mt s thuc c ch chn lc COX-2 t nh hng ti chc nng sinh l bnh
thng, gim tc dng khng mong mun.
2. Tc dng MM:
- Trn tiu ha: kch ng, au thng v, nng hn l lot d dy t trng, xut huyt tiu ha
- Trn mu: ko di thi gian ng mu, mt mu khng nhn thy qua - phn, tng nguy c chy mu
- Trn thn: gim lu lng qua thn, gim sc lc cu thn, nguy c nc, tng kali mu v vim
thn k
- Trn h hp: gy cn hen gi trn ngi khng b hen hoc lm tng cn hen ngi hen ph qun
- Cc tc dng khng mong mun khc: mn cm, c vi gan, d tt thai nhi (nu dng thuc trong 3
thng u), ko di thi k mang thai v chuyn d, xut huyt khi sinh
3. C: - Gim au mc nh v trung bnh, nht l au do vim.
- H st do mi nguyn nhn gy st.
- Chng vim cp v mn tnh.
4. Phn loi:
- Dn cht Acid salicylic.
- Dn cht Pyrazolon.
- Dn cht Indol.
- Dn cht Oxicam.
- Dn cht Acid propionic.
- Dn cht Acid phenylacetic.
- Dn cht Acid fenamic.
- Nhm Coxib.
- Nhm Aminophenol (dn cht Anilin).
- Dn cht Acid floctafenic
II THUC C TH
1. IBUPROFEN
H3C CH COOH
CH2 CH CH3
CH3
Tn khoa hc: Acid 2- (4- isobutylphenyl) propionic.
Bit dc: Mofen, Femafen, Ibulgan
1/ Ngun gc. Tng hp ha hc: iu ch t acid phenyl propionic.
28
TI LIU THAM KHO
2/ Tnh cht.
- Bt kt tinh trng hoc tinh th khng mu.
- tan: + Khng tan trong nc, tan trong dung dch kim v carbonat kim.
+ D tan trong aceton, ether, MeOH, cloroform.
- Tn / c = 75-78oC.
- Hp th UV, IR c trng, c gc quay cc ring
- Phn ng ca nhm phenyl
+ Nitro ha: tc dng vi HNO3 dn cht mu vng
+ Phn ng vi TT Marki HCHO/H2SO4 mu
- Tnh acid
3/ im nghim.
a. nh tnh:
- o Tn / c so vi cht chun.
- o ph hp th t ngoi, o gc quay cc
- SKLM
b. nh lng:
= Phng php acid-base: dd chun NaOH, ch th phenolphtalein (ha ch phm trong MeOH).
= pp o quang, HPLC
4/ Dc ng hc.
- Hp thu tt qua ng tiu ha, sau 2h t Cmax
- Thuc lin kt vi protein huyt tng rt cao 99%.
- Thi tr qua nc tiu.
5/ Tc dng, c ch.
a. Tc dng: h st, gim au, chng vim
- H st km khng dng lm thuc h st n thun.
- T/d chng vim, gim au mnh.
- Chng kt tp tiu cu yu hn Aspirin.
b. C ch: xem phn i cng
6/ Ch nh.
- Gim au nh v va nh thng kinh nhc u, au rng.
- iu tr vim khp dng thp, vim khp, vim c
7/ Tc dng MM.
- Bun nn nng rt d dy. Ko di thi gian chy mu, pht ban, chng mt
- Mn cm cho vi Aspirin ko dng khi bnh nhn d ng vi aspirin
- Gim bch cu ht, suy thn cp, vim thn k.
8/ Ch phm, liu dng.
- Ch phm: vin nn, vin nang 100-400mg; n 500mg; dng gel 5%.
- Liu: ngi ln 1,2 1,8g / 24h ; tr em 20mg /kg / 24h.
2. DICLOFENAC
Tn khoa hc: 2- (2,6 dicloroanilino) phenylacetat natri.
Bit dc: Voltaren, Difenac, Volfenac, cataflam.
1/ Ngun gc. Tng hp ha hc.
2/ Tnh cht.
a. L tnh:
- Bt kt tinh trng hoc vng nht.
- tan: hi tan trong nc, d tan trong MeOH, EtOH; t tan trong aceton, khng tan trong ether.
- Hp th UV, Ph IR c trng
b. Ha tnh: diclofenac d b oxy ha do nhm amin thm v ha tnh ca mui Natri
- Ch phm / MeOH + HNO3 c c mu nu.
- Ch phm / EtOH cho Phn ng vi Kalifericyanid, FeCl3 v HCl mu xanh.
- Cho Phn ng ca Na+ tc dng vi TT Streng cho kt ta vng
- P/ng ca ion Cl-: T/dng vi AgNO3 trng
3/ im nghim.
a. nh tnh:
- = Cc Phn ng trn
- o ph hp th t ngoi
29
TI LIU THAM KHO
b. nh lng:
- PP acid mi trng khan: Ha tan / CH3COOH; L = dung dch acid mnh HClO4; Xc nh im tng
ng = pp o th hoc ch th mu.
- Dng acid: L = dd KOH/MeOH dung mi l cloroform
- pp o quang (pp o ph hp th t ngoi)
4/ Dc ng hc.
- Hp thu tt qua ng tiu ha, thc n lm chm hp thu. t Cmax sau ung 2 3 gi
- Phn b: lin kt vi protein huyt tng 99%.
- Chuyn ha: qua gan ln u SKD cn 50%.
- Thi tr: qua nc tiu (65% ), T1/2 = 1,5h.
5/ Ch nh.
- iu tr cc cn au cp: au TK, au si thn, au bng kinh, au dy thn kinh
- iu tr vim khp, thoi ha khp cp v mn.
6/ Tc dng MM.
Tng t thuc chng vim khc:bun nn,nng rt d dy, gy mt bch cu ht
7/ Ch phm, liu dng.
- Ch phm: + Vin nn 25, 50, 100mg (dng bao bao tan / rut), dng gel dng ngoi.
+ Vin n 25 v 100mg, ng tim 75mg / 2ml, thuc nh mt 1%.
- Liu dng: au cp tnh: ung 50mg x 3 ln / 24h; hoc sng ung 50mg, ti t 1 vin n. Liu duy
tr: 75-100mg / 24h hoc ti t 1 vin n.
Chuyn 7: THUC KHNG HISTAMIN

I- I CNG V BNH:
1/ nh ngha: D ng l tnh trng bnh l ca phn ng min dch vi d nguyn, gy ra tn thng t
chc v ri lon chc nng cc c quan.
2/ Nguyn nhn.
- Bi: nh, gi sch, qun o, ng ph
- T bo biu b, vy, da lng sc vt.
- Thc phm, thuc, ha cht.
- Vi khun, nm mc, virus.
* c im d nguyn : c tnh khng nguyn kch thch c th sinh khng th kt hp c hiu vi
khng th tnh trng d ng.
3/ Triu chng.
a. c im chung:
- C tip xc vi d nguyn.
- Biu hin rt a dng, nhiu c quan khc nhau.
- Xut hin tng t, xen k vi lc hon ton bnh thng.
- Triu chng xut hin v thoi lui hon ton t ngt.
- C lin quan n tin s d ng
b. Cc th d ng thng gp:
-My ay: sn mu hng, xung quanh c vin , hnh trn hay bu dc.
- Vim mi, vim xoang d ng: ht hi, s mi nhiu, nu bi nhim th nuc mi c, c m.
- Hen ph qun thng xy ra ngay sau khi tip xc vi d nguyn.
- RLTH do di ng vi thc n.
- Chm: hay gp tr em.
- Nng: Shock phn v t vong nu khng cp cu kp thi.
4/ C ch d ng. c 3 giai on:
a. Giai an mn cm: D nguyn xm nhp c th ln u kch thch c th sinh khng th d ng
IgE.
b. Giai on sinh ha bnh:
- D nguyn xm nhp li vo c th.
- D nguyn + IgE trong mng t bo mast ph v t bo mast gii phng cht trung gian ha hc:
Histamin, serotonin.
c. Giai on sinh l bnh:
- Cc cht trung gian ho hc c gii phng, tc ng ln c quan gy ri lon chc nng hoc tn
thng t chc bnh l:
+ R lon vn mch.
+ Co tht c trn cc tng.
+ Gin mch, tng tnh thm mao mch
30
TI LIU THAM KHO
5/ iu tr.
a. Nguyn tc 1: Loi tr tc ng ca d nguyn.
+ Trnh tip xc vi d nguyn.
+ Gii mn cm c hiu: a d nguyn vo c th nhiu ln vi liu nh v tng dn hnh thnh
khng th bao vy IgG ngn cn d nguyn kt hp vi IgE khng pht sinh d ng.
b. Nguyn tc 2: iu tr triu chng.
+ Thuc khng H1 : gim s gii phng cht trung gian ha hc.
+ Corticoid: chng vim.
+ Theophylin v thuc kch thch giao cm: gim kh th, co tht ph qun.
1/ Histamin.
Phn ng to histamin:
CH2 CH NH2 CH2 CH2 NH2
Histamin decarboxylase
HN N COOH CO2 HN N
Histidin histamin
- Histamin l cht ni sinh, c to thnh t Histidin.
- Trong c th tn ti 2 dng: dng t do c hot tnh v dng lin hp ko c hot tnh. Dng lin hp
c d tr trong dng bo.
- D nguyn lm cho histamin lin hp gii phng ra cc cht trung gian ha hc v histamin t do gy
ra cc biu hin d ng nh :
+ Trn mch: gin mch, tng tnh thm thnh mch ph n, xung huyt.
+ Trn c trn: tng co bp c trn kh qun, ng tiu ha, tit niu, sinh dc.
+ Trn tuyn ngoi tit: tng tit dch nc bt, dch d dy
+ Trn TKTW: kch thch gy bn chn, kh ng, co git TE.
2/ hng Histamin receptor H1
a. Cu trc chung:
X C1 C2 N
b. Phn loi:
- Phn loi: Th h I: gm 5 nhm
+ Dn cht Ethanolamin (X l > CO-): diphenhydramin, dimenhydrinat.
+ Ethylendiamin (X l N v C C -): mepramin, methapyrilen.
+Alkylamin(X l C): chlopheniramin, phenyramin.
+ Piperazin (X l >N- v C C N<): cyclizin, Cinarizin.
+ Phenothiazin(X l N): promethazin, propiomazin.
- Th h II: gm 3 nhm:
+ Alkylamin: Acryvastin. + Piperazin: Cetirizin. + Piperidin:Astemizol, loratadin.
c. C ch: Cc thuc khng H1 i khng cnh tranh vi Histamin ti receptor H1 ti t bo ch ngn
chn c tc dng ca Histamin ln t bo ch.
d. Tc dng:
- Trn mch v HA:
+ Lm mt tc dng gin mch v tng tnh thm thnh mch ca Histain.
+ Lm gim hoc mt cc P/ vim, d ng, gim ph, gim nga.
- Trn c trn:
+ gim co tht c trn ng tiu ha gim au bng do d ng.
+ tc dng ko trit trn c trn ph qun khng dng ct cn hen.
- Trn tuyn ngoi tit: c ch s bi tit nc bt v nc mt do histamin.
- Trn TKTW:
+ Khng H1 th h 1 ( TH1 ) c tc dng c ch TKTW an thn, gy ng.
+ Kch thch thn kinh bn chn, kh ng; gp tr em d b co git.
+ Gim s tnh to, chm chp, m mng.
- Khng cholinergic: TH1 c tc dng ny lm thuc chng nn, say tu xe.
- Mt s thuc TH1 nh Prometazin c tc dng gy t ti ch.
e. Lin quan cu trc tc dng:
31
TI LIU THAM KHO
X = C l C* ng phn d c hot tnh ng phn L hu nh ko c tc dng

C2 = C* : ng phn L tc dng mnh hn ng phn d
Halogen gn vo nhn thm ( v tr para) lm tng hot tnh
f. Ch nh:
- Chng d ng: vim mi d ng, ni m ay, nga do d ng.
- Chng say tu xe: Cinarzin, Dimehydrinat, Promethazin.
- Hi chng Meinre.
- Nn v bun nn trong thai nghn: Promethazin
- Phi hp iu tr ho.
f. Tc dng MM:
- An thn, gy ng ( Th h 1) khng dng cho ngi li tu xe, vn hnh my mc.
- TH1 lm tng tc dng ca ru v thu c ch TKTW chng mt, mt mi.
- Trn tiu ha: n khng ngon, nn, bun nn (Th h 1)
- Khng cholinergic kh ming, kh mi hng (Th h 1 ).
g. Chng ch nh:
- Mn cm vi thuc; - Ngi c thai v cho con b.- Nhc c, Glocom, u x tin lit tuyn, tng nhn
p
h. Tng tc thuc:
- Tng tc dng c ch TKTW ca thuc an thn, gy ng, ru.
- Tng tc dng ca thuc khng cholinergic.
- Terphenadin phi hp vi Macrolid hoc Ketoconazon d c nguy c lon nhp tht, xon nh.
II THUC C TH:
1. CLORPHENIRAMIN MALEAT
Cl H
CH3 HC COOH
C CH2 CH2 N
CH3 HC COOH
Tn khoa hc: 3-(4-clorphenyl) -3-(2-pyridyl) propyldimethylamin hydromaleat.

BitCldc: Trimeton Allersan, Allergy, Clorphenan
CH3
1/ Ngun gc:CH Tng CH2 CHhp.
2
: Ngng
Cl + HN t 3-(4-clorphenyl)
Na NH2 -3-(2-pyridyl) 1-cloro propan vi
dymethylamin, c mt sodamid, c clopheniramin
CH3 ( base.
HCl ) To mui maleat = tc dng ng phn t vi
acid maleic
N
HC COOH
Cl H +
CH3 HC COOH
C CH2 CH2 N
CH3
Cl H
CH3 HC COOH
C CH2 CH2 N
CH3 HC COOH
2/ Tnh cht.
a) L tnh:
- Bt tinh th trng, khng mi.
- tan: + Tan trong nc v dung dch nc c pH 4-5.
+ Tan t trong ether, benzen.
- Hp th UV, IR, 0=0
b) Ha tnh : - Phn ng ca N bc 3; Phn ng ca ion Cl- ; Phn ng ca nhm maleic
32
TI LIU THAM KHO
3/ im nghim.
a. nh tnh:
- o ph hp th t ngoi
- Xc nh acid Maleic:
+ Kim ha dd ch phm bng NaOH chit b Clorpheniramin.
cch thy 15
+ 1 phn dch cn li, thm dd resorsinol / H2SO4 c Khng c mu.
+ 1 phn dch + dd Br2 un cch thy n si, ngui; thm dung dch
cch thy 15
resorsinol /H2SO4 c xut hin mu xanh lam.
- To ta clopheniramin picrat o Tn / c = 196 200oC
- o chy ca ch phm: Tn / c = 132 136oC.
- Phn ng vi thuc th chung ca alcaloid
- Phn ng vi AgNO3 to kt ta trng
b. nh lng:
- = pp o acid trong mi trng a. acetic khan, dd chun HClO4 0,1N ; ch th o in th.
- = pp o quang
4/ Ch nh.
- D ng ng h hp trn: vim mi d ng, s mi theo ma
- D ng ngoi da: m ay, mn nga
- Phi hp Adrenalin iu tr shock phn v.
- Phi hp vi thuc gim ho, gimau, h nhit, thuc iu tr hen.
5/ Ch phm, liu dng.
a. Ch phm:
- Vin nn 2mg, 4mg ; tim 10mg/ml, 100mg/ml.
- Siro 2mg/5ml.
- Vin tc dng chm, vin bc ng: 6,8,12mg.
b. Liu lng:
- Ngi ln: 4mg/ ln x 4-6 ln/ 24h.
- Tr em > 12 tui: 2mg/ ln x 3-6 ln/ 24h
* Ch : Khng dng dng thuc tc dng chm cho TE < 12 tui.
2. CETIRIZIN
Tn khoa hc:
Bit dc: Cezil,

1/ Ngun gc: Tng hp ton phn.
2/ Tnh cht.
a) L tnh:
- Bt tinh th trng, khng mi. Tan trong nc
- Hp th UV, IR c trng, c gc quay cc ring.
b) Ha tnh : tnh cht ca N bc 3 yu, ca nhn thm, ion Cl- .
3/ im nghim.
a. nh tnh:
- o ph hp th t ngoi
- o ph hng ngoi so snh vi ph ca cht chun, SKLM
- Gc quay cc ring
-Vi TT chung ca alcaloid.
- Nhn thm : Vi HNO3 mu .
-V c ha, phn ng ca Cl- : + AgNO3 ta trng.
-Vi FeCl3 mu hng.
b. nh lng:
- = pp o acid trong mi trng a. acetic khan, dd chun HClO4 0,1N ; ch th o in th.
33
TI LIU THAM KHO
- = pp o quang
4/ Ch nh.
- D ng ng h hp trn: vim mi d ng, s mi theo ma
- D ng ngoi da: m ay, mn nga
- Phi hp Adrenalin iu tr shock phn v.
- Phi hp vi thuc gim ho, gim au, h nhit, thuc iu tr hen.
- Khng c ch TKTW t gy bun ng
5/ Ch phm, liu dng.
a. Ch phm:
- Vin nn , nang 10mg .
b. Liu lng: ngi ln v tr em t 6 tui tr ln ung 1 vin 10 mg/ngy hoc 5 mg x 2 ln/ngy
6/ Chng ch nh
Nhng ngi c tin s d ng vi cetirizin, vi hydroxyzin.
7/ TDKMM:
Hay gp nht l hin tng ng g. T l gy nn ph thuc vo liu dng.
Ngoi ra thuc cn gy mt mi, kh ming, vim hng, chng mt, nhc u, bun nn.
CHUYN 8: AN THN DN CHT BENZODIAZEPIN V DL C

TD AN THN
I/ I CNG NHM THUC:
hi nim: Thuc an thn gy ng l thuc /c TKTW. Thuc an thn c tc dng gim lo lng bn
chn. Thuc ng td to ra trng thi bun ng v duy tr gic ng tng t gic ng sinh l.
A Nhm dn cht BENZODIAZEPIN
1. Cu trc: L dn cht 1,4 benzodiazepin.
2. Phn loi:
- Thuc td ko di: Clorazepat, diazepam
- Thuc td nhanh: Lorazepam, Temazepam
3. DH: Hp thu: c ng ung v ng tim
- Lin kt vi protein huyt tng t 70 99%; phn b vo hu ht cc dch c th, rau thai sa m.
- Chuyn ha qua enzym gan.
- Thgian bn thi: khc nhau ty thuc,
VD: T1/2 ngn: Triazolam 2-3h ; T1/2 trung bnh: alprazolam 12-15h; T1/2 di: Diazepam 20-80h
4. Tc dng, c ch:
* Tdng chung: - An thn, gy ng.
- Chng co git, gin c, gin mch, h HA nh, chng lon nhp.
* C ch: - Receptor of Benzodiazepin c nhiu v no, h lymbic & no gia -> cc receptor ny l 1
fn of fc hp GABA knh Cl- .
- Bnh thng khi cha dng benzodiazepin (BZD), cc receptor ca n b protein ni sinh (BZD ni sinh)
chim gi, khi GABA cng ko gn vo receptor GABA hon ton, knh Cl- ng. Khi BZD, do c i
lc vi GABA mnh hn nn y protein v chim ch, ng thi to thun li GABA gn c
vo receptor GABA lm knh Cl- m ra, Cl- vo t bo gy tng lu cc lm tng c ch TKTW. BZD ch
yu lm tng tn sut m knh Cl- qua trung gian GABA
- Benzodiazepin to thun li GABA gn c vo Receptor & gy c ch TKT
5. Lin quan gia cu trc v tc dng: Dn cht 5- phenyl 1,4 benzodiazepin.
* v tr C7: - Nu R2 l nhm ht in t (Cl, Br, NO2) tng hot tnh ca thuc; s ht in t cng
mnh hot tnh cng tng.
- Nu R2 l nhng nhm gii phng in t or nhng nhm ln gim hot tnh.
* v tr C5: - Gc phenyl v tr ny lm tng tc dng ca dn cht: v tr ortho (2, 6) l nhm ht
in t tng tc dng; v tr para gim tc dng.
* v tr C3: - If l nhm th alkyl tc dng;
- Nu l nhm OH s nh hng n dc ng hc ca thuc: + Nu ko c nhm OH hp cht t
phn cc T1/2 ln tc dng ko di.
+ If c nhm OH hp cht phn cc mnh tc dng ngn.
* Nu C5 l mt chc ceto. C4 l 1 gc methyl s to ra cht i khng vi ben zodiazepin ,
v d: Flumazenil.
34
TI LIU THAM KHO
6. C: Lo u, cng thng; Cc trng thi mt ng nng; ng kinh cn nh; Tin m; Cc bnh co

cng.
7. CC: Nhc c; Suy h hp; Suy gan, thn nng.
8. TTT: Vi cc thuc c ch TKT -> Hip ng.
- Vi cc thuc c ch or cm ng enzym Cyt P 450 -> tng or gim nng benzodiazepin
VD: Cimetidin /c chuyn ha benzodiazepin td v d gy ng c; Rifampicin gy cm ng enzym
tc dng ca benzodiazepin.
9. Tdkmm & c tnh: - Bun ng, chng mt, l ln, hay qun.
- c tnh cp (qu liu). c tnh mn (ko di): l thuc thuc.
B NHM DN CHT BARBITURAT
1. Cng thc chung :
2. Phn loi : Da vo thi gian tc dng, chia thnh 4Da
vo thi gian tc dng, chia thnh 4 nhm :
- Tc dng di: 8 12h : Phenobarbital, barbital,
butabarbital, aprobarbital
- Tc dng trung bnh : 4 8h : Amobarbital, pentobarbital,
...
- Tc dng ngn : 1 3h: Hexobarbital, secobarbital...
- Tc dng rt ngn: 30 60 pht: Thiopental, thiobarbital
3. Tc dng chung :
- An thn gy ng: barbital, pentobarbital...
- An thn gy ng km gin c vn : Phenobarbital, secobarbital...
4. C ch tc dng chung: c ch TKTW = cch to thun li cho acid gama-amino-butyric (GABA)
gn vo receptor GABA lm knh Cl- m ra, Cl- vo t bo gy tng lu cc lm tng c ch TKTW.
5. Ch nh chung: An thn, gy ng, tin m, chng ng kinh, chng co git...
II - Thuc c th: DIAZEPAM, PHENOBARBITAL
1. DIAZEPAM
Tn KH: 7-cloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-on.
Bit dc: Seduxen; Valium, Mekoluxen.
1/ iu ch:
NH2 NH CO
Br CH2
HBr H
O + C CH2Br O
Cl C Cl C H N
Ether
O
CH3
O
NH CO N
CH2
H Ether
O
Cl C H N N
Cl
Diazepam
2/ Tnh cht.
- Bt kt trng nh vng, khng mi.
- tan: + D tan trong cc dung mi hu c.
+ Kh tan trong nc.
- Tn/c = 131 135oC.
- Ha tnh: Ca nhm phenyl, phn ng mu, phn ng ca N bc 3 v phn ng ca ion Cl-
3/ im nghim.
a. nh tnh:
- Dung dch Diazepam/ H2SO4 c hunh quang mu xanh lc vng trong nh sng UV.
- Dng ph IR so snh ph chun, qut ph UV
- SKLM so snh vi cht chun
- Phn ng vi cc thuc th chung ca alcaloid
35
TI LIU THAM KHO
- Phn ng ca nhm phenyl :

