Bayani

Dabigatran etexilate mesylate (BIBR 1048MS) prodrug ne mai aiki da baki na Dabigatran. Dabigatran etexilate mesylate yana da tasirin anticoagulant kuma ana amfani dashi don rigakafin venousthromboembolism da bugun jini saboda fibrillation na atrial.

Fage

Bayani: IC50 Darajar: 4.5nM (Ki); 10nM (Thrombin-induced platelet aggregation) [1] Dabigatran mai juyawa ne kuma mai zaɓi, mai hana thrombin kai tsaye (DTI) yana fuskantar ci gaba na asibiti a matsayin prodrug na baki, dabigatran etexilate. in vitro: Dabigatran selectively da reversibly hana ɗan adam thrombin (Ki: 4.5 nM) da kuma thrombin-induced platelet aggregation (IC(50): 10 nM), yayin da nuna wani inhibitory sakamako a kan sauran platelet-stimulating agents.Thrombin ƙarni a cikin platelet. Plasma mara kyau (PPP), wanda aka auna kamar yadda aka hana yiwuwar thrombin endogenous (ETP) maida hankali dogara (IC(50): 0.56 microM). Dabigatran ya nuna tasirin anticoagulant mai dogara da maida hankali a cikin nau'ikan nau'ikan in vitro, yana ninka lokacin thromboplastin da aka kunna (aPTT), lokacin prothrombin (PT) da lokacin clotting ecarin (ECT) a cikin PPP na ɗan adam a ƙimar 0.23, 0.83 da 0.18 microM, bi da bi. 1]. a cikin vivo: Dabigatran ya tsawaita adadin aPTT-dogara bayan gudanarwar jijiya a cikin berayen (0.3, 1 da 3 mg/kg) da birai rhesus (0.15, 0.3 da 0.6 mg/kg). An lura da tasirin maganin rigakafi na lokaci- da lokaci tare da dabigatran etexilate da aka gudanar da baki ga berayen masu hankali (10, 20 da 50 mg / kg) ko birai rhesus (1, 2.5 ko 5 mg / kg), tare da matsakaicin tasirin da aka lura tsakanin 30 da 120 min bayan gudanarwa, bi da bi [1]. Marasa lafiya da aka yi wa dabigatran etexilate sun sami ƙarancin bugun jini na ischemic (3.74 dabigatran etexilate vs 3.97 warfarin) da ƙarancin haɗuwa da zubar jini na ciki da bugun jini na jini (0.43 dabigatran etexilate vs 0.99 warfarin) a cikin 1020 haƙuri [shekaru]. Gwajin gwaji na asibiti: Ƙididdigar Pharmacokinetics da Pharmacodynamics na Oral Dabigatran Etexilate a cikin marasa lafiya na Hemodialysis. Mataki na 1

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