Ingemuva

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, iyisivimbeli esinamandla se-molecule encane ye-factor Xa okuyisici sokuhlangana ngesikhathi esibucayi endleleni yokuhlangana kwegazi okuholela ekukhiqizeni i-thrombin kanye nokwakheka kwehlule.I-Rivaroxaban ibophezela ku-Tyr288 ephaketheni le-S1 le-factor Xa ngokusebenzisana kwe-Tyr288 kanye nengxenye ye-chlorine ye-chlorothiophene moiety.Ukuvinjelwa kuyabuyiseleka emuva (koff = 5x10-3s-1), kuyashesha (kon = 1.7x107 mol/L-1 s-1), futhi ngendlela encike ekugxiliseni ingqondo (Ki = 0.4 nmol/L).I-Rivaroxaban okwamanje ifundelwa ukwelashwa kwe-VTE, ukuvimbela izenzakalo zenhliziyo ezigulini ezine-acute coronary syndrome, ukuvimbela isifo sohlangothi ezigulini ezine-fibrillation ye-atrial.

Ireferensi

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

Incazelo

I-Rivaroxaban (BAY 59-7939) inamandla kakhulu,i-Factor Xa (FXa) inhibitor ekhethiwe futhi eqondile, ezuza inzuzo eqinile ku-anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

Ku-Vitro

I-Rivaroxaban (BAY 59-7939) iyi-inhibitor yomlomo, eqondile ye-Factor Xa (FXa) ekuthuthukisweni kokuvimbela nokwelashwa kwe-arterial and venous thrombosis.I-Rivaroxaban ivimbela ngokuncintisana i-FFa yomuntu (Ki 0.4 nM) ngokukhetha okukhulu okuphindwe ka-10 000 kunamanye ama-serine protease;iphinde ivimbele umsebenzi we-prothrombinase (IC50 2.1 nM).I-Rivaroxaban ivimbela i-endogenous FXa enamandla kakhulu ku-plasma yomuntu kanye ne-rabbit (IC50 21 nM) kune-plasma yegundane (IC50 290 nM).Ibonisa imiphumela ye-anticoagulant ku-plasma yomuntu, isikhathi se-prothrombin esiphindwe kabili (PT) futhi yenza kusebenze isikhathi se-thromboplastin esiyingxenye ku-0.23 no-0.69μM, ngokulandelana.

I-Rivaroxaban (i-BAY 59-7939) iyi-inhibitor enamandla futhi ekhethiwe, eqondile ye-FCa enomsebenzi omuhle kakhulu we-vivo kanye ne-bioavailability yomlomo omuhle.I-Rivaroxaban (BAY 59-7939), elawulwa yi-iv bolus ngaphambi kokungeniswa kwe-thrombus, inciphisa ukwakheka kwe-thrombus (ED50 0.1 mg/kg), ivimbela i-FFa, futhi yandisa umthamo we-PT ngokuncike.I-PT ne-FFa zithinteka kancane ku-ED50 (ukwanda okuphindwe ka-1.8 kanye nokuvinjelwa kwe-32%, ngokulandelana).Ku-0.3 mg/kg (umthamo oholela ekuvimbeleni cishe okuphelele kokubunjwa kwe-thrombus), i-Rivaroxaban inweba ngokulinganisela i-PT (3.2).±0.5-fold) futhi ivimbela umsebenzi we-FFa (65±3%).

Isitoreji

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