ASSESSMENT OF THE EFFECTS OF STEADY-STATE BUPROPION ON THE PHARMACOKINETIC PROFILE OF ZOLPIDEM IN HEALTHY VOLUNTEERS
ANA-MARIA GHELDIU 1, LAURIAN VLASE 2*, ADINA POPA 3, DANA MUNTEAN 2, CORINA BOCȘAN 4, ANCA BUZOIANU 4, MARIA NEAG 4, DANIEL LEUCUȚA 5, CORINA BRICIU 3
“Iuliu Hațieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania
1.Faculty of Pharmacy, Department of Pharmaceutical Botany
2.Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmacy
3.Faculty of Pharmacy, Department of Clinical Pharmacy
4.Faculty of Medicine, Department of Pharmacology, Toxicology and Clinical Pharmacology
5.Faculty of Medicine, Department of Medical Informatics and Biostatistics
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The study’s purpose was to evaluate if bupropion, an antidepressant agent, can influence the pharmacokinetic profile of zolpidem, a sedative/hypnotic drug, and its main metabolite (zolpidem phenyl-4-carboxylic acid, Z4CA). The open-label, non-randomized, sequential clinical trial consisted of two periods: Period 1, when each volunteer received a single dose of zolpidem 5 mg and Period 2, when a combination of zolpidem 5 mg and bupropion 300 mg was administered, after a 7-day pre-treatment with bupropion. Pharmacokinetic analysis used for the non-compartmental approach and safety evaluations were conducted during the study. Bupropion pre-treatment decreased mean Cmax and AUC0-∞ for zolpidem and increased the same parameters for Z4CA. Most of zolpidem’s pharmacokinetic parameters displayed statistically significant differences between study periods. These results demonstrated that a pharmacokinetic interaction does occur between these drugs, possibly due to CYP3A4 induction, hypothesis which needs to be further investigated.
