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Apixaban ndi choletsa chosankha komanso chosinthika cha Factor Xa chokhala ndi ma Ki a 0.08 nM ndi 0.17 nM mwa munthu ndi kalulu, motsatana[1].

Factor X, yomwe imadziwikanso ndi dzina loti Stuart-Prower factor, ndi puloteni ya coagulation cascade. Factor X imayendetsedwa, ndi hydrolysis, kukhala factor Xa ndi IX factor IX. Factor Xa ndi mawonekedwe oyambitsidwa a coagulation factorthrombokinase.Inhibiting Factor Xa ikhoza kupereka njira ina ya anticoagulation. Direct Xa inhibitors ndi anticoagulants otchuka [2].

In vitro: Apixabanhas adawonetsa kuchuluka kwa potency, kusankha, komanso kuchita bwino pa Factor Xa ndi Ki ya 0.08 nM ndi 0.17 nM ya Human Factor Xa ndi Rabbit Factor Xa, motsatana [1]. Apixaban amatalikitsa nthawi yotsekeka ya plasma wamba wamunthu ndi kuchuluka (EC2x) kwa 3.6, 0.37, 7.4 ndi 0.4 μM, zomwe zimafunikira motsatana kuwirikiza nthawi ya prothrombin (PT), nthawi yosinthidwa ya prothrombin (mPT), yoyambitsa nthawi ya thromboplastin ( APTT) ndi HepTest. Kupatula apo, Apixaban adawonetsa potency yapamwamba kwambiri mu plasma ya anthu ndi akalulu, koma potency yochepa mu plasma ya makoswe ndi agalu muzoyesa za PT ndi APTT [3].

Mu vivo: Apixaban adawonetsa ma pharmacokinetics abwino kwambiri okhala ndi chilolezo chochepa kwambiri (Cl: 0.02 L kg-1h-1), komanso kugawa kochepa (Vdss: 0.2 L / kg) mwa galu. Kupatula apo, Apixaban adawonetsanso moyo wapakatikati wokhala ndi T1 / 2 ya maola 5.8 ndi bioavailability yabwino yapakamwa (F: 58%) [1]. Mu arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) ndi akalulu opangidwa ndi magetsi a carotid arterial thrombosis (ECAT), Apixaban amapanga antithrombotic effect ndi EC50 ya 270 nM, 110 nM ndi 70 nM motengera mlingo[3] ]. Apixaban inhibited factor Xa ntchito ndi IC50 ya 0.22 μM mu kalulu ex vivo [4]. Mu chimpanzi, Apixaban adawonetsanso kugawa pang'ono (Vdss: 0.17 L kg-1), chilolezo chochepa cha machitidwe (Cl: 0.018 L kg-1h-1), ndi bioavailability yabwino yapakamwa (F: 59%) [5].

Zolozera:
Pinto DJP, Orwat MJ, Koch S, et al. Kupezeka kwa 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), yamphamvu kwambiri, yosankha, yothandiza, komanso orally bioavailable inhibitor of blood coagulation factor Xa[J]. Journal ya chemistry yamankhwala, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors monga Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, oral, direct and selective factor Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies[J]. Journal of Thrombosis ndi Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics ndi pharmacodynamics ya factor Xa inhibitor apixaban mu akalulu[J]. Journal of thrombosis ndi thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics ndi pharmacodynamics ya apixaban, amphamvu ndi selective factor Xa inhibitor[J]. European Journal of Drug Metabolism ndi Pharmacokinetics, 2011, 36 (3): 129-139.

Apixaban ndi choletsa chosankha komanso chosinthika cha Factor Xa chokhala ndi ma Ki a 0.08 nM ndi 0.17 nM mwa munthu ndi kalulu, motsatana[1].

Factor X, yomwe imadziwikanso ndi dzina loti Stuart-Prower factor, ndi puloteni ya coagulation cascade. Factor X imayendetsedwa, ndi hydrolysis, kukhala factor Xa ndi IX factor IX. Factor Xa ndi mawonekedwe oyambitsidwa a coagulation factorthrombokinase.Inhibiting Factor Xa ikhoza kupereka njira ina ya anticoagulation. Direct Xa inhibitors ndi anticoagulants otchuka [2].

In vitro: Apixabanhas adawonetsa kuchuluka kwa potency, kusankha, komanso kuchita bwino pa Factor Xa ndi Ki ya 0.08 nM ndi 0.17 nM ya Human Factor Xa ndi Rabbit Factor Xa, motsatana [1]. Apixaban amatalikitsa nthawi yotsekeka ya plasma wamba wamunthu ndi kuchuluka (EC2x) kwa 3.6, 0.37, 7.4 ndi 0.4 μM, zomwe zimafunikira motsatana kuwirikiza nthawi ya prothrombin (PT), nthawi yosinthidwa ya prothrombin (mPT), yoyambitsa nthawi ya thromboplastin ( APTT) ndi HepTest. Kupatula apo, Apixaban adawonetsa potency yapamwamba kwambiri mu plasma ya anthu ndi akalulu, koma potency yochepa mu plasma ya makoswe ndi agalu muzoyesa za PT ndi APTT [3].

Mu vivo: Apixaban adawonetsa ma pharmacokinetics abwino kwambiri okhala ndi chilolezo chochepa kwambiri (Cl: 0.02 L kg-1h-1), komanso kugawa kochepa (Vdss: 0.2 L / kg) mwa galu. Kupatula apo, Apixaban adawonetsanso moyo wapakatikati wokhala ndi T1 / 2 ya maola 5.8 ndi bioavailability yabwino yapakamwa (F: 58%) [1]. Mu arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) ndi akalulu opangidwa ndi magetsi a carotid arterial thrombosis (ECAT), Apixaban amapanga antithrombotic effect ndi EC50 ya 270 nM, 110 nM ndi 70 nM motengera mlingo[3] ]. Apixaban inhibited factor Xa ntchito ndi IC50 ya 0.22 μM mu kalulu ex vivo [4]. Mu chimpanzi, Apixaban adawonetsanso kugawa pang'ono (Vdss: 0.17 L kg-1), chilolezo chochepa cha machitidwe (Cl: 0.018 L kg-1h-1), ndi bioavailability yabwino yapakamwa (F: 59%) [5].

Zolozera:
Pinto DJP, Orwat MJ, Koch S, et al. Kupezeka kwa 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), yamphamvu kwambiri, yosankha, yothandiza, komanso orally bioavailable inhibitor of blood coagulation factor Xa[J]. Journal ya chemistry yamankhwala, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors monga Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, oral, direct and selective factor Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies[J]. Journal of Thrombosis ndi Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics ndi pharmacodynamics ya factor Xa inhibitor apixaban mu akalulu[J]. Journal of thrombosis ndi thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics ndi pharmacodynamics ya apixaban, amphamvu ndi selective factor Xa inhibitor[J]. European Journal of Drug Metabolism ndi Pharmacokinetics, 2011, 36 (3): 129-139.

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