+ Nitro ha: tc dng vi HNO3 dn cht mu vng
+ Phn ng vi TT Marki HCHO/H2SO4
- Phn ng ca ion Cl- : v c ha ri cho phn ng vi AgNO3
b. nh lng:
- PP o acid / mt khan : Ha tan / CH3COOH; L = dung dch acid mnh HClO4; Xc nh im
tng ng = pp o th hoc ch th mu.
- PP quang ph UV
4/ Dc H
Hp thu: c ng ung v ng tim, t Cmax sau 1 2h
- Lin kt vi protein huyt tng t 70 99%; phn b vo hu ht cc dch c th, rau thai sa m.
- Chuyn ha qua enzym gan.
- Thgian bn thi: T1/2 di: Diazepam 20-80h
5. Tc dng :
- Trn TKTW : c ch TKTW nn c t/dng an thn, gy ng
+ An thn , gim kch thch, cng thng, lo lng, hi hp.
+ Gy ng
+ Chng co git, ng kinh
- Gin c: tc dng gin c vn v c trn ngay c liu an thn
- Tc dng khc: Gin mch, h HA nh
6. C ch tc dng: (nh phn i cng)
Receptor of Benzodiazepin c nhiu v no, h lymbic & no gia -> cc receptor ny l 1 fn of fc
hp GABA knh Cl- .
- Bnh thng khi cha dng benzodiazepin (BZD), cc receptor ca n b protein ni sinh (BZD ni sinh)
chim gi, khi GABA cng ko gn vo receptor GABA hon ton, knh Cl- ng. Khi BZD, do c i
lc vi GABA mnh hn nn y protein v chim ch, ng thi to thun li GABA gn c
vo receptor GABA lm knh Cl- m ra, Cl- vo t bo gy tng lu cc lm tng c ch TKTW. BZD ch
yu lm tng tn sut m knh Cl- qua trung gian GABA
- Benzodiazepin to thun li GABA gn c vo Receptor & gy c ch TKT
7. ch nh: Lo u, cng thng; Cc trng thi mt ng nng; ng kinh cn nh; Tin m; Cc bnh co
cng.
8. CC: Nhc c; Suy h hp; Suy gan, thn nng.
9. TTT: Vi cc thuc c ch TKT -> Hip ng.
- Vi cc thuc c ch or cm ng enzym Cyt P 450 -> tng or gim nng benzodiazepin
10. Ch phm, liu dng.
- Vin nn, vin nang 2, 5, 10 mg
- ng tim 10mg/ 2ml, thuc n 5, 10mg, siro 2mg/ 5ml.
- Liu dng: Ngi ln 5-10mg/ln x 1 4 ln/24h ty ch nh; Gim liu vi tr em
2. PHENOBARBITAL
1. Cng thc :
Tn khoa hc : 5-ethyl-5-phenyl-1H,3H,5H-pyrimidin 2,4,6 triol
Tn khc : Phenobarbitone, phenemalum
2. Tnh cht
- Bt kt tinh mu trng, ko mi, v ng, bn trong khng kh
- Kh tan trong nc, tan trong ethanol v 1 s dung mi hu c, tan trong
NaOH v cc dd kim khc
- Ha tnh: Phn ng ca nhm barbiturat, phn ng ca nhm phenyl,
3. nh tnh :
- Dng ph IR so snh ph chun, qut ph UV
- SKLM so snh vi cht chun
- bng cc phn ng ha hc:
+ Cc phn ng chung ca Barbiturat
o T/d vi NaOH ( un nng) NH3 AgNO3
o T/d vi NaOH ( long) Mui Na+ trng keo Phc mu tm.
+ Phn ng ca nhm phenyl 2+
Nitro ha: tc dng vi HNO3 dn cht + Co mu vng
Phn ng vi TT Marki HCHO/H2SO4
36
TI LIU THAM KHO
+ Phn ng ca N bc 2: t/dng vi dd NaNO2/ HCl hp cht N-Nitroso amin c mu vng

3. nh lng : pp A hoc B
a. Phng php A: o kim/ mt khan (trc tip)
- Ha tan / DMF (dimethyl formamid)
- L = dung dch kim LiOCH3 , NaOCH3
- Xc nh im tng ng = pp o th hoc ch th mu.
b. Phng php B: Thm AgNO3 d trong dung mi pyridine. Chun pyridinium nitrat to thnh =
NaOC2H5 0,1N
Ngoi ra cn c th nh lng = pp o quang
4. Tc dng, c ch tc dng:
- tc dng trn TKTW gy c ch TKTW. Ty thuc liu lng m thuc c t/dng an thn, gy ng,
chng ng kinh, chng co git
+ An thn (liu thp): thuc lm gim lo lng, bn chn, to cm gic thoi mi, d chu, d dng i vo
gic ng
+ Gy ng (liu trung bnh): to gic ng tng t gic ng sinh l nhng c nhiu gic m
+ Chng ng kinh: (liu trung bnh hoc liu cao) thuc c tc dng chng ng kinh cn ln v ng
kinh cc b
- Tc dng trn cc c quan :
+ Liu T : gim nh hot ng ca cc c quan.
+ Liu cao: c ch tun hon, h hp, gin c trn. Gim chuyn ha,gim thn nhit, gim bi niu.
- Ngoi ra cn ca t/dng lm gim tc dng thuc kch thch TKT, tng tc dng thuc c ch TKT.
- C ch : c ch TKTW = cch to thun li cho acid gama-amino-butyric (GABA) gn vo receptor
GABA lm knh Cl- m ra, Cl- vo t bo gy tng lu cc lm tng c ch TKTW.
Ngoi ra, Phenobarbital cn tng cng cht dn truyn c ch glycin hoc (-) cht dn truyn kch
thch l acid glutamic, nng cao (-) knh Na+.
5. Dc ng hc:
- hp thu tt qua ng tiu ha. C th tim tnh mch nu cn, ko tim bp, tim di da v gy au v
d gy hoi t ni tim
- Sau khi ung 60 pht xut hin t/dng, duy tr c 8 12h
- lin kt vi protein huyt tng khong 50%, phn b rng cc m, no, qua c nhau thai, s m
- chuyn ha gan to cht chuyn ha ko hot tnh
- thi tr qua nc tiu
6. ch nh :
- co git, ng kinh cn ln, phng co git st cao tr nh
- tin m
- cc trng thi thn kinh b kch thch, lo u, cng thng
- cc trng thi mt ng nng,
- tng bilirubin huyt, vng da tr s sinh
- phi hp vi cc thuc khc iu tr cn au tht ngc, au na u, nhi mu no
7. Tc dng MM:
- bun ng, ng g, chng mt, mt iu ha ng tc,
- Ri lon chuyn ha porphyrin, d ng, gim hng cu.
8. Chng ch nh: suy h hp, suy gan nng, Ri lon chuyn ha porphyrin
9. Tng tc thuc:
- phenobarbital l cht gy cm ng mnh cc enzym chuyn ha thuc CYP450 v vy lm gim hoc
mt tc dng ca nhiu thuc phi hp: thuc chng ng mu dn xut coumarin, sulfamid chng tiu
ng, corticoid..
- cc thuc lm tng tc dng ca phenobarbital : thuc an TK, thuc c ch TK.
10. Ch phm, liu dng: ch phm Gardenal, vin nn 15,50 v 100mg. dng tim ng 1ml cha 200mg
Liu dng: an thn : 30 -120mg/24h; gy ng : 100 320mg trc khi ng; chng co git: 100
300mg/24h chia 2 3 ln
37
TI LIU THAM KHO
Chuyn 9: THUC CHNG NM.
I- I CNG V BNH:.
- Nhim nm l mt bnh ph bin, c th xy ra b mt c th hay su trong ni tng. Nguy c nhim
nm tng ln khi c th gim sc khng nh nhim HIV, cy ghp c quan, dng corticoid ko di,
m lu ngy
- Nm gy tn thng b mt: da, lng, tc, mng v.v thng gp cc loi nm nh Epidermophyton,
Microsporum, Trichophyton
- Nm gy tn thng ni tng: no, tim, phi, gan, rutv.v thng gp cc loi nm nh Aspegillus,
Candida, Histoplasma capsulatum
- Cc t chc nm pht trin chm v thng tn ti cc m kh thm thuc iu tr cc bnh nm
thng lu di v kh hn cc bnh nhim khun.
Phn loi:
* Da vo v tr tc dng: chia lm 2 nhm
+ Thuc tr nm b mt: Ketoconazol, Clotrimazol, Miconazol, Griseofulvin, Nystatin
+ Thuc tr nm ni tng: Amphotericin B, Ketoconazol, Fluconazol, Itraconazol
* Da vo cu trc ha hc: chia thnh 5 nhm.
+ Nhm Polyen: Amphotericin B, Nystatin, Natamycin.
+ Nhm Griseofulvin: Griseofulvin.
+ Nhm Flucytosin: Flucytosin.
+ Nhm Azol: Ketocnazol, Clotrimazol, Fluconazol
+ Cc thuc khc: Naftilin, Haloprogin, a. Benzoic, a. Salicylic.
III- C C THUC C TH:
1. FLUCONAZOL
Tn khoa hc: -(2,4-difluorophenyl)--(1H-1,2,4-triazol-1-yl-methyl)-1H-1,2,4-triazol-1-ethanol
Bit dc: Diflucan
1/ Ngun gc: Tng hp ha hc.
2/ Tnh cht.
- Bt kt tinh trng, hoc hu nh trng.
- tan: + Kh tan trong nc v ethanol
- Tn/c = 139oC.
- Ha tnh: nhn thm, tnh base rt yu
3/ im nghim.
a. nh tnh:
- o ph IR, ph UV ri so vi cht chun.
- SKLM
b. nh lng:- o ph t ngoi UV. PP o quang
4/ Dc ng hc.
- Hp thu: Tt qua ng tiu ha, ko b nh hng bi thc n v pH dch d dy
- Phn b: hu ht cc dch trong c th k c dch no ty
- Chuyn ha, thi tr: Chuyn ha gan.
- Thi tr qua nc tiu, T1/2 = 25 30h.
5/ Tc dng: c t/dng tt vi hu ht cc hng nm candida, k c nhim nm giai on cui ca
bnh nhn AIDS khng thuc
6/ Ch nh.
- nhim nm mng no do Cryptococus
- Nhim nm candida thc qun bnh nhn AIDS.
7/ Tc dng KMM: Bun nn, nn, au bng tiu chy, ban da v tng enzym gan
8/ Tng tc thuc: lm tng nng phenytoin trong mu nn lm tng c tnh ca phenytoin
9/ Ch phm, liu dng.
- Vin nn 200mg, hn dch 100mg/ 5ml, kem bi 2%, du gi 2%.
- Liu dng:
Tr nm ng tiu ha: 50mg/ln/24h trong 1 5 tun
Tr nm ton thn: 200 - 400mg/ln/24h trong 4 6 tun
Tr nm m o:liu duy nht 150mg
38
TI LIU THAM KHO
2. AMPHOTERICIN B
OH
H3C O OH OH
O OH OH OH OH
HO O OH
CH3
H O
H3C
O
OH NH2
H3C
O OH
Bit dc: Fungizone, Amphocin.

1- Ngun gc.
- c phn lp t x khun Streptomyces nodusus.
2- Tnh cht.
* L tnh:
- Bt kt tinh mu vng hoc vng cam.
- tan: + Khng tan / H2O v EtOH.
+ Tan trong dimethylsulphoxid v propylen glycol.
+ Rt kh tan trong trong MeOH.
- hp th UV, IR c trng
- c gc quay cc
* Ha tnh:
- Dy ni i lin hp nh tnh, nh lng bng o UV.
- Nhm NH2 tnh base.
- Nhm COOH tnh acid to mui hi tan/ H2O khi tc dng vi NaOH; HCl.
3- nh tnh
* nh tnh :
- o IR, so snh vi ph chun. qut UV
- o gc quay cc, SKLM
* nh lng bng phng php vi sinh vt; pp o quang, HPLC
4- Dc ng hc.
- Hp thu km qua ng tiu ha dng ng ung tr nm ng tiu ha.Tim TM tr nm
ton thn.
- Phn b: vo dch no ty t.
- Thi tr: bi tit chm qua thn, T1/2 = 24h.
5- Tc dng v c ch.
* Tc dng.
- Ph khng nm rng, tc dng c nm b mt v ni tng nh : Candida, Cryptococcus, Aspergillus,
Histoplasma
- Nng /c ti thiu vi cc loi nm t 0,03 - 1g/ ml.
* C ch: Thuc gn vo Ergosterol trn mng t bo nm thay i tnh thm ca mng t bo vi cc
ion K+ , Mg++ t bo nm b tiu dit.
6- Ch nh.
- Nm b mt: da, nim mc, ming, m o
- Nm ni tng: cc chng nhy cm = ng tim.
- D phng v iu tr nm cho bnh nhn suy gim min dch.
7- Tc dng MM.
- Phn ng chung: + st, rt run, au u, au c khp
+ Dng trc khng H1 hay Glucorticoid ngn chn td ny.
- c vi thn: gim sc lc cu thn, hoi t ng thn
- Tc dng KoMM khc: + c vi gan, thn
+ Thiu mu, gim K+ , Mg++ mu.
+ au, vim tc TM ni tim.
8- Tng tc thuc.
- Tng c tnh vi thn khi phi hp vi Aminosid, Cyclosporin
- Tng tc dng v c tnh vi mt s thuc nh Digitalis, Suxamethonium.
9- Ch phm, lu dng.
- Dng ung: + Vin nn 100mg
+ Hn dch, siro 10mg, 100mg/ ml
39
TI LIU THAM KHO
- Dng tim: + L thuc bt 50mg.

+ Dng Liposom hoc phc hp vi lipid: hn dch 100mg/ 20ml.
- Dng dng ngoi.
* Liu dng:
- Khi u 0,25mg/ kg, sau tng ln 1,5mg/ kg.
Ung 100 200mg/ ln x 4 ln/ ngy.
Chuyn 10: THUC PHNG V IU TR ST RT

I- I CNG V BNH:
1- Bnh st rt:
- L bnh truyn nhim do KST st rt Plasmodium gy ra.
- C 4 loi Plasmodium: P. falciparum ;P. Vivax ; P. Malariae ; P. ovale
- Vit Nam bnh st rt ch yu do P.falciparum ( 80-85%), thng gy st rt c tnh, P. vivax ( 15-
20% ).
- Bnh st rt ly truyn qua ng mu:
+ Qua cn trng trung gian: mui Anophen.
+ Qua ng truyn mu.
+ Ly t m sang con lc mang thai.
2- Chu k pht trin ca ST: 4 giai on.
2.1 Chu k tin hng cu;
Khi mui t, thoa trng truyn t muingi t bo gan pht trin thnh KST non (th phn lit
m ).
2.2 Chu k hng cu:
- KST non vo mu chui vo TB hng cu pht trin thnh th phn lit hng cu ph v
hng cu ra ngoi, tip tc chui vo hng cu khc gy cn st rt c chu k.
- Thi gian 1 chu k hng cu ca P. falciparum v P. vivax l 48h, Malariae l 72h.
2.3 Chu k ngoi hng cu:
- Vi P. vivax v malariae , sau chu k tin hng cu, mt s KST li gan pht trin thnh th n
gy st rt ti pht.
2.4 Th giao t ( th hu tnh )
- Mt s KST li huyt thanh pht trin thnh giao t. Khi mui ht mu giao t vo c th mui
pht trin thnh thoa trng c tr tuyn nc bt mui tip tc truyn bnh cho ngi khc.
1- Phn loi:
- Thuc ct cn st ( dit th phn lit trong H/C ): Quinin, Cloroquin, Artesunat.
- Thuc chng ti pht ( dit th v tnh chu k ngoi H/C ) : Primaquin.
- Thuc chng ly truyn ( dit giao t ) : Primaquin.
- Thuc d phng ( dit th v tnh chu k tin H/C ) : Chloroquin, Fansidar
2- Nguyn tc iu tri:
- Chn on v iu tr sm.
- Dng thuc c mc tiu, liu.
- iu tr trit , ton din.
3- Phc iu tr:
3.1 iu tr st rt thng:
Cch la chn thuc:
Nhm bnh Nghi st rt St rt do St rt do St rt nhim phi

nhn P.falciparum P.vivax hp
Di 3 tui Artesunat or Artesunat Chloroquin Artesunat
Chloroquin
T trn 3 tui Artesunat or CV-8 hoc Chloroquin + Artesunat +
Chloroquin Artesunat + Primaquin Primaquin
Primaquin
PNCT < 3 Artesunat or Quinin Chloroquin Quinin
thng Chloroquin
PNCT > 3 Artesunat or Artesunat Chloroquin Artesunat
thng Chloroquin
40
TI LIU THAM KHO
* iu tr ct cn:
- Vi P.vivax, P.malariae: Chloroquin.
- Vi P.falciparum: + cha khng thuc: Chloroquin, Fansidar
+ khng thuc: Quinin, Artesunat, Artemisinin + Mefloquin
* iu tr tit cn, dit giao bo
- Vi P.vivax: Primaquin ( Ko dng cho PNCT v tr em < 12 tui ).
- Vi P.falciparum: Pimaquin dng 1 liu 4 vin/24h.
3.2 iu tr st rt c tnh:
S dng u tin cc thuc:
+ Artesunat: l tim 60mg, vin n 50, 100mg
+ Quinin dihydroclorid hoc Quinin hydroclorid ng 500mg.
3.3 D phng st rt:
- PNCT ung 2 vin Chloroquin/ tun trong sut thai k.
- Khch du lch, ngi n cng tc ( trong vng 6 thng ): ung hng tun trong thi gian vng st rt,
v 4 tun sau khi ra khi vng st rt. Ung Mefloquin hoc Chloroquin nu KST SR cn nhy cm.
- Ngi mi n nh c vng st rt: ung trong vng 6 hng u, dng Mefloquin hoc Chloroquin
nu KST SR cn nhy cm.
III- THUC C TH :
1. QUININ
Tn khoa hc: 6-methoxyquinolin-4-yl)-(5-ethenyl-1-azabicyclo [2.2.2] oct-2-yl) methanol
Bit dc: quinamin
1- iu ch: l alcaliod chnh phn lp t v cy canh ki na
2- Tnh cht.
-quinin c tnh base, hp th UV, IR c trng.
3- im nghim.
* nh tnh:
- SKLM
- Qut ph UV, o IR so snh cht chun
- Phn ng To ta vi TT chung ca Alcaloid
* nh lng:
- o acid trong mi trng khan: ha tan / CH3COOH; nh lng = 1 acid mnh HClO4 0,1M; pht hin
im tng ng = cch o th or ch th mu tm tinh th.
- o quang
4- Dc ng hc.
Hp thu: qua ng ung, tim. t C max trong mu sau 1 -3 h
Phn b: gan, lch, phi. thuc qua c nhau thai v sa m. Lin kt vi protein huyt tng 90%.
Chuyn ha: gan
Thi tr: Thi tr ch yu qua nc tiu dng chuyn ha, T1/2 = 11h
5- Tc dng, c ch.
* Tc dng:
- Vi KST SR: t/dng dit th phn lit trong mu ca tt c cc KST st rt. Thuc ct cn nhanh v t
b khng. Qiunin c tc dng c vi KST khng cloroquin. Ngoi ra cn c tc dng dit c th giao
t ca: P.vivax, P.malariae
- Tc dng khc:
+ Trn TKTW: liu nh kch thch nh, liu cao c ch gy bun ng, gim au, tc dng hip ng vi
cc thuc c ch TK khc
+ Trn thn nhit: h st
+ trn tun hon: liu cao gy c ch tim, gin mch v h HA
+ trn c trn: lm tng co bp c trn t cung
+ trn tiu ha: lm tng tit dch tiu ha, liu nh gip n ngon d tiu, liu cao gy bun nn, tiu chy
* C ch:Nhn quinolein trong phn t quinin gn vo chui AND ca KST lm mt kh nng tch i v
sao chp m di truyn
6- Ch nh: Dit th phn lit trong mu c bit l P.falciparum khng chloroquin v cc thuc khc
7- Tc dng MM.
- nhc u, bun nn, nn, ri la th gic, chng mt, tai, d ng, gim bch cu, mt bch cu ht
8- Chng ch nh.
41
TI LIU THAM KHO
-bnh nhn tai, vim dy thn kinh th gic, ngi nhc c v ang mang thai
9- Ch phm, liu dng.
Vin nang quinin sulfat 200, 300, 320 mg, vin nn 260, 325mg; thuc tim quinin dihydroclorid
Li dng: theo cn nng 30mg/kg/24h x 7 ngy
2. MEFLOQUIN
6
7 5
H OH H
8
N
CF3 4
3
HCl
N 2
CF3
Tn khoa hc: [2,8-bis (trifuoromethyl)quinolin-4-yl](piperidin-2-yl) mathanol HCl
Bit dc: Lariam, Mephaquin.
1- Ngun gc: Tng hp ha hc.
2- Tnh cht.
* L tnh: Bt kt tinh trng hoc hi vng.Rt kh tan trong nc. D tan MeOH, tan trong EtOH. Hp
th UV, IR c trng
* Ha tnh: Tnh base, ha tnh ca HCl, nhn thm
3- im nghim
* nh tnh:
- Ch phm / H2SO4 c hunh quang xanh.
- o IR so snh cht chun, qut ph UV, SKLM.
- Xc nh Cl- bng AgNO3 ; to kt ta trng AgCl
- Xc nh F- bng CaCl2 CaF2 khng tan trong a.acetic long
* nh lng:
- o quang
im tng ng = cch o th or ch th mu tm tinh th.
4- Dc ng hc.
Hp thu: + ng ung SKD 80%, thc n lm tng hp thu.
+ ng tim gy kch ng mnh.
Phn b: + Lin kt protein huyt tng 98%.
+ Phn b rng ri trong c th, nht l gan, phi.
Thi tr: Chm v ch yu qua phn, T1/2 = 20 ngy.
5- Tc dng, c ch.
Tc dng:
- Dit th phn lit trong mu ca tt c cc KST, k c P.falciparum khng Chloroquin.
- thuc khng c tc dng ln giai on ngoi hng cu.
C ch:
+ c ch khu ly thc n ca KST.
+ To phc vi Hem ph v mng t bo KST.
+ Tng pH trong KST, ngn cn s xm nhp thuc vo trong hng cu
6- Ch nh.
- Phng v iu tr st rt do P.falciparum khng Chloroquin
- Tc dng chm v ko dng c ng tim ko thay th c Quinin trong iu tr st rt nng v
cp tnh.
7- Tc dng MM.
- Lu iu tr: RLTH nh, nhc u, chng mt.
- Liu cao: +RLTH nng, RL TK, tm thn, co git
+ RL th gic, thnh gic.
8- Chng ch nh.
- ng kinh v RL tm thn.
- Suy gan, thn nng.
- PNCT 3 thng u.
- Thn trng khi li xe v vn hnh my mc.
- Blook tim
42
TI LIU THAM KHO
9- Ch phm, liu dng.

- Lariam, Meflam: vin nn 250mg
- Fansimef: vin nn phi hp vi Fansidar.
- Liu dng: ngi ln ung 250mg/ ln x 1ln/ tun; hoc 1g/ 1thng.
10- Tng tc thuc.
- Phi hp vi Quinin, Quinidin / c adrenergic gy / c tim mch
3. ARTEMISININ V DN XUT
CH3
H3C
O O
O
O
CH3
O
1- Ngun gc: Chit xut t l Thanh cao hoa vng.
2- Tnh cht.
* L tnh: Bt kt tinh mu trng hoc tinh th hnh kim khng mu. khng mi, v ng.
tan: - Khng tan trong nc, tan trong MeOH, EtOH, Cloroform, D tan trong aceton, ethylacetat.
Hp th UV, IR c trng, c gc quay cc ring
* Ha tnh:
- Nhm chc lacton: ng dng tnh, lng
+ Thy phn = dd NaOH, lng NaOH d
+ Thy phn = dd NaOH, dch bn acetal cho phn ng vi AgNO3, TT Fehling.
+ Td vi NH2OH to acid hydroxamic, sau cho mu tm vi FeCl3.
- Nhm chc peroxyd: Tnh oxy ha (t, l).
+ Td vi KI iod ( mu nu)
+ Td vi sulfocromic to acid percromic tan trong ether cho lp ether mu xanh.
- Nhm chc C=O: Kh ha thnh DHA c tc dng mnh hn t bn tng hp cc dn cht tc
dng tt hn nh Artesunat; artemether; arteether.
* nh tnh, nh lng:
- Da vo cc phn ng trn
- o IR so snh vi ph chun. qut ph UV
- SKLM, o gc quay cc
nh lng:
- L = pp o quang, HPLC
- Thy phn = NaOH, nh lng NaOH d = pp tha tr
- L = PP o Iod to thnh
3- Dc ng hc.
* Hp thu:
- Artemisinin:
+ t tan trong nc dng ng ung v ng trc trng.
+ Ct cn nhanh, nhng thi tr qu nhanh t l ti pht cao.
- Artesunat:
+ Bn tng hp t Artemisinin
+ Tan trong nc dng ng tim TM.
- Artemether:
+ Bn tng hp t Artemisinin
+ Tan trong du dng ng tim bp.
* Phn b:
- Lin kt vi protein huyt tng 77%.
* Chuyn ha:
- Cc dn cht c chuyn ha thnh Dihydroartemisinin c td mnh > 5 ln Artemisinin
* Thi tr:
- Qua nc tiu.
4- Tc dng, c ch.
- Dit th phn lit trong mu ca mi KST SR, c bit SR th no do P.falciparum
- Khng dit c th giao bo.
43
TI LIU THAM KHO
- Khng tc dng ln giai on ngoi HC.

