Talaaga

O le Apixaban o se inhibitor sili ona filifilia ma toe faʻafoʻi o Factor Xa faʻatasi ai ma Ki tau o le 0.08 nM ma le 0.17 nM i le tagata ma le lapiti, i le faasologa [1].

Factor X, e lauiloa foi i le eponym Stuart-Prower factor, o se enzyme o le coagulation cascade.O le Factor X e fa'agaoioia, e ala ile hydrolysis, ile fa'ale Xa e lua itu IX.Factor Xa o le fa'agaoioia fomu o le coagulation factorthrombokinase. Inhibiting Factor Xa e mafai ona ofoina atu se isi auala mo anticoagulation.Direct Xa iniseti o anticoagulants lauiloa [2].

In vitro: Apixabanhas na faʻaalia se maualuga maualuga o le malosi, filifilia, ma le aoga ile Factor Xa ma le Ki o le 0.08 nM ma le 0.17 nM mo le Human Factor Xa ma le Rabbit Factor Xa, faasologa [1].Apixaban na faʻaumiina taimi faʻapipiʻi o le plasma masani o le tagata ma faʻatonuga (EC2x) o le 3.6, 0.37, 7.4 ma le 0.4 μM, lea e manaʻomia taʻitasi e faʻaluaina le taimi o le prothrombin (PT), suiga o le taimi o le prothrombin (mPT), faʻagaoioia vaega o le thromboplastin taimi ( APTT) ma HepTest.E le gata i lea, na faʻaalia e Apixaban le maualuga maualuga o le plasma o le tagata ma le lapiti, ae faʻaitiitia le malosi i le plasma ma le dog plasma i le PT ma le APTT assays [3].

In vivo: Apixaban na faʻaalia le pharmacokinetics sili ona lelei ma le kilia maualalo (Cl: 0.02 L kg-1h-1), ma le maualalo o le tufatufaina (Vdss: 0.2 L / kg) i le taifau.E le gata i lea, na faʻaalia foi e Apixaban se afa-ola lelei ma le T1 / 2 o 5.8 itula ma le lelei o le bioavailability oral (F: 58%) [1].I le arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) ma faʻataʻitaʻiga lapiti carotid arterial thrombosis (ECAT), na maua ai e Apixaban aʻafiaga antithrombotic ma le EC50 o le 270 nM, 110 nM ma le 70 nM i se fua faʻalagolago [3]. ].O le Apixaban na matua faʻalavelaveina le gaioiga Xa faʻatasi ma le IC50 o le 0.22 μM i le lapiti ex vivo [4].I le chimpanzee, na faʻaalia foi e Apixaban le laʻititi o le tufatufaina atu (Vdss: 0.17 L kg-1), maualalo le kilia o le tino (Cl: 0.018 L kg-1h-1), ma le lelei o le bioavailability oral (F: 59%) [5].

Fa'asinomaga:
Pinto DJP, Orwat MJ, Koch S, ma isi.Su'esu'ega o le 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), o se mea e sili ona malosi, filifilia, aoga, ma le faʻaogaina o le faʻaogaina o le toto o le toto Xa [J].Journal of chemistry medicinal, 2007, 50(22): 5339-5356.
Sidhu P S. Fa'atonu Tu'usa'o Xa Inhibitors e fai ma Anticoagulants[J].
Wong PC, Crain EJ, Xin B, ma isi.Apixaban, o se mea tuugutu, tuusao ma sili ona filifilia mea Xa inhibitor: in vitro, antithrombotic ma antihemostaticstudies [J].Journal of Thrombosis and Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, ma isi.Metabolism, pharmacokinetics ma pharmacodynamics o le mea Xa inhibitor apixaban i lapiti [J].Journal of thrombosis and thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al.Preclinical pharmacokinetics ma pharmacodynamics o le apixaban, o se mea malosi ma filifili Xa inhibitor [J].Tusitala Europa o fualaau faasaina metabolism ma pharmacokinetics, 2011, 36(3): 129-139.

