Effect of Activated Charcoal on Apixaban Pharmacokinetics in Healthy Subjects.

Autor:	Wang, Xiaoli, Mondal, Sabiha, Wang, Jessie, Tirucherai, Giridhar, Zhang, Donglu, Boyd, Rebecca, Frost, Charles
Předmět:	FIBRINOLYTIC agents CHARCOAL CONFIDENCE intervals CROSSOVER trials DRUG side effects MATHEMATICAL statistics REGRESSION analysis RESEARCH funding PARAMETERS (Statistics) REPEATED measures design DATA analysis software DESCRIPTIVE statistics
Zdroj:	American Journal of Cardiovascular Drugs; Apr2014, Vol. 14 Issue 2, p147-154, 8p, 2 Charts, 1 Graph
Abstrakt:	Background: Activated charcoal is commonly used to manage overdose or accidental ingestion of medicines. This study evaluated the effect of activated charcoal on apixaban exposure in human subjects. Methods: This was an open-label, three-treatment, three-period, randomized, crossover study of single-dose apixaban (20 mg) administered alone and with activated charcoal given at 2 or 6 h post-dose to healthy subjects. Blood samples for assay of plasma apixaban concentration were collected up to 72 h post-dose. Pharmacokinetic parameters, including peak plasma concentration ( C), time to C ( T), area under the concentration-time curve from time 0 to infinity (AUC), and terminal half-life ( T), were derived from apixaban plasma concentration-time data. A general linear mixed-effect model analysis of C and AUC was performed to estimate the effect of activated charcoal on apixaban exposure. Results: A total of 18 subjects were treated and completed the study. AUC for apixaban without activated charcoal decreased by 50 and 28 %, respectively, when charcoal was administered at 2 and 6 h post-dose. Apixaban C and T were similar across treatments. The mean T for apixaban alone (13.4 h) decreased to ~5 h when activated charcoal was administered at 2 or 6 h post-dose. Overall, apixaban was well tolerated in this healthy population, and most adverse events were consistent with the known profile of activated charcoal. Conclusion: Administration of activated charcoal up to 6 h after apixaban reduced apixaban exposure and facilitated the elimination of apixaban. These results suggest that activated charcoal may be useful in the management of apixaban overdose or accidental ingestion. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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