Talaaga

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, o se faʻamalosi laiti-molole inhibitor o mea Xa lea o se vaega coagulation i se juncture taua i le auala coagulation toto e mafua ai le gaosiga o le thrombin ma le fausia o clot.Rivaroxaban e fusifusia i le Tyr288 i le S1 taga o mea Xa e ala i le fegalegaleaiga a Tyr288 ma le chlorine suitulaga o le chlorothiophene moiety.O le faʻalavelave e mafai ona faʻafeiloaʻi (koff = 5x10-3s-1), vave (kon = 1.7x107 mol / L-1 s-1), ma i se tulaga faʻalagolago (Ki = 0.4 nmol / L).Rivaroxaban o loʻo suʻesuʻeina nei mo le togafitiga o le VTE, puipuia o mea e tutupu i le cardiovascular i tagata mamaʻi maʻi faʻamaʻi pipisi, puipuia o le stroke i tagata mamaʻi ma le fibrillation atrial.

Fa'asinomaga

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, ma Volker Laux.Rivaroxaban: o se mea fou ole fa'aogaina ole Xa inhibitor.Arterioscler Thromb Vasc Biol 2010;30(3): 376-381

Fa'amatalaga

Rivaroxaban (BAY 59-7939) e sili ona malosi,filifili ma tuusao Factor Xa (FXa) inhibitor, ausia se malosi malosi i le anti-FXa malosi (IC50 0.7 nM; Ki 0.4 nM).

I Vitro

Rivaroxaban (BAY 59-7939) o se fa'amalo tautala, Factor Xa (FXa) tuusaʻo i le atinaʻeina mo le puipuia ma le togafitia o le thrombosis arterial ma venous.Rivaroxaban fa'atauvaga fa'alavelave fa'alavelave FXa tagata (Ki 0.4 nM) fa'atasi ma> 10 000-sili atu le filifilia nai lo isi serine proteases;e taofia ai foi le gaioiga o le prothrombinase (IC50 2.1 nM).Rivaroxaban e faʻalavelaveina le endogenous FXa sili atu ona malosi i le plasma o le tagata ma le lapiti (IC50 21 nM) nai lo le plasma rat (IC50 290 nM).O loʻo faʻaalia ai aʻafiaga o le anticoagulant i le plasma tagata, faʻaluaina le taimi o le prothrombin (PT) ma faʻagaoioia le taimi o le thromboplastin i le 0.23 ma le 0.69.μM, ta'itasi.

Rivaroxaban (BAY 59-7939) o se malosi ma le filifilia, faʻatonu FXa inhibitor faʻatasi ma le sili ona lelei i le vivo gaioiga ma le lelei o le bioavailability oral.Rivaroxaban (BAY 59-7939), faʻatonuina e le iv bolus aʻo leʻi amataina le thrombus, faʻaitiitia le faʻavaeina o le thrombus (ED50 0.1 mg / kg), faʻalavelave FXa, ma faʻaumiina le fua o le PT faʻalagolago.O le PT ma le FXa e aafia laʻititi i le ED50 (1.8-faʻateleina faʻateleina ma 32% faʻasaina, faʻasologa).I le 0.3 mg / kg (dose e taʻitaʻia ai le faʻamaʻi atoa o le faʻavaeina o le thrombus), o Rivaroxaban e faʻalauteleina le PT (3.2).±0.5-paiga) ma faʻalavelaveina le gaioiga FXa (65±3%).

Teuina

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