Amavu n'amavuko

Apixaban ni intorezo ihitamo cyane kandi ihindagurika ya Factor Xa ifite Ki agaciro ka 0.08 nM na 0.17 nM mubantu ninkwavu.

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 bukora bwa coagulation factorthrombokinase.Kubuza Factor Xa bishobora gutanga ubundi buryo bwo kurwanya anticoagulation.Inhibitori ya Xa itaziguye ni anticoagulants ikunzwe [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 Human Factor 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 zisumba izindi muri plasma yumuntu ninkwavu, ariko imbaraga nke muri plasma nimbwa mubisubizo bya PT na APTT [3].

Muri vivo: Apixaban yasohoye imiti ya farumasi nziza cyane (Cl: 0.02 L kg-1h-1), nubunini buke bwo gukwirakwiza (Vdss: 0.2 L / kg) mu mbwa.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 thrombose (AVST), trombose yo mu mitsi (VT) hamwe na karotide arterial trombose (ECAT) yerekana urukwavu, Apixaban yakoze 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 yerekanye kandi urugero ruto rwo 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, nabandi.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, kandi ikanwa na bioavailable inhibitori yibintu byamaraso 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 murukwavu [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 intorezo ihitamo cyane kandi ihindagurika ya Factor Xa ifite Ki agaciro ka 0.08 nM na 0.17 nM mubantu ninkwavu.

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 bukora bwa coagulation factorthrombokinase.Kubuza Factor Xa bishobora gutanga ubundi buryo bwo kurwanya anticoagulation.Inhibitori ya Xa itaziguye ni anticoagulants ikunzwe [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 Human Factor 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 zisumba izindi muri plasma yumuntu ninkwavu, ariko imbaraga nke muri plasma nimbwa mubisubizo bya PT na APTT [3].

Muri vivo: Apixaban yasohoye imiti ya farumasi nziza cyane (Cl: 0.02 L kg-1h-1), nubunini buke bwo gukwirakwiza (Vdss: 0.2 L / kg) mu mbwa.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 thrombose (AVST), trombose yo mu mitsi (VT) hamwe na karotide arterial trombose (ECAT) yerekana urukwavu, Apixaban yakoze 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 yerekanye kandi urugero ruto rwo 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, nabandi.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, kandi ikanwa na bioavailable inhibitori yibintu byamaraso 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 murukwavu [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.

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