Ka morao

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, ke inhibitor e nyane ea molek'hule ea factor Xa e leng ntho e kopanyang nakong e mahlonoko tseleng ea ho kopanya mali e bakang moloko. ea thrombin le ho thehoa ha lesela. Rivaroxaban e tlamella Tyr288 ka pokothong ea S1 ea factor Xa ka tšebelisano ea Tyr288 le karolo ea chlorine ea chlorothiophene moiety. Thibelo e ka fetoha (koff = 5x10-3s-1), ka potlako (kon = 1.7x107 mol / L-1 s-1), le ka mokhoa o itšetlehileng ka mahloriso (Ki = 0.4 nmol / L). Hona joale Rivaroxaban e ntse e ithutoa bakeng sa phekolo ea VTE, ho thibela liketsahalo tsa pelo ho bakuli ba nang le lefu la pelo, ho thibela lefu la stroke ho bakuli ba nang le atrial fibrillation.

Referense

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

Tlhaloso

Rivaroxaban (BAY 59-7939) e matla haholo,khethang le ho toba Factor Xa (FXa) inhibitor, ho finyella phaello e matla ho anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

Ka Vitro

Rivaroxaban (BAY 59-7939) ke inhibitor ea molomo, e tobileng ea Factor Xa (FXa) ho nts'etsopele bakeng sa thibelo le kalafo ea arterial and venous thrombosis. Rivaroxaban ka tlhōlisano e thibela motho FXa (Ki 0.4 nM) ka > 10 000-makhetlo a ho khetha ho feta ho li-serine proteases tse ling; e boetse e thibela mosebetsi oa prothrombinase (IC50 2.1 nM). Rivaroxaban e thibela endogenous FXa ka matla ho plasma ea batho le ea mmutla (IC50 21 nM) ho feta plasma ea rat (IC50 290 nM). E bonts'a litlamorao tsa anticoagulant ho plasma ea motho, nako ea prothrombin habeli (PT) mme e kenya nako ea karolo ea thromboplastin ho 0.23 le 0.69μM, ka ho latellana.

Rivaroxaban (BAY 59-7939) ke e matla le e khethang, e tobileng ea FXa inhibitor e nang le ts'ebetso e ntle ea vivo le bioavailability e ntle ea molomo. Rivaroxaban (BAY 59-7939), e tsamaisoang ke iv bolus pele ho kenngoa ha thrombus, e fokotsa sebopeho sa thrombus (ED50 0.1 mg / kg), e thibela FXa, 'me e lelefatsa tekanyo ea PT ho itšetlehile ka eona. PT le FXa li ameha hanyenyane ho ED50 (keketseho ea 1.8-fold le 32% inhibition, ka ho latellana). Ka 0.3 mg / kg (thal dose e lebisang ho hoo e ka bang ho thibela ho feletseng ho thehoa ha thrombus), Rivaroxaban ka mokhoa o itekanetseng o lelefatsa PT (3.2).±0.5-fold) mme e thibela ts'ebetso ea FXa (65±3%).

Polokelo

Sebopeho sa lik'hemik'hale