Pharmacokinetic interaction of nelfinavir and methadone in intravenous drug users
- 1 March 2006
- journal article
- clinical trial
- Published by Wiley in Biopharmaceutics & Drug Disposition
- Vol. 27 (2), 61-68
- https://doi.org/10.1002/bdd.482
Abstract
The effect of nelfinavir 1250 mg twice daily (b.i.d.) on the pharmacokinetics of methadone was determined in 14 HIV‐negative methadone users. Design: The methadone dose (20–140 mg/day) was stabilized and fixed for at least 1 month before nelfinavir (1250 mg b.i.d. for 8 days) was added to the regimen. The concentrations of methadone enantiomers were measured before and during nelfinavir treatment, and the concentrations of nelfinavir and its active metabolite, AG1402, were measured during nelfinavir treatment. Adverse events and withdrawal/intoxication symptoms were monitored throughout the study. Results: Nelfinavir reduced the area under the concentration‐time curve of R‐methadone, and S‐methadone by 43% and 51%, respectively. Nelfinavir and AG1402 concentrations were within the normal range of historical data, and no subject experienced withdrawal symptoms during the study or required dose adjustment during or after the study. Conclusions: Although nelfinavir reduced the plasma concentrations of both R‐ and S‐methadone, it seems to have no impact on the maintenance dose of methadone. A routine reduction of methadone dose is not recommended when coadministered with nelfinavir. Copyright © 2005 John Wiley & Sons, Ltd.Keywords
This publication has 16 references indexed in Scilit:
- Stereoselective metabolism of methadone N‐demethylation by cytochrome P4502B6 and 2C19Chirality, 2003
- The Protease Inhibitor Lopinavir-Ritonavir May Produce Opiate Withdrawal in Methadone-Maintained PatientsClinical Infectious Diseases, 2003
- Absence of Opioid Withdrawal Symptoms in Patients Receiving Methadone and the Protease Inhibitor Lopinavir‐RitonavirClinical Infectious Diseases, 2002
- Pharmacokinetic Interactions between Nelfinavir and 3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase Inhibitors Atorvastatin and SimvastatinAntimicrobial Agents and Chemotherapy, 2001
- Pharmacokinetic Interactions of Nevirapine and Methadone and Guidelines for Use of Nevirapine to Treat Injection Drug UsersClinical Infectious Diseases, 2001
- Circulating Metabolites of the Human Immunodeficiency Virus Protease Inhibitor Nelfinavir in Humans: Structural Identification, Levels in Plasma, and Antiviral ActivitiesAntimicrobial Agents and Chemotherapy, 2001
- The pharmacokinetics of methadone in HIV‐positive patients receiving the non‐nucleoside reverse transcriptase inhibitor efavirenzBritish Journal of Clinical Pharmacology, 2001
- Effective Medical Treatment of Opiate AddictionJAMA, 1998
- EFFECTIVENESS OF METHADONE MAINTENANCE FOR HEROIN ADDICTIONPsychological Reports, 1998
- Involvement of Cytochrome P450 3A4 Enzyme in the N-Demethylation of Methadone in Human Liver MicrosomesChemical Research in Toxicology, 1996