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Med Pharm Rep. 2019 Apr;92(2):158-164. doi: 10.15386/mpr-1225. Epub 2019 Apr 25.

Pharmacokinetic interactions study between carvedilol and some antidepressants in rat liver microsomes - a comparative study.

Medicine and pharmacy reports

Maria Bianca Abrudan, Daniela Saveta Popa, Dana Maria Muntean, Ana Maria Gheldiu, Laurian Vlase

Affiliations

  1. Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.
  2. Department of Toxicology, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.

PMID: 31086844 PMCID: PMC6510361 DOI: 10.15386/mpr-1225

Abstract

BACKGROUND AND AIMS: Cardiovascular diseases and depressive disorders are some of the most frequent diseases. The probability of concomitant prescription of antihypertensive and antidepressive medication is increasing. The aim of this study was to investigate the enzyme inhibition by bupropion, sertraline and fluvoxamine on the metabolism of carvedilol using rat pooled liver microsomes and to assess the importance of these interactions from the pharmacokinetic mechanism point of view.

METHODS: Two substrate concentrations (0.5 and 1 μM) and four inhibitor concentrations (0, 0.1, 0.75 and 1.5 μM) were used for each tested inhibitor.

RESULTS: The results of the

CONCLUSION: The co-administration of tested antidepressants led to a significant alteration of carvedilol's metabolism

Keywords: CYP2D6; antidepressants; carvedilol; pharmacokinetics; rat liver microsomes

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