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1. Tc dng
1.1 Tc dng chng vim
C tc dng trn hu ht cc loi vim khng k n nguyn nhn
C ch chng vim:
- c ch sinh tng hp Protaglandin(PG) do c ch c hi phc
cyclooxygenase(COX) lm gim PGE2 v PGF1 l nhng cht trung gian ho hc
ca phn ng vim
Khi tn thng mng t bo gii phng phospholipid mng. Di tc dng ca
phospholipase A2 cht ny chuyn thnh acid arachidonic. Sau met mt di tc
dng ca lipooxygenase(LOX), acid arachidonic to thnh c leucotrien c tac sng co
kh qun, mt khc di tc dng cu cyclooxygenase, acid chidonic to ra PGE2(gy
vim au), prostacyclin(PGI2) v thromboxan A2(TXA2) tc ng n s lng ng
tiu cu.
C ch tc dng ca NSAIDs
Enzym cyclooxygenase(COX)
C 2 loi COX l COX-1 v COX-2.
COX-1 hay PGG/H2 synthetase-1 c tc dng duy tr cc hot ng sinh l
bnh thng ca t bo l mt enzym cu to. Enzym ny c mt hu ht cc m:
thn, d dy, ni mc mch mu, tiu cu.. Tham gia trong qu trnh sn xut cc PG
c tc dng iu ho cc chc phn sinh l , n nh ni mi, bo v t bo do cn
gi l enzym gi nh
COX-2 hay PGG/H synthetase-2 c chc phn thc y qu trnh vim. Thy
hu ht cc m vi nng rt thp, cc t bo tham gia vo phn ng vim(bch
cu n nhn, i thc bo, bao hot dch khp, t bo sn). Trong cc m vim, nng
d COX-2 cao ti 80 ln do cc kch thch vim gy cm ng v hot ho mnh COX2 V th COX-2 cn gi l enzym cm ng
CC PROSTAGLANDIN(PG)
1. Sinh tng hp:
PG c tng hp ngay ti mng t bo. Mng t bo cha nhiu phospholipid,
di tc dng ca phospholipase A2 ca mng s gii phng ra c acid bo t do
khng bo ho, cha 20 nguyn t C l acid arachidonc hay cn gi l acid eicosa5,6,11,14-tetraenoic, acid prostanoic. Acid arachidonic khi c gii phng ra s tr
thnh c cht cho nhiu enzym to ra c cht chuyn ho khc nhau: cc
prostaglandin, cc leucotrinen di teen gi chung l c eicosanoid
Ghi ch:
Cc loi PG
S sinh tng hp PG
- Gy sy thai lc
- Bo v nim mc d dy: Misoprostol(Cytotec): tng t PGE1
- iu tr lit dng: PGE1
- Duy tr ng thng ng mch: PGE1
- iu tr THA phi nguyn pht: PGI2
Cc nhm thuc NSAIDs
* Loi c ch COX khng chn lc:
- Nhm Salicyllic: Acid acetylsalicylic(Aspirin)
- Nhm Indol:
+ Indomethacin
+ Sundilac
- Nhm Pirazolon: Phenylbutazon
- Nhm acid enolic: Oxicam
- Nhm acid propionic: Ibuprofen, naprofen, ketoprofen
- Nhm dn xut acid phenylacetic: Diclofenac
- Nhm dn xut acid heteroarylacetic: Tolmetin, ketorolac
* Loi c ch chn loc COX-2:- Nhm furanon c nhm th diaryl: Rofecoxib
- Nhm pyrazol c nhm th diaryl: Celecoxib
- Nhm acid indol acetic: Etodolac
- Nhdm sulfonanilid: Nimesulid
+ Tenoxicam(Tilcotil): 20mg/ngy
+ Meloxicam(Mobic): vin nn: 7,5mg v 15mg, liu ti a 15mg/ngy
5. Nhm dn xut acid propionic:
- Liu thp c tc dng gim au, liu cao hn c tc dng chng vim
- Nhm ny t c tc dng ph hn nht l trn ng tiu ho do s dng
nhiu trong cc trng hp vim khp mn tnh
- Cc bit dc:
+ Ibuprofen: vin 200-300-400mg, liu 1200-1600mg/mgy
+ Naproxen: vin 250mg, liu 250 2 ln/ngy
+ Fenoproxen vin nang 300-600mg, liu 6004 ln/ngy
+ Ketoprofen: vin nang 50mg, liu 502-4 ln/ngy
6. Nhm dn xut ca acid phenylaceticiclofenac- Tc dng c ch COX
mnh hn indomethacin v nhiu thuc khc. Cn lm gim nng acid arachidonic
t do trong bch cu do ngn cn gii phng hc thu hi acid bo
- Hp thu nhanh v hon ton qua ng tiu ha nhng ch c 50% vo c
tun hon v chuyn ho trong qu trnh hp thu
- Thi gian bn thi l 1-2 gi nhng tch lu bao khp nn tc dng vn gi
c lu
- Ch inh trong vim khp mn tnh, cn dgn gim au trong vim c, au
sau m v au do kinh nguyt
- Tc dng ph t
- Liu: vin 50-100mg, liu 100-150mg/ngy