- Thi gian td ngn khng dng lm thuc d phng v chng ti pht.:
5- Ch nh: iu tr SR, ct cn SR.
6- Tc dng KMM: RLTH, nhc u, chng mt Chm nhp tim.
7- Chng ch nh: Khng dng cho PNCT < 3thng.
8- Ch phm, liu dng.
- Artemisinin:
+ Ung: ngy u 1g/ 24h chia 2ln, nhng ngy sau 500mg/ 24h x 4 ngy.
+ t hu mn: ngy u 1,25g/ 24h, nhng ngy sau 750mg/24h x 2-3 ngy.
- Artemether: ngy u 300mg/ 24h, nhng ngy sau 100mg/ 24h x 4 ngy.
Chuyn 11: THUC CHA GIUN S N

I- I CNG V BNH:
- Bnh giun sn ph bin trn th gii, ch yu cc nc km pht trin.
- Giun sn l ng vt a bo, k sinh nhiu c quan, ch yu l rut.
- nuc ta do kh hu nng m, iu kin v sinh km nhim giun sn rt cao.
- Cc loi giun sn khc nhau c s nhy cm khc nhau vi thuc xt nghim xc nh xem b
nhim loi giun sn no chn thuc cho ph hp.
* c im ca bnh giun sn:
1- Din bin lu di, nhiu thng, nhiu nm.
2- C thi hn nht nh (v giun sn ch tn ti trong mt chu k sinh sn)
3- Ph bin cc vng c iu kin thun li: kh hu nng m, VS mi trng km.
4- Tin trin m thm, lng l.
* Nguyn tc iu tr:
1- Kt hp iu tr vi phng bnh v ci to mi trng trnh ti nhim.
2- iu tr trn din rng, hng lot: c gia nh, c tp th, khu dn c.
3- S dng thuc ng vi tng loi giun sn b nhim.
4- Chn thuc t c c hiu qa, gi c ph hp vi cng ng.
II- i cng v nhm thuc.
* Thuc tr giun:
+ Trong lng rut: Mebendazol, Albendazol, Piperazin
+ Ngoi rut: Diethylcarbamazin, Suramin, Thiaendazol
* Thuc tr sn:
+ Trong lng rut: Niclosamid, Quinacrin
+ Ngoi rut: Praziquantel, Quinacrin, Chloroquin
III- THUC C TH.
1. ALBENDAZOL
O CH3
H
N O
6 1
2 NH
5 3
H3C 4
S N
Tn khoa hc: Methyl [5-(propylthio)- 1H-benzimidazol-2-yl) carbamat.
Bit dc: Zentel, Albenda, Albenza
2- Tnh cht:
* L tnh: Bt trng hoc hi vng. - Khng tan trong nc, EtOH, Ether. - Hp th UV, IR c trng
* Ha tnh: tnh base, ha tnh ca nhm chc ester, nhm chc amid, ha tnh ca nhn thm
3- im nghim.
* nh tnh:
+ o IR so snh vi cht chun, qut UV, SKLM
+ Bng cc phn ng nh tnh:
- Tnh base: Ch phm khng tan/ H2O, nhng khi thm HCl tan hon ton
- Nhm Amid: thy phn/ dd kim gii phng amin thm.
- Nhn thm: hp th UV.
- Ceton: cho mu vng m vi TT Dinitrobenzen/ EtOH.
- Nhm benzoyl: un si ch phm/ NaOH a.benzoic + FeCl3 kt ta mu hng tht.
* nh lng:
44
TI LIU THAM KHO
im tng ng = cch o th or ch th mu
- o quang, HPLC
4- Dc ng hc.
- Hp thu: Qua ng ung, SKD thp ( 20% ), Cht bo lm tng hp thu thuc.
- Thi tr: thi tr qua phn ( 90 95% ), Mt phn nh qua nc tiu.
5- Tc dng v c ch.
* Tc dng:
- Dit c nhiu loi giun: a, tc, mc, kim.
- Dit c trng giun v giun trng thnh.
- Liu cao c tc dng trn c nang sn v trng roi.
- Hiu qu iu tr: giun a, kim, tc 90-100%, giun mc 70%.
* C ch:
- c ch tng hp vi cu trc hnh ng /c s sinh sn ca giun.
- /c khng hi phc s hp thu glucose cn kit d tr glycogen thiu nng lng cho giun hot
ng.
6- Ch nh.
- Cc loi giun v u trng : ngi ln 400mg/ln, tr em 200mg/ln, liu duy nht
- Tr giun ln v sn dy: 400mg ln/ ngy t iu tr 3 14 ngy
- Tr nang sn: 10 - 15mg/kg/ngy chia 3 ln, t iu tr 28 ngy
- Tr u trng sn thn kinh: 5mg/kg/ngy x 3 ln/ngy, t iu tr 28 ngy
7- Chng ch nh: PNCT, Tr em < 2 tui, Mn cm vi thuc.
8- Tc dng KMM:
- RLTH: au bng, tiu chy, bun nn.
- Pht ban, nga.
- Td KMM ch yu do c t ca giun gii phng ra khi b phn hy.
9- Ch phm, liu dng: Zentel vin nn 200mg hoc 400mg, Hn dch ung 2% v 4% l 10ml.
2. NICLOSAMID
Cl
CONH NO2
OH
Cl
Tn khoa hc: 5-cloro-N-(2-cloro-4-nitrophenyl)-2-hydroxybenzamid.
Bit dc: Yomesan, Niclocide.
1- Ngun gc.
Tng hp ha hc.
COOH Cl Cl
OH
+ H2N PCl3
NO2 CONH NO2
To
Cl OH
Cl
5-cloro-salicylic 2-cloro-4-nitroanilin Niclosamid
2- Tnh cht.
* L tnh: Bt tinh th mn, mu hi vng.
Khng tan/ nc.t tan/ EtOH, CHCl3, ether, Tan/ aceton.
Hp th UV, IR c trng
* Ha tnh:
- Nhm OH phenol: + FeCl3 mui phc c mu.
- Nhm Amid:
+ un ch phm/ NaOH sn phm thy phn + Fe3+ to mu.
sn phm thy phn cho P to phm mu azo
45
TI LIU THAM KHO
- Nhm -NO2 : kh ha thnh amin thm nh tnh bng P to mu azo

- Nhn thm: hp th UV
3- im nghim.
* nh tnh:
- Da vo cc phn ng ha hc trn
- Bng pp qut ph UV, o hp th ring, SKLM.
* nh lng:
- L = PP o Nitric, xc nh im kt thc = o th
- L ion Cl- = pp trung ha
4- Dc ng hc: Hp thu rt t qua ng tiu ha.
5- Tc dng v c ch.
* Tc dng:
- Hp thu rt t qua rut iu tr sn k sinh trong lng rut.
- Tc dng vi cc lai sn dy.
- Khng c tc dng vi u trng cc m ngoi rut.
* C ch:Tc dng vo khu chuyn ha nng lng ca sn: /c tng hp Adenosin triphosphat ty
th. Cng c th do /c s hp thu glucose ca sn u v t sn b cht b tng ra ngoi theo
phn.
6- Ch nh: Cc loi sn k sinh trong rut.
7- Tc dng MM.
- RLTH: bun nn, nn, au bng, tiu chy.
- D ng: ban , mn nga.
8- Chng ch nh: TE di 4 tui, PNCT, cho con b.
9- Ch phm, liu dng.
- Ch phm: Niclocid, Cestocid vin nn 500mg
- Ung liu duy nht:
+ Ngui ln: 2g.
+ Tr em 11 34kg: 1g ; TE > 34kg: 1,5g
Ung bui sng lc i, nhai vin thuc vi mt t nc.
- Khng ung ru trc v sau khi ung thuc 1 ngy.
Chuyn 12: CC VITAMIN

I- I CNG V BNH:
1.1 nh ngha: Vitamin l nhng cht hu c, c th hu nh khng t tng hpc m phi a t
ngoi vo, vi mt lng rt nh so vi khu phn n hng ngy, c tc dng duy tr cc qu trnh
chuyn ha m bo s sinh trng v hot ng bnh thng ca c th.
1.2 Phn loi.
Da vo tan:
+ Vitamin tan trong du: A, D, E, K.
+ Vitamin tan trong nc: Cc vitamin nhm B, vitamin C, vitamin PP
1.3 Vai tr.
- Tham gia vo cu to enzym xc tc cho cc P chuyn ha trong c th.
V d: + Vit B1 l coenzym ca enzym chuyn ha Glucid
+ Vit B6 l coenzym ca enzym chuyn ha a.amin
- L tng sc khng, chng oxy ha, bo v cc t bo TK.
V d: Vitamin C, A, D, E, B12
- C vai tr tc ng qua li vi cc hormon:
V d: + Vit C vi hormon tuyn thng thn.
+ Vit B1 vi hormon sinh dc
+ Vit A, B1 vi tuyn gip, Vit D vi cn gip.
- Cc Vit c tc ng qua li vi nhau.
V d: khi thiu Vit B12 c th khng tng hp c acid Folic thiu mu.
1.4 Nhu cu v cc vitamin.
- Thay i ty theo la tui, gii tnh, sinh l ca c th.
- Khi thiu hay tha vitamin u gy ri lon chuyn ha ca c th.
* Nguyn nhn gy thiu vitamin:
- Do n ung khng
- Do nhu cu tng: PNCT, cho con b, ngi mi m dy.
46
TI LIU THAM KHO
- Do RL hp thu: ct d dy, bnh tiu chy ko di

- Do di truyn: thiu enzym hoc yu t hp thu.
- Dng cc thuc lm gim hp thu Vit.
* Nguyn nhn gy tha vitamin:
- Do lm dng thuc, thng l cc vit tan trong du.
- Do thc phm cha lng ln vit tan trong du: A, D, E, K.
1.5 c im chung ca cc vitamin.
* Cc vitamin tan trong du: A, D, E, K.
- Hp thu cng cc cht m vo vng tun hon chung.
- Qu trnh HT i hi phi c acid mt nh ha gip m tan vo trong mu.
- Khi dng qu liu tch ly trong m m ng c
- Do tch ly trong c th cc triu chng thng xut hin chm
- Bn vi nhit khng b ph hy khi nu nng.
* Cc vitamin tan trong nc: Cc vitamin nhm B, vitamin C, vitamin PP
- Hp thu rc tip qua thnh rut vo mu, khng cn cht nh ha.
- Lc c qua cu thn v thi tr qua nc tiu.
- Khng tch ly trong c th t gy c
II- THUC C TH:
1. THIAMIN (Vitamin B1)
H3C N
3 NH2 S1 CH2CH2OH
2 4 2 5
3 4 Cl-; HCl; ( Br-; HBr ); NO3-
1 5
N 6 N
+ CH3
Tn khoa hc: 3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-5-(2-hydroxyethyl)-4-methyl thiazolium chlorid
monohydroclorid (bromid hydrobromid; nitrat).
Bit dc:Aneurine, Betaxin, Biamin.
1- Ngun gc.
- thc vt: men bia, cm go, mm la m
- ng vt: tht, gan, trng
- iu ch: Tng hp ha hc gm 3 giai on.
+ G1: Tng hp dn cht Pyrimidin.
+ G2: Tng hp dn cht thiazol.
+ G3: Gn 2 cht vi nhau.
2- Tnh cht.
* L tnh:
- Tinh th khng mu hoc bt kt tinh trng nh.
- Mi ging men bia, v ng.
- D ht m khi tip xc vi khng kh, nh sng.
- tan: + D tan trong nc , kh tan trong EtOH, khng tan trong ether, benzen, cloroform.
* Ha tnh:
- Tnh base: phn ng dng tnh vi TT chung ca alkaloid ng dng trong nh tnh, nh lng
- Phn ng ca Cl-: Dd cho kt ta trng vi AgNO3
- P/ng ca ion Br- : Br + AgNO3 Vng
- Tnh cht ca pirimydin: T/dng vi acid silicovolframic trng
- Tnh cht vng thiazol: phn ng c trng ca vitamin B1
- Tnh cht nhm 2 hydroxyethyl : nhm ny d b ester ha hoc ether ha thiamin palmitat, thiamin
stearat, thiamin diphosphat
- Xc nh NO3- : tc dng vi FeSO4 m c + H2SO4 nh theo thnh ng nghim mt phn cch 2
lp c mu nu.
3- im nghim.
* nh tnh: nh tnh = SKLM, qut ph UV, bng cc phn ng ha hc trn
* nh lng:
- Phng php cn: To ta vi a. silicovolframic ri nh lng bng P2 cn.
47
TI LIU THAM KHO
- Phng php acid-base trong mi trng khan: ha tan / CH3COOH; nh lng = 1 acid mnh HClO4
0,1M; pht hin im tng ng = cch o th or ch th mu
- o quang, HPLC
4- Dc ng hc: D hp thu qua ng tiu ha. Thi tr qua nc tiu.
5- Tc dng.
- Tham gia vo chuyn ha Glucid.
+ B1 l coenzym ca E. Decarboxylase, xc tc cho P kh nhm carboxyl ca acid cetonic.
+ B1 l coenzym ca E. Transketalase, xc tc cho P chuyn nhm ceton trong chuyn ha Glucid.
- Thiu B1 ng cc cht cetonic trong mu RL chuyn ha t ph, suy tim, vim dy TK.
6- Tc dng KMM: D ng, c th Shock khi tim TM
7- Ch nh.
- Phng v iu tr bnh Beri-beri
- iu tr vim dy TK hng, cc dy TK ngoi bin
- Cc trng hp mt mi, km n, RLTH, suy dinh dng
8- Ch phm, liu dng.
- Ch phm: dng mui HCl, vin nn 100,500mg; thuc tim 100 v 200mg
- Liu dng: + Tr bnh Beri-beri: 40 - 100mg/ 24h
+ au dy TK: 100 500mg/ 24h.
2. PYRIDOXIN ( Vitamin B6)

N CH3
HCl
HOH2C OH
CH2OH
Tn khoa hc: (5-hydroxy-6-methylpyridin-3,4diyl) dimethanol hydroclorid.
Bit dc: Beesix, Doxine, Nestrex, Pyri
1- Ngun gc: C nhiu trong tht, gan, ng cc, rau qu
- iu ch: Tng hp ha hc.
2- Tnh cht.
* L tnh: Tinh th khng mu, hoc bt kt tinh trng.
- tan: + D tan trong nc, tan trong EtOH; Khng tan trong ether, cloroform
* Ha tnh:
- Nhn Pyridin:
+ Tnh base: + tc dng vi acid to mui.
+ To ta vi a. Silicovolframic, a. Phosphovolframic
+ Hp th UV
- Nhm Hydroxyphenol:
+ tnh acid: tan trong dd kim, tc dng vi Fe3+ to mu .
+ Tnh kh: D b oxy ha do tia UV bo qun trong l thy tinh mu, trnh as.
+ P th vo C6 , tc dng vi mui diazoni phm mu nit.
- Nhm methanol C5 : Khi vo c th, nhm ny b ester ha bi a. Phosphoric Pyridoxal phosphat
l 1 coenzym ca nhiu enzym xc tc cho qu trnh chuyn ha cc a.amin, hydratcarbon, cht bo.
3- im nghim.
* nh tnh: nh tnh = SKLM, qut ph UV, bng cc phn ng ha hc trn
* nh lng:
- Phng php cn: To ta vi a. silicovolframic ri nh lng bng P2 cn.
- Phng php acid-base trong mi trng khan: ha tan / CH3COOH; nh lng = 1 acid mnh HClO4
0,1M; pht hin im tng ng = cch o th or ch th mu
- o quang, HPLC
4- Dc ng hc.
- Hp thu: d HT qua ng tiu ha. - Chuyn ha gan thnh cht khng cn hot tnh.
- Thi tr ch yu qua nc tiu.
5- Tc dng.
- B6 ch yu tham gia vo chuyn ha a.amin, l coenzym ca cc enzym sau:
+ Transaminase ( SGOT v SGPT ): cc E ny chuyn nhm NH2 ca acid amin acid cetonic.
+ Decarboxylase:
48
TI LIU THAM KHO
Kh nhm CO2 chuyn acid Glutamic acid Gama aminobutyric (GABA) l cht dn truyn /c
TK
xc tc cho P chuyn Histidin Histamin ; Tryptophan Serotonin, l 2 cht c vai tr sinh l quan
trng.
+ Cynureninase: xc tc cho P chuyn Tryptophan a. Nicotinic.
+ Racemase: - Chuyn cc a.amin dng c hot tnh.
- Tng hp a. Arachidonic, tng hp Hem.
- Tham gia vo chuyn ha Lipid, Glucid, chuyn Protid Glucid, Lipid
6- Ch nh.
- Phng v iu tr cc trng hp thiu Vit B6
- Phng v iu tri mt s bnh TK do thuc nh Rimifon
7- Ch phm, liu dng.
- Ch phm: vin nn t 5 500mg, ng tim 100mg/ ml.
- Liu dng:
+ Phng bnh: ngi ln 2 2,5mg/ 24h, TE 2mg/ 24h.
+ iu tr: 50 1000mg/ 24h ty thuc mc ca bnh
3. ACID ASCORBIC
CH2OH
HCOH
O
O
OH OH
Tn khoa hc: 5-(1,2-dihydroxyethyl)-3,4-dihydroxy-5H-furan-2-on.
Tn khc: Vitamin C.
1- Ngun gc.
- C nhiu trong thc n thc vt nh: chanh, cam, qut, du, da hu , mt lng nh trong ng
vt.
- Tng hp ha hc.
2- Tnh cht.
* L tnh:
- Tinh th hoc bt kt tinh trng hoc hi vng, tip xc vi as s b vng dn.
- Trng thi kh Vit C kh bn vi khng kh, dng Dd nhanh chng b oxy ha.
- tan: + tan trong nc v EtOH, Khng tan trong ether, benzen, cloroform.
* Ha tnh:
- Ca nhm chc lacton
- Ca nhm hydroxy
- Ca dy ni i
- Quan trng nht l nhm endiol quyt nh ha tnh c bn ca Vit C : tnh acid v tnh kh ( d bi
oxy ha )
+ Tnh acid:
- D tan trong ccdung dch kim.
- Tc dng vi mui to mui mi
- /dng iu ch mui Ascorbat natri d tan trong nc iu ch dung dch tim c nng cao
v pH gn nh trung tnh.
- Tc dng vi Fe2+ hoc Fe3+ mui mu tm, ng dng nh tnh, nh lng
+ Tnh kh: Vic oxy ha acid Ascorbic xy ra 2 mc khc nhau:
* S oxy ha thun nghch Vit C thnh acid Dehydroascorbic tham gia xc tc cc qu trnh oxy
ha kh xy ra trong c th dng Vit C bo qun thc phm
49
TI LIU THAM KHO
CH2OH CH2OH
HCOH HOCH
O [O] O
O O
[H]
OH OH O O
* S oxy ha bt thun nghch bin Vit C Furfurol; 2,3-dicetogulonic, CO2 , H2O l nhng cht
khng c hot tnh v bin mu bo qun trong l thy tinh mu, trnh as
CH2OH
HCOH O
O O
O [O] C
H
OH OH Furfurol
3- im nghim.
* nh tnh:
- Ascorbic + vi Fe2+ hoc Fe3+ mui mu tm
- Lm mt mu xanh ca 2,6 diclorophenol indophenol, lm mt mu ca dd Iod, mt mu dd KMnO4
nh lng:
- nh lng = pp o kim, ch th l phenolphthalein, dung mi l nc.
- nh lng = pp o iod, chun = 2,6-diclorophenol indophenol
- PP o quang; PP so snh ph chun
4- Dc ng hc.
- Hp thu: hp thu d dng qua nim mc rut non.
- Phn b: vo hu ht cc m c bit tuyn yn, thng thn, no, bch cu.
- Thi tr: ch yu qua nc tiu di dng chuyn ha l Oxalat v Urat.
5- Tc dng, c ch.
Vit C tham gia vo nhiu qu trnh chuyn ha ca c th:
- Tham gia to colagen v mt s thnh phn khc to nn m lin kt xng, rng, mch mu
thiu vit C thnh mch mu ko bn chy mu chn rng, mng xng rng d rng
- Tham gia chuyn ha lipid, protid, glucid
- Tham gia tng hp cc catecholamin, hormon v thng thn.
- Xc tc cho qu trnh chuyn Fe3+ Fe2+ nn gip cho Fe2+ c hp thu hnh t trng ; v vy nu
thiu vit C thiu mu do thiu st.
- Tng to Interferon, lm gim nhy cm ca c th vi Histamin, chng li Stress gip c th tng sc
khng.
- Chng oxy ha bng cch trung ha cc gc t do bo v c ton vn mng t bo.
6- Ch nh.
- Phng v iu tr bnh thiu vit C (bnh Scorbut )
- Tng sc khng ca c th khi nhim c, nhim khun.
- Thiu mu.
- Phi hp vi cc thuc chng d ng.
7- Tc dng MM. Thng gp khi dng liu cao ko di:
- Lot d dy t trng, vim bng quang, tiu chy.
- Tng to si thn v bnh gout
- Shock phn v khi tim TM
- Tim TM liu cao d gy tan mu, gim bn HC.
8- Ch phm, liu dng.
- Ch phm: + vin nn, vin si 100, 200, 500, 1000mg
+ Dung dch tim 5%, 10% ng 1ml. 2ml, 5ml.
+ Dng ko ngm, phi hp vi cc vitamin khc.
- Liu dng: + D phng: 50 100mg/ 24h
+ iu tr: 200 500/ 24h
+ Chng Stress, tng sc khng dng liu cao hn nhng < 1g/ 24h.
50
TI LIU THAM KHO
4. VITAMIN A
CH3 CH3
H3C CH3 CH2OH
1 7 9 11 13 15
2 6 12
8 10 14
3 5
4
CH3 Retinol all trans
Tn khoa hc: Vitamin A l tn chung ch nhiu cht c hot tnh sinh hc tng t nhau, cht
thng c gi l vitamin A l Retinol.
1- Ngun gc.
- Trong ng vt: nhiu trong gan c thu, trng, c, tht, sa
- Trong thc vt: trong qa gc, c chua, c rt, rau xanh
* iu ch vitamin A:
- Phn lp t du gan c.
- Tng hp ha hc:
H CH3
O
C C CH C O O
Aceton
Citral Pseudoionon Beta ionon Vitamin A
H
2- Tnh cht.
* L tnh:
- L nhng tinh th hoc bn mng mu vng nht.
- tan: + Khng tan trong nc. Tan trong EtOH v cc dung mi hu c.
* Ha tnh:
- Do c dy ni i vit A d b oxy ha khng bn trong khng kh, nh sng bo qun ng
trong l mu, kn, trnh AS + thm cht chng oxy ha nh Tocoferol.
- Dy ni i lun phin hp th UV mu hi vng; ng dng nh tnh, nh lng
- Nhm alcol bc nht d ether, ester ha dng ester bn vng vi tc nhn oxy ha dng dc
dng l Retinol acetat, Retinol palmitat.
- Nhm alcol gn vi dy ni i lun phin vit A d b ph hy trong mi trng acid anhydro
vitamin A khng c hat tnh.
- Dy ni i lun phin kt thc bng nhm alcol vit A d to phm mu vi cc acid mnh nh a.
Percloric /d nh tnh, nh lng.
* nh tnh, nh lng:
- Bng cc phn ng nh trn
- nh lng = pp o quang, HPLC
3- Dc ng hc.
- Hp thu: qua ng ung v ng tim. hp thu Qua ng ung c th cn c acid mt lm
cht nh ha
- Phn b: Lin kt vi protein huyt tng ( globulin) vi t l thp.Vo cc t chc ca c th, d tr
nhiu gan
- Thi tr qua thn v qua mt.
4- Tc dng v c ch.
* Trn mt: To sc t vng mc gip iu tit mt lm cho mt nhn c trong iu kin thiu nh
sng.
C ch: + Trong bng ti: vit A (cis retinal) + Opsin sc t vng mc Rhodopsin l sc t nhy cm
vi nh sng c cng yu.
+ Khi ra nh sng: Rhodopsin b phn hy Opsin + Trans retinal. Sau trans retinal
chuyn dng thnh cis retinal.
+ Thiu vit A gim kh nng nhn trong bng ti bnh qung g.
* Trn da v nim mc:
+ Vit A cn thit cho qu trnh bit ha t bo biu m da v nim mc bo v s ton vn ca
cu trc v chc nng ca biu m nht l biu m tr ca mt.
+ Vit A lm tng tit cht nhy v /c s sng ha; nu thiu A gim tit cht nhy biu m b
keratin ha da b dy, kh, nt n.
* Trn xng:
51
TI LIU THAM KHO
+ Vit A cng Vit D gip cho s pht trin ca xng, nht l tr em.
+ Khi thiu Vit A tr em s b ci xng, chm ln.
* Trn h min dch:
+ Gip pht trin lch v tuyn c to ra lympho bo, tng tng hp protein min dch.
+ Vit A v tin Caroten c tc dng chng oxy ha, tng sc khng ca c th.
+ Khi thiu Vit A cn lm cho ng h hp, tit niu d b tn thng, thiu mu nhc sc.
5- Ch nh.
- iu tr v d phng cc triu chng thiu Vit A:
+ Cc bnh v mt: kh mt, qung g, vim lot gic mc.
+ Cc bnh v da: da kh, trng c, vy nn, vt thng lu lnh.
+ Tr em chm ln, ci xng, suy dinh dng.
+ B xung Vit A cho ngi x gan nguyn pht, tc mt, mt.
6- Chng ch nh.
- Tha Vit A v mn cm vi Vit A.
- Khng dng Vit A liu cao cho PNCT.
7- Tc dng MM.
- Ng c cp: + khi dng liu rt cao: ngi ln > 1.500.000UI/ ngy; TE > 300.000UI/ ngy.
+ Du hiu ng c: hoa mt, chng mt, bun nn, kch thch,nhc u, m sng,
cogit; tr em c th phng thp, co git.
- Ng c mn: + Khi dng liu cao 100.000UI/ ngy lin tc 10-15 ngy.
+ Du hiu c trng: mt mi, d kch thch, chn n, st cn, RLTH, gan lch to, mi
nt n, tc mng kh gin d gy, chy mu, thiu mutr em tng p lc ni s, ngng pht trin
xng di, PNCT d b qui thai.
8- Ch phm, liu dng.
- Ch phm: + Retinol vin nang cng, nang mm 5000UI, 50000UI.
+ ng tim 20.000; 50.000; 100.000UI
+ Vin nang phi hp Vit D: 5000UI Vit A + 400UI Vit D.
- Liu dng: + Phng thiu Vit A: 5000-10.000UI/ ngy.
+ iu tr thiu Vit A: 30.000UI/ ngy, dng trong 1 tun
5. VITAMIN D
Tn khc: Calciferol.
21 26
H3C 22 23 CH3 CH3
24 H3C
20 25
12 CH CH3
18 27 3
17
11 13 16
15
hv
19 14
1 9 8
2 10
3 7
4
HO 5 HO
6
7-dehydrocholesterol Previtamin D3
H3C CH3
CH3
CH2
HO
Vitamin D3
1- Ngun gc.
- C trong thc n ngun gc ng vt: lng trng, b sa, du c tht di dng tin Vit D nh
Ergosterol
- ngi 7-dehydrocholesterol c trong t chc lipid di da, di tc dng ca tia t ngoi vitamin
D
- iu ch: s trn; vit D gm cc cht t D2 n D7, nhng 2 vitamin hay c s dng l vitamin
D2 ( Ergocalciferol ) v D3 ( Cholecalciferol )
52
TI LIU THAM KHO
- Vitamin D3 ( cholecalciferol ) cha c hot tnh sinh hc, vo c th n b hydroxyl ha Calcifediol ,

