Pharmacokinetic and pharmacodynamic of bupropion: integrative overview of relevant clinical and forensic aspects

• Type: Article in International Scientific Journal
• Date: 2019

Authors

Costa, R (Author) Other; Oliveira, NG (Author) Other; Ricardo Jorge Dinis Oliveira (Author) FMUP

Journal

Title: Drug Metabolism Reviews

Vol. 51

Pages: 293-313

ISSN: 0360-2532

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 21 Citations

Scopus - 20 Citations

Other information

Authenticus ID: P-00Q-ZSN

DOI: 10.1080/03602532.2019.1620763

Abstract (EN): Bupropion is an atypical antidepressant of the aminoketone group, structurally related to cathinone, associated with a wide interindividual variability. An extensive pharmacokinetic and pharmacodynamic review of bupropion was performed, also focusing on chemical, pharmacological, toxicological, clinical and forensic aspects of this drug without a limiting period. Bupropion is a chiral, basic, highly lipophilic drug, clinically used as racemate that undergoes extensive stereoselective metabolism. Its major active metabolites, hydroxybupropion, threohydrobupropion, and erythrohydrobupropion reach higher plasma concentrations than bupropion. Bupropion exerts its effects mainly by inhibiting dopamine and norepinephrine reuptake and by blocking several nicotinic receptors. Recent reports highlight recreational use of bupropion via intranasal insufflation and intravenous use. Seizures, insomnia, agitation, headache, dry mouth, and nausea are some of the reported adverse effects. Neurologic effects are major signs of intoxication that should be carefully managed. Finally, the characterization of the polymorphic enzymes involved in the metabolism of bupropion is essential to understand factors that may influence the interindividual and intraindividual variability in bupropion metabolite exposure, including the evaluation of potential drug-drug interactions and pharmacogenetic implications.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 21