Amavu n'amavuko

Rivaroxaban, 5-chloro-N - [[(5S) -2-oxo-3- [4- -carboxamide, ni imbaraga ntoya ya molekile ikingira ibintu Xa nikintu coagulation mugihe gikomeye mumihanda ya coagulation yamaraso bigatuma habaho kubyara trombine no gushiraho imyenda. Rivaroxaban ihuza Tyr288 mu mufuka wa S1 w'ikintu Xa binyuze mu mikoranire 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 mu kuvura VTE, gukumira indwara zifata umutima n’umutima ku barwayi bafite syndrome ikaze ya coronary, kwirinda indwara y’imitsi ku barwayi bafite fibrillation yo mu mubiri.

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 no kuvura trombose ya arterial na venine. Rivaroxaban irushanwa irwanya abantu FXa (Ki 0.4 nM) hamwe na> 10 000 yikubye inshuro 10 kurenza izindi poroteyine za serine; irabuza kandi ibikorwa bya prothrombinase (IC50 2.1 nM). Rivaroxaban ibuza FXa endogenous cyane muri plasma yabantu 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 cya 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 yo mu kanwa. Rivaroxaban (BAY 59-7939), iyobowe na iv bolus mbere yo kwinjizwa kwa trombus, igabanya imiterere ya trombus (ED50 0.1 mg / kg), ikabuza FXa, kandi ikongerera PT urugero. PT na FXa bigira ingaruka nkeya 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%).

Ububiko

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