cht ny n thn , do tc dng ca E. 1--hydroxylase Calcitriol c tc dng. Hot tnh ca enzym
ny c iu ha bi nng Calci, phosphat, vit D n vo v c kch thch bi hormon tuyn cn
gip.
H3C CH3
OH
CH3
OH CH
2
HO
Calcitriol
2- Tnh cht.
* L hc:
- Tinh th hnh kim, khng mu,khng mi
- tan: Khng tan trong nc, tan trong cc dung mi hu c ether, cloroform
- Hp th UV
* Ha tnh:
- H dy ni i:
+ D b oxy ha bi To, khng kh nht l khi c mt mui v c nh tricalci phosphat Ca3(PO4)2
khng nn dng dng vin c thm mui v c, tt nht l dung dch du v n bn vng hn.
+ Hp th bc x t ngoi nh tnh, nh lng bng o UV
+ Vit D tc dng vi Stibi triclorid/ cloroform mu vng cam ( T, .lng )
- Cu trc kiu Sterol:
+ Vit D tc dng vi H2SO4/ cloroform + anhydrid acetic mu chuyn dn sang tm ri sang xanh
nh tnh.
+ Km bn/ acid; bn trong mi trng kim, trung tnh.
* nh tnh, nh lng:
- Bng cc phn ng nh trn
3- Dc ng hc.
- Hp thu: Qua nim mc rut nh mui mt v lipid.
- Phn b: Lin kt vi globulin huyt tng, tch ly gan, xng, c, nim mc rut
- Chuyn ha gan v thn nh E. 1--hydroxylase Calcitriol c tc dng sinh hc
- Thi tr ch yu qua phn, mt phn nh qua nc tiu, T1/2 = 19 48h.
4- Tc dng v c ch.
* Tham gia vo qu trnh to xng:
+ Lm tng hp thu calci v phosphat rut.
+ Tng ti hp thu calci ng ln gn.
+ Tham gia qu trnh calci ha sn tng trng.
Vit D cn thit cho s pht trin bnh thng ca tr em.
* iu ha nng calci/ mu:
+ iu ha nng calci/ mu theo c ch trn calci/ mu lun hng nh.
+ Nu calci/ mu gim th vit D + hormon cn gip s huy ng calci t xng ra n nh nng
calci/ mu
* Tham gia qu trnh bit ha t bo biu m, /c tng sinh t bo ung th.
* Khi thiu vit D: rut khng hp thu calci v phospho Ca2+/ mu gim Ca2+ b huy ng t xng
ra n nh Ca2+/ mu hu qu tr em chm ln, ci xng, chn vng king Ngi ln b tha
xng, long xng d gy xng.
5- Ch nh.
- Phng v iu tr ci xng do thiu Vit D.
- Phng v iu tr long xng, gy xng bnh l.
- Chng co git do suy tuyn cn gip.
- iu tr h calci mu.
- Mt s bnh ngoi da nh x cng b.
6- Tc dng MM.
- Dng qu liu gy tng calci huyt, tng calci niu, au nhc xng khp; nu dng ko di si
thn, tng HA.
53
TI LIU THAM KHO
- Suy nhc, mt mi, nhc u, bun nn

7- Chng ch nh.
- Tng calci mu
- Bnh cp tnh gan thn
- Lao phi ang tin trin.
- Mn cm vi Vit D
8- Ch phm, liu dng.
* Ch phm:
- Vit D3 (Cholecalciferol) dung dch ung, tim 300.000 600.000UI
- Vit D2 (Ergocalciferol) vin bao ng, vin nang 500 1000UI, dung dch du ung 25000, 50.000 v
200.000UI; dung dch du tim 600.000UI
* Liudng:
- Phng ci xng: 6 thng tim bp hoc ung 1 ng vit D3 300.000UI
- Tr ci xng: 10.000 20.000UI chia 2 3ln x 6 8 tun
- Tr long xng: 600.000UI x 6 thng/ ln.
- Tr tng d co git: 50.000 200.000UI/ 24h x 2ln/ tun.
6. VITAMIN E
CH3
H3C 8 O
1 1 4 8 CH3
7 2 12
6 3 CH3 CH3 CH3 CH3
5 4
HO
CH3
Tn khc: Alpha tocoferol.
Tn khoa hc:2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl) chroman-6-ol
Bit dc :Amino-Opti-E; Liqui-E; Vita-PlusE.
1- Ngun gc, iu ch.
* Ngun gc:
- Vit E c nhiu trong du thc vt: du cm, du lc, trong cc ht ny mm, rau xanh.
- ng vt hu nh khng tng hp c vit E, c mt lng rt nh trong lng trng, gan.
- Vit E gm , , , tocoferol trong tocoferol c hot tnh mnh nht.
* iu ch:
- Phn lp t du cc ht ang ny mm nh ht bng, u tng bng phng php ct phn t
dch m c vit E.
- Tng hp ha hc: 2,3,5-trimethyl hydroquinon + Phytol tocoferol
CH3
CH3
H3C OH
+
CH3 CH3 CH3 CH3
HO
HO
CH3 ZnCl2
tocoferol
2- Tnh cht.
* L tnh:
- Lng snh nh du, mu vng sng, khng mi, khng v.
- Khng tan trong nc, tan trong EtOH v cc dung mi hu c.
- C gc quay cc ring
* Ha tnh:
- Do trong phn t c C* c ng phn quang hc. Cc ng phn hu tuyn (dng D) c hot tnh
mnh hn ng phn t tuyn (dng L)
- Nhm hydroxy phenol: c tnh kh, tnh acid tocoferol d b oxy ha bi t ngoi, mui KL nng, mt
kim bo qun vit E trong l mu kn, trnh AS
+ ch phm l tocoferol acetat hoc succinat bn hn vi tc nhn oxy ha.
+ Vit E tc dng vi HNO3 Ortho tocoferylquinon mu + orthophenylen diamin to sn phm
azo c hunh quang.
+ Tc dng vi FeCl3 tocoferylquinon mu vng + ,- dipyridinyl .
- Cc Tocoferol c R5, R7 = -H th d tham gia P th: tc dng vi mui diazoni to phm mu azo.
54
TI LIU THAM KHO
- Nhn chroman: hp th mnh UV nh tnh, nh lng.

3- im nghim.
* nh tnh:
- Da vo cc phn ng trn.
- o ph hp th t ngoi
* nh lng:
- o quang, HPLC
- o Ceri, ch th l diphenylamin ( chuyn t khng mu sang mu xanh )
4- Dc ng hc.
- Hp thu: qua nim mc rut, cn c acid mt lm cht nh ha.
- Phn b: + lin kt vi lipoprotein huyt tng
+ phn b rng ri vo cc m
+ tch ly nhiu gan v cc m m.
- Thi tr: ch yu qua mt, qua phn.
5- Tc dng, c ch.
- Chng oxy ha: ngn cn oxy ha cc thnh phn thit yu ca t bo, ngn cn s to thnh cc sn
phm oxy ha c hi bo v t bo khi s tn cng ca cc gc t do bo v c tnh ton vn
ca mng t bo.
- Tc dng hip ng vi vit C, vit A, Selen. c bit vit E bo v vit A khi b oxy ha.
- Khi thiu vit E: RL thn kinh, tht iu, rung git nhn cu, gim nhy cm xc gic, d tn thng da,
c v tim, v hng cu. Trn c quan sinh dc tn thng c th dn n v sinh.
6- Ch nh.
- Phng v iu tr thiu vit E.
- Kt hp vi vit A, vit C, Selen lm thuc chng oxy ha
- Phi hp iu tr da xy thai, v sinh , thiu tinh trng, RL tin mn kinh, thiu mu tan mu, teo c,
lon dng c
7- Tc dng MM.
- RLTH: bun nn, nn, y hi, tiu chy
- Mn cm vi thuc.
8- Ch phm, liu dng.
* Ch phm:
- Vin nn, vin bao ng, vin nang mm: 50, 100, 200, 250mg
- Dung dch tim: 30, 100, 200mg/ml
- Thuc m, kem dng ngoi phi hp vi cc thuckhc.
* Liu dng:
- Ngi ln: ung 10 100mg/ 24h, tim bp 30 200mg/ ln/ tun.
- Tr em: ung 10 50mg x 2-3ln/ tun, tim bp 30 100mg/ tun.
Chuyn 13: PENICILLIN V CC KHNG SINH B N TNG HP

-LACTAM
I- I CNG V BNH. (chung cho cc chuyn khng sinh)
1- Khi nim:
Nhim khun l mt bnh ph bin hay gp, tc nhn gy bnh l cc loi vi khun nh cu khun, trc
khun, xon khun
iu tri cc bnh nhm khun bng cc loi khng sinh, c nhiu loi khng sinh v mi loi vi khun
thng nhy cm vi mt s loi khng sinh nht nh Khng sinh .
2- Nguyn tc s dng khng sinh: 5 nguyn tc.
+ Ch s dng khng sinh khi c nhim khun: xc inh nhim khun da vo xt nghim tm vi khun
v da vo cc triu chng lm sng.
+ Phi bit la chn khng sinh hp l: La chn KS Ph hp vi VK gy bnh, la chn KS theo v
tr gy bnh, La chn KS theo c a BN: tr em, PNCT, ngi cao tui, bnh nhn suy thn, suy gan...
+ Phi bit nguyn tc phi hp khng sinh: nhm ni rng ph tc dng, tng hiu qu iu tr v
gim khng thuc.
+ Phi bit s dng khng sinh ng thi gian quy nh.
+ D phng KS hp l: phng nhim khun hoc ngn nga nhim khun ti pht
II- I CNG V H NG SINH:
1-nh ngha:
55
TI LIU THAM KHO
Khng sinh l nhng cht c ngun gc vi sinh vt, c bn tng hp hoc tng hp ha hc. Vi liu
thp c tc dng km hm hoc tiu dit vi sinh vt gy bnh.
2- C ch tc dng ca khng sinh: 5 c ch.
a. c ch tng hp vch t bo vi khun:
Vch t bo c cu to t peptidoglycan l thnh phn quan trng m bo tnh vng chc ca t
bo, v vy rt cn thit cho s pht trin ca vi khun. KS can thip vo s thnh lp peptidoglycan qua
cc giai on:
giai on 1: hnh thnh uridin diphosphat (UDP) acetyl muramin pentapeptid, kt qu l to
thnh pentapeptid
vd: cycloserin c cu trc tng t D alanin nn (-) gn D alanin thnh lp pentapeptid.
giai on 2: P kt hp UDP acetyl muramin pentapeptid v UDP acetylglucosamin thnh chui
di.
Vd: Bacitracin can thip vo qu trnh dephosphorin ca lipid mang s vn chuyn UDP acetyl
muramin b gin on khng kt hp c vi UDP acetylglucosamin
giai on 3: to lin kt ngang gia cc peptidoglycan vi s c mt ca transpeptidase.
Vd: vancomycin gn vo D ala D ala tn cng ca pentapeptid mi hnh thnh trong chui
peptidoglycan c ch P transglycosylase ngn cn to li peptidoglycan ca vch t bo vi khun.
b. Tc ng ln qu trnh tng hp protein ca V :
- Gn vo cc tiu n v 30S hoc 50S lm gin qu trnh tng hp protein ca vi khun nn c TD km
khun
Vd: cloramphenicol (-) tng hp protein ca VK = cch gn vo phn 50S ca ribosom (-) P chuyn
peptid, (-) to thnh lin kt peptid.
Tetracyclin (-) tng hp protein ca VK = cch gn vo phn 30S ca ribosom nn (-) aminoacyl ARNt
mi vo v tr tip nhn trn phc hp ARNm - ribosom vic gn thm aa vo chuipeptid ang c
tng hp b gin on
- Gn vo cc tiu n v 30S ca ribosom lm sai lech655 qu trnh tng hp protein cn thit ca VK
nn c TD dit khun.
Vd: cc aminoglycosid gn vo tiu v 30S ca ribosom gy bin dng ribosom v tc ng n qu trnh
tng hp protein theo 3 cch sau;
- cn tr vic to thnh phc hp khi u.
- gy c sai m tiu v 30S.
- chuyn cc polysom thnh monosom.
c. c ch tng hp acid nhn
* c ch tng hp vch t bo vi khun: gm Penicillin,Cephalosporin,Vancomycin,Bacitracin..
- Vch t bo VK c cu to t peptidoglycan, tc dng m bo tnh vng chc ca t bo rt cn
cho s tn ti v pht trin ca t bo VK.
- Cc KS dit khun /c giai on cui ca qu trnh tng hp vch t bo VK ko c vch che ch v
b tiu dit.
* Tc ng ln qu trnh tng hp protein ca vi khun: gm (/c 50S) l Macrolid, Lincosamid, Phenicol;
v (/c 30S) l Tetracyclin, Aminosid
- KS gn vo cc tiu n v 50S v 30S gy bin dng Ribosom sai lch m di truyn VK ko tng
hp c protein cn thit b tiu dit.
* c ch tng hp acid nhn: gm Quinolon, Rifampicin
- KS /c tng hp ADN do /c ADN gyrase t bo VK ko c kh nng m vng sao chp c
(Quinolon)
- /c tng hp ARN do /c tng hp ARN polymerase (Rifampicin)
* Thay i tnh thm mng t bo: gm Polymycin, Amphotericin, KS chng nm.
- Mng t bo VK l ni trao i cht gia t bo VK v mi trng bn ngoi.
- Mng c tnh thm chn lc vi cc ion duy tr s n nh cc thnh phn bn trong mng.
- Cc KS tc ng ln mng RL tnh thm mng, lm cc ion Mg2+, Ca2+, K+ thot ra ngoi nhiu RL
trao i cht ca t bo VK VK b tiu dit.
* c ch tng hp acid Folic: Co-trimoxazol
- Co-trimoxazol (Sulfamethoxazol+ Trimethoprim) c kh nng /c cnh tranh vi cc enzym ny, c th:
Sulfamethoxazol /c dihydrofolat synthetase; cn Trimethoprim /c dihydrofolat reductase ngng tng
hp v chuyn ha acid folic VK b tiu dit.
3- Phn loi khng sinh :

* Da vo tnh nhy cm ca VK vi KS:
56
TI LIU THAM KHO
- KS dit khun: c MBC tng ng vi MIC( MBC / MIC xp x = 1) v d dng t c MBC trong
huyt tng. Nhm ny gm: penicillin, cephalosporin, aminosid, polymyxin
- KS km khun: c MBC > MIC ( MBC / MIC >4) v kh t c nng bng MBC trong huyt tng.
Nhm ny gm: tetracyclin, chloramphenicol, macrolid.
Cch phn loi ny c ngha trong lm sang, gip thy thuc s dng KS c hiu qu.
* Da vo c ch tc dng ca KS:
- Thuc c ch tng hp vch t.bo VK: -lactam, vancomycin, bacitracin, fosfomycin.
- Thuc c ch or thay i tng hp protein of VK: tetracyclin, chloramphenicol, macrolid, lincosamid v
aminoglycoside.
- Thuc c ch tng hp acid nhn: quinolone, rifampicin.
- Thuc c ch chuyn ha: co- trimoxazol.
- Thuc lm thay i tnh thm of mng t.bo: polymycin, amphotericin.
* Da vo cu trc ha hc: chia thnh cc nhm sau:
- Nhm beta lactam:
+ Penicilin: benzylpenicilin, oxacilin, ampicillin
+ Cephalosporin: cephalexin, cefaclor, cefotaxim
+ Cc beta lactam khc: carbapenem, monobactam, cht c ch beta lactamase
- Nhm Aminoglycoside( aminosid): streptomycin, gentamycin, tobramycin
- Nhm Macrolid: erythromycin, clarithromycin, spiramycin
- Nhm lincosamid: lincomycin, clindamycin.
- Nhm Phenicol: chloramphenicol, thiamphenicol.
- Nhm Tetracycin: tetracycin, doxycycline
- Nhm Peptid:
+ Glucopeptid: vancomycin.
+ Polypeptid: polymycin, bacitracin.
- NHm Quinolone: acid nalidixic, ciprofloxacin, ofloxacin
- Nhm Co- trmoxazol: co- trmoxazol
III- Khng sinh nhm Penicillin.
1- Ngun gc: Ch yu tng hp bng phng php vi sinh (sinh tng hp) hoc bn tng hp t
A6AP (6APA)
2- Cu trc ha hc: Thuc nhm khng sinh -lactam. Cu trc c vng -lactam lin hp vi vng 5
cnh (thiazolidin)
3- Phn loi : chia thnh cc nhm sau
+ Nhm cc penicilin t nhin (thng gi l nhm 1): penicilin G, penicilin V v dn cht trc tip ca
hai khng sinh ny (nh penicillin G benzathin, penicillin G procain)
+ Nhm cc penicilin bn tng hp khng penicilinase (hay gi l nhm M): nh methicilin, cc
isoxazolylpenicilin (cloxacilin, dicloxacilin ..), nafcilin
+ Nhm cc penicillin ph rng aminobenzylpenicillin (ampicilin, amoxicilin)
+ Nhm cc penicillin khng trc khun m xanh (P. aeruginosa): VD cc carboxy benzylpenicilin (carbenicilin,
ticarcilin), ureidobenzylpenicilin (piperacilin, mezlocillin, azlocillin, ...)
4- C ch tc dng
+ Peptidoglycan l thnh phn c bn to nn tnh vng chc ca vch t bo vi khun. Qu trnh tng hp
peptidoglycan c thc hin nh enzym D-alanin transpeptidase
+ Cc khng sinh nhm penicilin c kh nng acyl ha cc D-alanin transpeptidase, lm cho qu trnh
tng hp peptidoglycan khng thc hin c. Sinh tng hp vch t bo b ngng li
+ Mt khc cc penicilin cn hot ha enzym t phn gii murein hydroxylase lm tng phn hy vch t
bo vi khun. Kt qu l vi khun b tiu dit
+ Cc vi khun Gram m do vch t bo t peptidoglycan nn t nhy cm vi cc penicilin. Hn na cc
vi khun Gram m c lp v phospholipid bao ph bn ngoi lm cc penicilin kh thm qua, v vy ni
chung cc penicilin t tc dng trn vi khun Gram m. Tuy nhin mt s penicilin ph rng nh
amoxicilin a nc nn c th i qua cc knh porin trn mng t bo vi khun Gram m v ni rng ph
trn cc vi khun ny
5- Tc dng MM.
- D ng: mn nga, m ay, shock phn v.
- RLTH: bun nn, nn, tiu chy
6- C ch khng thuc.
Cc VK c th khng penicillin gm:
+ VK khng c vch t bo: VK Gr(-)
+ VK to ra -lactamase (Penicillinase)
57
TI LIU THAM KHO
+ VK khng c receptor ca penicillin, hoc vch TB ngn khng cho penicilin thm qua, khng cho
penicillin gn vo receptor.
+ Enzym t phn gii (murein hydroxylase) ca vi khun khng c hot ha.
THUC C TH :
1- BENZYL PENICILLIN (PENICILLIN G)

H H
C6H5 CH2 CO NH S
6 5 4 CH3
3
7 B 1A
N 2 CH3
O H COOK (Na)
Tn khoa hc: Kali (2S,5R,6R )-3,3-dimethyl-7-oxo-6-[(phenylacetyl)amino]-thia-1-
azabicyclo[3.2.0]heptan-2-carboxylat.
Tn khc:Benzylpenicillin kali (natri)
1- Tnh cht, kim nghim.
* L tnh: Bt kt tinh trng ng. Tan/ dd kim, t tan/ nc,1 s tan/ dd acid long (c NH2)
- Do c C bt i gc quay cc D nh tnh, nh lng.
- Hp th hng ngoi dng ph IR nh tnh.
- Hp th UV nh tnh, nh lng, th tp = o UV, HPLC
Tnh cht ha hc:
Tnh acid. Mui Na, K d tan/nc. Mui vi base amin phn t ln kh tan/nc, dng vi tc dng
ko di.
M vng -lactam bi -lactamase to acid penicilloic
Thy phn vng -lactam bi kim (-OH), acid (H+)
P/ cng hp i nhn vi amin, hydroxylamin, alcol vo vng lactam to ester hoc amid ca acid
penicilloic.
Vi hydroxylamin to acid hydroxamic to phc mu vi ion kim loi.
Oxy ha bi H2SO4 c hoc hn hp H2SO4 c/formol to ra hn hp mu.
nh tnh:
Qut ph UV, so snh vi cht chun
Qut ph IR, so snh vi cht chun
o gc quay cc ring.
Phn ng vi hydroxylamin vi Fe3+ cho mu . Cc ion kl khc (Zn2+, Cd2+, Pb2+, Hg2+) xc tc p/
thy phn.
P/ vi HCHO/H2SO4 cho mu nu sau khi un cch thy.
nh lng:
o quang, HPLC
PP o iod: thy phn, trung ha kim, n nh pH, thm lng tha iod, nh lng iod d bng natri
thiosulfat, ch th h tinh bt.
o thy ngn: thy phn, trung ha kim, n nh pH, l = Hg(NO3)2
PP vi sinh vt: th vng v khun gy ra bi ch phm trn mt chng vi khun nht nh. So snh vi
mu chun
2- Dc ng hc.
- Hp thu:Penicillin G b mt hot tnh bi dch v ch yu dng ng tim.
+ t Cmax sau tim 15 30 pht, duy tr tc dng 4h.
- Phn b: lin kt vi protein huyt tng 60 80 %, vo hu ht cc m v dch c th.
+ Qua hng ro mu no km, khi b vim th thuc xm nhp tt hn.
+ Qua c rau thai, sa m
- Thi tr: ch yu qua thn, T1/2 = 30 60 pht, suy thn T1/2 = 7 10h
3- Ph tc dng.
- L khng sinh ph hp, tc dng ch yu trn VK Gr(+) nh t cu, lin cu, ph cu; trc khun un
vn, than, bch hu xon khun giang mai.
- Mt s VK Gr(-) nh lu cu, mng no cu.
4- Ch nh.
- Nhim khun h hp, TMH
- Nhim khun huyt
- Vim xng ty cp v mn.
- Vim ni tm mc do lin cu.
58
TI LIU THAM KHO
- Giang mai, lu, un vn, hoi th, bch hu

5- Tc dng MM.
- Penicillin G c c tnh thp, nhng d gy d ng (my ay, mn nga, ngoi ban..), shock phn v,
- Vim tnh mch huyt khi, thiu mu, tan mu, gim bch cu
6- Chng ch nh: D ng vi Penicillin.
7- Tng tc thuc.
- Gim tc dng khi kt hp vi Tetracyclin, Erythromycin do lm chm tc pht trin ca VK
- Dng ng thi vi Probenecid (thuc iu tr gout) chm thi tr, tng nng , ko di tc dng
ca penicillin.
- Thuc khng vim NSAID lm ko di T1/2 ca penicillin.
8- Ch phm, liu dng.
- Ch phm: Benzyl penicillin l bt pha tim t 600.000 - 10 triu UI.
- Liu dng:
+ Ngi ln: 1 4 triu UI/ 24h, chia 2 4 ln.
+ Tr em: t 50.000 100.000 UI/ kg/ 24h chia 2 4 ln.
2. PHENOXYMETHYL PENICILLIN (penicillin V)

