The effect of ritonavir on the pharmacokinetics of meperidine and normeperidine.
Pharmacotherapy
; 20(5): 549-53, 2000 May.
Article
in En
| MEDLINE
| ID: mdl-10809341
ABSTRACT
STUDY OBJECTIVE:
To determine the effects of ritonavir on the pharmacokinetics of meperidine and normeperidine.DESIGN:
Open-label, crossover, pharmacokinetic study.SETTING:
United States government research hospital.SUBJECTS:
Eight healthy volunteers who tested negative for the human immunodeficiency virus. INTERVENTION Subjects received oral meperidine 50 mg and had serial blood samples collected for 48 hours. They then received ritonavir 500 mg twice/day for 10 days, followed by administration of a second 50-mg meperidine dose and collection of serial samples. MEASUREMENTS AND MAINRESULTS:
Plasma samples were assayed for meperidine, normeperidine, and ritonavir. Meperidine's area under the curve (AUC) decreased in all subjects by a mean of 67+/-4% in the presence of ritonavir (p<0.005). Mean +/- SD maximum concentration was decreased from 126+/-47 to 51+/-21 ng/ml. Normeperidine's mean AUC was increased 47%, suggesting induction of hepatic metabolism.CONCLUSION:
Meperidine's AUC is significantly reduced, not increased, by concomitant ritonavir. Based on these findings, the risk of narcotic-related adverse effects from this combination appears to be minimal. However, increased concentrations of normeperidine suggest a potential for toxicity with increased dosages or long-term therapy.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Cholinesterase Inhibitors
/
HIV Protease Inhibitors
/
Ritonavir
/
Analgesics, Opioid
/
Meperidine
Type of study:
Clinical_trials
/
Prognostic_studies
Limits:
Adult
/
Female
/
Humans
/
Male
Language:
En
Journal:
Pharmacotherapy
Year:
2000
Document type:
Article
Affiliation country: