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

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, clin...

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Bibliographic Details
Published in:Drug metabolism reviews 2019-07, Vol.51 (3), p.293-313
Main Authors: Costa, Rafaela, Oliveira, Nuno G., Dinis-Oliveira, Ricardo Jorge
Format: Article
Language:English
Subjects:
Animals
Antidepressive Agents, Second-Generation - adverse effects
Antidepressive Agents, Second-Generation - chemistry
Antidepressive Agents, Second-Generation - pharmacokinetics
Antidepressive Agents, Second-Generation - pharmacology
Bupropion
Bupropion - adverse effects
Bupropion - chemistry
Bupropion - pharmacokinetics
Bupropion - pharmacology
forensic and clinical aspects
Forensic Toxicology
Humans
metabolism
pharmacodynamics
pharmacokinetics
polymorphisms
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Summary: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.
ISSN:0360-2532
1097-9883
DOI:10.1080/03602532.2019.1620763