Sharaxaada

Dabigatran etexilate mesylate (BIBR 1048MS) waa daawada afka ee firfircoon ee Dabigatran.Dabigatran etexilate mesylate waxay leedahay saameyn liddi ku ah xinjirowga lidka ku ah waxaana loo isticmaalaa kahortaga xinjirowga dhiigga iyo istaroogga sababtoo ah fibrillation atrial.

Asalkii hore

Sharaxaad: IC50 Qiimaha: 4.5nM (Ki);10nmin vitro: Dabigatran si xulashada iyo dib-u-celinta waxay joojisay thrombin bini'aadamka (Ki: 4.5 nM) iyo sidoo kale isku-darka trombobin-induced platelet (IC(50): 10 nM), iyada oo aan muujineynin wax saameyn ah oo ku saabsan wakiilada kale ee kicinta platelet. Plasma liidata (PPP), oo lagu qiyaaso awoodda thrombin ee endogenous (ETP) ayaa la xakameeyey ku-tiirsanaanta (IC(50): 0.56 microM).Dabigatran waxay muujisay saamaynta xinjirowga lidka-ku-tiirsan ee noocyada kala duwan ee vitro, taas oo labanlaabaysa wakhtiga qayb ka mid ah thromboplastin (aPTT), wakhtiga prothrombin (PT) iyo wakhtiga xinjirowga ecarin (ECT) ee PPP ee bini'aadamka ee 0.23, 0.83 iyo 0.18 microM, siday u kala horreeyaan. 1].gudaha vivo: Dabigatran waxay dheeraysay qiyaasta aPTT-ku-tiirsanaanta ka dib maamulka xididada ee jiirka (0.3, 1 iyo 3 mg/kg) iyo daanyeerka rhesus (0.15, 0.3 iyo 0.6 mg/kg).Saamaynta xinjirowga lidka ku ah qiyaasta iyo waqtiga-ku-tiirsanaanta ayaa lagu arkay dabigatran etexilate oo afka laga maamulo jiirka miyirka leh (10, 20 iyo 50 mg/kg) ama daanyeerka rhesus (1, 2.5 ama 5 mg/kg), oo leh saamaynta ugu badan ee lagu arkay inta u dhaxaysa 30 iyo 120 min ka dib maamulka, siday u kala horreeyaan [1].Bukaannada lagu daweeyay dabigatran etexilate waxay la kulmeen istaroog yar oo ischaemic ah (3.74 dabigatran etexilate vs 3.97 warfarin) iyo in yar oo isku darka dhiigbaxa intracranial iyo dhiigbaxa dhiigbaxa (0.43 dabigatran etexilate vs 0.99 warfarin) 1020 bukaan ah.Tijaabada caafimaad: Qiimaynta Farmacokinetics iyo Pharmacodynamics ee Dabigatran Etexilate Oral ee Bukaannada Hemodialysis.Wajiga 1aad

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