O
H H
C6H5 O CH2 C HN S
6 5 4 CH3
3
7 B 1A
N 2 CH3
O H COOH(K)
Tn khoa hc: Acid (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenoxyacetamido)-4-thia-1-azabicyclo [3.2.0]-

heptan-2-carboxylic.
Tn khc: Penicillin V
Bit dc: V-cillin, Vegacillin
1- Tnh cht, kim nghim.
* L tnh: Bt kt tinh trng ng. kh tan trong nc, khng tan trong du, d tan trong EtOH 96%
- Do c C bt i gc quay cc D nh tnh, nh lng.
- Hp th hng ngoi dng ph IR nh tnh.
- Hp th UV nh tnh, nh lng, th tp = o UV, HPLC
Tnh cht ha hc:
Tnh acid. Mui Na, K d tan/nc. Mui vi base amin phn t ln kh tan/nc, dng vi tc dng
ko di.
M vng -lactam bi -lactamase to acid penicilloic
Thy phn vng -lactam bi kim (-OH), acid (H+)
P/ cng hp i nhn vi amin, hydroxylamin, alcol vo vng lactam to ester hoc amid ca acid
penicilloic.
Vi hydroxylamin to acid hydroxamic to phc mu vi ion kim loi.
Oxy ha bi H2SO4 c hoc hn hp H2SO4 c/formol to ra hn hp mu.
nh tnh:
o gc quay cc ring.
thy phn.
xc nh acid phenoxyacetic bng TLC.
nh lng:
o quang, HPLC
PP o iod: thy phn, trung ha kim, n nh pH, thm lng tha iod, nh lng iod d bng natri
thiosulfat, ch th h tinh bt.
o thy ngn: thy phn, trung ha kim, n nh pH, l = Hg(NO3)2
PP vi sinh vt: th vng v khun gy ra bi ch phm trn mt chng vi khun nht nh. So snh vi
mu chun
2- Dc ng hc.
59
TI LIU THAM KHO
- Hp thu: Bn vi dch v ch yu dng ng ung, SKD 60%. Thc n lm gim hp thu thuc, t
Cmax sau khi ung 30 60 pht
- Phn b: lin kt protein huyt tng 80%
- Chuyn ha gan.
- Thi tr: ch yu qua nc tiu, T1/2 = 30 60 pht, suy thn T1/2 = 4h
3- Ph tc dng.
- L khng sinh ph hp, tc dng ch yu trn VK Gr(+) nh t cu, lin cu, ph cu; trc khun un
vn, than, bch hu xon khun giang mai.
- Mt s VK Gr(-) nh lu cu, mng no cu.
4- Ch nh.
- Nhim khun h hp, TMH
- Nhim khun huyt
- Vim xng ty cp v mn.
- Vim ni tm mc do lin cu.
- Giang mai, lu, un vn, hoi th, bch hu
5- Tc dng MM.
- Penicillin G c c tnh thp, nhng d gy d ng (my ay, mn nga, ngoi ban..), shock phn v,
- Vim tnh mch huyt khi, thiu mu, tan mu, gim bch cu
6- Chng ch nh: D ng vi Penicillin.
7- Tng tc thuc.
- Gim tc dng khi kt hp vi Tetracyclin, Erythromycin do lm chm tc pht trin ca VK
- Dng ng thi vi Probenecid (thuc iu tr gout) chm thi tr, tng nng , ko di tc dng
ca penicillin.
- Thuc khng vim NSAID lm ko di T1/2 ca penicillin.
8- Ch phm, liu dng.
- Ch phm: Penicillin V (Ospen) vin nn 200.000, 400.000, 1 triu UI.
- Liu dng: Ngi ln v TE > 12 tui: 400.000 800.000 UI/ ln x 3 4ln/ 24h.
+ TE < 12 tui: 40.000 - 80.000UI/ kg/ 24h
- Ung xa ba n.
AMOXICILLIN
H O
H H
HO C C HN S
6 5 4 CH3
3
NH2 7 B 1A
N 2 CH3 3H2O
O H COOH
Tn khoa hc:Acid (2S,5R,6R)-6-[(R)-2-amino-2-4-hydroxyphenyl) acetamido]-3,3-dimethyl-7-oxo-4-thia-

1-azabicyclo[3.2.0]-heptan-2-carboxylic.
Bit dc: Clamoxyl; Hiconcil.
1- Ngun gc: Bn tng hp t A6AP (acyl ha A6AP bng D(-)-2-(p-hydroxyphenyl)glycin
2- Tnh cht
* L tnh:
+ Bt kt tinh (tinh th) mu trng, v ng, kh tan trong nc, kh tan trong cc dung mi hu c
(ether, cloroform), tan trong cc dung dch acid hoc kim long.
+ Hp th UV, IR
+ C gc quay cc ring
* Ha tnh:
+ C tnh acid
+ D b m vng -lactam bi cc tc nhn kim, -lactamase, cc tc nhn i nhn (bn vi acid dch v
d dy)
+ Phn ng ca aminoacid vi TT Ninhydrin hoc TT Fehling
+ Phn ng mu vi tc nhn oxi ha nh H2SO4, TT Marki (HCHO/ H2SO4)
3- im nghim.
* nh tnh:
+ o ph hng ngoi (IR), so snh vi ph ca cht chun
60
TI LIU THAM KHO
+ Sc k lp mng (so snh vi cht chun i chiu)

+ Phn ng mu vi TT: H2SO4 m c hoc TT Marki (HCHO/ H2SO4)
+ Phn ng vi hydroxylamin to dn cht acid hydroxamic, sau to phc mu vi ion kim loi ha tr
II, III
* nh lng:
+ PP o iod hoc PP o thy ngn
+ PP o quang hoc HPLC
4- Ph khng khun: Amoxicilin c tc dng vi c vi khun Gram dng v Gram m
+ Vi vi khun Gram dng:
- Tc dng trn lin cu (Streptococcus), t cu (Staphylococcus), ph cu (Pneumococcus)
- B mt hot tnh bi beta lactamase nn hu nh khng c tc dng i vi cc vi khun tit
penicilinase
+ Vi vi khun Gram m:
- Tc dng trn cc chng a kh v k kh Gram m nh Escherichia coli, Enterococci, Salmonella,
Shigella
- Cc chng vi khun khng amoxicilin: Pseudomonas, Klebsiella, Serratia, Acinetobacter, Bacteroid v
cc Proteus indol (+)
5- Dc ng hc.
- Hp thu:
+ Amoxicilin bn vng vi acid dch v nn c th dng qua ng tiu ha.
+ Amoxicilin hp thu qua ng tiu ha nhanh v hon ton hn ampicilin (khi ung cng lng, nng
nh trong huyt tng ca amoxicilin cao gp 2 ln so vi ampicilin). Do c tnh hp thu ny, mc d
amoxicilin v ampicilin c hot ph tng t nhau nhng khi s dng ng ung nn la chn
amoxicilin
- Phn b: Thuc phn b nhanh vo cc m v dch c th. Thuc qua c nhau thai v sa m, vo
dch no ty km tr khi mng no b vim
- Thi tr: ch yu qua thn.
6- Ch nh.
+ Cc nhim khun h hp trn do vi khun nhy cm: vim xoang, vim tai gia, vim ph qun cp v
mn, vim np thanh qun
+ Nhim khun ng tit niu khng bin chng do E.coli
+ Phi hp trong phc iu tr H. Pylori
+ Cc nhim khun khc do VK nhy cm: nhim khun tiu ha, nhim khun huyt
7- Ch phm, liu dng.
- Ch phm: Amoxicillin, Clamoxyl, Hiconcil
+ Vin nang 500mg, vin nn 1g
+ Gi bt 250mg/5ml; l bt 250mg/5ml
- Liu dng:
+ Ngi ln v TE > 12 tui: 250 500mg/ ln x 2-3 ln/ 24h; tim bp, TM 1g/ln x 2 -3 ln/ 24h.
+ TE < 10 tui: 125 250mg/ ln x 3 ln/ 24h; tim bp 50 100mg/kg/24h
IV- KHNG SINH CEPHALOSPORIN:

1- Ngun gc.
- Cephalosporin t nhin c phn lp t mi trng nui cy nm Cephalosporin acrmonium
- Bn tng hp t acid 7-amino cephalosporinic ( 7ACA )
2- Phn loi: Da vo ph khng khun chia cephalosporin thnh 4 th h:
+ Th h I:Gm Cephalothin, Cephalexin, Cephradin, Cephadroxil
- Ph tc dng trung bnh
- Tc dng mnh trn Gr (+): t cu, lin cu, ph cu; yu trn Gr (-): E.coli, Klebsiella, Proteus,
Shigella.
- Khng bn, d b -lactamase ph hy.
+ Th h II: Gm Cephaclor, Cefuroxim, Cephamandol
- Tc dng mnh hn trn Gr (-), yu hn trn Gr (+) so vi th h I
- Bn vi -lactamase
+ Th h III:Gm Cefotaxim, Ceftazidin, Cefixim, Cefpodoxim, Cefoperazon, Ceftriaxon
- Trn Gr (+) km I nhng c ph rng, mnh trn Gr (-); khng -lactamase ca Gr(-) mnh hn II
- Tc dng tt trn Gr (-) k kh, c tc dng trn VK ng rut, mt s hot tnh cao trn Pseudomonas
- Mt s thm tt vo dch no ty.
+ Th h IV: i din l Cefepim.
- Hot ph v tc dng trn Gr (-) nh III, nhng mnh hn.Trn Gr (+) tc dng mnh hn so vi III
61
TI LIU THAM KHO
- Khng nhiu -lactamase

THUC C TH :
1. CEPHALEXIN
H O
H H
C C HN S
1
7 6 2
H2O
NH2 8 5 3
N 4
O CH3
COOH
Tn khoa hc: Acid 7-(- amino--phenylacetamido)-3-methylcephem-4-carboxylic monohydrat.
Bit dc: Kelflex; Keforal
1- Tnh cht.
- Bt kt tinh trng, hi c mi lu hunh. t tan trong nc, tan trong dung dch kim long.
* Ha tnh:
Tnh acid do 4-COOH
M vng -lactam bi -lactamase
Thy phn vng -lactam bi kim (-OH), acid (H+) bi kim (-OH) hay acid (H+) (mnh) to acid
cephalosporoic .
P/ cng hp i nhn vi amin, hydroxylamin, alcol vo vng lactam.
Vi hydroxylamin cho acid hydroxamic to phc mu vi ion kim loi.
Oxy ha bi H2SO4 c hoc hn hp H2SO4 c-formol to ra hn hp mu
2- im nghim:
nh tnh:
o gc quay cc ring
thy phn.
nh lng:
o quang, HPLC
PP trung ha da vo 4-COOH.
PP o iod, o thy ngn (tng t penicillin)
PP vi sinh (so snh vi ks chun).
3- Dc ng hc.
- Hp thu: tt qua ng tiu ha. t Cmax sau 1-2h.
- Phn b: rng khp c th, qua rau thai v sa m.
- Chuyn ha: hu nh khng chuyn ha trong c th
- Thi tr: ch yu qua nc tiu, T1/2 = 1 1,5h
4- Ph tc dng, c ch.
Ph tc dng trung bnh
- Tc dng mnh trn Gr (+): t cu, lin cu, ph cu; yu trn Gr (-): E.coli, Klebsiella, Proteus,
Shigella.
- Khng bn, d b -lactamase ph hy
5- Ch nh.
- iu tr cc nhim khun thng thng do VK nhy cm.
+ Nhim khun h hp, TMH
+ Nhim khun tit niu, sinh dc.
+ Nhim khun da, m mm, xng, rng.
6- Tc dng MM.
- Cc Phn ng d ng: nga, ban da, my ay
- Gy c vi thn vim thn k.
- RLTH: nn, bun nn, au bng, tiu chy
- Bi nhim nm ming, m o, rut kt
7- Chng ch nh.
- D ng vi Cephalosporin.
- Thn trng vi ngi suy thn, d ng vi penicillin
8- Tng tc thuc.
62
TI LIU THAM KHO
- Dng ng thi vi aminosid, furosemid tng c tnh vi thn.

- Probenecid lm chm thi tr ko di tc dng ca cephalosporin.
2. CEFUROXIM NATRI
O
H H
C HN S
1
7 6 2
O C
8 5 3 O
N N 4
O CH2 C NH2
OCH3 COONa
O
Bit dc: efurox, Zinacef
1- Tnh cht.
- Bt kt tinh trng, ht m. tan trong nc, rt t tan trong ethanol, ko tan trong ether.
* Ha tnh:
M vng -lactam bi -lactamase ????? Hi li Thy
cephalosporoic .
P/ th i nhn vi cc tc nhn i nhn vo 3-CH2OCOCH3 (nu cn) B thy phn bi esterase, H+,
OH-; sau thy phn to deacetylcephalacton khng c hot tnh
2- im nghim:
nh tnh:
o gc quay cc ring
thy phn.
nh lng:
o quang, HPLC
3- Dc ng hc.
- Hp thu: qua ng tiu ha km, dng ng tim, Tim TM 1g, t Cmax trong mu l 75 - 125g/
ml
- Phn b: qua rau thai, sa m, dch no ty
- Thi tr: qua nc tiu dng cha chuyn ha.
4- Ph tc dng v c ch.
Tc dng mnh hn trn Gr (-), yu hn trn Gr (+) so vi th h I
- Bn vi -lactamase
5- Ch nh.
- iu tr cc nhim khun thng thng do VK nhy cm.
+ Nhim khun h hp, TMH
+ Nhim khun tit niu, sinh dc.
+ Nhim khun da, m mm, xng, rng.
6- Tc dng MM.
7- Chng ch nh.
8- Ch phm, liu dng.
- Zinat vin nn 250, 500mg; l bt ung 125mg/5ml; gi bt 125mg/5ml
63
TI LIU THAM KHO
- Zinacef l bt pha tim 750mg

- Liu dng:
+ Ngi ln: ung 0,25-0,5g/ ln x 3 ln; tim 0,75- 1,5g x 3 ln
+ Tr em: 30-100mg/kg chia 3 ln.
3. CEFOTAXIM NATRI
O
H H
C HN S1
7 6 2
N C
8 5 3 O
H2N N 4
N
S O CH2 C CH3
OCH3 COONa
O
Bit dc: Claforan
1- Tnh cht.
- Ch phm bt mu trng or trng ng
- D tan trong nc, t tan trong MeOH, khng tan trong Ether.
* Ha tnh:
cephalosporoic .
2- im nghim:
nh tnh:
o gc quay cc ring
thy phn.
nh lng:
o quang, HPLC
2- Dc ng hc.
- Hp thu: HT km qua ng tiu ha dng ng tim
- Phn b: Rng khp vo cc m v dch c th. Xm nhp tt vo dch no ty, nht l khi vim. Qua
c rau thai v sa m
- Chuyn ha, thi tr: chuyn ha gan, thi tr qua thn.
3- Ph tc dng.
Trn Gr (+) km I nhng c ph rng, mnh trn Gr (-); khng -lactamase ca Gr(-) mnh hn II
- Mt s thm tt vo dch no ty.
4- Ch nh.
iu tr cc nhim khun nng khng cephalosporin th h 1 v 2.
- Vim mng no, p xe no
- Nhim khun huyt, vim mng trong tim.
- Nhim khun h hp, tiu ha, ng mt,tit niu, sinh dc
- D phng nhim khun trong phu thut.
5- Tc dng MM.
64
TI LIU THAM KHO

6- Chng ch nh.
7- Ch phm, liu dng.
- Claforan: l bt tim 1g
- Liu dng:
+ Ngi ln: 1 - 2g/ ln x 2 4 ln/ ngy.
+ Tr em: 100-200mg/kg/24h chia 2-3 ln
4. CEFTRIAXON NATRI
O
H H
C HN S1 H3C N ONa
N 7 6 2 N
C
8 5 3
H2N N 4
N O
S O CH2 S N
OCH3 COONa
Bit dc: Rocephin.
1- Tnh cht.
- Dang mui dinatri l bt tinh th mu trng n vng nht
- D tan trong nc, t tan trong EtOH
Hp th UV, IR c trng, c gc quay cc ring
* Ha tnh:
cephalosporoic .
2- im nghim:
nh tnh:
o gc quay cc ring
thy phn.
nh lng:
o quang, HPLC
3- Ph tc dng.
- Trn Gr (+) km I nhng c ph rng, mnh trn Gr (-); khng -lactamase ca Gr(-) mnh hn II
- Mt s thm tt vo dch no ty. ngoi ra thuc tc dng tt trn lu cu.
4- Ch nh.
- iu tr chn lc vi lu cu khng c bin chng.
- Vim mng no TE do H.influenzae, mng no cu, nhim khun nng do trc khun Gr (-)
- Cc nhim khun xng khp, bng, ng h hp di, sinh dc tit niu
- Phng nhim khun trong phu thut.
5- Tc dng MM.
6- Chng ch nh.
65
TI LIU THAM KHO
7- Ch phm, liu dng.
- L bt pha tim 0,25 ; 0,5 ; 1g ; 2g.
- Liu dng: + Tim bp, TM 1-2g/ ln; vim mng no 2g/ ln x 2ln/ ngy
+ Bnh lu: tim bp liu duy nht 1g.
Chuyn 14: KHNG SINH AMINOSID

I- I CNG V NHM THUC:
1- Cu trc.
- Aminosid l nhng hp cht trong phn t gm nhng phn t ng amin lin kt glycosid vi nhau
Genin O Ose
- Phn Genin: l vng Cyclitol ( polyalcol ng vng )
+ Dn cht 1,3-diaminocyclitol. Dn cht Deoxy-2-streptamin c 2 nhnh ng gn vo cc v tr 4,5
hoc 4,6. Dn cht 1,4-diaminocyclitol
- Phn ng (Ose): l cc ng amin 5 cnh hoc 6 cnh trung tnh.
2- iu ch.
- Amnosid t nhin c chit xut bng phng php ln men cc chng VSV nh Streptomyces,
Micromonospora, Bacillius.
- Phng php trao i ion qua Cationid
3- Ph tc dng c ch
- Tc dng mnh trn Gr (-), trn Gr (+) th km penicilin
- Khng hp thu qua ng tiu ha dng ng tim, dng ng ung tr nhim khun ti rut.
- C ch:Aminosid qua mng t bo gn vo tiu n v 30S ca Ribosom bin dng Ribosom
sai lch m di truyn to ra cc protein khng cn thit cho VK b tiu dit
- C ch khng aminosid:
- VK to ra cc enzym tc ng vo mt s v tr trn phn t aminosid lm KS mt hiu lc
4- Tc dng MM.
- Vi thnh gic: gy RL tin nh, c tai RL chc nng thnh gic tai, chng mt, ic khng hi
phc.
- Vi thn: + Tn thng , hoi t ngthn
+ Vim thn k
- D ng: myay, ban , vim da trc vy
- Cc TD KMM khc: c ch dn truyn thn kinh c lit h hp, suy h hp.
II- THUC C TH:
1. STREPTOMYCIN SULFAT
NH NH
OH
L streptose O
H3C 1' H2N C HN 2 NH C NH2
3 1
CHO 4 6
CH2OH 2' 5
O HO OH 3H2SO4
HO O
1'' O OH
''
2 L glucosamin 2 Streptidin
HO NHCH3
2
1- Ngun gc v iu ch.
- c phn lp t mi trng nui cy Streptomyces griseus.
2- c im cu to:
- ng streptose c 1 nhm aldehyd (-CHO)
- 3 trung tm base: 2 guanin + 1 amin II:
- 2 phn t streptomycin to mui vi 3 H2SO4.
2- Tnh cht.
L tnh:
66
TI LIU THAM KHO
Bt kt tinh hoc v nh hnh mu trng, dng base tan/nc v dung mi hu c mc khc

nhau
Bn pH gn trung tnh, thy phn chm trong mi trng acid
Khng c hp th UV bc sng ln hn 220nm
Ph IR c trng
C gc quay cc ring
Ha tnh:
- Tnh base mnh d to mui vi cc acid, Ch phm dd l mui sulfat, rt d tan/H2O, pH gn trung
tnh. Dd vng bn/MT trung tnh, d b phn hy khi un nng (bt pha tim)
- Tnh kh: Streptomycin (-CHO)
+ TT Fehling, un Cu2O gch
- Phn ng to maltol: Thy phn/ MT acid hoc kim mt hot tnh (streptidin, streptobiosamin)
Phn ng to maltol mu :
Dd streptomycin/NaOH + FeCl3 mu tm khi soi trn nh sng
- Nhm guanidin:
+ Thy phn gii phng NH3.
+ T/d vi naphtol v natri hypobromid/OH- to mu tm.
- Acid kt hp: nh tnh ion SO42- bng BaCl2 trng
3- im nghim:
nh tnh
- Bng pp qut ph UV, o hp th ring, SKLM. o gc quay cc
- = cc p/ng trong phn ha tnh
nh lng:
o quang, HPLC
= PP vi sinh
nh lng o kim (loi tr nh hng base mnh ca nhm guanidin bng cch thm formaldehyd )
4- Dc ng hc.
- Hp thu: t qua ng tiu ha, khng b ph hy bi acid dch v , bn vng vi penicillinase dng
ng tim bp, ngoi ra dng ng ung tr nhim khun ti rut. t Cmax sau khi tim bp 30-60
pht, duy tr tc dng 8-12h
- Phn b: t lin kt vi protein huyt tng, Khuych tn vo dch ngoi bo, qua c rau thai v sa
m, khng vo c dch no ty
- Thi tr: ch yu qua nc tiu, T1/2 = 2-4h.
- u im ni bt ca Streptomycin l tc dng tt vi VK lao giai on sinh sn
- Tc dng trn VK gy bnh phong, dch hch, trc khun ng rut.
6- Ch nh.
- Ch yu dng iu tr lao v phi phi hp vi cc thuc
- Cc nhim khun do VK Gram (-), bnh dch hch.
- Nhim khun tiu ha, chun b cho phu thut tiu ha.
- Phi hp nhm penicillin iu tr vim mng trong tim do lin cu
7- Tc dng MM.
- Gy c tnh vi thnh gic mnh nht: Ri lon tin nh, c tai gy tai, gim thnh lc v ic ko hi
phc
- gy c vi thn
8- Ch phm, liu dng.
- Ch phm: l bt pha tim 1g dng mui sulfat.
- Liu dng:
+ iu tr lao: 15 20mg/kg/24h, t iu tr 2 thng, phi hp vi cc thuc tr lao khc
+ Cc bnh khc : 1 2g/24h, chia 2 ln
2. GENTAMICIN SULFAT
Bit dc: Cidomycin, Garamycin
L mui sulfat ca hn hp Gentamicin C1 , C1a , C2 , C2a
67
TI LIU THAM KHO
1- Ngun gc : l hn hp khng acid c cu trc gn nha. c chit xut t mi trng nui cy

M.purpura, M.echnospora
2- Tnh cht.
* L hc: Bt kt tinh mu trng, khng mi, v ng, ht m
- D tan trong nc, kh tan trong dung mi hu c; bn trong pH acid.
- C gc quay cc ring
R3
R2 CNH R1 H2N NH2
O 3 1 O
5'
1" CH3
1' 5 OH
3' O O 3" OH
OH 2"
NH2 NHCH3
* Ha hc: Tnh base do c nhiu nhm amin bc 1, bc 2 to mui tan vi acid.
2- im nghim.
* nh tnh:
- SKLM so vi chun.
- To phc mu tm vi Ninhydrin
* nh lng:
- PP VSV: + Chng VK th l Bacillus pumilus.
+ Hot lc KS: 590 UI/ 1mg cht th.
3- Dc ng hc.
- Hp thu: t qua ng tiu ha, khng b ph hy bi acid dch v , bn vng vi penicillinase dng
ng tim bp, ngoi ra dng ng ung tr nhim khun ti rut. t C max sau khi tim bp 30-60
pht, duy tr tc dng 8-12h
- Phn b: t lin kt vi protein huyt tng, Khuych tn vo dch ngoi bo, qua c rau thai v sa
m, khng vo c dch no ty
- Thi tr: ch yu qua nc tiu, T1/2 = 2-4h.
4- Ph tc dng, c ch
- Ngoi ra cn tc dng vi Actinomyces v Mycoplasma.
5- Ch nh.
- Nhim khun nng do Gr (-) mc phi bnh vin nh: nhim khun ng mt, nhim khun huyt,
vim mng no, phi, xng khp, tit niu
- D phng phu thut.
- Phi hp vi Penicillin, Quinolon, Clindamycin, Metronidazol nng cao hiu lc khng khun.
6- Tc dng MM.
- Vi thnh gic: gy RL tin nh, c tai RL chc nng thnh gic tai, chng mt, ic khng hi
phc.
- Vi thn: + Tn thng , hoi t ngthn
+ Vim thn k
7- Chng ch nh.
- Tn thng thn, thnh gic.
- D ng vi Gentamycin
8- Tng tc thuc.
- Tng c tnh vi thn khi kt hp vi: Aminosid khc, Vancomycin, Cephalosporin, Furosemid
- Vi cc thuc /c dn truyn TK c tng nguy c gin c.
- Tng k vi Penicillin, Cephalosporin, Furosemid, Heparin v P vi cht c pH kim, hoc thuc
khng bn vi acid khng trn ln cc thuc ny khi tim.
9- Ch phm, liu dng.
- ng tim 40mg/ 2ml, 80mg/ 2ml
- Liu dng: + Ngi ln v TE: 3-5mg/ kg/ 24h chia 2-3 ln.
- Gim liu bnh nhn suy thn, ngi gi, TE.
68
TI LIU THAM KHO
Chuyn 15: KHNG SINH NHM MACROLID

I- I CNG V NHM THUC.
1- c im cu trc chung.
L cc Glycosid thn lipid ( Lipophil ): Genin O Ose
* Phn Genin:
- Vng lacton c t 12 17 nguyn t Carbon
- Nhm th trn vng lacton: + Hydroxy ( OH )
+ Alkyl
+ Aldehyd c trng cho macrolid 16 C
+ Ceton c trng cho macrolid 14 C.
* Phn ng ( Ose ):
+ ng trung tnh
+ ng amin c tnh kim, tc dng vi acid mi tan/ nc.
2- Phn loi.
Da vo s nguyn t ca vng lacton:
- Vng 14 C: Erythromycin, Clarithromycin, Roxithromycin, Dirithromycin.
- Vng 15 C: Azithromycin
- Vng 16 C: Josamycin, Spiramycin.
3- Ngun gc.
- Thin nhin: chit xut t mi trng nui cy Streptomyces
- Bn tng hp: t ch phm thin nhin, thay i mt s nhm th nhm khc phc cc nhc im
ca m nh:
+ Thay nhm ceton C10 bng dn cht Oxim Roxithromycin.
+ Thay OH C7 bng nhm OCH3 ( methoxy ) Clarithromycin
+ M rng vng lac ton ra 15 nguyn t ( c 1N ) Azithromycin
4- Ph tc dng.
- VK Gr (+): T cu, ph cu, lin cu, trc khun than, bch hu
- VK Gr (-): Lu cu, Mng no cu.
- Mt s VK ym kh: Mycoplasma, Rickettsia, Clammydia
- Khng nhy cm vi phn ln Gr (-) do KS kh thm vo ni bo VK.
II- THUC C TH:

1. ERYTHROMYCIN
( Macrolid 14 nguyn t )
Bit dc: Erymax, Retcin
1- Ngun gc.
- Chit xut t mi trng nui cy Streptomyces: Chit bng dung mi hu c t dch nui cy sau khi
kim ha tinh ch thu sn phm dc dng.
- Bn tng hp
2- Tnh cht.
* L tnh: Bt mu trng nh vng, v rt ng.
- Bn pH 7-8; khng bn pH < 4.
- tan: rt t tan trong nc, tan trong ether v cloroform
* nh tnh:
- Ch phm + xanhthydrol / ( HCl + CH3COOH ) cch thy mu .
- Ch phm + HCl c mu vng
- SKLM so vi Erythromycin chun
* nh lng:
- HPLC
- PP Vi sinh vt.
3- Dc ng hc.
- Hp thu:
+ Qua ng ung v trc trng.
+ SKD t 30 60%
+ t Cmax sau khi ung 1-2h.
- Phn b:
+ Vo khp cc dch ca c th, qua rau thai, sa m
+ Cc Macrolid u t nng cao gan, mt, lch nhng khng vo c dch no ty
69
TI LIU THAM KHO
- Chuyn ha gan, thi tr ch yu qua phn.

