Imvelaphi

I-Apixaban yi-inhibitor ekhethiweyo kunye ne-reversible inhibitor ye-Factor Xa enexabiso le-Ki ye-0.08 nM kunye ne-0.17 nM kumntu kunye nomvundla, ngokulandelanayo[1].

I-Factor X, ekwabizwa ngegama elithi Stuart-Prower factor, yi-enzyme ye-coagulation cascade. I-Factor X iyasebenza, nge-hydrolysis, ibe yi-factor Xa zombini i-IX. I-Factor Xa yindlela esebenzayo ye-coagulation factorthrombokinase.I-Inhibiting Factor Xa inokunika enye indlela yokulwa ne-anticoagulation. Direct Xa inhibitors zithandwa anticoagulants [2].

I-In vitro: I-Apixabanhas ibonise iqondo eliphezulu lamandla, ukukhetha, kunye nokusebenza kakuhle kwi-Factor Xa kunye ne-Ki ye-0.08 nM kunye ne-0.17 nM ye-Human Factor Xa kunye ne-Rabbit Factor Xa, ngokulandelanayo [1]. I-Apixaban yandisa amaxesha okujika kwe-plasma yomntu eqhelekileyo kunye nokugxininiswa (EC2x) ye-3.6, 0.37, 7.4 kunye ne-0.4 μM, efunekayo ngokulandelanayo ukuphindaphinda ixesha le-prothrombin (PT), ixesha le-prothrombin elilungisiweyo (mPT), i-activated partial thromboplastin time ( APTT) kunye neHepTest. Ngaphandle koko, i-Apixaban ibonise amandla aphezulu kwi-plasma yabantu kunye nomvundla, kodwa amandla amancinci kwi-rat kunye ne-dog plasma kuzo zombini ii-PT kunye ne-APTT assays [3].

Kwi-vivo: I-Apixaban ibonise i-pharmacokinetics egqwesileyo enemvume ephantsi kakhulu (Cl: 0.02 L kg-1h-1), kunye nomthamo ophantsi wokusabalalisa (Vdss: 0.2 L / kg) kwinja. Ngaphandle koko, i-Apixaban iphinde ibonise i-half-life half-life kunye ne-T1 / 2 yeeyure ze-5.8 kunye ne-bioavailability yomlomo omhle (F: 58%) [1]. Kwi-arteriovenous-shunt thrombosis (AVST), i-venous thrombosis (VT) kunye ne-carotid arterial thrombosis (ECAT) imodeli yomvundla, i-Apixaban ivelise iziphumo ze-antithrombotic kunye ne-EC50 ye-270 nM, i-110 nM kunye ne-70 nM ngendlela exhomekeke kwi-dose [3]. ]. I-Apixaban inhibited kakhulu xa umsebenzi nge-IC50 ye-0.22 μM kumvundla ex vivo[4]. Kwi-chimpanzee, i-Apixaban nayo yabonisa umthamo omncinci wokusabalalisa (Vdss: 0.17 L kg-1), imvume ephantsi yenkqubo (Cl: 0.018 L kg-1h-1), kunye ne-bioavailability yomlomo omhle (F: 59%) [5].

IiReferensi:
Pinto DJP, Orwat MJ, Koch S, et al. Ukufunyanwa kwe-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), inamandla kakhulu, ikhetha, iyasebenza, kwaye ngomlomo bioavailable inhibitor of blood coagulation factor Xa[J]. Ijenali yekhemistri yonyango, i-2007, i-50 (22): 5339-5356.
Sidhu P S. Factor Direct Xa Inhibitors njenge Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. I-Apixaban, i-oral, ngokuthe ngqo kunye ne-high selective factor Xa inhibitor: in vitro, antithrombotic kunye ne-antihemostaticstudies[J]. Ijenali ye-Thrombosis kunye ne-Haemostasis, i-2008, i-6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. I-Metabolism, i-pharmacokinetics kunye ne-pharmacodynamics ye-factor Xa inhibitor apixaban kwimivundla[J]. Ijenali ye-thrombosis kunye ne-thrombolysis, i-2010, i-29 (1): 70-80.
Yena K, uLuettgen JM, uZhang D, et al. I-pharmacokinetics ye-preclinical kunye ne-pharmacodynamics ye-apixaban, into enamandla kunye nekhethiweyo ye-Xa inhibitor[J]. Ijenali yaseYurophu ye-metabolism yeziyobisi kunye ne-pharmacokinetics, i-2011, i-36 (3): 129-139.

