Dc l v c ch tc dng

Paracetamol (acetaminophen hay N-acetyl-p-aminophenol) l cht chuyn ha c hot tnh ca phenacetin, l thuc gim au - h st hu hiu c th thay thaspirin; tuy vy, khc vi aspirin, paracetamol khng c hiu qu iu tr vim. Vi liu ngang nhau tnh theo gam, paracetamol c tc dng gim au v h st tng t nh aspirin. Paracetamol lm gim thn nhit ngi bnh st, nhng him khi lm gim thn nhit ngi bnh thng. Thuc tc ng ln vng di i gy h nhit, ta nhit tng do gin mch v tng lu lng mu ngoi bin. Paracetamol, vi liu iu tr, t tc ng n h tim mch v h hp, khng lm thay i cn bng acid base, khng gy kch ng, xc hoc chy mu d dy nh khi dng salicylat, v parac etamol khng tc dng trn cyclooxygenase ton thn, ch tc ng n cyclooxygenase/prostaglandin ca h thn kinh trung ng. Paracetamol khng c tc dng trn tiu cu hoc thi gian chy mu. Khi dng qu liu paracetamol mt cht chuyn ha l N-acetyl-benzoquinonimin gy c nng cho gan. Liu bnh thng, paracetamol dung np tt, khng c nhiu tc dng ph ca aspirin. Tuy vy, qu liu cp tnh (trn 10 g) lm thng tn gan gy cht ngi, v nhng v ng c v t vn bng paracetamol tng ln mt cch ng lo ngi trong nhng nm gn y. Ngoi ra, nhiu ngi trong c c thy thuc, dng nh khng bit tc dng chng vim km ca paracetamol.

Dc ng hc
Hp thu
Paracetamol c hp thu nhanh chng v hu nh hon ton qua ng tiu ha. Thc n c th lm vin nn gii phng ko di paracetamol chm c hp thu mt phn v thc n giu carbon hydrat lm gim t l hp thu ca paracetamol. Nng nh trong huyt tng t trong vng 30 n 60 pht sau khi ung vi liu iu tr.

Phn b
Paracetamol phn b nhanh v ng u trong phn ln cc m ca c th. Khong 25% paracetamol trong mu kt hp vi protein huyt tng.

Thi tr
Na i huyt tng ca paracetamol l 1,25 - 3 gi, c th ko di vi liu gy c hoc ngi bnh c thng tn gan. Sau liu iu tr, c th tm thy 90 n 100% thuc trong nc tiu trong ngy th nht, ch yu sau khi lin hp trong gan vi acid glucuronic (khong 60%),acid sulfuric (khong 35%) hoc cystein (khong 3%); cng pht hin thy mt lng nh nhng cht chuyn ha hydroxyl - ho v kh acetyl. Tr nh t kh nng glucuro lin hp vi thuc hn so vi ngi ln.

Paracetamol b N-hydroxyl ha bi cytochrom P450 to nn N -acetyl-benzoquinonimin, mt cht trung gian c tnh phn ng cao. Cht chuyn ha ny bnh thng phn ng vi cc nhm sulfhydryl trong glutathion v nh vy b kh hot tnh. Tuy nhin, nu ung liu cao paracetamol, cht chuyn ha ny c to thnh vi lng lm cn kit glutathion ca gan; trong tnh trng , phn ng ca n vi nhm sulfhydryl ca protein gan tng ln, c th dn n hoi t gan.

Ch nh
Paracetamol c dng rng ri trong iu tr cc chng au v st t nh n va. au Paracetamol c dng gim au tm thi trong iu tr chng au nh v va. Thuc c hiu qu nht l lm gim au cng thp c ngun gc khng phi ni tng. Paracetamol khng c tc dng tr thp khp. Paracetamol l thuc thay th salicylat (c a thch ngi bnh chng ch nh hoc khng dung np salicylat) gim au nh hoc h st. St Paracetamol thng c dng gim thn nhit ngi bnh st, khi st c th c hi hoc khi h st, ngi bnh s d chu hn. Tuy vy, liu php h st ni chung khng c hiu, khng nh hng n tin trnh ca bnh c bn, v c th che lp tnh trng bnh ca ngi bnh.

Chng ch nh
Ngi bnh nhiu ln thiu mu hoc c bnh tim, phi, thn hoc gan. Ngi bnh qu mn vi paracetamol. Ngi bnh thiu ht glucose-6-phosphat dehydro-genase (G6PD).

