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Nhm thc hin: T 4 O1K66 :

1.Nguyn Th Thy MSV: 1101514


2.Trng Th Hin MSV: 1101153
3.Quch Th Vn Anh MSV:
4.Vng c Thanh MSV: 0901147
5.Thiu Mnh Hng MSV:1101260
6. Nguyn Qu Hu MSV: 1101261
7.Nguyn Hu Ngh MSV:1101361
TRNG I HC DC H NI
B MN DC L
I.t vn
Cc thuc khng sinh nhm macrolid rt ph bin trong iu tr chng
nhim khun, nht l nhim khun Gram (+) . Tuy nhin, do tnh trng
lm dng v ty tin trong iu tr khin cho nhiu thuc trong nhm
ny tr nn km tc dng hn trc.
V vy, vic c hiu bit chuyn su v nhm khng sinh ny se giup cc
Dc si, Bc si a ra c phc iu tr tt nht cho tng bnh
nhn tng hiu qua iu tr; giam c tinh, tc dng ph; giam khng
thuc. Bi thao lun ny se cung cp mt ci nhn tng quan v nhm
khng sinh ny.
II- TNG QUAN V KHNG SINH
MACROLID
1. c im cu trc ca nhm
3. Ph khng khun
5. Mi lin quan c tnh Dc ng hoc/Dc lc hc
4. C ch khng khng sinh ca vi khun
6. Ch nh lm sng
2. C ch tc dng
8. Tng tc thuc
7. Tc dng khng mong mun chnh
9. Mt s i din chnh ca nhm
Macrolide
1.c im cu trc chung ca nhm
L cc glycoside thn lipid:

O
Genin Ose
n
Gm mt nhn l
vng lacton 12-17C
ng trung tnh
v ng amin
O
O
O
CH
3
HO
H
3
C
CH
3
CH
3
O
H
3
C
O
HO
CH
3
N CH
3
H3C
OH
H
3
C
CH
3
OH
O
O
OH
O
H
3
C
CH
3
CH
3
Erythromycin
Phn loi


1.c im cu trc chung ca nhm
2. C ch tc dng ca Macrolid
Gn vo tiu n v 50S ca ribosom

Ngn khng cho phc hp acid
amin-t-ARNthc hingii m di truyn
(ngn cn s chuyn v ca peptid)

Ngn s tng hp protein cho
vi khun
c ch qu trnh tng hp Protein ca vi khun
50S
30S
Acid amin
ARNt
ARNt
V tr
cho
V tr
nhn
Macrolid
X
ARNm

C ch khc: Kch thch thc bo ca bch cu trung tnh
=>tng kh nng dit khun ca bch cu
Km
khun
Cu
khun
G(+)
Trc
khun
G(-)
Cu
khun
G (-)
Ph tc
dng
3. Ph tc dng
Ph trung bnh, ch yu trn vi khun Gram
(+), t trn vi khun Gram(-)
Trc
khun
G (+)
Khc
Listeria,
bacillus
anthracis
Neisseria
(mng no
cu, lu cu)
Legionella,
H.influenza
Mt s vi khun
ym kh,
Mycoplasma,
Chlamydia
Lin cu,
ph cu, t
cu
3.Ph tc dng:
Khng nhy cm vi phn ln vi khun G(-) ??????????
=>Do khng sinh kh thm nhp vo ni bo vi khun
=> Ch yu iu tr Vi khun G (+), vi khun ym kh cc
c quan su trong c th
Ph macrolid gn ging penicillin nhng rng hn, l s
thay th ph bin cho bnh nhn d ng Penicillin.
4.C ch khng khng sinh ca vi
khun
1. khng t nhin:
Trc khun G(-) khng t nhin, do khng sinh khng thm qua c Trn
thnh t bo vi khun
2. khng thu nhn:
Cu khun G(+) : t cu, lin cu, ph cu:
Gim tnh thm ca thnh vi khun vi thuc => Thuc khng xm nhp c
vo t bo
Thay i ch tc dng:cc vi khun khng mcrolid do thay i cc receptor
trn tiu n v 50S.
To enzyme phn hy hoc bin i khng sinh: Vi khun ng rut
(Enterbacteriaceae) tit ra esterase thy gii cu trc ca cc macrolid
C s khng cho xy ra gia cc khng sinh cng nhm, nht l cc
macrolid c in
Cc Macrolid bn tng hp mi nh Clarithromycin, Azithromycin c th dng
iu tr cc vi khun khng cc macrolid c in
4.C ch khng khng sinh ca vi
khun

