Pharmacokinetics and pharmacodynamics of dextromethorphan: clinical and forensic aspects

• Type: Article in International Scientific Journal
• Date: 2020

Authors

Silva, AR (Author) Other; Ricardo Jorge Dinis Oliveira (Author) FMUP

Journal

Title: Drug Metabolism Reviews

Vol. 52

Pages: 258-282

ISSN: 0360-2532

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 4 Citations

Scopus - 5 Citations

Other information

Authenticus ID: P-00S-4Y7

DOI: 10.1080/03602532.2020.1758712

Abstract (EN): Dextromethorphan (DXM) is a safe and effective antitussive agent present in several over the counter cough and cold medications. At higher doses, it causes psychoactive effects, making it appealing for abuse. In this work, the pharmacokinetics and pharmacodynamics of DXM with clinical and forensic relevance were extensively reviewed. DXM and related known metabolizing enzymes and metabolites were searched in books and in PubMed (U.S. National Library of Medicine) without a limiting period. Major metabolic pathways include sequential O-demethylation and N-demethylation of DXM, yielding dextrorphan (DXO), the major active metabolite, and 3-hydroxymorphinan, the bi-demethylated product, respectively. The demethylation order described may reverse being the resultant mid product 3-methoxymorphinan. UDP-glucuronosyltranferase produces glucuronide conjugates. Genotypic variations in enzymes and interactions with other drugs can result in large inter-individual variability in the pharmacological and toxicological effects produced. Knowing the metabolism of DXM may help to better understand the inter-individual variability in the pharmacokinetics and pharmacodynamics and to avoid adverse effects.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 25