O le Apixaban o se inhibitor sili ona filifilia ma toe faʻafoʻi o Factor Xa faʻatasi ai ma Ki tau o le 0.08 nM ma le 0.17 nM i le tagata ma le lapiti, i le faasologa [1].

Factor X, e lauiloa foi i le eponym Stuart-Prower factor, o se enzyme o le coagulation cascade.O le Factor X e fa'agaoioia, e ala ile hydrolysis, ile fa'ale Xa e lua itu IX.Factor Xa o le fa'agaoioia fomu o le coagulation factorthrombokinase. Inhibiting Factor Xa e mafai ona ofoina atu se isi auala mo anticoagulation.Direct Xa iniseti o anticoagulants lauiloa [2].

In vitro: Apixabanhas na faʻaalia se maualuga maualuga o le malosi, filifilia, ma le aoga ile Factor Xa ma le Ki o le 0.08 nM ma le 0.17 nM mo le Human Factor Xa ma le Rabbit Factor Xa, faasologa [1].Apixaban na faʻaumiina taimi faʻapipiʻi o le plasma masani o le tagata ma faʻatonuga (EC2x) o le 3.6, 0.37, 7.4 ma le 0.4 μM, lea e manaʻomia taʻitasi e faʻaluaina le taimi o le prothrombin (PT), suiga o le taimi o le prothrombin (mPT), faʻagaoioia vaega o le thromboplastin taimi ( APTT) ma HepTest.E le gata i lea, na faʻaalia e Apixaban le maualuga maualuga o le plasma o le tagata ma le lapiti, ae faʻaitiitia le malosi i le plasma ma le dog plasma i le PT ma le APTT assays [3].

In vivo: Apixaban na faʻaalia le pharmacokinetics sili ona lelei ma le kilia maualalo (Cl: 0.02 L kg-1h-1), ma le maualalo o le tufatufaina (Vdss: 0.2 L / kg) i le taifau.E le gata i lea, na faʻaalia foi e Apixaban se afa-ola lelei ma le T1 / 2 o 5.8 itula ma le lelei o le bioavailability oral (F: 58%) [1].I le arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) ma faʻataʻitaʻiga lapiti carotid arterial thrombosis (ECAT), na maua ai e Apixaban aʻafiaga antithrombotic ma le EC50 o le 270 nM, 110 nM ma le 70 nM i se fua faʻalagolago [3]. ].O le Apixaban na matua faʻalavelaveina le gaioiga Xa faʻatasi ma le IC50 o le 0.22 μM i le lapiti ex vivo [4].I le chimpanzee, na faʻaalia foi e Apixaban le laʻititi o le tufatufaina atu (Vdss: 0.17 L kg-1), maualalo le kilia o le tino (Cl: 0.018 L kg-1h-1), ma le lelei o le bioavailability oral (F: 59%) [5].

Fa'asinomaga:
Pinto DJP, Orwat MJ, Koch S, ma isi.Su'esu'ega o le 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), o se mea e sili ona malosi, filifilia, aoga, ma le faʻaogaina o le faʻaogaina o le toto o le toto Xa [J].Journal of chemistry medicinal, 2007, 50(22): 5339-5356.
Sidhu P S. Fa'atonu Tu'usa'o Xa Inhibitors e fai ma Anticoagulants[J].
Wong PC, Crain EJ, Xin B, ma isi.Apixaban, o se mea tuugutu, tuusao ma sili ona filifilia mea Xa inhibitor: in vitro, antithrombotic ma antihemostaticstudies [J].Journal of Thrombosis and Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, ma isi.Metabolism, pharmacokinetics ma pharmacodynamics o le mea Xa inhibitor apixaban i lapiti [J].Journal of thrombosis and thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al.Preclinical pharmacokinetics ma pharmacodynamics o le apixaban, o se mea malosi ma filifili Xa inhibitor [J].Tusitala Europa o fualaau faasaina metabolism ma pharmacokinetics, 2011, 36(3): 129-139.

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