1. Hp thu:
Hp thu kh tt qua h tiu ha ( nht l rut non) => C sinh kh dng ng
ung tt.
Mi trng acid dch vi: Mt tc dng ( vi erythromycin dng base, macrolid
mi kh ngb)
Thc n lm gim hp thu thuc ( vi macrolid c in)
2. Phn b:
T l lin kt huyt tng khong 70% ( thay i ty loi macrolid)
Phn b rng ri cc c quan: gan, tuyn tin lit, phi,..
Khng qua hng ro mu no,dch no ty( tr khi vim) nhng qua c nhau
thai v sa m
Nng thuc tp trung cao ti phi v tai mi hng
5.Mi lin quan gia c tnh dc ng
hc/Dc lc hc
5.Mi lin quan gia c tnh dc ng
hc/Dc lc hc
3. Chuyn ha:
Ch yu gan, di dng dimethyl ha mt tc dng
4. Thi tr:
Ch yu qua mt , mt phn nh qua nc tiu
=> Ngi b suy thn t b nh hng
5. Ch nh lm sng
- iu tr nhim trng ng h hp, tai mi hng, da, sinh dc,..
- Thay th penicillin cho bnh nhn d ng Pen khi nhim t cu, lin cu, ph cu
- D phng vim ni tm mc trong phu thut rng ming cho bnh nhn mc bnh van tim
6.Tc dng khng mong mun
Ch yu gy ri lon tiu ha: au bng, bun nn, tiu
chy, y hi (Cc macrolid mi t tc dng ph hn)
D ng da: pht ban, nga,
Erythromycin tim tnh mch: c th gy kch ng, vim
tc tnh mch, c tnh thnh gic nu dng liu cao=>
khc phc: ko di thi gian truyn
Gan: men gan tang, mt trong gan
Chng ch nh cho ngi b suy gan nng
8.Tng tc thuc
Tng tc dng v c
tnh cc thuc s dng
cng: Warfarin,digoxin,
Theophylin,
MACROLID
Erythromycin+
theophylin: tng nng
, c tnh ca
theophylin: Nn,nh
trng ngc, co git,
Clarithromycin +
Simvastatin: tiu c vn,
au c, yu c.
Khng phi hp cc
macrolid vi nhau
Khng phi hp
Macrolid vi
Lincosamid v
Cloramphenicol
8.Mt s i din chnh
1.Erythromycin:
y l macrolid u tin, phn lp t x khun Streptomyces erythreus
Bit dc : Erythrocin, Adamycin

O
O
O
CH3
HO
H3C
CH3
CH3
O
H3C
O
HO
CH3
N CH3
H3C
OH
H3C
CH3
OH
O
O
OH
O
H3C
CH3
CH3
Erythromycin
8.Mt s i din chnh:
Tuy nhin, cu trc ca erythromycin c nhiu im yu
Tm cc dn cht mi vi cc tnh cht c ci thin
Cc dn cht bn tng hp
Bn hn trong
acid dch v
Sinh kh dng,
T 1/2 ci thin
t tc dng
ph hn
8.Mt s i din chnh
O
O
O
CH
3
HO
H
3
C
CH
3
CH
3
O
H
3
C
O
HO
CH
3
N CH
3
H
3
C
OH
H
3
C
CH
3
OH
O
O
OH
O
H
3
C
CH
3
CH
3
Erythromycin
R1
R2
R3
=

