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 fa'atosina mole mole laiti malosi o le factor Xa lea o se mea e fa'amalo ai i se fa'alavelave ogaoga i le ala fa'amalo toto e mafua ai le fa'atupuina o le thrombin ma le faʻavaeina o le gaʻo. Rivaroxaban e fusifusia i le Tyr288 i le S1 taga o le factor Xa e ala i fegalegaleaiga a Tyr288 ma le chlorine suitulaga o le chlorothiophene moiety. O le faʻalavelave e mafai ona toe faʻafoʻi (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 malosi anti-FXa (IC50 0.7 nM; Ki 0.4 nM).

I Vitro

Rivaroxaban (BAY 59-7939) o se fa'aitu'u tautala, tuusao Factor Xa (FXa) inhibitor i le atinae mo le puipuia ma le togafitia o arterial ma venous thrombosis. Rivaroxaban faʻatauvaʻa faʻalavelave faʻalavelave FXa tagata (Ki 0.4 nM) faʻatasi 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 FXa endogenous sili atu i le tagata ma le lapiti plasma (IC50 21 nM) nai lo plasma rat (IC50 290 nM). E faʻaalia ai aʻafiaga o le anticoagulant i le plasma o le tagata, faʻaluaina le taimi o le prothrombin (PT) ma faʻagaoioia vaega o le thromboplastin taimi ile 0.23 ma le 0.69.μM, ta'itasi.

Rivaroxaban (BAY 59-7939) o se malosi ma filifili, faʻatonu FXa inhibitor faʻatasi ai ma gaioiga sili ona lelei i le vivo 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 o loʻo aʻafia teisi i le ED50 (1.8-faʻateleina ma le 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 faʻaumiina lelei le PT (3.2).±0.5-piilima) ma faʻalavelaveina le gaioiga FXa (65±3%).

Teuina

Fa'asologa o vaila'au