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Exploring CYP2B6 activity by measuring the presence ofnevirapine hydroxy metabolites in plasma.
- Source :
-
Turkish journal of medical sciences [Turk J Med Sci] 2016 Dec 20; Vol. 46 (6), pp. 1875-1881. Date of Electronic Publication: 2016 Dec 20. - Publication Year :
- 2016
-
Abstract
- Background/aim: Nevirapine is a reverse-transcriptase inhibitor widely used in combination therapy to treat HIV infection. Nevirapine is extensively metabolized in the liver and CYP2B6 is mainly responsible for oxidation of 3-hydroxynevirapine (3-OH NVP). This study aims to explore CYP2B6 activity by measuring 2-hydroxynevirapine (2-OH NVP) and 3-OH NVP in plasma and to identify factors associated with nevirapine pharmacokinetic parameters.<br />Materials and Methods: A total of 112 patients were recruited and treated with nevirapine-based antiretroviral therapy. Plasma nevirapine and metabolite concentrations were assayed using high-performance liquid chromatography via liquid-liquid extraction.<br />Results: Thirty-nine (34.8%) of the patients had no 3-OH NVP detected in their plasma while 2-OH NVP was detected in all patients. Metabolite concentrations were low compared to nevirapine. Positive correlations were observed between nevirapine and its metabolites, 2-OH NVP (P < 0.01) and 3-OH NVP (P = 0.012). Nevirapine concentration was decreased when concomitantly administered with methadone. Univariate analysis showed that ALT level, AST level, and detection of 3-OH NVP were associated with nevirapine pharmacokinetic parameters.<br />Conclusion: The variability of nevirapine pharmacokinetic parameters was caused by liver enzymes and the presence of 3-OH NVP metabolites. The presence of 3-OH NVP can probably be used to distinguished CYP2B6 activity and efficacy of nevirapine in patients with HIV infection.
Details
- Language :
- English
- ISSN :
- 1300-0144
- Volume :
- 46
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Turkish journal of medical sciences
- Publication Type :
- Academic Journal
- Accession number :
- 28081342
- Full Text :
- https://doi.org/10.3906/sag-1503-116