- Ph tc dng trung bnh, ch yu trn Gr (+) : lin cu, t cu, ph cu, bch hu
- Trn Gr (-): lu cu, mng no cu.
- Tc dg trn cc VK ni bo Mycoplasma, Rickettsia, Clammydia, xon khun giang mai, VK c hi
Mycobacterium kansasii.
- Khng tc dg trn VK Gr (-) a kh.
* C ch:
- C tc dng km khun do Ery gn vo tiu v 50S ca Ribosom ngn cn chuyn v peptidylARNt
t v tr tip nhn sang v tr trao i thng tin cc aminoacylARNt mi khng th vo v tr tip nhn
cc acid amin khng gn vo chui peptit ang thnh lp khng tng hp c protein cn thit
cho VK
5- Ch nh.
iu tr cc nhim khun nhy cm vi Eythromycin:
+ Nhim khun h hp, da, m mm, h sinh dc tit niu.
+ D phng thp khp thay th penicillin.
6- Tc dng MM.
- t c, t tc dng KMM s dng nhiu trong khoa nhi.
- D ng: vim gan, vng da, lon nhp
7- Chng ch nh.
- Vim gan.
- Ri lon Porphyrin
- Mn cm vi thuc
8- Tng tc.
- /c enzym chuyn ha thuc microsom gan ca nhiu thuc:
+ Theophylin, Ergotamin, Methyprednisolon, lovastatin, Carbamazepin, a.Valproic tng tc dng v
c tnh khi phi hp vi cc thuc trn.
+ Hip ng tc dng vi Warfin, Digoxin, Bromocriptin tc dng v c tnh
+ Khi phi hp vi Terfenadin, Astemizol c cho tim, xon nh.
- Ngc li khi phi hp vi Macrolid khc hoc Lincosamid cnh tranh v tr tc dng gim tc
dng km khun.
9- Ch phm, liu dng.
* Ch phm:
- Erythromycin bt pha hn dch ung 125mg/ 5ml.
- Vin nn, vin nang, vin bao tan 250, 500mg
- Dng dng ngoi: M tra mt 0,5% ( Acneryne ), dung dch cn ( Eryfluid ), kem, thuc m ( Erythrogel)
2%, 4%.
* Liu dng:
- Ngi ln: 1-2g/ 24h chia 2-4 ln.
- Tr em: 30mg/ kg/ 24h
2. SPIRAMYCIN
CH3 OH
CHO N(CH3)2
R2O CH3
10 8
CH2 HO 1" 2"
O
2'
O O CH3 OR3
12 6
1' O
CH3
D mycaminose
4
14 OCH3
1
3 OR1
16 O
CH3 O
Tn khc: Rovamycin.
Spiramycin dc dng: Dng base ca hn hp Spiramycin I, II, III
+ Spiramycin I: C43H74N2O14
+ Spiramycin II: C45H76N2O15
70
TI LIU THAM KHO
+ Spiramycin III: C46H78N2O15

1- Ngun gc.
- Chit xut t mi trng nui cy Streptomyces: Chit bng dung mi hu c t dch nui cy sau khi
kim ha tinh ch thu sn phm dc dng.
- Bn tng hp
2- Tnh cht.
* L tnh:
- Bt kt tinh trng nh vng nht
- tan: + Tan t trong nc
+ Tan c trong acid
+ D tan trong cc dung mi hu c: MeOH, EtOH, Aceton
* nh tnh:
- Ha Spiramycin / H2SO4 m c cho mu nu
- o UV
* nh lng:
- Bng phng php vi sinh vt: hot lc > 3900 UI/ 1mg cht th.
3- Dc ng hc.
- Hp thu: Nhanh nhng khng hon ton qua ng tiu ha.
- Phn b:
+ Thuc vo c dch ph qun, nc bt, xoang, xng khp, rau thai, sa m nhng khng dch
no ty.
+ Lin kt protein huyt tng km
- Chuyn ha gan
- Thi tr: ch yu qua phn, T1/2 = 8h
4- Ph khng khun. G
- Ph tc dng mnh hn, ch yu trn Gr (+) : lin cu, t cu, ph cu, bch hu
- Trn Gr (-): lu cu, mng no cu.
- Tc dg trn cc VK ni bo Mycoplasma, Rickettsia, Clammydia, xon khun giang mai, VK c hi
Mycobacterium kansasii.
- Khng tc dg trn VK Gr (-) a kh.
* C ch:
- C tc dng km khun do Ery gn vo tiu v 50S ca Ribosom ngn cn chuyn v peptidylARNt
t v tr tip nhn sang v tr trao i thng tin cc aminoacylARNt mi khng th vo v tr tip nhn
cc acid amin khng gn vo chui peptit ang thnh lp khng tng hp c protein cn thit
cho VK
5- Ch nh.
- Cc nhim khun ng h hp.
- Cc nhim khun da, c, xng, tit niu, sinh dc.
- Phng nga vim mng no do no m cu
- D phng thp tim cp bnh nhn d ng vi penicillin.
- Tr nhim Toxoplasma ngi mang thai
6- Ch phm v liu dng.
* Ch phm:
- Rovamycin vin nn 1,5 v 3 triu UI, bt pha hn dch ung 0,375 v 0,750 MU
* Liu dng:
- Ngi ln: 6-9 triu UI/ 24h chia 2-3 ln
- Tr em: 0,75- 3 triu UI/ 24h chia 2-3 ln.
3, AZITHROMYCIN
N(CH3)2
CH3 2'
H3C 10 98 HO O
1'
H3C N OH O CH3
HO 12 D des os amin
6
2H2O
H3C H3C
14 OCH3
15 4
CH3
HO CH3
1" 2"
H5C2 O
1 O
2
CH3 CH3 OH
O
O
L cladinos e
71
TI LIU THAM KHO
Tn khoa hc: Methyl-aza-11-desoxo-10 homoerythromycin A

1- Ngun gc: - c bn tng hp t Erythromycin A
2- Tnh cht.
* L tnh: Bt mu trng nh vng, v rt ng.
- Bn pH 7-8; khng bn pH < 4.
- tan: rt t tan trong nc, tan trong ether v cloroform
* nh tnh:
- Ch phm + xanhthydrol / ( HCl + CH3COOH ) cch thy mu .
- Ch phm + HCl c mu vng
- SKLM so vi Erythromycin chun
* nh lng:- HPLC - PP Vi sinh vt.
3- Dc dng hc.
- Hp thu nhanh, thc n lm gim hp thu thuc.
- Phn b: rng khp c th; c bit thuc t nng trong t bo cao hn trong huyt tng 10-100
ln iu tr tt khi nhim VK ni bo
4- Ph tc dng.
- Tc dng c trn Gr (-)
- Tc dng mnh trn H.influenzae, M.catahalis, Neisseria, VK ni bo nh Mycoplasma, Rickettsia,
Clammydia; VK c hi bnh nhn HIV/AIDS
5- Ch nh.
iu tr cc nhim khun nhy cm vi Eythromycin:
+ Nhim khun h hp, da, m mm, h sinh dc tit niu.
+ D phng thp khp thay th penicillin.
6- Tc dng MM.
- t c, t tc dng KMM s dng nhiu trong khoa nhi.
- D ng: vim gan, vng da, lon nhp
7- Chng ch nh.
- Vim gan.
- Ri lon Porphyrin
- Mn cm vi thuc
8- Ch phm, liu dng.
- Azithromycin (Zithromax, Azicin, Aziwok) vin nang, vin nn 125, 250, 500mg hn dch ung 250mg/
5ml
- Ngi ln: Ngy u 500mg/24h chia 1-2 ln; nhng ngy sau 250mg/ 24h ; t iu tr 5 ngy.
Chuyn 16: C C CHT H NG HUN NHM QUINOLON &

H NG SINH THC VT
I- I CNG V NHM THUC.
1- Cu trc.
O
R1 5 4 COOH
6 3
7 B A 2
8 1
R2 N
R
a s l dn cht ca acid 1,4- dihydro-4-oxo-quinolein-3-carboxylic.
2- Phn loi: Chia lm 2 th h:
- Quinolon th h I: Gm cc cht khng gn F (tr Flumequin), hin ch dng Nalidixic
c ph tc dng hp, ch c tc dng trn vk Gr(-) v ch yu iu tr nhim khun tit niu.
- Quinolon th h II:C gn F (C6): u c nguyn t fluor trong phn t, c hot tnh trn vk Gr(-) mnh
hn th h I, tc dng nhanh v mnh hn th h I. Ngoi cc vk Gr(-), chng cn c tc dng ln c vk
Gr(+). Thuc c tc dng dit khun ton thn
* Dc ng hc: Hp thu nhanh qua ng tiu ho. Thc n lm chm hp thu. Thi tr qua thn.
3- C ch tc dng.
72
TI LIU THAM KHO
- Qu trnh c ch tng hp acid nhn: quinolon gn vo topoisomerase II (gyrase) ca VK lm mt hot

tnh enzym. Do khng c kh nng m vng xon thc hin vic sao chp m di truyn nn VK b tiu
dit.
- To phc vi kim loi ha tr 2 ca cc Protein cha cc KL ny ion ha cc phc thnh phc c
hot tnh cao vi cc enzym chuyn ha mt tc dng ca enzym
4- Lin quan gia cu trc v tc dng.

- V tr 1: R = -C2H5, -C3H7, -OCH3 cho cc cht c tc dng tt.
- V tr 6: lun mang F cho cc Fluoroquinilon th h 2.
- V tr 7: l nhn piperazinyl-1 cho cc cht c tc dng tt trn trc khun m xanh.
- V tr 8: l F hoc OCH3 tng tc dng ca thuc v gim khng thuc ca Gr (+).
5- Ch nh.
- Th h I: ch yu dng trong cc nhim khun ng niu khng c bin chng.
- Th h II:
+ Nhim khun ng niu cp v mn , k c c bin chng.
+ Nhim khun ton thn: xng khp, m mm.
+ Vim mng no, vim ni tm mc, vim phc mc, nhim khun huyt.
6- Tc dng MM.
- Thn kinh: Nhc u, chng mt, bun ng.
- Ri lon th gic, thnh gic.
- Xng khp: gy au nhc, km pht trin xng khp nht l tui ang pht trin.
- Mu: tng bch cu a kim, gim bch cu lympho, a nhn, gim tiu cu.
- RLTH: bun nn, nn, au bng, tiu chy.
- Cc tc dng KMM khc: tng cm th nh sng, d ng.
7- Chng ch nh.
- PNCT v cho con b.
- TE < 16 tui.
- Ngi thiu men G-6DP v c nguy c thiu mu.
- Ngi c tin s ng kinh, co git.
II- THUC C TH.
1. ACID NALIDIXIC
O
5 4 COOH
6 3
7 2
1
H3C N N
C2H5
Tn khoa hc: Acid 1-ethyl-7-methyl-1,4-dihydro-4-oxo-1,8-naphtyridin-3-carboxylic
Bit dc: Negram, Nelidic.
1- Tnh cht.
* L tnh: Bt tinh th trng hoc vng nht
- tan: Khng tan trong nc. Tan trong methylenclorid, cc dung dich kim long. t tan trong aceton,
alcol.
* nh tnh: + o UV,mi trng:NaOH.
+ TLC th tp cht
+ P mu: Ch phm/ HCL + -naphtol/ EtOH mu cam.
* nh lng: Phng php o acid:
+ Mi trng: methylenclorid propanol nc.
+ Dung dch chun: NaOH/ EtOH.
+ Ch th: o in th.
2- Dc ng hc.
- Hp thu: Nhanh gn nh hon ton qua ng tiu ha. Ung 1g, t Cmax = 20 - 50g/ ml, sau 2h
- Phn b: t nng cao trong nc tiu (20 - 50g/ ml ); t qua rau thai v sa m.
- Chuyn ha: mt phn thnh acid hydronalidixic c hot tnh gn ging m
- Thi tr: thi ht qua nc tiu trong vng 24h.
3- Ph v c ch tc dng.
- Ph: + Ch yu trn Gr (-) nh E.coli, Proteus, Klebsiella, Enterobacter
+ Khng c td trn vi khun Gr (+) v VK k kh.
73
TI LIU THAM KHO
- C ch: c ch AND-gyrase c ch tng hp AND ca VK.

4- Ch nh.
- Nhim khun tit niu, sinh dc do cc VK gram (-): Vim bng quang, vim b thn, vim niu qun
- Vim ng tiu ha do VK Gr (-) : vim d dy, vim rut
5- Tc dng MM: Nhc u, chng mt, bun ng, ri lon th gic, tiu chy, bun nn, pht ban,
gim tiu cu.
6- CC: Mn cm vi thuc, PNCT v cho con b, tr em di 3 thng tui, bnh nhn suy thn, ri lon
to mu, ng kinh.
7- tng tc.
- Thuc lm tng nng trong huyt tng, tng tc dng ca theophylin, cafein, dn xut coumarin
- Cc cht kim ha nc tiu, cc thuc khng acid d dy lm gim tc dng ca acid nalidixic
6- Ch phm, liu dng.
- Negram, vin nn, vin nang , hn dch.
- Liu dng: + Ngi ln: 1g x 4ln/ 24h x 7ngy.
+ tr em > 3 thng: 50mg/ kg/ 24h chia 4ln.
2. CIPROFLOXACIN HYDROCLORID
O
F COOH
HCL H2O
N N
HN
Tn khoa hc: Acid 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolein carboxylic
monohydroclorid monohydrat.
Bit dc: Cicloxan, Ciproxin, Ciflox
1- Tnh cht.
* L tnh: Bt kt tinh hi vng.
- tan: Tan trong nc, kh tan / MeOH, rt kh tan / EtOH, khng tan/ Aceton, Dicloromethan.
* nh tnh:
- IR, SKLM
- Th tp lin quan bng TLC
* nh lng: HPLC
2- Dc ng hc.
- Hp thu: qua ng tiu ha .sinh kh dng khong 70 -80%. Thc n v antacid lm chm hp thu.
- Phn b: Rng khp trong cc m v dch c th.
+ t qua hng ro mu no ngi bnh thng, qua tt khi mng no b vim
+ Qua c rau thai, sa m.
- Thi tr: ch yu qua thn, T1/2 = 3 10h
3- C ch:
- c ch AND-gyrase c ch tng hp AND ca VK.
4- Ch nh:
Cc nhim khun do vk a kh gram (-) v vk gram (+) nhy cm
- Nhim khun ng tit niu, sinh dc, tiu ha, h hp
- Cc nhim khun xng, khp, m mm
- Cc nhim khun khc: vim mng no, vim mng trong tim, vim mng bng, nhim khun huyt
nhm ny nn dng cho cc nhim khun nng v cc nhim khun khng cc thuc thng thng
5- TDKMM:
- RLTH.
- au nhc, km pht trin xng khp nht l tui ang pht trin
- nhc u, chng mt, bun ng, kch ng TK, ng kinh nht l khi dng cng Theophylin
- tng bch cu a eosin, gim bch cu lymfo, gim bch cu a nhn, gim tiu cu, thiu mu
- d ng, nhy cm vi as
6- Chng ch nh: Mn cm vi thuc, PNCT v cho con b, tr em di 16 tui
7- Tng tc thuc.
- Thuc lm chm hp thu Cipro: Antacid, thuc c cha ion LK ha tr 2, thuc chng ung th nh
Vincristin, Cyclophosphamid, Doxorubicin
74
TI LIU THAM KHO
- Thuc lm tng tc dng ca Cipro: thuc chng vim ko steroid (Ibuprofen, Indomethacin) do cnh
tranh lin kt vi Protein huyt tng.
- Qinolon c ch enzym chuyn ha tng td ca thuc chng ng, Theophylin
5- Ch phm, liu dng.
- Ciprofloxacin: vin nn, nang 250 500mg; dd tim truyn 2mg/ ml; thuc nh mt 3,5mg/ ml
- Liu dng: 250 750mg/ ngy x 5 7 ngy.
Chuyn 17: THUC CHNG VIM STEROID & D. LIU CHA

SAPONIN STEROID
I- I CNG V THUC CHNG VIM STEROID:
1. cu trc chung ca nhm: ol-21-dion-3,20 ptegna-4-en
* Lin quan cu trc v tc dng:
O
20 21
18 CH3
12
17 OH
11 13 OH
16
19 CH3 14 15
1 9
2 10 8
3 5 7
4 6
O
Pregna-4-en-17,21-dihydroxy-3,10-dion
- V tr 17 phi c nhm OH
- V tr 11 phi c nhm OH v tr mi c hot tnh sinh hc. nu cha nhm khc (nh ceto) th khi
vo c phi chuyn sang dng 11- hydroxy mi c tc dng
- Thm dy ni i 1 (v tr 4,5) tc dng chng vim tng, tc dng gi mui v nc gim
- V tr 16 nu c nhm OH hoc CH3 tc dng chng vim hi gim nhng gim mnh tc dng gi
mui, nc
- Gn halogen (tt nht l flo) vo v tr 9 th tc dng chuyn ha glucid v mui khong u tng
- to vng cetonic 16, 17 tng tc dng ti ch
2- tc dng dc l:
- Chuyn ha cc cht: Chuyn ha glucid, lipid, protid, chuyn ha mui, nc
- Tc dng trn cc c quan v tuyn yn: trn TKTW, tiu ha, trn mu v t chc ht
- Chng vim, chng d ng v c ch min dch.
3- Ch nh iu tr
- iu tr thay th khi v thng thn ko tit hormon (thiu nng tuyn thng thn)
- iu tr cc bnh t min nh: lupus ban h thng, vim khp dng thp, thp tim v dng trong cc
phu thut cy ghp c quan chng phn ng loi mnh ghp ca c th
- iu tr d ng, shock phn v v cc bnh lin quan n phn ng d ng nh: hen ph qun, vim mi
d ng, my ay, vim da tip xc.
- Ch nh khc : Vim c, khp, vim da, chn on hi chng cushing.
4- Tc dng MM v cch khc phc:
- Tc dng ln s tng trng ca tr em. Khc phc: hn ch k n cho tr, ch k khi tht cn thit,
dinh dng hp l (tng m, canxi), khuyn khch vn ng
- Gy xp xng. Khc phc: dinh dng hp l (tng m, canxi), khuyn khch vn ng, dng
hormon sinh dc khi c th
- Lot d dy t trng: khc phc: dng khng H2 ( cimetidin, ranitidin), dng cc antacid nhng ko
c ung cng mu cch nhau 2h
- c ch HPA hoc ngc li cushing. Khc phc: gim liu t t, trnh lm dng thuc
5- Nhng iu cn ch khi dng Corticoid.
- Nn chn mc liu thp nht c hiu qu v trnh dng ko di.
- Nn chn loi c thi gian bn thi ngn hoc va.
- Suy thng thn l mt tai bin khi dng Corticoid, thng xy ra khi dng ko di hoc iu tr cho
ngi cao tui. trnh suy Thng thn cp khng ngng thuc t ngt, ngay c vi mc liu thp
nhng vi thi gian ko di.
- C th gp hin tng mt mi, chn n, trm cm sau khi ngng thuc, nhng hin tng ny s mt
i sau mt thi gian
75
TI LIU THAM KHO
- Khi dng cc ch phm c tc dng gi mui nc (Hydrocortison, Cortison, Prednisolon, Prednison),

cn ch lng Na+ c s dng nh sau:
+ Hn ch lng Na+ khi iu tr khong 10mg Prednisolon/ ngy.
+ King mui hon ton khi dng liu cao ( > 0,5mg/ kg/ 24h tnh theo liu Prednisolon ); hoc khi b
ph, tng HA
- Lng K+ phi , nu thiu phi b xung K+ hoc dng ch n giu K+
- Phi gim st K+ mu khi dng Corticoid liu cao, ko di, nht l khi phi hp vi thuc li tiu thi K+.
- Khi iu tr ko di, phi b xung Ca++ khong 1g/ ngy kt hp vi khong 400 v vitamin D
- iu chnh ch n: Tng protein, hn ch glucid, ng, cht bo.
II. THUC C NGUN GC HO DC:
1. HYDROCORTISON ACETAT
21
O CH2 O C CH3
C 20
H 18 CH3
O
HO 12
17 OH
11 13
16
19 CH3 H 14 15
1
2 10 8
H H
3 5 7
4 6
O
Tn khoa hc: 11, 17, 21- trihydroxy pregn-4-en-3,20-dion-21-acetat
Tn khc: Cortisol acetat
Bit dc: Cortef, Colifoam
1- iu ch: = pp Bn tng hp t Diosgenin, Cholesterol hoc mt Sterol khc
2- Tnh cht, nh tnh, dnh lng.
* Tnh cht:
+ L tnh: Bt kt tinh trng hoc gn nh trng. thc t ko tan trong nc, kh tan trong ethanol v
methylen clorid
- hp th UV, IR c trng, c gc quay cc ring
+ Ha tnh v kim nghim:
- tnh kh : do nhm 17 ceton
+ tc dng vi thuc th fehling to ta gch Cu2O
+ Tc dng vi AgNO3-NH3 to ta en ca Ag
+ Tc dng vi thuc th Tetrazolium clorid to mu
- Phn ng ngng t do nhm ceton v tr 3 v 20: tc dng vi phenylhydrazin to ta mu vng
phenylhydrazon
- Do c dy ni i hp th bc x t ngoi nn : nh lng = pp o ph hp th vng t ngoi
- phn ng vi H2SO4 to mu nu v hunh quang mu xanh
- Nhm chc acetyl : thy phn to acid acetic xc nh = dd FeCl3 hoc = phn ng to ethyl acetat
3- Tc dng, tc dng MM, ch nh xem phn i cng
4- Chng ch nh: lot d dy t trng, mn cm vi thuc, nhim nm virus, ang dng vaccin sng,
Thn trng khi dng cho bnh nhn b i tho ng, ph, cao huyt p, long xng
4- Dc ng hc.
- Hp thu: tt qua nhiu ng ung, IV, IM, bi trn da, phun m
- Phn b:
+ vo tt c cc m trong c th, qua c rau thai, sa m
+ Lin kt vi Protein huyt tng > 90%
- Chuyn ha,: chuyn ha gan,
- Thi tr: qua thn
5- Ch phm, Liu dng:
- Vin nn 10mg, hn dch 125mg/5ml, thuc m tra mt
- Liu tn cng: 60 100mg /24h
- Liu duy tr: 20 80mg/24h, ung, tim bp
2. PREDNISOLON
76
TI LIU THAM KHO
20
O 21
C
H 18 CH3
HO 12
17 OH OH
11 13
16
19 CH3 H 14 15
1
2 10 8
H H
3 5 7
4 6
O
Cng thc: ch khc Hydrocortison l c thm 1
Tn khoa hc: 11, 17, 21- trihydroxy pregn-1, 4-dien-3,20-dion
Bit dc: Delta-cortef, Hydrocortancyl, Prenisol
1- iu ch: Dng Corynebacterium simplex loi hydro ca Hydrocortison v tr 1 v 2
2- Tnh cht, kim nghim
- * Tnh cht:
methylen clorid
phenylhydrazon
- Phn ng mu vi H2SO4 c, sau 5 mu m, hunh quang nu/ UV 365; pha long = nc
mu nht dn v hunh quang vng/ UV 365 v c ta bng xm
3- Dc ng hc.
- Hp thu: tt qua nhiu ng ung, bi trn da, phun m
- Phn b:
- Thi tr: qua thn
Tc dng :
- L thuc c thi gian tc dng trung bnh 12-36h
- Tc dng chng vim > Hydrocortison 4 - 5 ln
- t gi Na+ v H2O t ph v tng HA
- /c mnh ACTH
6- Ch phm, Liu dng:
- Vin nn, nang 5mg, thuc m, kem 0,5% v 1%
- Ung 5 60mg /24h
3. DEXAMETHASON
O 20 21
C CH2OH
H 18 CH3
HO 12 OH
11 13 17
16 H
19 CH3 H 14 15
1 CH3
2 10 8
F H
3 5 7
4 6
O
Cng thc: khc vi Prednisolon l c thm 9-F v 16-CH3.
Tn khoa hc: 9-fluoro-11, 17, 21-trihydroxy-16 methyl-pregn-1,4-dien-3,20-dion
77
TI LIU THAM KHO
Bit dc: Dexadron, Dexason, Decacort