OCH2CH2
CH2
N
O
8.Mt s i din chnh
Roxithromycin Azithromycin
Clarithromycin
Thay nhm ceton(C10)=
dn cht oxim
Khng to OH bn
cetal ni vi OH (C7)
bn vi acid
Sinh kh dng tt hn
Ph hp nhng mnh
hn erythromycin 2-
10 ln
Bit dc: Rulid,
rovamycin
-M rng vng lacton ra 15
nguyn t cha 1 Ni t
-Ch nh tng t
Clarithromycin, t tc dng
ph hn erythromycin




Bit dc: Zithromax

Thay OH (C7) c
OCH3 khng to bn
acetal vi ceto
Bn vi acid
t kch ng d dy, sinh
kh dng tt hn



Bit dc: Claritex
III.S khc bit v c tnh dc l ca :
erythromycin, clarithromycin,azithromycin
Erythromycin Clarithromycin Azithromycin
Hp
thu
-Dng base b mt hot tnh
bi acid dch v
=> S dng dng vin bao
tan trong rut hoc dng
mui v ester ( stearat,
estolat, ethylsuccinat) c
hp thu tt hn
-Dn cht estolat hp thu tt
nht qua ng ung nhng
tc dng ph gy suy chc
nng gan => khng dng cho
ngi bnh gan
-Thc n cn tr s hp thu.
-F= 30-65% ty dng bo
ch


- Khng b phn hy
bi acid dch v
- Mc hp thu khng b
nh hng bi thc
n=> ung bt c lc
no
- Hp thu tt nhng
chu s chuyn ha
qua gan ln u cao
nn lm sinh kh
dng thuc m gim
xung F= 55%

- n nh trong acid
- Thc n lm gim hp
thu khong 50% =>
ung cch xa ba n
- F=38%
III.S khc bit v c tnh dc l ca :
erythromycin, clarithromycin,azithromycin
T l thuc trong m-huyt thanh: Azithromycin>Clarithromycin>Erythromycin
( Azithromycin cao do tch l trong m, thc bo ln hn => AUC thp hn
Erythromycin Clarithromycin Azithromycin
Chuyn
ha v thi
tr
T1/2=1,5-3h - T1/2= 3-7h( liu 500mg)
- Thi tr ch yu qua nc tiu
nn c li cho cc nhim khun
tit niu,sinh dc hn thuc khc
trong nhm

T1/2= 25-48h

Ph tc
dng
Ph tc dng trung
bnh

-Hot tnh vi Gram(+) tt hn
Erythromycin v Azithromycin

-Tc dng trn vi khun
Gram(+) yu hn mt cht
so vi erythromycin, nhng
mnh hn trn mt s vi
khun Gram (-)

III. S khc bit c tnh dc l
III. S khc bit c tnh dc l
Erythromycin Clarithromycin Azithromycin
Ch nh -D phng thp khp cp
Dng cho bnh nhn d ng
khng sinh beta-lactam
- liu dng: ngi ln ung
0,1-1g/ ln x 2 ln /24h
- Vt tri erythromycin khi
iu tr H.Pylori nn thng
dng phi hp iu tr vim
lot d dy t trng
-Liu dng : ung 250-
500mg/ln x 2 ln /24h , t
7-14 ngy
-c th iu tr nhim
khun ng tiu ha
do nhy cm vi mt s
chng vi khun ng
rut Gram (-)
-Liu dung: ngi ln
ung 250mg/ ln/ 24h
IV.Kt lun
- V dc l:
Macrolid c ph tc dng ch yu trn vi khun Gram(-), t hiu lc trn vi khun
Gram (-),
Macrolid hp thu kh tt qua ng tiu ha, phn b rng cc c quan, chuyn ha
gan v thai tr ch yu qua mt
Cc macrolid bn tng hp c cai thin v nhiu mt so vi macrolid c in
- p dng trong lm sng:
iu tr nhim khun ng h hp, rng ming, sinh dc,..
Dng bo ch hay dung: vin nn vin nang ung.
Ch nguy c tng tc thuc, nht l vi thuc khng histamin
- Cc thuc khng sinh nhm macrolid rt ph bin trong iu tr chng nhim khun. Tuy
nhin, do tnh trng lm dng v ty tin trong iu tr khin cho nhiu thuc trong
nhm ny tr nn km tc dng hn trc. Do vy

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