Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors

Pontus B Persson Institute of Vegetative Physiology, Berlin, GermanyApixaban and rivaroxaban are oral factor Xa inhibitors. In a recent issue of Clinical Pharmacology: Advances and Applications, Frost et al compare apixaban (2.5 mg, twice daily) to rivaroxaban (10 mg, once daily) with regard to thei...

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Autor principal:	Persson PB
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/7fb12ddd872743268a0c49ac5aabbd12
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spelling	oai:doaj.org-article:7fb12ddd872743268a0c49ac5aabbd122021-12-02T06:11:24ZPharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors1179-1438https://doaj.org/article/7fb12ddd872743268a0c49ac5aabbd122015-05-01T00:00:00Zhttp://www.dovepress.com/pharmacodynamics-and-pharmacokinetics-of-oral-factor-xa-inhibitors-peer-reviewed-article-CPAAhttps://doaj.org/toc/1179-1438Pontus B Persson Institute of Vegetative Physiology, Berlin, GermanyApixaban and rivaroxaban are oral factor Xa inhibitors. In a recent issue of Clinical Pharmacology: Advances and Applications, Frost et al compare apixaban (2.5 mg, twice daily) to rivaroxaban (10 mg, once daily) with regard to their pharmacokinetics and pharmacodynamics.1 Both oral factor Xa inhibitors have similar half-lives. Moreover, as may seem intuitive, the twice daily regime of apixaban revealed a less pronounced peak-to-trough plasma concentration ratio than rivaroxaban which is given once daily. The latter finding lead the authors to suggest a more constant anticoagulant effect of twice-daily apixaban, when compared to the once daily dose of rivaroxaban.Suggesting more constant anticoagulation by the twice-daily apixaban regimen is premature due to the author’s disregard of a crucial pharmacokinetic feature: drug accumulation. Apixaban may have accumulated during the twice-daily regimen, as indicated by the increasing trough values (see values for 12h and 24h in Figure 2 of that study). That Figure claims to show data at steady state, however, trough values rise, indicating drug accumulation after a time period, when a steady state is usually reached (5 half-lives). Uncontrolled accumulation cannot be ruled out.View original paper by Frost and colleagues.Persson PBDove Medical PressarticleTherapeutics. PharmacologyRM1-950ENClinical Pharmacology: Advances and Applications, Vol 2015, Iss default, Pp 77-78 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Therapeutics. Pharmacology RM1-950
spellingShingle	Therapeutics. Pharmacology RM1-950 Persson PB Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors
description	Pontus B Persson Institute of Vegetative Physiology, Berlin, GermanyApixaban and rivaroxaban are oral factor Xa inhibitors. In a recent issue of Clinical Pharmacology: Advances and Applications, Frost et al compare apixaban (2.5 mg, twice daily) to rivaroxaban (10 mg, once daily) with regard to their pharmacokinetics and pharmacodynamics.1 Both oral factor Xa inhibitors have similar half-lives. Moreover, as may seem intuitive, the twice daily regime of apixaban revealed a less pronounced peak-to-trough plasma concentration ratio than rivaroxaban which is given once daily. The latter finding lead the authors to suggest a more constant anticoagulant effect of twice-daily apixaban, when compared to the once daily dose of rivaroxaban.Suggesting more constant anticoagulation by the twice-daily apixaban regimen is premature due to the author’s disregard of a crucial pharmacokinetic feature: drug accumulation. Apixaban may have accumulated during the twice-daily regimen, as indicated by the increasing trough values (see values for 12h and 24h in Figure 2 of that study). That Figure claims to show data at steady state, however, trough values rise, indicating drug accumulation after a time period, when a steady state is usually reached (5 half-lives). Uncontrolled accumulation cannot be ruled out.View original paper by Frost and colleagues.
format	article
author	Persson PB
author_facet	Persson PB
author_sort	Persson PB
title	Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors
title_short	Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors
title_full	Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors
title_fullStr	Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors
title_full_unstemmed	Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors
title_sort	pharmacodynamics and pharmacokinetics of oral factor xa inhibitors
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/7fb12ddd872743268a0c49ac5aabbd12
work_keys_str_mv	AT perssonpb pharmacodynamicsandpharmacokineticsoforalfactorxainhibitors
_version_	1718400060318810112

Pharmacodynamics and Pharmacokinetics of oral factor Xa inhibitors

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