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I-Apixaban iyi-inhibitor ekhetha kakhulu futhi ebuyiseleka emuva ye-Factor Xa enamanani e-Ki angu-0.08 nM no-0.17 nM kumuntu nonogwaja, ngokulandelanayo[1].

I-Factor X, eyaziwa nangokuthi i-Stuart-Prower factor, iyi-enzyme ye-coagulation cascade.I-Factor X icushiwe, nge-hydrolysis, ibe yi-factor Xa ngazo zombili i-factor IX.I-Factor Xa iwuhlobo olucushiwe lwe-coagulation factorthrombokinase.I-Inhibiting Factor Xa ingase inikeze enye indlela yokunqanda ukuphuma kwegazi.Ama-Direct Xa inhibitors ama-anticoagulant adumile [2].

I-In vitro: I-Apixabanhas ibonise izinga eliphezulu lamandla, ukukhetha, kanye nempumelelo ku-Factor Xa ene-Ki ye-0.08 nM kanye ne-0.17 nM ye-Human Factor Xa kanye ne-Rabbit Factor Xa, ngokulandelana [1].I-Apixaban yandisa izikhathi zokujiya kwe-plasma yomuntu evamile ngokugxila (EC2x) kwe-3.6, 0.37, 7.4 kanye no-0.4 μM, okudingekayo ngokulandelana ukuze kuphindwe kabili isikhathi se-prothrombin (PT), isikhathi se-prothrombin esilungisiwe (mPT), isikhathi esicushiwe se-thromboplastin esiyingxenye ( APTT) kanye ne-HepTest.Ngaphandle kwalokho, i-Apixaban ibonise amandla aphezulu kakhulu ku-plasma yomuntu neyogwaja, kodwa amandla amancane ku-plasma yamagundane nenja kuzo zombili izivivinyo ze-PT ne-APTT [3].

Ku-vivo: I-Apixaban ibonise i-pharmacokinetics enhle kakhulu enemvume ephansi kakhulu (Cl: 0.02 L kg-1h-1), kanye nevolumu ephansi yokusabalalisa (Vdss: 0.2 L/kg) enja.Ngaphandle kwalokho, i-Apixaban iphinde yabonisa isigamu sempilo emaphakathi ne-T1/2 yamahora we-5.8 kanye ne-bioavailability yomlomo omuhle (F: 58%) [1].Ku-arteriovenous-shunt thrombosis (AVST), i-venous thrombosis (VT) kanye namamodeli anogwaja we-carotid arterial thrombosis (ECAT), i-Apixaban ikhiqize imiphumela ye-antithrombotic nge-EC50 ye-270 nM, 110 nM kanye ne-70 nM ngendlela encike kumthamo[3 ].I-Apixaban ivimbele kakhulu umsebenzi we-factor Xa nge-IC50 ye-0.22 μM ku-rabbit ex vivo[4].Ku-chimpanzee, i-Apixaban iphinde yabonisa umthamo omncane wokusabalalisa (Vdss: 0.17 L kg-1), imvume ephansi ye-systemic (Cl: 0.018 L kg-1h-1), kanye ne-bioavailability yomlomo omuhle (F: 59%) [5].

Izithenjwa:
Pinto DJP, Orwat MJ, Koch S, et al.Ukutholwa 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), inhibitor enamandla kakhulu, ekhethayo, esebenzayo, kanye ne-oral bioavailable inhibitor ye-blood coagulation factor Xa[J].Ijenali yekhemikhali yezokwelapha, 2007, 50 (22): 5339-5356.
I-Sidhu P S. I-Direct Factor Xa Inhibitors njengama-Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al.I-Apixaban, i-oral, eqondile futhi ekhetha kakhulu factor Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies[J].Ijenali ye-Thrombosis kanye ne-Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al.I-Metabolism, i-pharmacokinetics kanye ne-pharmacodynamics ye-factor Xa inhibitor apixaban konogwaja[J].Ijenali ye-thrombosis kanye ne-thrombolysis, 2010, 29(1): 70-80.
He K, Luettgen JM, Zhang D, et al.I-preclinical pharmacokinetics kanye ne-pharmacodynamics ye-apixaban, into enamandla futhi ekhethiwe ye-Xa inhibitor[J].Ijenali yaseYurophu yezidakamizwa ze-metabolism kanye ne-pharmacokinetics, 2011, 36 (3): 129-139.

