Apixaban
Asalkii hore
Apixaban waa xakameyn heer sare ah oo la xushay oo dib loo rogi karo Factor Xa oo leh qiimaha Ki ee 0.08 nM iyo 0.17 nM ee bini'aadamka iyo bakaylaha, siday u kala horreeyaan[1].
Factor X, oo sidoo kale loo yaqaan eponym Stuart-Prower factor, waa enzym ka mid ah cascade xinjirowga. Factor X waxa lagu hawlgeliyay, hydrolysis, oo galay factor Xa labada qodob ee IX. Factor Xa waa qaabka firfircoon ee xinjirowga dhiigga ee xinjirowga lidka ku ah. Direct Xa inhibitors waa daawada xinjirowga lidka ku ah ee caanka ah [2].
In vitro: Apixabanhas waxay soo bandhigtay heer sare oo awood ah, xulashada, iyo waxtarka Factor Xa oo leh Ki of 0.08 nM iyo 0.17 nM ee Factor Human Xa iyo Bakaylaha Factor Xa, siday u kala horreeyaan [1]. Apixaban waxay ku dheeraatay waqtiyada xinjirowga ee balasmaha caadiga ah ee bini'aadamka iyada oo la eegayo (EC2x) ee 3.6, 0.37, 7.4 iyo 0.4 μM, kuwaas oo loo baahan yahay si ay u labanlaabaan wakhtiga prothrombin (PT), waqtiga prothrombin ee wax laga beddelay (mPT), wakhtiga qayb ka mid ah thromboplastin firfircoon. APTT) iyo HepTest. Ka sokow, Apixaban waxay muujisay awoodda ugu sareysa ee bini'aadamka iyo balasmaha bakaylaha, laakiin awood yar oo ku jirta balasmaha jiirka iyo eyga labadaba PT iyo APTT assays [3].
In vivo: Apixaban waxay soo bandhigtay farmashiyaha ugu fiican oo leh nadiifin aad u hooseeya (Cl: 0.02 L kg-1h-1), iyo mugga hoose ee qaybinta (Vdss: 0.2 L / kg) ee eyga. Ka sokow, Apixaban waxay sidoo kale muujisay nolol badhkeed dhexdhexaad ah oo leh T1 / 2 ee saacadaha 5.8 iyo bioavailability afka oo wanaagsan (F: 58%) [1]. Marka la eego xinjirowga xididada-shunt xinjirowga (AVST), xinjirowga xididka (VT) iyo korantada dhexdhexaadka ah ee carotid arterial thrombosis (ECAT) moodooyinka bakaylaha, Apixaban waxay soo saartay saameynaha antithrombotic ee EC50 ee 270 nM, 110 nM iyo 70 nM qaab ku-tiirsan. ]. Apixaban waxay si weyn u joojisay dhaqdhaqaaqa Xa ee IC50 ee 0.22 μM ee bakaylaha ex vivo[4]. Chimpanzee, Apixaban waxay sidoo kale muujisay mugga yar ee qaybinta (Vdss: 0.17 L kg-1), nadiifinta nidaamka hooseeya (Cl: 0.018 L kg-1h-1), iyo noole-biovailability afka oo wanaagsan (F: 59%) [5].
Tixraacyo:
Pinto DJP, Orwat MJ, Koch S, iyo al. Helitaanka 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), aad u awood badan, xulashada, waxtarka leh, iyo afka Xa[J]. Joornaalka Kiimikada daawada, 2007, 50 (22): 5339-5356.
Sidhu P S. Factor Direct Xa Inhibitors sida xinjirowga lidka ku ah [J].
Wong PC, Crain EJ, Xin B, iyo al. Apixaban, oo ah arrin afka ah, toos ah oo aadka loo xushay Xa inhibitor: in vitro, antithrombotic iyo antihemostatics[J]. Journal of Thrombosis and Hemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, iyo al. Dheef-shiid kiimikaad, farmacokinetics iyo farmacodynamics ee factor Xa inhibitor apixaban ee bakaylaha[J]. Journal of thrombosis iyo thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, iyo al. Farmashiyaha hore ee daawada iyo farmacodynamics of apixaban, oo ah arrin awood leh oo la xushay Xa inhibitor [J]. Joornaalka Yurub ee dheef-shiid kiimikaad iyo dawooyinka dawooyinka, 2011, 36 (3): 129-139.
