PMID: 11318772Apr 25, 2001Paper

A single dose of methadone inhibits cytochrome P-4503A activity in healthy volunteers as assessed by the urinary cortisol ratio

British Journal of Clinical Pharmacology
D W BoultonC L DeVane

Abstract

To examine the effect of a single oral dose of methadone on cytochrome P450 (CYP) 3A activity using the urinary 6beta-hydroxycortisol to cortisol ratio (UCR) as a marker of CYP3A activity. A single oral dose (0.2 mg kg-1) of rac-methadone was administered to eight healthy female volunteers. Frequent blood samples and all urine over seven time periods was collected for 96 h following dosing. The UCR and the concentration of the major CYP3A metabolite of methadone, EDDP, were measured in urine. Methadone enantiomer concentrations were determined in plasma and urine. All quantifications were performed by validated high performance liquid chromatography assays. In all volunteers a significant decline of the UCR from immediately predose values was observed at the 4-8 and 8-12 h collection periods (P < 0.05, 95% CI for the differences: 0.4,16 and 0.6,16, respectively) with a return to immediately predose values after 2-3 days, suggesting methadone was an inhibitor of CYP3A. The UCR was found to be significantly correlated with the amount of EDDP excreted in the urine and with the area under the plasma concentration vs time profile for total (R + S) methadone, supporting in vitro data that CYP3A is primarily responsible for EDDP forma...Continue Reading

References

Mar 1, 1975·Clinical Pharmacology and Therapeutics·E AnggårdH R Sullivan
Aug 1, 1975·Clinical Pharmacology and Therapeutics·K VerebelyR Resnick
Jan 22, 1976·The New England Journal of Medicine·P F Finelli
May 13, 1976·The New England Journal of Medicine·M J KreekL M Giusti
Oct 1, 1968·The Journal of Pharmacy and Pharmacology·A H BeckettM M Hassan
Oct 1, 1984·The American Journal of Psychiatry·S J Liu, R I Wang
Jan 1, 1982·European Journal of Clinical Pharmacology·M I NilssonL M Gunne
Oct 15, 1994·BMJ : British Medical Journal·M FarrellJ Strang
Oct 1, 1996·Journal of Pharmacokinetics and Biopharmaceutics·G R Wilkinson
Nov 14, 1997·British Journal of Clinical Pharmacology·K WolffG T Tucker
Jan 22, 1998·Archives of General Psychiatry·C B EapN Scherbaum
Jul 15, 1998·Clinical Pharmacology and Therapeutics·M N CobbP M Rainey
May 8, 1999·British Journal of Clinical Pharmacology·D J FosterF Bochner
Jun 26, 1999·British Journal of Clinical Pharmacology·A Rostami-HodjeganG T Tucker
Oct 8, 1999·Clinical Pharmacology and Therapeutics·M T KinironsG R Wilkinson
Dec 10, 1999·Journal of Pain and Symptom Management·N A Hagen, E Wasylenko
Jan 21, 2000·Pharmacotherapy·S M Geletko, A D Erickson

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Citations

Apr 15, 2005·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Ehab S El DesokyJean-Pascal Siest
Mar 1, 2003·Drug and Alcohol Dependence·Marc ShindermanChin B Eap
May 21, 2004·British Journal of Clinical Pharmacology·David J R FosterFelix Bochner
Sep 12, 2009·Respiratory Physiology & Neurobiology·Daniel A N SilvermanGeorge D Olsen
May 20, 2014·British Journal of Clinical Pharmacology·Sreeneeranj KasichayanulaFrank LaCreta
Sep 24, 2002·The Annals of Pharmacotherapy·Tony Antoniou, Alice Lin-In Tseng

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