Mechanism of efavirenz influence on methadone pharmacokinetics and pharmacodynamics.

  title={Mechanism of efavirenz influence on methadone pharmacokinetics and pharmacodynamics.},
  author={Evan D. Kharasch and Dale Whittington and Dustin Ensign and Christine J Hoffer and Pamela Sheffels Bedynek and Shane Campbell and Kristi K Stubbert and Amanda Crafford and Amy E London and Taekrho Kim},
  journal={Clinical pharmacology and therapeutics},
  volume={91 4},
Mechanisms by which efavirenz diminishes methadone plasma concentrations are unknown. This investigation determined efavirenz influence on clinical methadone disposition and miosis, intravenous and oral alfentanil clearance (hepatic and intestinal cytochrome P450 3A4/5 (CYP3A4/5) activity), fexofenadine disposition (intestinal transporters activity), and efavirenz clearance and 8-hydroxylation (CYP2B6 activity), and human hepatocyte effects. Efavirenz induced systemic and oral alfentanil… CONTINUE READING

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