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Dabigatran etexilate mesylate (BIBR 1048MS) bụ ọgwụ na-arụsi ọrụ ike nke Dabigatran.Dabigatran etexilate mesylate nwere mmetụta anticoagulant ma jiri ya mee ihe maka prophylaxis nke venousthromboembolism na ọrịa strok n'ihi fibrillation atrial.

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Nkọwa: IC50 Uru: 4.5nM (Ki);10nM (Mkpokọta platelet na-ebute Thrombin) [1] Dabigatran bụ ihe ntụgharị na nhọrọ, onye na-emechi thrombin kpọmkwem (DTI) na-enwe ọganihu ụlọ ọgwụ dị elu dị ka prodrug na-arụ ọrụ ọnụ, dabigatran etexilate.in vitro: Dabigatran nke nhọrọ na ngbanwe na-egbochi thrombin mmadụ (Ki: 4.5 nM) yana thrombin-induced platelet aggregation (IC(50): 10 nM), ebe ọ na-egosi enweghị mmetụta mgbochi na ndị ọzọ na-akpali akpali platelet. Thrombin ọgbọ na platelet. Plasma dara ogbenye (PPP), nke a tụrụ dị ka ikike thrombin endogenous (ETP) na-egbochi itinye uche na-adabere na ya (IC (50): 0.56 microM).Dabigatran gosipụtara mmetụta anticoagulant na-adabere na ntinye uche na ụdị dị iche iche na vitro, na-eme ka oge thromboplastin na-arụ ọrụ (aPTT), oge prothrombin (PT) na ecarin clotting oge (ECT) na PPP mmadụ na ntinye nke 0.23, 0.83 na 0.18 microM, n'otu n'otu. 1].na vivo: Dabigatran gbatịpụrụ dose aPTT dabere na nchịkwa eriri afọ na oke (0.3, 1 na 3 mg / kg) na enwe rhesus (0.15, 0.3 na 0.6 mg / kg).A na-ahụ mmetụta mgbochi ọgwụ mgbochi dose na oge dabere na dabigatran etexilate nke a na-enye oke n'ọnụ (10, 20 na 50 mg/kg) ma ọ bụ enwe rhesus (1, 2.5 ma ọ bụ 5 mg / kg), yana nsonaazụ kachasị n'etiti 30 na 120. min mgbe nchịkwachara, n'otu n'otu [1].Ndị ọrịa a na-emeso dabigatran etexilate nwere obere ọrịa strok ischemic (3.74 dabigatran etexilate vs 3.97 warfarin) yana obere ọbara ọgbụgba intracranial jikọtara ọnụ na ọrịa strok hemorrhagic (0.43 dabigatran etexilate vs 0.99 warfarin) kwa afọ 1020.Nnwale ụlọ ọgwụ: Nyocha nke Pharmacokinetics na Pharmacodynamics nke Oral Dabigatran Etexilate na ndị ọrịa Hemodialysis.Nkeji1

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