1- iu ch: Bn tng hp t Diosgenin
2- Tnh cht, kim nghim
- * Tnh cht:
methylen clorid
phenylhydrazon
- Th nguyn t F: v c ha ri tin hnh th theo hng dn, dd cho mu
3- Dc ng hc.
- Hp thu: tt qua nhiu ng ung, tim IM, IV, bi trn da, phun m
- Phn b:
- Thi tr: qua thn
Tc dng :
- L thuc c thi gian tc dng di 36-72h.
- t nh hng n chuyn ha mui nc.
- Chng vim > Hydrocortison 30 ln.
- iu tr cc trng hp vim cp, shock phn v, ph no cp.
- c ch mnh s tng trng, lm tng t l mt xng v c ch trc di i Tuyn yn Thng
thn.
6- Ch phm, Liu dng:
- Vin nn 0,5mg v 1mg, ng tim 5mg/ml; 15mg/3ml
Ung 3 6mg /24h ; tim 4 20mg/ ngy tim bp, tim TM
III- Dc liu cha Saponin steroid.
A- i cng.
1- nh ngha.
- Saponin l mt nhm Glycosid ln, gp rng ri trong thc vt
- c im:
+ Lm gim sc cng b mt, to nhiu bt khi lc vi nc, c tc dng nh ha v ty sch.
+ Lm v hng cu ngay nng rt long,
+ c vi c, v Saponin lm tng tnh thm ca biu m ng h hp lm mt cc cht in gii
cn thit.
+ Kch ng nim mc gy ht hi, mt; c tc dng long m, li tiu; liu cao gy nn ma i
lng.
+ C th to phc vi cholesterol hoc cc cht 3--hydroxysteroid khc.
- Da theo cu trc ha hc chia lm 2 loi:
+ Saponin triterpenoid
+ Saponin steroid
2- Saponin steroid.
Phn loi da vo cu trc ha hc: c 6 nhm
1, Nhm Spirostan.
- L ngun nguyn liu quan trng bn tng hp cc thuc Steroid
- V d: Sarsasapogenin
2, Nhm Furostan.
- Cu trc tng t nhm Spirostan, khc l vng F b bin i
- V d: Sarsaparillsid
3, NhmAminofurostan.
78
TI LIU THAM KHO
- V d: Jurubin.
4, Nhm Spirosolan.
- V d: Solasonin (c l x)
5, Nhm Solanidan.
- V d: Solanin (mm khoai ty)
6, Saponin c cu trc mch nhnh.
- V d: + Polypodosaponin.
+ Oslandin.
Chuyn 18: THUC IU TR VIM LOT D DY - T TRNG

I- I CNG V BNH:
1- nh ngha:
Lot d dy t trng l mt bnh mn tnh. Tn thng l nhng vt lot t nim mc d dy rut, c
th xm ln su hn qua lp di nim mc, v tr hay gp l lot b cong nh, mn v, hang v v hnh
t trng.
2- Sinh l bnh lot d dy t trng
- D dy hot ng c bnh thng nh s cn bng gia 2 qu trnh: qu trnh bi tit dch v v qu
trnh bo v. bnh lot d dy xy ra khi tng qu trnh bi tit, gim qu trnh bo v
- Nhng yu t nh hng n lot d dy t trng:
+ yu t XH: cng thng thn kinh
+ yu t th trng: tnh gia nh, bnh c th do mn cm i vi 1 khng nguyn no
+ Yu t ni tit: Ri lon ni tit gy tng tit dch v, gy lot (vd: tng tit corticoid)
+ yu t thuc: Corticoid, cc thuc chng vim ko steroid, ru..lm gim qu trnh bo v
+ Do nhim khun Helicobacter pylori (HP)
3- Nguyn tc v mc ch iu tr:
- Gim yu t gy lot: dng thuc lm gim tit HCl (cc cht gim tit) hoc trung ha HCl (cc
antacid)
- Tng yu t bo v: cc thuc bao bc, che ch nim mc (sucralfat) hoc tng tit cht nhy (
Misoprostol )
- Dit H.pylori: khng sinh
4- Phc iu tr khi HP (+):* Cc thuc c trong phc , dng phi hp cc thuc sau:
+ Cc cht gim tit: khng H2 hoc chn bm Proton
+ Khng sinh: 2 trong s 4 KS sau: Amoxicilin, Clarithromycin, Tetrecyclin, Imidazol ( Metronidazol
hoc Tinidazol )
+ Bismuth hu c: TDB, hoc CBS
* Cu to ca phc :
+ Phc b 3: 2KS + cht gim tit ( chn bm Proton hoc khng H2 )
Omeprazol + Amoxicilin + Clarithromycin
Omeprazol + Clarithromycin + Metronidazol
+ Phc b 4: 2KS + cht gim tit + Bismuth
Omeprazol + h/c Bismuth + Tetracyclin + Metronidazol
Omeprazol + h/c Bismuth + Tetracyclin + Amoxicilin
iu tr tn cng 1-2 tun, duy tr 4 6 tun.
1- Phn loi thuc cha vim lot d dy t trng:
+ Nhm thuc hn ch qu trnh bi tit dch v
- Thuc khng acid (antacid): Maalox, Gastropulgite, Phosphalugel
- thuc khng receptor H2 histamin : Cimetidin, Ranitidin, Famotidin
- Thuc khng acetylcholin receptor M1 cholinergic (RM1) : Pirenzepin, telenzepin
- Thuc khng gastrin : Proglumid
- Thuc c ch bm proton : omeprazol, lansoprazol
+ Nhm tng cng yu t bo v: Prostaglandin ( Misoprostol ), Sucralfat, cc ch phm ca bismuth
+ Nhm tr nhim khun HP : Khng sinh: Amoxicilin, Tetracyclin, Clarithromycin..kt hp vi thuc c
ch bm proton
III- THUC C TH :
1. CIMETIDIN
( Thuc khng Receptor H2 Histamin )
79
TI LIU THAM KHO
H
N
1
CH3
2 5 N CN
3 4
N CH2 S CH2 CH2 NH C NH CH3
Tn khoa hc: 2-cyano-1-methyl-3-[2-[[(5-methylimidazol-4-yl)-methyl]-thio] ethyl] guanidin.
Bit dc: Tagamet, Peptol
1- V cu to ha hc, tt c u c 1 d vng 5 cnh, 1 mch nhnh CH2SCH2CH2-R. Tn gi
..tidin.
CTCT chung : Ar CH2 S CH2 - R
2- Tnh cht :
* L tnh: Bt kt tinh trng hoc hu nh trng,
- tan: t tan trong nc, tan trong EtOH, cc acid v c long, kh tan trong Cloroform, khng tan
trong Ether.
- Hp th UV; IR c trng
* Ha tnh: ha tnh ca nhn thm, tnh base
3- im nghim:
* nh tnh:
- Bng pp qut ph UV, o hp th ring, SKLM
- N trong phn t tnh base yu. Tnh base mnh do N v tr 3 trong vng tc dng vi acid to
mui. ng dng diu ch dng mui d tan / H2O pha dung dch tim.
- Cimetidin/ H2O to hn dch c + HCl hn dch trong tr li + a. Silicovolframic to ta
- T/dng vi acid citric/anhydrid acetic tm
- V c ha vi s c mt ca Br2 /HNO3 SO42- . nhn bit = BaCl2 trng BaSO4
* nh lng:
- L = pp o acid/mt khan: ha tan / CH3COOH; nh lng = 1 acid mnh HClO4 0,1M; pht hin im
tng ng = cch o th or ch th mu.
4- Dc ng hc
- hp thu nhanh v hon ton qua ng tiu ha, t nng cao trong huyt tng sau 1 2h
- Sinh kh dng qua ng ung khong 30 80%; gn vi protein huyt tng mc trung bnh : 50%
- Chuyn ha gan khong 30%
- Qua c dch no ty v rau thai, sa m
- Thi tr qua thn trn 60% di dng ko chuyn ha. thi gian bn thi 1,5 2,3 h
5- C ch tc dng
- Do cng thc gn ging Histamin khng H2 tranh chp vi Histamin ti RH2 t bo thnh d dy
/c tit acid do cc nguyn nhn gy tng tit histamin d dy ( VD: cng ph giao cm, thc n,
tng tit gastrin)
- Lm gim tit c s lng v nng HCl
- Thuc khng c td trn RH1 m ch c td trn RH2
6- Tc dng
- c ch RH2 :
+ Lm gim bi tit acid dch v ( do c kch thch bi histamin, gastrin, cng ph giao cm)
+ Khng nh hng n bi tit cc dch tiu ha khc v chc nng d dy.
- Tc dng khng lin quan n /c RH2 :
+ Cimetidin /c Cyt P450 gan, Ranitidin t td, Famotidin Ko td ln Cyt P450
+ Cimetidin gy khng Androgen do gn vo R- Androgen.
7- Ch nh :.
- Lot d dy t trng: rt hiu qu vi lot cp tnh.
- Hi chng Zollinger-Ellison ( HC tng tit acid do cc khi u gy tng tit gastrin tuyn ty )
- iu tr chng tro ngc d dy-thc qun
- Lm gim tit dch v trong cc trng hp lot ng tiu ha c lin quan n tng tit dch v ( vim
lot thc qun, lot ming ni d dy rut )
8- TD KMM.
- RLTH: bun nn, to bn, tiu chy
- RLTKT: chng mt, nhc u, ng g
- au khp, au c
- Cimetidin c th gy h HA, lon nhp tim khi tim TM.
80
TI LIU THAM KHO
Him gp:
- Ni tit: Cimetidin khng androgen v tang tit prolactin chng v to, lit dng, gim tinh dch.
- RL to mu: thiu mu, gim bch cu
- Gan: mt do cimetidin,
- Do pH tng mt s VK to Nitrosamin t thc n gy ung th.
9- TNG T C THUC.
- Cimetidin /c Cyt P450 gan thay i SKD, tng tc dng v c tnh ca cc thuc chuyn ha qua
Cyt P450 , tng T1/2 ca cc thuc: Phenyltoin, Theophylin, Phenobarbitan
- Antacid lm gim hp thu khng H2 nn ung ch nhau 1 2h
10- CHNG CH NH.
- PNCT v cho con b: do thuc qua c rau thai v sa m dng khi cn thit
- Thn trng khi tim cimetidin phng tt HA, lon nhp tim.
11- CH PHM, LIU DNG.
- Cimetidin ( Tagamet)
+ Vin nn 200, 300, 400, 800mg. Dd ung 300mg/ 15ml. Dd tim 200mg/ 2ml
+ Liu dng: ung 200mg x 3ln/ ngy v 400mg trc khi i ng. t iu tr ko di 4 8 tun.
Liu duy tr 400mg/ ngy trc khi i ng.
+ Khi lot ang tin trin, chy mu d dy, nn tim bp hoc TM 4 8 ng/ ngy. Sau 7 ngy
chuyn sang dng ung.
OMEPRAZOL
( Thuc c ch H+/ K+ ATPase )
O
H
N S
N CH3
CH3O N
OCH3
CH3
Tn khoa hc: 5-methoxy-2-[[(4-methoxy-3,5-dimethylpyridin-2-yl) methyl] sulfinyl]- 1H-bezimidazol.
Bit dc: Omez, Losec, Prilosec.
1- Tnh cht
* L tnh: Bt kt tinh trng hoc hu nh trng.
- tan: rt t tan/ nc, tan trong MeOH, EtOH v Dd kim long
- C gc quay cc ( v c trung tm bt i )
* Ha tnh.
- Tnh acid do H v tr 1 mang li, tnh acid ny l do hiu ng cm ng ca nhm Sulfinyl gy ra.
+ Ch phm/ H2O hn dch c + NaOH, lc trong tr li
+ Trung ha kim d, td vi KL nng hoc KL mu to mui kt ta hoc mui mu.
- Tnh cht ca nhn thm: hp th UV
- tnh base: Tnh base do nhn pyridin mang li:
+ Ch phm/ H2O hn dch c + HCl, lc trong tr li
+ t/dng vi 1-cloro 2,4 dinotrobenzen mu tm
+ T/dng vi Na2CO3 , un nng mi pyridine c bit
+ t/dng vi tt chung ca alkaloid to mu hoc to ta.
- V c ha vi s c mt ca Br2 /HNO3 SO42- . nhn bit = BaCl2 trng BaSO4
- P/ng ca nhm methoxyphenyl : p/ng vi TT marqui to mu
2- Kim nghim:
nh Tnh
Bng pp qut ph UV, o hp th ring, SKLM
C tnh acid: pKa1 = 8,7. Tan trong cc dd kim to mui. Cc mui ny cho ta hoc phc mu vi
mt s ion kim loi.
C tnh base: pKa2= 3,97. Tan trong cc dd acid v c. Cho p/ vi cc TT alcaloid.
= cc phn ng ha hc trong phn ha tnh
nh lng
L = pp o quang, HPLC, o gc quay cc
81
TI LIU THAM KHO
L = pp o acid/mt khan: ha tan / CH3COOH; nh lng = 1 acid mnh HClO4 0,1M; pht hin im
tng ng = cch o th or ch th mu.
3- DC NG HC.
- Hp thu: nhanh qua ng tiu ha, thay i ty thuc liu v pH d dy. SKD ng ung 70%
- Phn b: Gn mnh vo Pr huyt tng
- Chuyn ha: qua gan, thi tr qua thn 80%, T1/2 = 30 90 pht.
3- C CH T C DNG.
- /c H+/K+ ATPase
- Khi vo c th pH < 5, omeprazol c Proton ha thnh 2 dng: acid Sulphenic v Sulphenamic
- 2 cht ny gn thun nghch vi nhm sulfhydryl ca H+/K+ ATPase t bo thnh d dy /c bi
tit acid do bt k nguyn nhn no.
4- T C DNG.
- /c c hiu v khng hi phc bm Proton, do tc dng chn lc trn t bo thnh d dy td nhanh
v hiu qu cao.
- t nh hng n khi lng dch v, s bi tit Pepsin, yu t ni ti d dy, v s co bp ca d
dy.
5- CH NH.
- Lot d dy tin trin hoc dng khng H2 m khng c hiu qu.
- hi chng Zollinger Ellison v hi chng tro ngc d dy, thc qun.
6- T C DNG MM.
- RLTH: bun nn, to bn, tiu chy
- RLTKT: chng mt, nhc u, ng g
- Do /c tit acid pH tng mt s VK to Nitrosamin t thc n gy ung th.
7- CHNG CH NH.
- Mn cm vi thuc.
- Lot d dy c tnh.
- PNCT v cho con b.
8- CH PHM, LIU DNG.
- Omeprazol ( Losec, Mopral ): vin nn, vin bao tan trong rut 20mg
+ iu tri lot d dy t trng: 20 40mg/ ngy x 4 6 tun.
+ iu tr tro ngc: 20 40mg/ ngy x 4 12 tun.
+ iu tr Zolliger Ellison: > 120mg/ ngy x 4 tun.
Chuyn 19: THUC IU TR HO HEN

I- I CNG V BNH.
1. HO
* nh ngha: Ho l mt ng tc th mnh, t ngt gm 3 thi k:
+ Ht vo su v nhanh.
+ Bt u th ra nhanh, mnh + s tham gia ca cc c th ra; np thanh mn ng li p sut
lng ngc tng cao.
+ Thanh mn m ra t ngt khng kh trong phi c tng ra ngoi.
* C ch:
Cc thnh phn ca phn x ho gm:
+ Kch thch cc Receptor ho nim mc hng, thanh qun, KQ, PQ.
+ Xung ng t R ho si cm gic ca dy X truyn v trung tm ho ( hnh ty)
+ T trung tm ho, xung ng si vn ng ca dy X, TK ty, TK honh c th ra iu
khin ng tc th ra
+ S phi hp co c thanh qun, c honh, bng, thnh ngc th ra mnh cc cht nhy, vt l
ng h hp b y ra ngoi.
* Nguyn nhn.
- Cc bnh ng h hp.
- Bnh tim mch gy tng p lc tiu tun hon.
- Do tc dng KMM ca thuc
2. HEN PH QUN
* nh ngha: HPQ l mt bnh ca h h hp, c trng bi s tc nghn ng th c hi phc, vim
mn tnh v tng tnh p ng ca ng th i vi nhiu kch thch khc nhau.
* C ch:
82
TI LIU THAM KHO
Khi ht phi KN phc hp IgE KN c hnh thnh v gn vo t bo mast v t bo mast gii

phng cht trung gian ha hc (histamin, leucotrien, prostaglandin), ng thi hot ha bch cu i toan
mt lot P:
+ Co tht c trn PQ.
+ Ph n nim mc PQ.
+ Tng tit nhy ca nim mc PQ.
+ Tn thng v bong nim mc PQ.
Nhng yu t trn phi hp tc nghn ng th.
* Triu chng:
- Lm sng:
+ Xy ra t ngt, khi thi tit thay i.
+ Khi u tc ngc, ho khan
+ Cn kh th tng, kh th chm, kh th ra.
+ C ting c c.
+ Khm: phi c ran rt, ran ngy; nhp tim nhanh, huyt p tng
+ Sau cn kh th: ho nhiu, khc ra m.
- Cn lm sng:
+ X quang phi:
- Lng ngc v c honh km di ng
- Cc xng sn nm ngang
- 2 phi qu sng.
+ Chc nng h hp:
Ri lon thng kh tc nghn biu hin bng:
- Ch s FEV1, PEF, Tiffeneau gim.
- VC bnh thng.
- Ch s sc cn ng th tng
Test kch thch ph qun v test gin PQ (+)
+ Kh mu: PaO2 ; PaC2; SaO2; pH mu : toan h hp.
+ Test da v d nguyn (+).
* iu tr:
Mc tiu iu tr:
- iu tr kp thi cc cn hen cp, v t hen cp
- iu tr d phng cc cn hen c hen t xy ra hn.
- Duy tr chc nng h hp bnh thng hoc ti u.
- m bo cht lng cuc sng
- u tin dng thuc ht hn ch tc dng ph
- D phng tc nghn phi khng hi phc, hn ch t vong.
Thuc iu tr:
a- Thuc ct cn.
- Khi c cn: dng thuc gin ph qun nh Salbutamol, Terbutalin dng ht
- Khi c cn hen nng: Thuc gin ph qun (kh dung, ung, tim TM ) + Corticoid (Hydrocortison)
tim tnh mch.
b- Thuc d phng cn hen.
- Corticoid:
+ Thng dng dng kh dung : Beclomethason (Becotid, Beclofort)
+ Dng ung: Prednisolon
+ Dng tim tnh mch: Hydrocortison
- Sodium cromoglycat: l thuc lm n nh mng t bo mast v cct bo vim khc.
1. CODEIN
Tn khoa hc: 3-methoxy-4,5-epoxy-7,8-didehydro-17-methyl

morphinan-6-ol monohydrat.
1- Ngun gc, iu ch: codein l methylmorphin
- Bn tng hp t Morphin
- iu ch: Methyl ha Morphin bng trimethyl phenylamoni
hydroxyd
83
TI LIU THAM KHO
CH3
+
OH-
H3C N CH3 H3C N CH3
MORPHIN +
CODEIN + + H2O
2- Tnh cht
* L tnh: Tinh th khng mu hay bt kt tinh trng, Khng mi, v ng
- tan: t tan trong nc, tan nhiu hn trong nc si, tan trong EtOH, cloroform v acid long.
* Ha tnh:
- Khng c nhm OH phenol bn hn Morphin
Khng tan trong kim mnh
Khng cho mu vi FeCl3 , nhng khi loi CH3 gii phng nhm OH
t do (un vi H2SO4) th s cho mu vi FeCl3
- Ha tnh ca N bc 3
3- im nghim.
* nh tnh:
- o gc quay cc
- Ph IR, UV so vi chun
- Ch phm/ H2SO4 + FeCl3 un nng xanh lam + HNO3 c mu .
- Phn ng vi thuc th chung ca Alcaloid
* nh lng:
- PP o acid/ mt khan: Ha tan / CH3COOH; L = dung dch acid mnh HClO4; Xc nh im tng
ng = pp o th hoc ch th mu
- o quang, HPLC
4- Dc ng hc:
- Hp thu qua ng ung, sau khi ung 1 2h, tc dng xut hin v ko di 4 6h
- Thuc qua c nhau thai
- Chuyn ha gan v thi tr qua thn
5- Tc dng v ch nh: Gim au v gim ho
- Gim au km morphin, thng phi hp vi gim au ngoi vi (Efferalgan codein, Dafalgan codein)
- c ch trung tm ho gim ho mnh
6- Chng ch nh: Mn cm vi thuc, tr em di 1 tui, bnh gan, suy h hp
7- Ch phm v liu dng:
Vin nn 15, 30, 60mg; ng tim 15, 30, 60mg/ml ngoi ra cn c dng phi hp trong ch phm gim
au, gim ho
Liu dng:
- Gim au: 15 60mg/ln, mi ln dng cch nhau 4h, ti a 240mg/24h
- gim ho : 10 20mg/ln x 3 4 ln/24h
* Liu lng:
- Ung : 0,05g/ ln; 0,2g/ 24h.
- Tim: 0,03 0,08g/ 24h.
2. SALBUTAMOL SULPHAT
CH3
HO CH CH2 NH C CH3 H2SO4
OH CH3
CH2OH
2
Tn khoa hc: 1(4-hydroxy-3-hydroxymethyl phenyl)-2-(terbutylamino) ethanol
Bit dc: Albuterol, Sultamol.
1- Tnh cht: Bt kt tinh trng hoc gn trng, v hi ng
- tan: Hi tan trong nc; Tan trong EtOH 96%; kh tan trong Ether
2- Ha tnh- kim nghim
84
TI LIU THAM KHO
* nh tnh:
- o IR, UV, SKLM
- = phn ng mu : Ch phm/ Natri tetraborat + 4-aminophenazon + Kali fericyanid + Cloroform lc
v yn cho tch lp lp Cloroform mu cam.
* nh lng:
- PP o acid/ mt khan: Ha tan / CH3COOH; L = dung dch acid mnh HClO4; Xc nh im tng
ng = pp o th hoc ch th mu - o quang, HPLC
3- Dc ng hc.
- Hp thu: dng ng ung hoc kh dung
+ Ung c tc dng sau 30 pht v duy tr td 4-6 h
+ khi dng = Kh dung thuc c tc dng sau 2-3 pht.
4- Tc dng v c ch.
- Thuc kch thch chn lc Receptor 2 adrenergic lm tng tng hp AMP vng lm gin c trn
kh ph qun, gin c trn t cung, mch mu v kch thch c vn.
5- Ch nh: Hen ph qun, Da non.
6- Tc dng MM.
- Run c, nh trng ngc, nhp tim nhanh, nhc u, chng mt, mt ng.
- Khi dng ko di quen thuc.
7- Chng ch nh.
- Lon nhp tim.
- Suy mch vnh.
- Tng HA.
- Ngi c thai 3 thng u.
8- Ch phm, liu dng.
- Salbutamol (Ventolin, Albuterol ): vin nn 2mg, 4mg;
- Kh dung: 100g/ ln ht x 4ln/ 24h.
- Ung: 2 4mg/ ln x 3 -4 ln/ 24h.
Chuyn 20: THUC IU TR BNH I TH O NG

I- I CNG V BNH:
1- nh ngha:T l mt bnh mn tnh, gy ra bi s thiu ht tng i hoc tuyt i insulin, dn
n cc RL chuyn ha hydrat carbon. Bnh c c trng bi tnh trng tng ng huyt mn tnh
v cc RL chuyn ha.
2- Phn loi:
- i tho ng typ I: T ph thuc insulin
- i tho ng typ II: T khng ph thuc insulin
- i tho ng cc typ c hiu khc:
+ T th pht: do bnh l ty ngoi tit, ni tit
+ T khi mang thai
+ Ri lon dung np Glucose.
3- C ch bnh sinh:
* i tho ng typ I:
a/ T typ I l mt bnh t min:
Cc t bo ca tiu o Langerhans b ph hy theo c ch t min dch:
+ C s thm nhim ca lympho T trong cc t bo
+ C t khng th khng tiu o Langerhans trong mu.
+ C khng th khng insulin trong mu ( c khi cha dng insulin )
+ C khng th khng Glutamat decarboxylase trong mu
khi c triu chng LS th hu ht cc t bo b ph hy kh nng tit insulin ca cc t bo
cn rt t v cn kit dn.
b/ H gen nhy cm:
Nhng i tng d nhy cm vi T typ I thng c khng nguyn HLA DR3 v HLA DR4
c/ Yu t mi trng:
Nhim khun, nhim c, Stress
* i tho ng typ II:
- Tng tnh khng Insulin:
+ Gim td ca insulin do gim th th insulin t bo.
+ Gim kh nng kt dnh ca insulin vo th th
- Ri lon tit insulin:
85
TI LIU THAM KHO
+ Tng insulin mu b tr.

