Fage

Rivaroxaban, 5-chloro-N-[[(5S) -2-oxo-3-[4- (3-oxomorpholin-4-yl) phenyl]-1,3-oxazolidin-5-yl]methyl] thiophene-2 -carboxamide, shine mai hana ƙananan ƙwayoyin ƙwayoyin cuta na factor Xa wanda shine ma'anar coagulation a wani muhimmin lokaci a cikin hanyar haɗin jini wanda ya haifar da tsararru. thrombin da samuwar jini. Rivaroxaban yana ɗaure zuwa Tyr288 a cikin aljihun S1 na factor Xa ta hanyar hulɗar Tyr288 da chlorine maimakon chlorothiophene moiety. Hani yana iya juyawa (koff = 5x10-3s-1), mai sauri (kon = 1.7x107 mol / L-1 s-1), kuma a cikin hanyar da aka dogara da hankali (Ki = 0.4 nmol / L). A halin yanzu ana nazarin Rivaroxaban don maganin VTE, rigakafin cututtuka na zuciya da jijiyoyin jini a cikin marasa lafiya da ke fama da ciwo mai tsanani, rigakafin bugun jini a cikin marasa lafiya da fibrillation.

Magana

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, da Volker Laux. Rivaroxaban: sabon mai hanawa Xa. Arterioscler Thromb Vasc Biol 2010; 30 (3): 376-381

Bayani

Rivaroxaban (BAY 59-7939) yana da ƙarfi sosai,Zaɓaɓɓen da kai tsaye Factor Xa (FXa) mai hanawa, samun nasara mai ƙarfi a cikin ƙarfin anti-FXa (IC50 0.7 nM; Ki 0.4 nM).

A cikin Vitro

Rivaroxaban (BAY 59-7939) shine mai hanawa na baka, kai tsaye Factor Xa (FXa) mai hanawa a cikin ci gaba don rigakafi da kuma maganin thrombosis na arterial da venous. Rivaroxaban gasa yana hana FXa ɗan adam (Ki 0.4 nM) tare da> 10 000-ninka mafi girman zaɓi fiye da sauran ƙwayoyin cuta na serine; Hakanan yana hana ayyukan prothrombinase (IC50 2.1 nM). Rivaroxaban yana hana FXa endogenous mafi ƙarfi a cikin jini na ɗan adam da zomo (IC50 21 nM) fiye da ƙwayar bera (IC50 290 nM). Yana nuna tasirin anticoagulant a cikin plasma ɗan adam, lokacin prothrombin sau biyu (PT) kuma yana kunna lokaci na thromboplastin a 0.23 da 0.69.μM, bi da bi.

Rivaroxaban (BAY 59-7939) mai ƙarfi ne kuma zaɓi, mai hana FXa kai tsaye tare da kyakkyawan aiki a cikin vivo da ingantaccen yanayin rayuwa na baka. Rivaroxaban (BAY 59-7939), wanda iv bolus ke gudanarwa kafin shigar da thrombus, yana rage haɓakar thrombus (ED50 0.1 mg/kg), yana hana FXa, kuma yana tsawaita adadin PT dogara. PT da FXa sun shafi dan kadan a ED50 (ƙara 1.8-ninka da 32% hanawa, bi da bi). A 0.3 MG / kg (kashi wanda ke haifar da kusan cikakkiyar hana haɓakar thrombus), Rivaroxaban yana tsawaita PT (3.2) a matsakaici.±0.5-ninka) kuma yana hana ayyukan FXa (65±3%).

Adana

Tsarin sinadaran