Papamuri

Ko te Apixaban he tino whiriwhiri me te aukati i te Factor Xa me nga uara Ki o 0.08 nM me te 0.17 nM i roto i te tangata me te rapeti, ia [1].

Ko te Factor X, e mohiotia ana e te eponym Stuart–Prower factor, he whākōkī o te rourou coagulation. Ka whakahohehia te Tauwehe X, ma te waiwai, hei tauwehe Xa ma te tauwehe IX e rua. Ko te Factor Xa te ahua whakahohe o te coagulation factorthrombokinase.Inhibiting Factor Xa ka taea te tuku i tetahi tikanga rereke mo te anticoagulation. Ko nga aukati Xa Direct he anticoagulants rongonui [2].

In vitro: I whakaatu a Apixabanhas i te kaha o te kaha, te whiriwhiringa, me te kaha ki runga i te Factor Xa me te Ki o 0.08 nM me te 0.17 nM mo te Human Factor Xa me te Rabbit Factor Xa, ia [1]. I whakaroahia e Apixaban nga wa o te toto o te plasma tangata noa me nga kukū (EC2x) o 3.6, 0.37, 7.4 me 0.4 μM, e hiahiatia ana kia rua te wa prothrombin (PT), te wa prothrombin whakarereke (mPT), te wa thromboplastin wahanga ( APTT) me te HepTest. I tua atu, i whakaatuhia e Apixaban te kaha teitei o te plasma tangata me te rapeti, engari he iti ake te kaha o te kiore me te plasma kuri i roto i nga whakamatautau PT me te APTT [3].

I roto i te vivo: I whakaatuhia e Apixaban nga rongoa rongoa pai me te iti rawa o te waatea (Cl: 0.02 L kg-1h-1), me te iti o te tohatoha (Vdss: 0.2 L/kg) i roto i te kuri. I tua atu, i whakaatu ano a Apixaban i te haurua o te ora me te T1 / 2 o nga haora 5.8 me te pai o te koiora-waha (F: 58%) [1]. I roto i te arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) me te hiko takawaenga carotid arterial thrombosis (ECAT) tauira rapeti, i hangaia e Apixaban nga paanga antithrombotic me te EC50 o 270 nM, 110 nM me te 70 nM i roto i te tikanga o te horopeta [3]. ]. I tino whakakorehia e Apixaban nga mahi tauwehe Xa me te IC50 o 0.22 μM i roto i te rapeti ex vivo [4]. I roto i te chimpanzee, i whakaatu ano a Apixaban i te iti o te tohatoha o te tohatoha (Vdss: 0.17 L kg-1), te iti o te waatea o te punaha (Cl: 0.018 L kg-1h-1), me te pai o te koiora waha (F: 59%) [5].

Tohutoro:
Pinto DJP, Orwat MJ, Koch S, et al. Te kitenga o te 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), he tino kaha, he kowhiri, he whai hua, he waatea ki te waha. te aukati o te tauwehe toto coagulation Xa[J]. Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
Sidhu PS. Tikanga Tikanga Xa Inhibitors hei Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Ko te Apixaban, he aukati Xa-waha, tika me te tino whiriwhiri: in vitro, antithrombotic me te antihemostaticstudies[J]. Journal of Thrombosis and Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics me pharmacodynamics o te tauwehe Xa inhibitor apixaban i roto i te rapeti [J]. Journal of thrombosis and thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. pharmacokinetics preclinical me te pharmacodynamics o te apixaban, he mea kaha me te whiriwhiri i te aukati Xa [J]. Te hautaka a te Pakeha mo te rongoa rongoa me te rongoa rongoa, 2011, 36 (3): 129-139.

Ko te Apixaban he tino whiriwhiri me te aukati i te Factor Xa me nga uara Ki o 0.08 nM me te 0.17 nM i roto i te tangata me te rapeti, ia [1].

Ko te Factor X, e mohiotia ana e te eponym Stuart–Prower factor, he whākōkī o te rourou coagulation. Ka whakahohehia te Tauwehe X, ma te waiwai, hei tauwehe Xa ma te tauwehe IX e rua. Ko te Factor Xa te ahua whakahohe o te coagulation factorthrombokinase.Inhibiting Factor Xa ka taea te tuku i tetahi tikanga rereke mo te anticoagulation. Ko nga aukati Xa Direct he anticoagulants rongonui [2].

In vitro: I whakaatu a Apixabanhas i te kaha o te kaha, te whiriwhiringa, me te kaha ki runga i te Factor Xa me te Ki o 0.08 nM me te 0.17 nM mo te Human Factor Xa me te Rabbit Factor Xa, ia [1]. I whakaroahia e Apixaban nga wa o te toto o te plasma tangata noa me nga kukū (EC2x) o 3.6, 0.37, 7.4 me 0.4 μM, e hiahiatia ana kia rua te wa prothrombin (PT), te wa prothrombin whakarereke (mPT), te wa thromboplastin wahanga ( APTT) me te HepTest. I tua atu, i whakaatuhia e Apixaban te kaha teitei o te plasma tangata me te rapeti, engari he iti ake te kaha o te kiore me te plasma kuri i roto i nga whakamatautau PT me te APTT [3].

I roto i te vivo: I whakaatuhia e Apixaban nga rongoa rongoa pai me te iti rawa o te waatea (Cl: 0.02 L kg-1h-1), me te iti o te tohatoha (Vdss: 0.2 L/kg) i roto i te kuri. I tua atu, i whakaatu ano a Apixaban i te haurua o te ora me te T1 / 2 o nga haora 5.8 me te pai o te koiora-waha (F: 58%) [1]. I roto i te arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) me te hiko takawaenga carotid arterial thrombosis (ECAT) tauira rapeti, i hangaia e Apixaban nga paanga antithrombotic me te EC50 o 270 nM, 110 nM me te 70 nM i roto i te tikanga o te horopeta [3]. ]. I tino whakakorehia e Apixaban nga mahi tauwehe Xa me te IC50 o 0.22 μM i roto i te rapeti ex vivo [4]. I roto i te chimpanzee, i whakaatu ano a Apixaban i te iti o te tohatoha o te tohatoha (Vdss: 0.17 L kg-1), te iti o te waatea o te punaha (Cl: 0.018 L kg-1h-1), me te pai o te koiora waha (F: 59%) [5].

Tohutoro:
Pinto DJP, Orwat MJ, Koch S, et al. Te kitenga o te 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), he tino kaha, he kowhiri, he whai hua, he waatea ki te waha. te aukati o te tauwehe toto coagulation Xa[J]. Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
Sidhu PS. Tikanga Tikanga Xa Inhibitors hei Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Ko te Apixaban, he aukati Xa-waha, tika me te tino whiriwhiri: in vitro, antithrombotic me te antihemostaticstudies[J]. Journal of Thrombosis and Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics me pharmacodynamics o te tauwehe Xa inhibitor apixaban i roto i te rapeti [J]. Journal of thrombosis and thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. pharmacokinetics preclinical me te pharmacodynamics o te apixaban, he mea kaha me te whiriwhiri i te aukati Xa [J]. Te hautaka a te Pakeha mo te rongoa rongoa me te rongoa rongoa, 2011, 36 (3): 129-139.

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