Thn trng
Paracetamol tng i khng c vi liu iu tr. i khi c nhng phn ng da gm ban dt sn nga v my ay; nhng phn ng mn cm khc gm ph thanh qun, ph mch v nhng phn ng kiu phn v c th t khi xy ra. Gim tiu cu, gim bch cu v gim ton th huyt cu xy ra vi vic s dng nhng dn cht p - aminophenol, c bit khi dng ko di cc liu ln. Gim bch cu trung tnh v ban xut huyt gim tiu cu xy ra khi dng paracetamol. Him gp mt bch cu ht ngi bnh dng paracetamol. Ngi b phenylceton - niu (ngha l, thiu ht gen xc nh tnh trng ca phenylalanin hydroxylase) v ngi phi hn ch lng phenylalanin a vo c th phi c cnh bo l mt s ch phm paracetamol cha aspartam, s chuyn ha trong d dy - rut thnh phenylalanin sau khi ung. Mt s dng thuc paracetamol c trn th trng cha sulfit c th gy phn ng kiu d ng, gm c phn v v nhng cn hen e da tnh mng hoc t nghim trng hn mt s ngi qu mn. Khng

bit r t l chung v qu mn vi sulfit trong dn chng ni chung, nhng chc l thp; s qu mn nh vy c v thng gp ngi bnh hen nhiu hn ngi khng hen. Phi dng paracetamol thn trng ngi bnh c thiu mu t trc, v chng xanh tm c th kh ng biu l r, mc d c nhng nng cao nguy him camethemoglobin trong mu. Ung nhiu ru c th gy tng c tnh vi gan ca paracetamol; nn trnh hoc hn ch ung ru.

Thi k mang thai

Cha xc nh c tnh an ton ca paracetamol dng khi thai nghn lin quan n tc dng khng mong mun c th c i vi pht trin thai. Do , ch nn dng paracetamol ngi mang thai khi tht cn.

Thi k cho con b

Nghin cu ngi m dng paracetamol sau khi cho con b, khng thy c tc dng kh ng mong mun tr nh b m.

Tc dng khng mong mun (ADR)

Ban da v nhng phn ng d ng khc thnh thong xy ra. Thng l ban hoc my ay, nhng i khi nng hn v c th km theo st do thuc v thng tn nim mc. Ngi bnh mn cm vi salicylat him mn cm vi paracetamol v nhng thuc c lin quan. Trong mt s t trng hp ring l, paracetamol gy gim bch cu trung tnh, gim tiu cu v gim ton th huyt cu.

t gp, 1/1000 < ADR < 1/100

Da: Ban. D dy - rut: Bun nn, nn. Huyt hc: Lon to mu (gim bch cu trung tnh, gim ton th huyt cu, gim bch cu), thiu mu. Thn: Bnh thn, c tnh thn khi lm dng di ngy.

Him gp, ADR < 1/1000

Khc: Phn ng qu mn.

Hng dn cch x tr ADR

Nu xy ra nhng tc dng khng mong mun nghim trng, ngng dng paracetamol. V iu tr, xin c phn: "Qu liu v x tr".

Liu lng v cch dng

Cch dng
Paracetamol thng dng ung. i vi ngi bnh khng ung c, c th dng dng thuc n t trc trng; tuy vy liu trc trng cn thit c cng nng huyt tng c th cao hn liu ung.

Liu lng
Khng c dng paracetamol t iu tr gim au qu 10 ngy ngi ln hoc qu 5 ngy tr em, tr khi do thy thuc hng dn, v au nhiu v ko di nh vy c th l du hiu ca mt tnh trng bnh l cn thy thuc chn on v iu tr c gim st. Khng dng paracetamol cho ngi ln v tr em t iu tr st cao (trn 39,5OC), st ko di trn 3 ngy hoc st ti pht, tr khi do thy thuc hng dn, v st nh vy c th l du hiu ca mt bnh nng cn c thy thuc chn on nhanh chng. gim thiu nguy c qu liu, khng nn cho tr em qu 5 liu paracetamol gim au hoc h st trong vng 24 gi, tr khi do thy thuc hng dn. gim au hoc h st cho ngi ln v tr em trn 11 tui, liu paracetamol thng dng ung hoc a vo trc trng l 325 - 650 mg, c 4 - 6 gi mt ln khi cn thit, nhng khng qu 4 g mt ngy; liu mt ln ln hn (v d 1 g) c th hu ch gim au mt s ngi bnh. gim au hoc h st, tr em c th ung hoc a vo trc trng c 4 - 6 gi mt ln khi cn, liu xp x nh sau: tr em 11 tui, 480 mg; tr em 9 - 10 tui, 400 mg; tr em 6 - 8 tui, 320 mg; tr em 4 - 5 tui, 240 mg; v tr em 2 - 3 tui, 160 mg. Tr em di 2 tui c th ung liu sau y, c 4 - 6 gi mt ln khi cn: tr em 1 - 2 tui, 120 mg; tr em 4 - 11 thng tui, 80 mg; v tr em ti 3 thng tui, 40 mg. Liu trc trng cho tr em di 2 tui dng ty theo mi bnh nhi. Liu ung thng dng ca paracetamol, di dng vin nn gii phng ko di 650 mg, gim au ngi ln v tr em 12 tui tr ln l 1,3 g c 8 gi mt ln khi cn thit, khng qu 3,9 g mi ngy. Vin nn paracetamol gii phng ko di, khng c nghin nt, nhai hoc ha tan trong cht lng.

