Ubushinwa Rivaroxaban abakora nabatanga |CPF

Rivaroxaban

Ibisobanuro bigufi:

Izina rya API	Kwerekana	Ibisobanuro	DMF yo muri Amerika	EU DMF	CEP
Rivaroxaban	Anticoagulant	Mu nzu	TDP

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Ibisobanuro birambuye

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KUBONA UMUSARURO

Amavu n'amavuko

Rivaroxaban, 5-chloro-N - [[(5S) -2-oxo-3- [4- (3- -carboxamide, ni imbaraga ntoya ya molekile ikingira ibintu Xa ikaba ari coagulation mugihe gikomeye cyinzira yo guhuza amaraso bigatuma habaho trombine no kwibumbira hamwe.Rivaroxaban ihuza Tyr288 mumufuka wa S1 yibintu Xa binyuze mumikoranire ya Tyr288 hamwe na chlorine isimbuza chlorothiophene.Kubuzwa birashobora guhinduka (koff = 5x10-3s-1), byihuse (kon = 1.7x107 mol / L-1 s-1), kandi muburyo bushingiye ku kwibanda (Ki = 0.4 nmol / L).Muri iki gihe Rivaroxaban irimo kwigwa kugira ngo ivure VTE, irinde indwara zifata umutima n’umutima ku barwayi bafite syndrome de acute coronary, kwirinda indwara y’imitsi ku barwayi bafite fibrillation atriel.

Reba

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, na Volker Laux.Rivaroxaban: ikintu gishya cyo munwa Xa inhibitor.Arterioscler Thromb Vasc Biol 2010;30 (3): 376-381

Ibisobanuro

Rivaroxaban (BAY 59-7939) nimbaraga nyinshi，guhitamo no kuyobora Factor Xa (FXa) inhibitor, kugera ku nyungu zikomeye mubushobozi bwo kurwanya FXa (IC50 0.7 nM; Ki 0.4 nM).

Muri Vitro

Rivaroxaban (BAY 59-7939) ni umunwa, utaziguye Factor Xa (FXa) inhibitor mugutezimbere no gukumira indwara ya arterial na venine trombose.Rivaroxaban irushanwa irwanya abantu FXa (Ki 0.4 nM) hamwe na> 10 000 inshuro nyinshi guhitamo kuruta izindi poroteyine;irabuza kandi ibikorwa bya prothrombinase (IC50 2.1 nM).Rivaroxaban ibuza FXa endogenous cyane muri plasma yumuntu ninkwavu (IC50 21 nM) kuruta plasma yimbeba (IC50 290 nM).Yerekana ingaruka za anticoagulant muri plasma yabantu, gukuba kabiri prothrombine (PT) kandi ikora tromboplastine igice kuri 0.23 na 0.69μM, kimwe.

Rivaroxaban (BAY 59-7939) nimbaraga zikomeye kandi zitoranya, ziyobora FXa inhibitor hamwe nibikorwa byiza bya vivo hamwe na bioavailable nziza.Rivaroxaban (BAY 59-7939), iyobowe na iv bolus mbere yo kwinjira muri trombus, igabanya imiterere ya trombus (ED50 0.1 mg / kg), ikabuza FXa, kandi ikongerera urugero rwa PT.PT na FXa bigira ingaruka nke kuri ED50 (kwiyongera inshuro 1.8 na 32% bibujijwe).Kuri 0.3 mg / kg (ikinini kiganisha hafi yo guhagarika trombus), Rivaroxaban yongerera PT mu buryo bushyize mu gaciro (3.2)±0.5-inshuro) kandi ibuza ibikorwa bya FXa (65±3%).

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