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Pharmaceutics. 2021 Jun 13;13(6). doi: 10.3390/pharmaceutics13060876.

Changes in the Pharmacokinetics and Pharmacodynamics of Sildenafil in Cigarette and Cannabis Smokers.

Pharmaceutics

Mohammed Murtadha, Mohamed Ahmed Raslan, Sarah Farid Fahmy, Nagwa Ali Sabri

Affiliations

  1. Department of Clinical Pharmacy, Ain Shams University, Cairo 11865, Egypt.
  2. Drug Research Center, Clinical Research and Bioanalysis Department, Cairo 11865, Egypt.

PMID: 34199328 PMCID: PMC8231986 DOI: 10.3390/pharmaceutics13060876

Abstract

Sildenafil citrate, a widely-used oral therapy for erectile dysfunction, is a cytochrome P3A4 (CYP3A4) enzyme substrate. Studies have reported that this substrate has an inhibitory effect on CYP3A4 enzymes in long-term cigarette and cannabis smokers, which predominantly mediate the hepatic elimination of sildenafil. Cigarette and/or cannabis smoking could therefore alter the exposure of sildenafil. The aim of this study was to examine the effect of smoking cigarettes and/or cannabis on the pharmacokinetics, pharmacodynamics, safety and tolerability of sildenafil. Thirty-six healthy human subjects were equally divided into three groups: non-smokers, cigarette smokers and cannabis smokers. Each group was administered a single dose of sildenafil (50 mg tablets). The primary outcome measures included the maximum concentration of sildenafil in plasma (C

Keywords: cannabis; cytochrome P3A4; drug interactions; erectile dysfunction; oxidative stress; pharmacodynamics; pharmacokinetics; safety; sildenafil; smokers

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