Asalkii hore

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4- (3-oxomorpholin-4-yl) phenyl]-1,3-oxazolidin-5-yl]methyl] thiophene-2 -carboxamide, waa xayndaab yar oo awood leh oo xakameynaya factor Xa kaas oo ah xinjirowga dhiigga ee marxaladda muhiimka ah ee dariiqa xinjirowga dhiigga taasoo keentay jiilka thrombin iyo samaynta xinjirowga. Rivaroxaban waxay ku xidhan tahay Tyr288 ee jeebka S1 ee factor Xa iyada oo loo marayo isdhexgalka Tyr288 iyo koloriinta beddelka unugyada chlorothiophene. Xannibaadda ayaa dib loo rogi karaa (koff = 5x10-3s-1), degdeg ah (kon = 1.7x107 mol/L-1 s-1), iyo hab ku-tiirsanaan ah (Ki = 0.4 nmol/L). Rivaroxaban hadda waxaa lagu bartaa daaweynta VTE, ka hortagga dhacdooyinka wadnaha iyo xididdada bukaanada qaba xanuunka 'coronary syndrome', ka hortagga istaroogga ee bukaanada qaba fibrillation atrial.

Tixraac

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, iyo Volker Laux. Rivaroxaban: Cunsurka afka cusub ee Xa inhibitor. Arterioscler Thromb Vasc Biol 2010; 30 (3): 376-381

Sharaxaada

Rivaroxaban (BAY 59-7939) waa mid aad u awood badan,Xulashada iyo tooska ah Factor Xa (FXa) inhibitor, gaaritaanka faa'iido xoog leh oo ka soo horjeeda awoodda FXa (IC50 0.7 nM; Ki 0.4 nM).

In Vitro

Rivaroxaban (BAY 59-7939) waa afka, toos ah Factor Xa (FXa) inhibitor ee horumarinta ee ka hortagga iyo daaweynta halbowlayaasha iyo xididdada xididdada dhiigga. Rivaroxaban si tartan ah u joojiya FXa bini'aadamka (Ki 0.4 nM) oo leh> 10 000-laab doorasho ka weyn marka loo eego proteases kale ee serine; waxay sidoo kale joojisaa dhaqdhaqaaqa prothrombinase (IC50 2.1 nM). Rivaroxaban waxay si ka xoog badan u joojisaa FXa-da endogenous ee balasmaha aadanaha iyo bakaylaha (IC50 21 nM) marka loo eego balasmaha jiirka (IC50 290 nM). Waxay muujinaysaa saamaynta xinjirowga lidka ku ah ee balasmaha bini'aadamka, labanlaabida waqtiga prothrombin (PT) waxayna kicisaa qayb qayb ah thromboplastin 0.23 iyo 0.69μM, siday u kala horreeyaan.

Rivaroxaban (BAY 59-7939) waa awood iyo xulasho, toos ah FXa inhibitor oo leh firfircooni aad u wanaagsan iyo noole afka oo wanaagsan. Rivaroxaban (BAY 59-7939), oo ay maamusho iv bolus ka hor xinjirowga dhiigga, waxay yaraynaysaa samaynta thrombus (ED50 0.1 mg/kg), waxay joojisaa FXa, waxayna kordhisaa qiyaasta PT si ku xiran. PT iyo FXa waxyar ayay saameeyeen ED50 (1.8-laab koror iyo 32% xannibaad, siday u kala horreeyaan). Marka loo eego 0.3 mg/kg (qiyaas u horseedaya in si buuxda loo joojiyo samaynta thrombus), Rivaroxaban waxay si dhexdhexaad ah u dheeraysaa PT (3.2)±0.5-laab) oo waxay joojisaa dhaqdhaqaaqa FXa (65±3%)

Kaydinta

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