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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
medicine
Pharmacokinetics and safety of etravirine administered once or twice daily after 2 weeks treatment with efavirenz in healthy volunteers
Journal of Acquired Immune Deficiency Syndromes, Volume 52, No. 2, Year 2009
Notification
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Description
OBJECTIVE: To assess the pharmacokinetics of etravirine once and twice daily without and with a preceding efavirenz intake period in healthy volunteers. METHODS: Volunteers were randomized to receive etravirine 400 mg once daily (arm 1) or 200 mg twice daily (arm 2) for 14 days. All subjects underwent a washout period of 14 days and then took efavirenz 600 mg once daily for 14 days. Arm 1 and 2 restarted etravirine once and twice daily for 14 days. Etravirine pharmacokinetics was assessed for each phase (before and after efavirenz 14-day intake) on days 1 and 14. Efavirenz concentrations were measured daily for 14 days after intake withholding. Pharmacokinetic parameters were compared (before and after efavirenz 14-day intake) by determining geometric mean ratios and 90% confidence intervals. RESULTS: Twenty-five subjects (9 female) completed the study. Steady-state etravirine pharmacokinetic parameters were significantly lower after efavirenz intake in the once-daily and twice-daily arms: geometric mean ratios and 90% confidence intervals were 0.71 (0.62 to 0.81) for AUC 0-24, 0.78 (0.70 to 0.86) for Cmax, 0.67 (0.49 to 0.91) for Ctrough for once daily; and 0.72 (0.63 to 0.81) for AUC 0-12, 0.79 (0.70 to 0.90) for Cmax, and 0.63 (0.54 to 0.73) for Ctrough for twice daily. All subjects had detectable efavirenz concentrations 7 days after stopping efavirenz intake, 5 above the suggested minimum effective concentration of 1000 ng/mL. CONCLUSIONS: The induction effect of efavirenz persists for at least 2 weeks after stopping drug intake. The decrease in etravirine is not considered clinically significant. Further clinical data are warranted. Copyright © 2009 by Lippincott Williams & Wilkins.
Authors & Co-Authors
Boffito, Marta A.
United Kingdom, London
Chelsea and Westminster Hospital
Jackson, Akil G.A.
United Kingdom, London
Chelsea and Westminster Hospital
Lamorde, Mohammed
United Kingdom, London
Chelsea and Westminster Hospital
Ireland, Dublin
Trinity College Dublin
Back, David J.
United Kingdom, Liverpool
University of Liverpool
Waters, Laura Jane
United Kingdom, London
Chelsea and Westminster Hospital
Asboe, David
United Kingdom, London
Chelsea and Westminster Hospital
Gazzard, Brian George L.
United Kingdom, London
Chelsea and Westminster Hospital
Pozniak, Anton Louis
United Kingdom, London
Chelsea and Westminster Hospital
Statistics
Citations: 31
Authors: 8
Affiliations: 4
Identifiers
Doi:
10.1097/QAI.0b013e3181b061d0
ISSN:
15254135
Participants Gender
Female