I-Apixaban iyi-inhibitor ekhetha kakhulu futhi ebuyiseleka emuva ye-Factor Xa enamanani e-Ki angu-0.08 nM no-0.17 nM kumuntu nonogwaja, ngokulandelanayo[1].

I-Factor X, eyaziwa nangokuthi i-Stuart-Prower factor, iyi-enzyme ye-coagulation cascade.I-Factor X icushiwe, nge-hydrolysis, ibe yi-factor Xa ngazo zombili i-factor IX.I-Factor Xa iwuhlobo olucushiwe lwe-coagulation factorthrombokinase.I-Inhibiting Factor Xa ingase inikeze enye indlela yokunqanda ukuphuma kwegazi.Ama-Direct Xa inhibitors ama-anticoagulant adumile [2].

I-In vitro: I-Apixabanhas ibonise izinga eliphezulu lamandla, ukukhetha, kanye nempumelelo ku-Factor Xa ene-Ki ye-0.08 nM kanye ne-0.17 nM ye-Human Factor Xa kanye ne-Rabbit Factor Xa, ngokulandelana [1].I-Apixaban yandisa izikhathi zokujiya kwe-plasma yomuntu evamile ngokugxila (EC2x) kwe-3.6, 0.37, 7.4 kanye no-0.4 μM, okudingekayo ngokulandelana ukuze kuphindwe kabili isikhathi se-prothrombin (PT), isikhathi se-prothrombin esilungisiwe (mPT), isikhathi esicushiwe se-thromboplastin esiyingxenye ( APTT) kanye ne-HepTest.Ngaphandle kwalokho, i-Apixaban ibonise amandla aphezulu kakhulu ku-plasma yomuntu neyogwaja, kodwa amandla amancane ku-plasma yamagundane nenja kuzo zombili izivivinyo ze-PT ne-APTT [3].

Ku-vivo: I-Apixaban ibonise i-pharmacokinetics enhle kakhulu enemvume ephansi kakhulu (Cl: 0.02 L kg-1h-1), kanye nevolumu ephansi yokusabalalisa (Vdss: 0.2 L/kg) enja.Ngaphandle kwalokho, i-Apixaban iphinde yabonisa isigamu sempilo emaphakathi ne-T1/2 yamahora we-5.8 kanye ne-bioavailability yomlomo omuhle (F: 58%) [1].Ku-arteriovenous-shunt thrombosis (AVST), i-venous thrombosis (VT) kanye namamodeli anogwaja we-carotid arterial thrombosis (ECAT), i-Apixaban ikhiqize imiphumela ye-antithrombotic nge-EC50 ye-270 nM, 110 nM kanye ne-70 nM ngendlela encike kumthamo[3 ].I-Apixaban ivimbele kakhulu umsebenzi we-factor Xa nge-IC50 ye-0.22 μM ku-rabbit ex vivo[4].Ku-chimpanzee, i-Apixaban iphinde yabonisa umthamo omncane wokusabalalisa (Vdss: 0.17 L kg-1), imvume ephansi ye-systemic (Cl: 0.018 L kg-1h-1), kanye ne-bioavailability yomlomo omuhle (F: 59%) [5].

Izithenjwa:
Pinto DJP, Orwat MJ, Koch S, et al.Ukutholwa 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), inhibitor enamandla kakhulu, ekhethayo, esebenzayo, kanye ne-oral bioavailable inhibitor ye-blood coagulation factor Xa[J].Ijenali yekhemikhali yezokwelapha, 2007, 50 (22): 5339-5356.
I-Sidhu P S. I-Direct Factor Xa Inhibitors njengama-Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al.I-Apixaban, i-oral, eqondile futhi ekhetha kakhulu factor Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies[J].Ijenali ye-Thrombosis kanye ne-Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al.I-Metabolism, i-pharmacokinetics kanye ne-pharmacodynamics ye-factor Xa inhibitor apixaban konogwaja[J].Ijenali ye-thrombosis kanye ne-thrombolysis, 2010, 29(1): 70-80.
He K, Luettgen JM, Zhang D, et al.I-preclinical pharmacokinetics kanye ne-pharmacodynamics ye-apixaban, into enamandla futhi ekhethiwe ye-Xa inhibitor[J].Ijenali yaseYurophu yezidakamizwa ze-metabolism kanye ne-pharmacokinetics, 2011, 36 (3): 129-139.

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