Ibisobanuro

Dabigatran etexilate mesylate (BIBR 1048MS) ni prodrug ikora mu kanwa ya Dabigatran. Dabigatran etexilate mesylate igira ingaruka zirwanya anticoagulant kandi ikoreshwa mugukingira indwara ya venousthromboembolism na stroke kubera fibrillation atriel.

Amavu n'amavuko

Ibisobanuro: IC50 Agaciro: 4.5nM (Ki); 10nM (Igiteranyo cya Thrombin-iterwa na platine) muri vitro: Dabigatran yatoranije kandi ihindura trombine yumuntu (Ki: 4.5 nM) kimwe no guteranya trombine iterwa na platine (IC (50): 10 nM), mugihe nta ngaruka zibuza izindi mikorere itera platine.Icyerekezo cya trombine muri platine. -plasma 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, zikubye kabiri igihe cya tromboplastine cyakoreshejwe 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 bitewe nubuyobozi 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 etexilate ya dabigatran yatanzwe mu kanwa ku mbeba zizi (10, 20 na 50 mg / kg) cyangwa inkende za rhesus (1, 2.5 cyangwa 5 mg / kg), hamwe n'ingaruka nini zagaragaye hagati ya 30 na 120 min nyuma yubuyobozi, buri kimwe [1]. Abarwayi bavuwe na dabigatran etexilate bahuye nubwonko buke bwa ischemic (3.74 dabigatran etexilate vs 3.97 warfarin) hamwe na haemorrhage 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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