Fage

Apixaban babban zaɓi ne da mai hanawa na Factor Xa tare da kimar Ki na 0.08 nM da 0.17 nM a cikin mutum da zomo, bi da bi [1].

Factor X, wanda kuma aka sani da eponym Stuart-Prower factor, wani enzyme ne na coagulation cascade. An kunna Factor X, ta hanyar hydrolysis, zuwa cikin factor Xa ta biyu factor IX. Factor Xa shine nau'in da aka kunna na coagulation factor thrombokinase. Inhibiting Factor Xa zai iya ba da wata hanya ta dabam don maganin rigakafi. Direct Xa inhibitors sanannen magungunan anticoagulants [2].

A cikin vitro: Apixabanhas ya nuna babban matsayi na ƙarfi, zaɓi, da inganci akan Factor Xa tare da Ki na 0.08 nM da 0.17 nM don Factor Factor Xa da Rabbit Factor Xa, bi da bi [1]. Apixaban ya tsawaita lokutan clotting na plasma na al'ada na al'ada tare da ƙididdiga (EC2x) na 3.6, 0.37, 7.4 da 0.4 μM, waɗanda ake buƙata don ninka lokacin prothrombin (PT), lokacin prothrombin da aka gyara (mPT), lokacin kunna thromboplastin lokaci (lokacin thromboplastin). APTT) da kuma HepTest. Bayan haka, Apixaban ya nuna mafi girman ƙarfi a cikin jini na ɗan adam da zomo, amma ƙarancin ƙarfi a cikin bera da plasma na kare a duka gwajin PT da APTT [3].

A cikin vivo: Apixaban ya nuna kyakkyawan magungunan pharmacokinetics tare da ƙarancin izini (Cl: 0.02 L kg-1h-1), da ƙananan ƙananan rarraba (Vdss: 0.2 L / kg) a cikin kare. Bayan haka, Apixaban kuma ya nuna matsakaicin rabin rayuwa tare da T1 / 2 na sa'o'i 5.8 da ingantaccen yanayin rayuwa na baka (F: 58%) [1]. A cikin thrombosis arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) da lantarki tsaka-tsaki carotid arterial thrombosis (ECAT) zomo model, Apixaban ya samar da antithrombotic effects tare da EC50 na 270 nM, 110 nM da 70 nM a cikin wani kashi-dogara hanya. ]. Apixaban ya hana aikin factor Xa tare da IC50 na 0.22 μM a cikin zomo ex vivo[4]. A cikin chimpanzee, Apixaban kuma ya nuna ƙaramin ƙarar rarraba (Vdss: 0.17 L kg-1), ƙarancin tsarin tsarin (Cl: 0.018 L kg-1h-1), da kuma kyakkyawan yanayin rayuwa na baka (F: 59%) [5].

Magana:
Pinto DJP, Orwat MJ, Koch S, et al. Gano 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), mai matukar ƙarfi, zaɓi, inganci, da baki bioavailable inhibitor na jini coagulation factor Xa[J]. Jaridar Magungunan Magunguna, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors a matsayin Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, na baka, kai tsaye da kuma zaɓi mai mahimmanci Xa inhibitor: in vitro, antithrombotic da antihemostatics [J]. Jaridar Thrombosis da Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics da pharmacodynamics na factor Xa inhibitor apixaban a zomaye[J]. Jaridar thrombosis da thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics da pharmacodynamics na apixaban, mai ƙarfi da zaɓin factor Xa inhibitor [J]. Jaridar Turai na Magungunan Magunguna da Magunguna, 2011, 36 (3): 129-139.

Apixaban babban zaɓi ne da mai hanawa na Factor Xa tare da kimar Ki na 0.08 nM da 0.17 nM a cikin mutum da zomo, bi da bi [1].

Factor X, wanda kuma aka sani da eponym Stuart-Prower factor, wani enzyme ne na coagulation cascade. An kunna Factor X, ta hanyar hydrolysis, zuwa cikin factor Xa ta biyu factor IX. Factor Xa shine nau'in da aka kunna na coagulation factor thrombokinase. Inhibiting Factor Xa zai iya ba da wata hanya ta dabam don maganin rigakafi. Direct Xa inhibitors sanannen magungunan anticoagulants [2].

A cikin vitro: Apixabanhas ya nuna babban matsayi na ƙarfi, zaɓi, da inganci akan Factor Xa tare da Ki na 0.08 nM da 0.17 nM don Factor Factor Xa da Rabbit Factor Xa, bi da bi [1]. Apixaban ya tsawaita lokutan clotting na plasma na al'ada na al'ada tare da ƙididdiga (EC2x) na 3.6, 0.37, 7.4 da 0.4 μM, waɗanda ake buƙata don ninka lokacin prothrombin (PT), lokacin prothrombin da aka gyara (mPT), lokacin kunna thromboplastin lokaci (lokacin thromboplastin). APTT) da kuma HepTest. Bayan haka, Apixaban ya nuna mafi girman ƙarfi a cikin jini na ɗan adam da zomo, amma ƙarancin ƙarfi a cikin bera da plasma na kare a duka gwajin PT da APTT [3].

A cikin vivo: Apixaban ya nuna kyakkyawan magungunan pharmacokinetics tare da ƙarancin izini (Cl: 0.02 L kg-1h-1), da ƙananan ƙananan rarraba (Vdss: 0.2 L / kg) a cikin kare. Bayan haka, Apixaban kuma ya nuna matsakaicin rabin rayuwa tare da T1 / 2 na sa'o'i 5.8 da ingantaccen yanayin rayuwa na baka (F: 58%) [1]. A cikin thrombosis arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) da lantarki tsaka-tsaki carotid arterial thrombosis (ECAT) zomo model, Apixaban ya samar da antithrombotic effects tare da EC50 na 270 nM, 110 nM da 70 nM a cikin wani kashi-dogara hanya. ]. Apixaban ya hana aikin factor Xa tare da IC50 na 0.22 μM a cikin zomo ex vivo[4]. A cikin chimpanzee, Apixaban kuma ya nuna ƙaramin ƙarar rarraba (Vdss: 0.17 L kg-1), ƙarancin tsarin tsarin (Cl: 0.018 L kg-1h-1), da kuma kyakkyawan yanayin rayuwa na baka (F: 59%) [5].

Magana:
Pinto DJP, Orwat MJ, Koch S, et al. Gano 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), mai matukar ƙarfi, zaɓi, inganci, da baki bioavailable inhibitor na jini coagulation factor Xa[J]. Jaridar Magungunan Magunguna, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors a matsayin Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, na baka, kai tsaye da kuma zaɓi mai mahimmanci Xa inhibitor: in vitro, antithrombotic da antihemostatics [J]. Jaridar Thrombosis da Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics da pharmacodynamics na factor Xa inhibitor apixaban a zomaye[J]. Jaridar thrombosis da thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics da pharmacodynamics na apixaban, mai ƙarfi da zaɓin factor Xa inhibitor [J]. Jaridar Turai na Magungunan Magunguna da Magunguna, 2011, 36 (3): 129-139.

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