Tng tc thuc
Ung di ngy liu cao paracetamol lm tng nh tc dng chng ng ca coumarin v dn cht indandion. Tc dng ny c v t hoc khng quan trng v lm sng, nn paracetamol c a dng hn salicylat khi cn gim au nh hoc h st cho ngi bnh ang dng coumarin hoc dn cht indandion. Cn phi ch n kh nng gy h st nghim trng ngi bnh dng ng thi phenothiazin v liu php h nhit. Ung ru qu nhiu v di ngy c th lm tng nguy c paracetamol gy c cho gan. Thuc chng co git (gm phenytoin, barbiturat, carbamazepin) gy cm ng enzym microsom th gan, c th lm tng tnh c hi gan ca paracetamol do tng chuyn ha thuc thnh nhng cht c

hi vi gan. Ngoi ra, dng ng thi isoniazid vi paracetamol cng c th dn n tng nguy c c tnh vi gan, nhng cha xc nh c c ch chnh xc ca tng tc ny. Nguy c paracetamol gy c tnh gan gia tng ng k ngi bnh ung liu paracetamol ln hn liu khuyn dng trong khi ang dng thuc chng co git hoc isoniazid. Thng khng cn gim liu ngi bnh dng ng thi liu iu tr paracetamol v thuc chng co git; tuy vy, ngi bnh phi hn ch t dng paracetamol khi ang dng thuc chng co git hoc isoniazid. n nh v bo qun Bo qun thuc di 40 oC, tt nht l 15 - 30 oC; trnh ng lnh dung dch hoc dch treo ung.

Qu liu v x tr
Biu hin
Nhim c paracetamol c th do dng mt liu c duy nht, hoc do ung lp li liu ln paracetamol (v d, 7,5 - 10 g mi ngy, trong 1 - 2 ngy), hoc do ung thuc di ngy. Hoi t gan ph thuc liu l tc dng c cp tnh nghim trng nht do qu liu v c th gy t vong. Bun nn, nn v au bng thng xy ra trong vng 2 - 3 gi sau khi ung liu c ca thuc. Methemoglobin - mu, dn n chng xanh tm da, nim mc v mng tay l mt du hiu c trng nhim c cp tnh dn cht p - aminophenol; mt lng nh sulfhemoglobin cng c th c sn sinh. Tr em c khuynh hng to methemoglobin d hn ngi ln sau khi ung paracetamol. Khi b ng c nng, ban u c th c kch thch h thn kinh trung ng, kch ng v m sng. Tip theo c th l c ch h thn kinh trung ng; sng s, h thn nhit; mt l; th nhanh, nng; mch nhanh, yu, khng u; huyt p thp v suy tun hon. Try mch do gim oxy huyt tng i v do tc dng c ch trung tm, tc dng ny ch xy ra vi liu rt ln. Sc c th xy ra nu gin mch nhiu. Cn co git ngt th gy t vong c th xy ra. Thng hn m xy ra trc khi cht t ngt hoc sau vi ngy hn m. Du hiu lm sng thng tn gan tr nn r rt trong vng 2 n 4 ngy sau khi ung liu c. Aminotransferase huyt tng tng (i khi tng rt cao) v nng bilirubin trong huyt tng cng c th tng; thm na, khi thng tn gan lan rng, thi gian prothrombin ko di. C th 10% ngi bnh b ng c khng c iu tr c hiu c thng tn gan nghim trng; trong s 10% n 20% cui cng cht v suy gan. Suy thn cp cng xy ra mt s ngi bnh. Sinh thit gan pht hin hoi t trung tm tiu thy tr vng quanh tnh mch ca. nhng trng hp khng t vong, thng tn gan phc hi sau nhiu tun hoc nhiu thng.

iu tr
Chn on sm rt quan trng trong iu tr qu liu paracetamol. C nhng phng php xc nh nhanh nng thuc trong huyt tng. Tuy vy, khng c tr hon iu tr trong khi ch kt qu xt nghim nu bnh s gi l qu liu nng. Khi nhim c nng, iu quan trng l phi iu tr h tr tch cc. Cn ra d dy trong mi trng hp, tt nht trong vng 4 gi sau khi ung. Liu php gii c chnh l dng nhng hp cht sulfhydryl, c l tc ng mt phn do b sung d tr glutathion gan.

N-acetylcystein c tc dng khi ung hoc tim tnh mch. Phi cho thuc ngay lp tc nu cha n 36 gi k t khi ung paracetamol. iu tr vi N - acetylcystein c hiu qu hn khi cho thuc trong thi gian di 10 gi sau khi ung paracetamol. Khi cho ung, ha long dung dch N - acetylcystein vi nc hoc ung khng c ru t dung dch 5% v phi ung trong vng 1 gi sau khi pha. Cho ung N - acetylcystein vi liu u tin l 140 mg/kg, sau cho tip 17 liu na, mi liu 70 mg/kg cch nhau 4 gi mt ln. Chm dt iu tr nu xt nghim paracetamol trong huyt tng cho thy nguy c c hi gan thp. Tc dng khng mong mun ca N - acetylcystein gm ban da (gm c my ay, khng yu cu phi ngng thuc), bun nn, nn, a chy v phn ng kiu phn v. Nu khng c N - acetylcystein, c th dng methionin. Ngoi ra c th dng than hot v/hoc thuc ty mui, chng c kh nng lm gim hp th paracetamol.