Amavu n'amavuko

Apixaban ni intore ihitamo cyane kandi ihindagurika ya Factor Xa ifite agaciro ka Ki 0,08 nM na 0.17 nM mubantu ninkwavu [1].

Factor X, izwi kandi ku izina rya Stuart - Prower factor, ni enzyme ya coagulation cascade. Factor X ikora, na hydrolysis, mubintu Xa kubintu byombi IX. Factor Xa nuburyo bukoreshwa bwa coagulation factorthrombokinase. Kubuza Factor Xa bishobora gutanga ubundi buryo bwo kurwanya anticoagulation. Inhibitori ya Xa itaziguye ni imiti igabanya ubukana [2].

Muri vitro: Apixabanhas yerekanye imbaraga nyinshi, guhitamo, no gukora neza kuri Factor Xa hamwe na Ki ya 0.08 nM na 0.17 nM kuri Factor Human Xa na Factor Xa, [1]. Apixaban yongereye igihe cyo kwambara cya plasma isanzwe yumuntu hamwe nibitekerezo (EC2x) bya 3.6, 0.37, 7.4 na 0.4 μM, bisabwa kugirango bikubye kabiri prothrombine (PT), byahinduwe na prothrombine (mPT), bikora tromboplastine igice ( APTT) na HepTest. Byongeye kandi, Apixaban yerekanye imbaraga nyinshi muri plasma yumuntu ninkwavu, ariko imbaraga nke muri plasma yimbeba nimbwa mubisobanuro bya PT na APTT [3].

Muri vivo. Uretse ibyo, Apixaban yerekanye kandi ubuzima buciriritse hamwe na T1 / 2 byamasaha 5.8 hamwe na bioavailable yo mu kanwa (F: 58%) [1]. Muri arteriovenous-shunt trombose (AVST), trombose de vine (VT) hamwe na karotide arterial trombose (ECAT) yerekana urukwavu, Apixaban yatanze ingaruka za antithrombotic hamwe na EC50 ya 270 nM, 110 nM na 70 nM muburyo buterwa na dose. ]. Apixaban yabujije cyane ibikorwa Xa hamwe na IC50 ya 0.22 μM muri urukwavu ex vivo [4]. Muri chimpanzee, Apixaban yerekanaga kandi ingano yo gukwirakwiza (Vdss: 0.17 L kg-1), sisitemu yo hasi (Cl: 0.018 L kg-1h-1), hamwe na bioavailable yo mu kanwa (F: 59%) [5].

Reba:
Pinto DJP, Orwat MJ, Koch S, n'abandi. Ivumburwa rya 1- (4-mikorerexyphenyl) -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), ikomeye cyane, ihitamo, ikora neza, hamwe na bioavailable inhibitor y'amaraso agabanuka Xa [J]. Ikinyamakuru cya chimie chimique, 2007, 50 (22): 5339-5356.
Sidhu P S. Ibintu bitaziguye Xa Inhibitori nka Anticoagulants [J].
Wong PC, Crain EJ, Xin B, nibindi. Apixaban, umunwa, utaziguye kandi uhitamo cyane Xa inhibitor: muri vitro, antithrombotic na antihemostaticstudies [J]. Ikinyamakuru cya Thrombose na Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, n'abandi. Metabolism, pharmacokinetics na pharmacodynamics yibintu Xa inhibitor apixaban mu nkwavu [J]. Ikinyamakuru cya trombose na trombolysis, 2010, 29 (1): 70-80.
We K, Luettgen JM, Zhang D, n'abandi. Preclinical pharmacokinetics na pharmacodynamics ya apixaban, ikintu gikomeye kandi gitoranya Xa inhibitor [J]. Ikinyamakuru cyo mu Burayi cy’ibiyobyabwenge na farumasi, 2011, 36 (3): 129-139.

Apixaban ni intore ihitamo cyane kandi ihindagurika ya Factor Xa ifite agaciro ka Ki 0,08 nM na 0.17 nM mubantu ninkwavu [1].

Factor X, izwi kandi ku izina rya Stuart - Prower factor, ni enzyme ya coagulation cascade. Factor X ikora, na hydrolysis, mubintu Xa kubintu byombi IX. Factor Xa nuburyo bukoreshwa bwa coagulation factorthrombokinase. Kubuza Factor Xa bishobora gutanga ubundi buryo bwo kurwanya anticoagulation. Inhibitori ya Xa itaziguye ni imiti igabanya ubukana [2].

Muri vitro: Apixabanhas yerekanye imbaraga nyinshi, guhitamo, no gukora neza kuri Factor Xa hamwe na Ki ya 0.08 nM na 0.17 nM kuri Factor Human Xa na Factor Xa, [1]. Apixaban yongereye igihe cyo kwambara cya plasma isanzwe yumuntu hamwe nibitekerezo (EC2x) bya 3.6, 0.37, 7.4 na 0.4 μM, bisabwa kugirango bikubye kabiri prothrombine (PT), byahinduwe na prothrombine (mPT), bikora tromboplastine igice ( APTT) na HepTest. Byongeye kandi, Apixaban yerekanye imbaraga nyinshi muri plasma yumuntu ninkwavu, ariko imbaraga nke muri plasma yimbeba nimbwa mubisobanuro bya PT na APTT [3].

Muri vivo. Uretse ibyo, Apixaban yerekanye kandi ubuzima buciriritse hamwe na T1 / 2 byamasaha 5.8 hamwe na bioavailable yo mu kanwa (F: 58%) [1]. Muri arteriovenous-shunt trombose (AVST), trombose de vine (VT) hamwe na karotide arterial trombose (ECAT) yerekana urukwavu, Apixaban yatanze ingaruka za antithrombotic hamwe na EC50 ya 270 nM, 110 nM na 70 nM muburyo buterwa na dose. ]. Apixaban yabujije cyane ibikorwa Xa hamwe na IC50 ya 0.22 μM muri urukwavu ex vivo [4]. Muri chimpanzee, Apixaban yerekanaga kandi ingano yo gukwirakwiza (Vdss: 0.17 L kg-1), sisitemu yo hasi (Cl: 0.018 L kg-1h-1), hamwe na bioavailable yo mu kanwa (F: 59%) [5].

Reba:
Pinto DJP, Orwat MJ, Koch S, n'abandi. Ivumburwa rya 1- (4-mikorerexyphenyl) -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), ikomeye cyane, ihitamo, ikora neza, hamwe na bioavailable inhibitor y'amaraso agabanuka Xa [J]. Ikinyamakuru cya chimie chimique, 2007, 50 (22): 5339-5356.
Sidhu P S. Ibintu bitaziguye Xa Inhibitori nka Anticoagulants [J].
Wong PC, Crain EJ, Xin B, nibindi. Apixaban, umunwa, utaziguye kandi uhitamo cyane Xa inhibitor: muri vitro, antithrombotic na antihemostaticstudies [J]. Ikinyamakuru cya Thrombose na Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, n'abandi. Metabolism, pharmacokinetics na pharmacodynamics yibintu Xa inhibitor apixaban mu nkwavu [J]. Ikinyamakuru cya trombose na trombolysis, 2010, 29 (1): 70-80.
We K, Luettgen JM, Zhang D, n'abandi. Preclinical pharmacokinetics na pharmacodynamics ya apixaban, ikintu gikomeye kandi gitoranya Xa inhibitor [J]. Ikinyamakuru cyo mu Burayi cy’ibiyobyabwenge na farumasi, 2011, 36 (3): 129-139.

Imiterere yimiti