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Dabigatran Etexlate Mesylate

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Orukọ API	Itọkasi	Sipesifikesonu	US DMF	EU DMF	CEP
Dabigatran Etexlate Mesylate	Anticoagulant	Ninu Ile

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Dabigatran etexilate mesylate (BIBR 1048MS) jẹ oogun ti nṣiṣe lọwọ ẹnu ti Dabigatran.Dabigatran etexilate mesylate ni awọn ipa anticoagulant ati pe a lo fun idena ti iṣọn-ẹjẹ iṣọn-ẹjẹ ati ọpọlọ nitori fibrillation atrial.

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Apejuwe: IC50 Iye: 4.5nM (Ki);10nM (Akopọ platelet ti o fa Thrombin) [1] Dabigatran jẹ iparọ-pada ati yiyan, inhibitor thrombin taara (DTI) ti n gba idagbasoke ile-iwosan to ti ni ilọsiwaju bi prodrug ti nṣiṣe lọwọ ẹnu, dabigatran etexilate.in vitro: Dabigatran ti o yan ati ki o tun ṣe idiwọ thrombin eniyan (Ki: 4.5 nM) bakanna bi iṣọpọ thrombin-induced platelet (IC (50): 10 nM), lakoko ti o ṣe afihan ipa ti ko ni idinamọ lori awọn aṣoju-ara-ara-ara-ara miiran. pilasima talaka (PPP), ti a ṣe bi agbara thrombin endogenous (ETP) ni idinamọ ifọkansi-igbẹkẹle (IC (50): 0.56 microM).Dabigatran ṣe afihan awọn ipa anticoagulant ti o gbẹkẹle ifọkansi ni ọpọlọpọ awọn eya ni fitiro, ilọpo meji akoko thromboplastin apakan ti a mu ṣiṣẹ (aPTT), akoko prothrombin (PT) ati akoko didi ecarin (ECT) ninu PPP eniyan ni awọn ifọkansi ti 0.23, 0.83 ati 0.18 microM, lẹsẹsẹ. 1].ni vivo: Dabigatran pẹ iwọn lilo aPTT ni igbẹkẹle lẹhin iṣakoso iṣọn-ẹjẹ ninu awọn eku (0.3, 1 ati 3 mg/kg) ati awọn obo rhesus (0.15, 0.3 ati 0.6 mg/kg).Iwọn-ati awọn ipa anticoagulant ti o gbẹkẹle akoko ni a ṣe akiyesi pẹlu dabigatran etexilate ti a nṣakoso ni ẹnu si awọn eku mimọ (10, 20 ati 50 mg/kg) tabi awọn obo rhesus (1, 2.5 tabi 5 mg/kg), pẹlu awọn ipa ti o pọju ti a ṣe akiyesi laarin 30 ati 120 min lẹhin isakoso, lẹsẹsẹ [1].Awọn alaisan ti a tọju pẹlu dabigatran etexilate ni iriri diẹ ninu awọn ikọlu ischemic (3.74 dabigatran etexilate vs 3.97 warfarin) ati idinku idapọ inu iṣọn-ẹjẹ inu ati awọn ikọlu iṣọn-ẹjẹ (0.43 dabigatran etexilate vs 0.99 warfarin) fun 1020 alaisan-ọdun.Idanwo ile-iwosan: Ayẹwo ti Pharmacokinetics ati Pharmacodynamics ti Oral Dabigatran Etexilate ni Awọn alaisan Hemodialysis.Ipele 1

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