Talaaga

Apixaban o se inhibitor sili ona filifilia ma toe faʻafoʻiina 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 fa'ailoga IX. Factor Xa o le fa'agaioiina 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, i le faasologa [1]. Apixaban na faʻaumiina taimi faʻapipiʻi o le plasma masani o le tagata ma le 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), faʻaleleia le taimi o le prothrombin (mPT), faʻagaoioia vaega taimi thromboplastin ( APTT) ma le HepTest. E le gata i lea, o Apixaban na faʻaalia le maualuga maualuga i le plasma o le tagata ma le lapiti, ae itiiti le malosi i le plasma ma le dog plasma i le PT ma le APTT suʻega [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 feololo 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 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 faʻaogaina tautala. fa'atosina ole toto fa'ameamea Xa[J]. Journal of chemistry medicinal, 2007, 50(22): 5339-5356.
Sidhu P S. Fa'atonu Fa'atonu 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.

Apixaban o se inhibitor sili ona filifilia ma toe faʻafoʻiina 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 fa'ailoga IX. Factor Xa o le fa'agaioiina 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, i le faasologa [1]. Apixaban na faʻaumiina taimi faʻapipiʻi o le plasma masani o le tagata ma le 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), faʻaleleia le taimi o le prothrombin (mPT), faʻagaoioia vaega taimi thromboplastin ( APTT) ma le HepTest. E le gata i lea, o Apixaban na faʻaalia le maualuga maualuga i le plasma o le tagata ma le lapiti, ae itiiti le malosi i le plasma ma le dog plasma i le PT ma le APTT suʻega [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 feololo 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 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 faʻaogaina tautala. fa'atosina ole toto fa'ameamea Xa[J]. Journal of chemistry medicinal, 2007, 50(22): 5339-5356.
Sidhu P S. Fa'atonu Fa'atonu 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.

Fa'asologa o vaila'au