Apixaban waa xakameyn heer sare ah oo la xushay oo dib loo rogi karo Factor Xa oo leh qiimaha Ki ee 0.08 nM iyo 0.17 nM ee bini'aadamka iyo bakaylaha, siday u kala horreeyaan[1].
Factor X, oo sidoo kale loo yaqaan eponym Stuart-Prower factor, waa enzym ka mid ah cascade xinjirowga. Factor X waxa lagu hawlgeliyay, hydrolysis, oo galay factor Xa labada qodob ee IX. Factor Xa waa qaabka firfircoon ee xinjirowga dhiigga ee xinjirowga lidka ku ah. Direct Xa inhibitors waa daawada xinjirowga lidka ku ah ee caanka ah [2].
In vitro: Apixabanhas waxay soo bandhigtay heer sare oo awood ah, xulashada, iyo waxtarka Factor Xa oo leh Ki of 0.08 nM iyo 0.17 nM ee Factor Human Xa iyo Bakaylaha Factor Xa, siday u kala horreeyaan [1]. Apixaban waxay ku dheeraatay waqtiyada xinjirowga ee balasmaha caadiga ah ee bini'aadamka iyada oo la eegayo (EC2x) ee 3.6, 0.37, 7.4 iyo 0.4 μM, kuwaas oo loo baahan yahay si ay u labanlaabaan wakhtiga prothrombin (PT), waqtiga prothrombin ee wax laga beddelay (mPT), wakhtiga qayb ka mid ah thromboplastin firfircoon. APTT) iyo HepTest. Ka sokow, Apixaban waxay muujisay awoodda ugu sareysa ee bini'aadamka iyo balasmaha bakaylaha, laakiin awood yar oo ku jirta balasmaha jiirka iyo eyga labadaba PT iyo APTT assays [3].
In vivo: Apixaban waxay soo bandhigtay farmashiyaha ugu fiican oo leh nadiifin aad u hooseeya (Cl: 0.02 L kg-1h-1), iyo mugga hoose ee qaybinta (Vdss: 0.2 L / kg) ee eyga. Ka sokow, Apixaban waxay sidoo kale muujisay nolol badhkeed dhexdhexaad ah oo leh T1 / 2 ee saacadaha 5.8 iyo bioavailability afka oo wanaagsan (F: 58%) [1]. Marka la eego xinjirowga xididada-shunt xinjirowga (AVST), xinjirowga xididka (VT) iyo korantada dhexdhexaadka ah ee carotid arterial thrombosis (ECAT) moodooyinka bakaylaha, Apixaban waxay soo saartay saameynaha antithrombotic ee EC50 ee 270 nM, 110 nM iyo 70 nM qaab ku-tiirsan. ]. Apixaban waxay si weyn u joojisay dhaqdhaqaaqa Xa ee IC50 ee 0.22 μM ee bakaylaha ex vivo[4]. Chimpanzee, Apixaban waxay sidoo kale muujisay mugga yar ee qaybinta (Vdss: 0.17 L kg-1), nadiifinta nidaamka hooseeya (Cl: 0.018 L kg-1h-1), iyo noole-biovailability afka oo wanaagsan (F: 59%) [5].
Tixraacyo:
Pinto DJP, Orwat MJ, Koch S, iyo al. Helitaanka 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), aad u awood badan, xulashada, waxtarka leh, iyo afka Xa[J]. Joornaalka Kiimikada daawada, 2007, 50 (22): 5339-5356.
Sidhu P S. Factor Direct Xa Inhibitors sida xinjirowga lidka ku ah [J].
Wong PC, Crain EJ, Xin B, iyo al. Apixaban, oo ah arrin afka ah, toos ah oo aadka loo xushay Xa inhibitor: in vitro, antithrombotic iyo antihemostatics[J]. Journal of Thrombosis and Hemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, iyo al. Dheef-shiid kiimikaad, farmacokinetics iyo farmacodynamics ee factor Xa inhibitor apixaban ee bakaylaha[J]. Journal of thrombosis iyo thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, iyo al. Farmashiyaha hore ee daawada iyo farmacodynamics of apixaban, oo ah arrin awood leh oo la xushay Xa inhibitor [J]. Joornaalka Yurub ee dheef-shiid kiimikaad iyo dawooyinka dawooyinka, 2011, 36 (3): 129-139.
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