Mbiri

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3--[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, ndi mphamvu yaying'ono-molecule inhibitor ya factor Xa yomwe ndi coagulation factor pa nthawi yovuta kwambiri ya magazi coagulation njira zomwe zimapangitsa kuti m'badwo thrombin ndi kupanga magazi kuundana. Rivaroxaban imamangiriza ku Tyr288 mu S1 thumba la factor Xa kudzera mu kuyanjana kwa Tyr288 ndi chlorine mmalo mwa chlorothiophene moiety. Kuletsa kumasinthidwa (koff = 5x10-3s-1), mofulumira (kon = 1.7x107 mol/L-1 s-1), komanso modalira ndende (Ki = 0.4 nmol/L). Rivaroxaban panopa akuphunziridwa zochizira VTE, kupewa zochitika mtima mtima odwala pachimake coronary syndrome, kupewa sitiroko odwala matenda fibrillation.

Buku

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, and Volker Laux. Rivaroxaban: oral factor Xa inhibitor yatsopano. Arterioscler Thromb Vasc Biol 2010; 30 (3): 376-381

Kufotokozera

Rivaroxaban (BAY 59-7939) ndi wamphamvu kwambiri,kusankha ndi mwachindunji Factor Xa (FXa) inhibitor, kupeza phindu lamphamvu mu anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

Mu Vitro

Rivaroxaban (BAY 59-7939) ndi pakamwa, mwachindunji Factor Xa (FXa) inhibitor mu chitukuko pofuna kupewa ndi kuchiza arterial ndi venous thrombosis. Rivaroxaban amaletsa mpikisano wa FXa (Ki 0.4 nM) ndi> 10 000-kusankha kwakukulu kusiyana ndi ma serine proteases ena; imalepheretsanso ntchito ya prothrombinase (IC50 2.1 nM). Rivaroxaban imalepheretsa endogenous FXa mwamphamvu kwambiri mu plasma ya anthu ndi akalulu (IC50 21 nM) kuposa plasma ya makoswe (IC50 290 nM). Imawonetsa zotsatira za anticoagulant mu plasma yaumunthu, kuwirikiza kawiri nthawi ya prothrombin (PT) ndikuyambitsa nthawi ya thromboplastin pa 0.23 ndi 0.69μM, motero.

Rivaroxaban (BAY 59-7939) ndi yamphamvu komanso yosankha, yolunjika FXa inhibitor yokhala ndi ntchito yabwino kwambiri ya vivo komanso bioavailability yapakamwa. Rivaroxaban (BAY 59-7939), yoyendetsedwa ndi iv bolus isanayambe kulowetsedwa kwa thrombus, imachepetsa mapangidwe a thrombus (ED50 0.1 mg / kg), imalepheretsa FXa, ndipo imatalikitsa mlingo wa PT modalira. PT ndi FXa zimakhudzidwa pang'ono pa ED50 (kuwonjezeka kwa 1.8-fold and 32% inhibition, motero). Pa 0.3 mg/kg (mlingo womwe umatsogolera ku kuletsa kwathunthu kwa mapangidwe a thrombus), Rivaroxaban mozama amatalikitsa PT (3.2)±0.5-fold) ndikuletsa ntchito ya FXa (65±3%).

Kusungirako

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