+ Tng tin cht khng c hot tnh ( Proinsulin )
+ Mt tnh cht tit insulin theo tng t.
- Yu t di truyn: c tnh cht gia nh.
- C th bo ph: l yu t tng nguy c T typ II.
- Ch n ung, sinh hot khng ph hp, t vn ng
4- Sinh l bnh.
* i tho ng typ I:
- Thiu insulin tuyt i t bo khng c cung cp glucose hu qu:
+ M chuyn a.amin huydrat carbon tng glucose/ mu.
+ M d tr s b chuyn ha sn phm cui cng l cc a.bo t do.
- S oxy ha cc a.bo t do thnh cc th ceton hu qu:
+ Cc th ceton c chuyn t m vo mu ceton vglucose mu. c 2 s b o thi vo
nc tiu.
+ Th ceton lm pH mu gim nhim toan ceton
+ S thi ceton & glucose qua nc tiu mt nc + in gii hn m.
- Tng glucose huyt mn tnh tn thng mch mu & cc bin chng khc.
* i tho ng typ II:
- Thiu insulin tng i do insulin khng pht huy c tc dng nn:
+ Glucose vo trong c & t bo m khng sinh th ceton.
+ Do tng p lc thm thu glucose mu c th rt cao hn m
- Tng glucose huyt mn tnh tn thng mch mu & cc bin chng khc.
5- Triu chng.
C IM T TYP I T TYP II
Tui khi pht < 40 > 40
Th trng Gy Bo hoc bnh
thng
Insulin mu Thp hoc khng o Bnh thng hoc
c cao
Kt hp vi HLA c C Khng
hiu
Tin s T trong gia Thng khng c Thng c
nh
Triu chng + Khi pht t ngt + Khi pht & tin
+ HC tng ng trin m thm
huyt + Khng bc l
( n nhiu, ung cc triu chng LS
nhiu, i nhiu, gy + Ceton niu (-)
nhiu )
+ Ceton niu (+)
Bin chng cp tnh Nhim toan ceton Hn m do tng p
lc thm thu.
6- Tiu chun chn on:

- Mu ng huyt bt k > 11,1mmol/ lit, km triu chng LS.
- ng huyt lc i > 7mmol/ lit
- ng huyt 2h sau khi ung 75g glucose: > 11,1mmol/ lit.
7- Bin chng:
Bin chng CP TNH Bin chng MN TNH Bin chng KHC

+ Nhim toan ceton: typI + Mch mu ln: suy vnh, + Nhim khun: c hi
+ Hn m do tng p lc thm thu: vim M chi di, cc M + tn thng da: lot bn,
typ II khc, tai bin mch no, tng cng chn
+ H ng huyt: dng thuc qu HA + Khp: kh cng khp
liu; bn b i + Mch mu nh: vng mc,
thn, thn kinh
8- iu tr:
* T typ I: Liu php Insulin v 4 nguyn tc:
Liu php Insulin:
86
TI LIU THAM KHO
+ n nh ng huyt cho BN
+ Liu dng, ng dng: ty thuc vo cch sinh hot ca BN.
Ch n:
+ Khu phn n cn bng (50% Glucid; 30 - 5% Lipid; 10 15% Protid )
- Cung cp dinh dng
- Hn ch loi ng hp thu nhanh
+ Nhu cu nng lng ph thuc BN
+ Chia thnh nhiu ba v gi n phi u.
im sot ng huyt:
+ nh lng ng huyt thng xuyn iu chnh liu thuc ph hp.
Gio dc BN:
+ Kin thc & nguyn tc iu tr BN phi hp vi BS trong iu tr
hm nh k:
+ Theo di bin chng.
* T typ II:
Ch n:
- BN bo ph:
+ n t calo ( < 1200 Kcal/ ngy ), gim 20 25% so vi nhu cu NL.
+ Chia 3 ba/ ngy
+ Cn bng khu phn; hn ch ng hp thu nhanh.
- BN cn nng bnh thng:
+ Lng calo ty thuc BN nhng phi cn bng.
Vn ng th lc:
+ iu chnh ty la tui v tnh trng BN
Thuc h ng huyt:
c ch nh sau khi ch n v vn ng th lc trong kim sot ng huyt b tht bi.
+ Sulfonylurea: dng cho BN cn nng trung bnh v tha cn nh.
+ Biguanid: BN bo ph.
+ Nu kim sot ng cha tt: tng liu hoc phi hp thuc.
+ Dng Insulin n thun hoc phi hp nu thuc h ng huyt tht bi.
im sot ng huyt; gio dc BN; khm nh k: nh T typ I.
II- THUC C TH:
1. ACARBOSE
Tn chung quc t: Acarbose.
Tn KH: O-4,6-dideoxy-4-[[4,5,6-trihydroxy-3-(hydroxymethyl)-2cyclohexen-1-yl]amino]--D-
glucopyranosyl- (14)O-]--D-glucopyranosy-(14)-D-glucose.
Bit dc : Glucobay
1- Ngun gc: L mt oligosaccarid c iu ch bng qu trnh ln men ca VK Actinoplanes
utahensis.
2- Tnh cht:
* L tnh : Bt trng hoc hu nh trng , tan trong nc, pKa 5,1 .
* Ha tnh:
87
TI LIU THAM KHO
3- im nghim:
* nh tnh:
* nh lng:
3- Tc dng, c ch.
- Acarbose c tc dng c ch cnh tranh thun nghch vi -amylase v - glucosid hydrolase m cc
enzym ny tham gia thy phn tinh bt thnh oligosaccarid lm gim nng glucose/ mu
- Acarbose khng gy tng tit Insulin, khng gy gim ng huyt.
4- Ch nh: i tho ng typ II.
5- Liu dng: 25mg/ ln ; 3 ln/ ngy trc mi ba n . Sau 4-8 tun chnh liu.
6- Tc dng MM.
- Tng acid Lactic toan mu
- Ming c v kim loi, bun nn, nn, tiu chy
- Dng ko di chn n, ng ming, st cn.
7- Chng ch nh: PNCT, suy gan, thn, suy tim, suy h hp.
8- Ch phm : Vin nn 25mg, 50mg , 100mg .
2. METFORMIN HYDROCLORID
H3C H
N N NH2
H3C HCl
NH NH
Tn khoa hc: 1,1-dimethylbiguanid hydroclorid.
Bit dc: Apo-Metformin, Glucophage, Glycon, Novo-Metformin.
1- Ngun gc:Tng hp ha hc
2- Tnh cht.
* L tnh: Tinh th trng
- tan: D tan/ H2O, kh tan/ EtOH; Khng tan trong aceton
* Ha tnh: ca nhm Biguanid, ca HCl kt hp
3- im nghim:
* nh tnh:
- Phn ng ca Nhm Biguanid:
+ T/d dd kim to NH3 lm xanh giy qu.
+ T/d vi - naphtol/ mt kim v natrihybromid to mu hng.
+ Tnh base yu: t/dng vi tt chung ca alcaloid
- Nhm HCl kt hp: t/d vi AgNO3 trng
* nh lng:
- PP o acid trong mi trng khan: ( ha tan / CH3COOH; nh lng = 1 acid mnh HClO4 0,1M; pht
hin im tng ng = cch o th or ch th mu.
- L phn acid kt hp = PP trung ha or PP o bc
88
TI LIU THAM KHO
3- Tc dng, c ch.
- Cc dn xut Biguanid c ch hp thu glucose rut.
- Tng nhp glucose vo t bo
- Kch thch phn hy v c ch ti to glucose
- Ngoi ra cn tc dng lm gim lipid mu.
4- Ch nh: i tho ng typ II.
5- Tc dng MM.
- Tng acid Lactic toan mu
- Ming c v kim loi, bun nn, nn, tiu chy
- Dng ko di chn n, ng ming, st cn.
6- Chng ch nh: PNCT, suy gan, thn, suy tim, suy h hp.
7- Ch phm, liu dng.
- Glucophage vin nn 500, 850, 1000mg - Liu dng: 1 3g/ 24h.
3. GLIBENCLAMID
Cl
O O
C NH CH2 CH2 SO2 NH C NH
OCH3
Tn khoa hc: 1-[4-[2-(5-cloro-2-methoxybenzamido) ethyl] benzensulfonyl]-3- cyclohexylure
Tn khc: Glyburid
Bit dc: DiaBeta; Novo-glyburid.
1- Tnh cht.
* L tnh: Bt kt tinh trng
- tan: tan trong cc dd kim long. Kh tan trong MeOH, EtOH thc t khng tan trong nc, ether.
* Ha tnh:ca nhn thm, ca nhm sulfonylure, ca ion Cl-
2- im nghim
* nh tnh:
- Nhn thm: hp th t ngoi.
- Nhm chc Sulfonylure: tnh acid yu, d b thy phn/ kim gii phng NH3 xanh giy qu ; acid
ha gii phng CO2
- V c ha = cht oxi ha Br2/HNO3 : SO4-2 nhn bit = cch cho t/dng vi BaCl trng
* nh lng:
- PP o kim trong mi trng khan: ha tan / DMF ( dimethyl formamid) ; nh lng = 1 dd kim mnh (
LiOCH3, NaOCH3); tm im tng ng = o th or ch th mu
3- Dc ng hc.
- Hp thu tt qua ng tiu ha.
- Phn b: lin kt mnh vi protein huyt tng 90 - 99%
- Chuyn ha gan, thi tr qua nc tiu; T1/2 = 3h.
4- Tc dng v c ch.
- Kch thch trc tip t bo o Langerhans tng sn xut insulin gim glucose mu.
- Lm tng s lng Receptor ca insulin cc t bo tc dng ca insulin.
- c ch nh tc dng ca Glucagon h glucose mu.
5- Ch nh: i tho ng typ II (khng ph thuc insulin)
6- Tc dng KMM: H ng huyt, RL tiu ha, vng da mt, D ng
7- Chng ch nh: i ng typ I, PNCT, ngi suy gan thn
8- Tng tc thuc.
- Cnh tranh v tr gn vi protein huyt tng tng tc dng ca cc thuc: Dicoumarol, Phenyltoin
Salicylat, Phenylbutazol, Sulfamid
- Thuc lm tng tc dng ca Sulfonylure: Cloramphenicol, IMAO, Probenecid
- Thuc lm gim tc dng ca Sulfonylure: Corticoid, thuc trnh thai, Rifampicin
- c bit khng phi hp Sulfonylure + thuc /c Adrenergic v gy nhp tim nhanh, tng huyt ng
v h glucose mu.
89
TI LIU THAM KHO
9- Ch phm, liu dng.

- Glyburid: vin nn 1,25 n 5mg
- Liu dng: 2,5 20 mg/ 24h.
Chuyn 21: THUC IU TR UNG TH

I- AI CNG V BNH:
1- nh ngha:
- Ung th l mt bnh c tnh do s tng sinh bt thng t bo v m ca c th. Trong bnh ung th,
cc t bo sinh sn mt cch v hn khng tun theo c ch kim sot v pht trin c th.
2- c im:
- Bnh c qu trnh pht sinh, pht trin lu di m khng c triu chng. Pht hin c khi khi u pht
trin nhanh v gy RL chc nng ca c th; giai on cui thng au d di.
- Khc vi khi u lnh tnh, ung th pht trin ti ch v xm ln vo cc m lnh xung quanh, di cn ti
hch bch huyt v cc c quan khc trong c th.
- C 2 loi ung th thng gp:
+ Ung th biu m (Carcinom): Xut pht t biu m ca cc tng, cc c quan. K biu m thng di
cn theo ng bch huyt.
+ Ung th t chc lin kt (Sarcom): Xut pht t t bo ca t chc lin kt ca c th. Sarcom
thng di cn theo ng mu.
3- Chu k t bo:
- Chu k t bo l qu trnh phn chia t bo, din ra c t bo bnh thng ln t bo ung th, gm 4
pha:
+ Pha G1 ( tin tng hp ADN ): Tng hp cc thnh phn cn thit chun b cho tng hp ADN.
+ Pha S: Tng hp ADN.
+ Pha G2 ( Tin gin phn ): Nhn c sp xp li chun b cho gin phn.
+ Pha M (gin phn ): T bo m tch thnh 2 t bo con.
+ Pha Go (Pha ngh ): TB khng phn chia, khng chuyn ha tch cc, nhng s tr li chu k TB khi
c kch thch thuc rt kh tc ng vo pha ny l nguyn nhn gy ti pht bnh.
II- I CNG V THUC.
1- Phn loi.
* Da vo v tr tc ng trn chu k t bo:
- Thuc tc ng c hiu theo 1 pha:
+ Trn pha M: Alc ca Da cn, dn xut Taxan, Epipodophyllotoxin.
+ Trn pha S: nhm khng chuyn ha.
- Thuc tc ng trn nhiu pha ca chu k t bo: Alkyl ha, cc khng sinh.
- thuc tc ng ko c hiu trn chu l t bo: cytarabin
* Da vo cu trc ha hc v c ch:
- Nhm khng chuyn ha.
- Nhm Alkyl ha.
- Nhm chng phn bo.
- Nhm khng sinh.
- Nhm hormon v khng hormon.
- Nhm enzym.
- Nhm thay i p ng min dch.
2- S khng thuc ca t bo ung th.
* C ch:
- Tng cng sa cha ADN b tn thng.
- To cc by gn vo thuc mt tc dng ca thuc.
- Gim tch ly thuc nng khng t dit TB ung th.
- Thay i ch enzym, hot tnh enzym chuyn ha lm gim hoc mt tc dng ca enzym.
3. Tc dng:
- nhm khng chuyn ha: c ch cnh tranh hoc c ch tng hp purin, pyrimidin or acid folic l nhng
cht quan trng trong tng hp acid nucleic
- Nhm alkyl ha: chuyn ha to ra gc alkyl. Cc gc alkyl s lin kt cng ha tr vi guanin v tr N 7
ca c 2 mt, ngn cn s tch i v sao chp do c ch tng hp AND, ARN t bo ung th ko
nhn ln
- Nhm chng phn bo: cc thuc gn chn lc vo cc tubulin nn ngn cn s tp hp ca cc dimer
tubulin lm tan r thoi gin phn v c ch s tch i ca cc nhim sc th lm t bo ung th b tiu
dit
90
TI LIU THAM KHO
- nhm khng sinh: cc khng sinh thng xen vo gia phn t AND hoc to lin kt cho gia 2 phn
t AND gy tn thng AND nn c ch s phn chia t bo
- Nhm hormon v khng hormon: c ch bi tit hoc i khng tc dng hormon
- Nhm thay i p ng min dch: c ch tc dng khc nhau, Vd: interleukin kch thch min dch, c
ch s tng trng v lan truyn ca khi u.
3- Tc dng MM.
- Trn ty xng: c vi ty xng gim HC, BC, tiu cu.
- Trn h tiu ha: bun nn, nn, tiu chy, lot rut, lot ming
- Trn thn kinh: d cm, ri loan hnh vi, c x, ng lm, ic.
- Vi da, tc: xm da, rng tc, hi u.
- Cc tc dng KMM khc: suy tim, lon nhp, vim phi, RL chc nng gan, thn.
4- Nguyn tc s dng thuc chng ung th.
- Ch dng khi c chn on r rng bng Xno t bo.
- Dng thuc phi kt hp phu thut + chiu x.
- Dng phi hp nhiu thuc tng hiu qu, gim khng thuc.
- La chn thuc phi ph hp loi ung th, giai on bnh, th trng BN
- Chn liu v ng dng thch hp.
III- THUC C NGUN GC HO DC:
1 VINPLASTIN SULFAT
Tn khc: Velban,
2- Tnh cht.
* L tnh:
- Bt kt tinh mu trng hoc vng nht, d ht m
- tan: ch phm tan/ 10 phn nc, thc t ko tan trong EtOH, Ether.
- Ha tnh: phn ng ca nhn indol
* nh tnh: o IR, UV, SKLM
= phn ng: ha ch phm vo dd mi pha ca vanilin trong HCl th c mu hng
* nh lng:
- HPLC, so snh vi chun
3- Dc ng hc.
- Hp thu: Qua ng ng tim tnh mch
- Phn b: rng khp c th, tp trung nhiu gan, lch, mt, ko vo dch no ty.
- Chuyn ha : gan
- Thi tr: Qua mt (40 70%), 1 phn thi qua nc tiu
4- Tc dng v c ch.
- Thuc chng ung th loi chng phn bo
* C ch: cc thuc gn chn lc vo cc tubulin nn ngn cn s tp hp ca cc dimer tubulin lm tan
r thoi gin phn v c ch s tch i ca cc nhim sc th lm t bo ung th b tiu dit
5- Ch nh.
- iu tr bnh bch cu cp, bnh hodgkin, u lympho ko hodgkin, u nguyn bo thn kinh, sarcom
lympho, sarcom li..
- Ung th v, t cung, ung th phi t bo nh, ung th tuyn gip
6- Tc dng MM.
- c vi thn kinh, co git, d cm, gim or mt trng lc c, mt phn x su
- RL tiu ha, h hp, gim bch cu, tiu cu, vim li, rng tc, vim da, vim c, ri lon kinh nguyt,
mt tinh trng.
7- Chng ch nh.
- suy ty, bnh thn kinh, chiu tia x X vng tnh mch ca v gan
- Nhim khun, nhim virut
- ngi mang thai, cho con b, mn cm vi thuc
8- Ch phm, liu dng:
- L 5mg hoc 10mg ch phm ng kh km 1 ng dung mi
- Liu 5,5 7,4mg/m2 da /tun.
91
TI LIU THAM KHO
2 FLUOROURACIL
H
N O
4 2
5 1 NH
F
O
Tn khoa hc: 5-fluoro pyrimidindion- 2,6.
Tn khc: 5-FU, Phthoruracilum, Adrucil, Arumel.
1- Tnh cht.
* L tnh:
- Bt kt tinh trng, hoc gn nh trng, khng c mi.
- tan: + Tan trong 80 phn nc, 170 phn EtOH, 55 phn MeOH.
+ Khng tan trong Cloroform, Ether, Benzen.
* nh tnh:
- o IR, SKLM
* inh lng:
- Dung mi: Dimethylfmamid
- Dd chun: Tetrabutylaminonium hydroxyd
- Ch th: Thimol xanh.
2- Dc ng hc.
- Hp thu: ng tim TM v bi ngoi da.
- Phn b: Khuych tn nhanh vo vo t chc ung th: ty xng, nim mc rut, Vo c dch no
ty.
- Chuyn ha gan.
- Thi tr: Qua phi 60%; Qua thn.
3- Tc dng v c ch.
- Thuc chng ung th km t bo loi khng Pyrimidin
* C ch:
+ 5-FU khi vo c th 5-fluoro-2-deroxyuridin-5-monophosphat (5-FdUMP)
+ 5-FdUMP cnh tranh vi Deroxyuridin monophosphat (dUMP) nn /c Thymidilat synthetase gy
thiu Thymidin cho qu trnh tng hp ADN lm t bo ung th b tiu dit.
4- Ch nh.
- iu tr cc khi u ng tiu ha : thc qun, d dy, ty, gan
- K biu m ng h hp, K v, K bung trng, K da.
5- Tc dng MM.
- Vim lot da, nim mc
- Tiu chy, xut huyt tiu ha, nn, bun nn
- c vi mu, rng tc, au ngc, thay i in tim
6- Ch phm, liu dng.
- ng tim 250mg/ 5ml, 500mg/ 10ml. Thuc m 5% tub 20g.
- Liu dng: 6 12mg/ kg/ 24h. Liu ti a: 80mg /24h.
92
TI LIU THAM KHO

Hoa Duoc 46

Uploaded by

Document Information

Original Title

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

Hoa Duoc 46

Uploaded by

Copyright:

Available Formats

n thi l thuyt tng hp -T 3 lp C4K46 2015

Chuyn 1: THUC IU TR LAO

II A CNG V NHM THUC:

Tn khoa hc: Hydrazid ca acid isonicotinic (Isonicotinohydrazid) NH2

+ DD ch phm trong nc tc dng vi dd CuSO4 to mu xanh da tri v c ta. un nng dd

+ pH kim: d b oxy ha bi O2 to ra Quinon.

CHUYN 2 : THUC H ST GIM AU CHNG VIM

II- I CNG V NHM THUC:

1/ Phn loi thuc h st, gim au, chng vim :

DN CHT THUC C TH T C DNG

Acid salicylic: tc dng vi FeCl3 tm

- Hp thu tt qua ng tiu ha.

NO2 NH2 NHCOCH3

- Ch phm + H2SO4 To c mi a. acetic.

- PP o quang : o UV trong mi trng MetOH hoc kim

- Cho t t H tinh bt vo khi bt kp trn, nho thnh khi m

- Khi thay i nhm OH C3 ; C6 trong phn t morphin th tc dng dc l v c tnh DH thay i

- au nng hoc au khng p ng vi cc thuc gim au khc nh si mt, si thn, ung th

- L cht c tng hp ha hc, iu ch t benzyl clorid.

- Gy to bn v b tiu nhng t hn morphin .

CHUYN 4 : THUC LI TIU

- Tng thi tr K+ theo 2 c ch :

Tn khoa hc: Acid-4-chloro-5-sulfamoyl-2-[ (2-furanylmethyl )amino] benzoic.

- Nhm amin thm: (tnh base)

Ar [ N+ = N ] Cl ( mui diazoni) + naphtol Ar N = N - naphtol ( mu )

Bit dc: Apo- hydro, Hypothiazid, Hydro-chlor.

- un vi dd kim gii phng NH3 lm xanh giy qu .

- Khng tng thi tr HCO3- khngnhim acid mu.

CHUYN 5 : THUC IU TR TNG HUYT P

- Nhm 5: Thuc c ch h RAA

1/ Ngun gc: Tng hp. + NH3

Chuyn 6: THUC CHNG VIM NSAIDs V DC LIU CHA

Chuyn 7: THUC KHNG HISTAMIN

X = C l C* ng phn d c hot tnh ng phn L hu nh ko c tc dng

Tn khoa hc: 3-(4-clorphenyl) -3-(2-pyridyl) propyldimethylamin hydromaleat.

Bit dc: Cezil,

CHUYN 8: AN THN DN CHT BENZODIAZEPIN V DL C

6. C: Lo u, cng thng; Cc trng thi mt ng nng; ng kinh cn nh; Tin m; Cc bnh co

- Phn ng ca nhm phenyl :

+ Phn ng ca N bc 2: t/dng vi dd NaNO2/ HCl hp cht N-Nitroso amin c mu vng

Chuyn 9: THUC CHNG NM.

Bit dc: Fungizone, Amphocin.

- Dng tim: + L thuc bt 50mg.

Chuyn 10: THUC PHNG V IU TR ST RT

Nhm bnh Nghi st rt St rt do St rt do St rt nhim phi

9- Ch phm, liu dng.

- Khng tc dng ln giai on ngoi HC.

Chuyn 11: THUC CHA GIUN S N

- Nhm -NO2 : kh ha thnh amin thm nh tnh bng P to mu azo

Chuyn 12: CC VITAMIN

- Do RL hp thu: ct d dy, bnh tiu chy ko di

2. PYRIDOXIN ( Vitamin B6)

- Vitamin D3 ( cholecalciferol ) cha c hot tnh sinh hc, vo c th n b hydroxyl ha Calcifediol ,

- Suy nhc, mt mi, nhc u, bun nn

- Nhn chroman: hp th mnh UV nh tnh, nh lng.

Chuyn 13: PENICILLIN V CC KHNG SINH B N TNG HP

3- Phn loi khng sinh :

1- BENZYL PENICILLIN (PENICILLIN G)

- Giang mai, lu, un vn, hoi th, bch hu

2. PHENOXYMETHYL PENICILLIN (penicillin V)

Tn khoa hc: Acid (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenoxyacetamido)-4-thia-1-azabicyclo [3.2.0]-

Tn khoa hc:Acid (2S,5R,6R)-6-[(R)-2-amino-2-4-hydroxyphenyl) acetamido]-3,3-dimethyl-7-oxo-4-thia-

+ Sc k lp mng (so snh vi cht chun i chiu)