Variation in the CYP2D6 genotype is not associated with carvedilol dose changes in patients with heart failure

J Clin Pharm Ther. 2014 Aug;39(4):432-8. doi: 10.1111/jcpt.12154. Epub 2014 Mar 27.

Abstract

What is known and objective: Carvedilol is the standard of care for heart failure (HF) patients. Carvedilol is partially metabolized by the highly polymorphic enzyme, CYP2D6. To reach an effective dose while avoiding adverse drug reactions (ADRs), testing of CYP2D6 genotype prior to carvedilol initiation may be considered. The objectives of this study were to determine CYP2D6 metabolic genotypes in an Israeli cohort of HF patients and to investigate the relationship between genotype, carvedilol dose and number of ADRs to determine the importance of CYP2D6 genotyping prior to treatment initiation.

Methods: Ninety-three patients with HF on carvedilol were CYP2D6 genotyped and classified as poor (PM), intermediate (IM), extensive (EM) or ultrarapid (UM) metabolizers. Carvedilol dose and ADRs were calculated and correlated with genotype using linear regression statistic analysis.

Results and discussion: The distribution of the CYP2D6 phenotype in the Israeli population with HF is similar to the European general population. There were no significant differences of carvedilol dose and number of ADRs among genotype groups. Genotype group affiliation and number of adverse drug reactions were not predictive of carvedilol dose changes.

What is new and conclusion: Genotype group affiliation and number of adverse drug reactions were not predictive of carvedilol dose during therapy for patients with HF. The Israeli CYP2D6 phenotype distribution in HF patients was consistent with the frequency in the general European population.

Keywords: CYP2D6; adverse drug reactions; carvedilol; heart failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-1 Receptor Antagonists / administration & dosage*
  • Adrenergic alpha-1 Receptor Antagonists / adverse effects
  • Adrenergic alpha-1 Receptor Antagonists / therapeutic use
  • Adrenergic beta-Antagonists / administration & dosage
  • Adrenergic beta-Antagonists / adverse effects
  • Adrenergic beta-Antagonists / therapeutic use
  • Aged
  • Carbazoles / administration & dosage*
  • Carbazoles / adverse effects
  • Carbazoles / therapeutic use
  • Carvedilol
  • Cytochrome P-450 CYP2D6 / genetics*
  • Dose-Response Relationship, Drug
  • Female
  • Genotype
  • Heart Failure / drug therapy*
  • Heart Failure / genetics
  • Humans
  • Israel
  • Linear Models
  • Male
  • Middle Aged
  • Pharmacogenetics
  • Polymorphism, Genetic
  • Propanolamines / administration & dosage*
  • Propanolamines / adverse effects
  • Propanolamines / therapeutic use
  • Retrospective Studies

Substances

  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic beta-Antagonists
  • Carbazoles
  • Propanolamines
  • Carvedilol
  • Cytochrome P-450 CYP2D6