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
1Faculty of Pharmacy, Department of Pharmaceutical Botany
2Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmacy
3Faculty of Pharmacy, Department of Clinical Pharmacy
4Faculty of Medicine, Department of Pharmacology, Toxicology and Clinical Pharmacology
5Faculty of Medicine, Department of Medical Informatics and Biostatistics
*corresponding author: laurian.vlase@umfcluj.ro
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Abstract:
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.

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