Ibisobanuro

Dabigatran etexilate mesylate (BIBR 1048MS) ni prodrug ikora mumanwa ya Dabigatran.Dabigatran etexilate mesylate igira ingaruka za anticoagulant kandi ikoreshwa mugukingira indwara ya venousthromboembolism na stroke bitewe na fibrillation atriel.

Amavu n'amavuko

Ibisobanuro: IC50 Agaciro: 4.5nM (Ki);10nM (Igiteranyo cya Thrombin-iterwa na platine)muri vitro: Dabigatran yahisemo kandi ihinduranya trombine yabantu (Ki: 4.5 nM) kimwe na trombine iterwa na platine (IC (50): 10 nM), mugihe nta ngaruka zibuza kubindi bikoresho bikurura platine. -pasima ntoya (PPP), yapimwe nkibishobora guterwa na endogenous trombine (ETP) yabujijwe kwibanda cyane (IC (50): 0.56 microM).Dabigatran yerekanye ingaruka ziterwa na anticoagulant ziterwa nubwoko butandukanye muri vitro, bikubye inshuro ebyiri gukora tromboplastine igice (aPTT), igihe cya prothrombine (PT) nigihe cyo kwambika ecarin (ECT) muri PPP yabantu kuri 0.23, 0.83 na 0.18 microM. 1].muri vivo: Dabigatran yongereye urugero rwa APTT nyuma yubuyobozi bwimitsi yimbeba (0.3, 1 na 3 mg / kg) hamwe ninguge za rhesus (0.15, 0.3 na 0,6 mg / kg).Ingaruka ziterwa na anticoagulant ziterwa nigihe hamwe na dabigatran etexilate yatanzwe mukanwa ku mbeba zizi (10, 20 na 50 mg / kg) cyangwa inkende za rhesus (1, 2.5 cyangwa 5 mg / kg), hamwe ningaruka nini zagaragaye hagati ya 30 na 120 min nyuma yubuyobozi, buri kimwe [1].Abarwayi bavuwe na dabigatran etexilate bahuye nindwara ya ischemic nkeya (3.74 dabigatran etexilate vs 3.97 warfarin) hamwe na haemorrhagic interacranial hamwe na haemorrhagic (0.43 dabigatran etexilate vs 0.99 warfarin) kumyaka 100 yumurwayi [2].Igeragezwa rya Clinical: Isuzuma rya Pharmacokinetics na Pharmacodynamics ya Oral Dabigatran Etexilate yo mu barwayi ba Hemodialysis.Icyiciro1

Ububiko

Ikigeragezo cya Clinical

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