I-Apixaban yi-inhibitor ekhethiweyo kunye ne-reversible inhibitor ye-Factor Xa enexabiso le-Ki ye-0.08 nM kunye ne-0.17 nM kumntu kunye nomvundla, ngokulandelanayo[1].

I-Factor X, ekwabizwa ngegama elithi Stuart-Prower factor, yi-enzyme ye-coagulation cascade. I-Factor X iyasebenza, nge-hydrolysis, ibe yi-factor Xa zombini i-IX. I-Factor Xa yindlela esebenzayo ye-coagulation factorthrombokinase.I-Inhibiting Factor Xa inokunika enye indlela yokulwa ne-anticoagulation. Direct Xa inhibitors zithandwa anticoagulants [2].

I-In vitro: I-Apixabanhas ibonise iqondo eliphezulu lamandla, ukukhetha, kunye nokusebenza kakuhle kwi-Factor Xa kunye ne-Ki ye-0.08 nM kunye ne-0.17 nM ye-Human Factor Xa kunye ne-Rabbit Factor Xa, ngokulandelanayo [1]. I-Apixaban yandisa amaxesha okujika kwe-plasma yomntu eqhelekileyo kunye nokugxininiswa (EC2x) ye-3.6, 0.37, 7.4 kunye ne-0.4 μM, efunekayo ngokulandelanayo ukuphindaphinda ixesha le-prothrombin (PT), ixesha le-prothrombin elilungisiweyo (mPT), i-activated partial thromboplastin time ( APTT) kunye neHepTest. Ngaphandle koko, i-Apixaban ibonise amandla aphezulu kwi-plasma yabantu kunye nomvundla, kodwa amandla amancinci kwi-rat kunye ne-dog plasma kuzo zombini ii-PT kunye ne-APTT assays [3].

Kwi-vivo: I-Apixaban ibonise i-pharmacokinetics egqwesileyo enemvume ephantsi kakhulu (Cl: 0.02 L kg-1h-1), kunye nomthamo ophantsi wokusabalalisa (Vdss: 0.2 L / kg) kwinja. Ngaphandle koko, i-Apixaban iphinde ibonise i-half-life half-life kunye ne-T1 / 2 yeeyure ze-5.8 kunye ne-bioavailability yomlomo omhle (F: 58%) [1]. Kwi-arteriovenous-shunt thrombosis (AVST), i-venous thrombosis (VT) kunye ne-carotid arterial thrombosis (ECAT) imodeli yomvundla, i-Apixaban ivelise iziphumo ze-antithrombotic kunye ne-EC50 ye-270 nM, i-110 nM kunye ne-70 nM ngendlela exhomekeke kwi-dose [3]. ]. I-Apixaban inhibited kakhulu xa umsebenzi nge-IC50 ye-0.22 μM kumvundla ex vivo[4]. Kwi-chimpanzee, i-Apixaban nayo yabonisa umthamo omncinci wokusabalalisa (Vdss: 0.17 L kg-1), imvume ephantsi yenkqubo (Cl: 0.018 L kg-1h-1), kunye ne-bioavailability yomlomo omhle (F: 59%) [5].

IiReferensi:
Pinto DJP, Orwat MJ, Koch S, et al. Ukufunyanwa kwe-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), inamandla kakhulu, ikhetha, iyasebenza, kwaye ngomlomo bioavailable inhibitor of blood coagulation factor Xa[J]. Ijenali yekhemistri yonyango, i-2007, i-50 (22): 5339-5356.
Sidhu P S. Factor Direct Xa Inhibitors njenge Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. I-Apixaban, i-oral, ngokuthe ngqo kunye ne-high selective factor Xa inhibitor: in vitro, antithrombotic kunye ne-antihemostaticstudies[J]. Ijenali ye-Thrombosis kunye ne-Haemostasis, i-2008, i-6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. I-Metabolism, i-pharmacokinetics kunye ne-pharmacodynamics ye-factor Xa inhibitor apixaban kwimivundla[J]. Ijenali ye-thrombosis kunye ne-thrombolysis, i-2010, i-29 (1): 70-80.
Yena K, uLuettgen JM, uZhang D, et al. I-pharmacokinetics ye-preclinical kunye ne-pharmacodynamics ye-apixaban, into enamandla kunye nekhethiweyo ye-Xa inhibitor[J]. Ijenali yaseYurophu ye-metabolism yeziyobisi kunye ne-pharmacokinetics, i-2011, i-36 (3): 129-139.

Ubume beMichiza