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Association of common polymorphisms in β1-adrenergic receptor with antihypertensive response to carvedilol

Dayong Si1, Juan Wang, Ying Xu

  • 1*School of Life Science, Jilin University, Changchun, China; †Key-Lab for Evolution of Past Life and Environment in Northeast Asia, Ministry of Education, Jilin University, Changchun, China; ‡Division of Nephrology, The First Hospital of Jilin University, Changchun, China; and §Department of Cardiology, China-Japan Union Hospital of Jilin University, Changchun, China.

Journal of Cardiovascular Pharmacology
|October 8, 2014
PubMed

Insights

Genetic variations in the beta-1 adrenergic receptor (ADRB1) significantly impact carvedilol

Area of Science:

  • Pharmacogenomics
  • Cardiovascular Medicine
  • Genetics

Background:

  • Interpatient variability in blood pressure response to carvedilol is significant.
  • Carvedilol is a nonselective beta-blocker used for hypertension.
  • Adrenergic receptor gene polymorphisms may influence drug efficacy.

Purpose of the Study:

  • To investigate the impact of common beta-adrenergic receptor gene polymorphisms on the antihypertensive efficacy of carvedilol.
  • To evaluate the role of ADRB1 and ADRB2 gene variants in carvedilol response.

Main Methods:

  • A double-blind monotherapy study involving 87 essential hypertensive patients from China.
  • Blood pressures were measured before and after 7 days of carvedilol treatment (10 mg/d).
  • Genotyping for ADRB1 (Ser49Gly, Arg389Gly) and ADRB2 (Gly16Arg, Glu27Gln) polymorphisms using PCR-RFLP.

Main Results:

  • Patients homozygous for ADRB1 Arg389 showed a significantly greater reduction in diastolic blood pressure (DBP) compared to ADRB1 Gly389 homozygotes (10.61 vs. 2.62 mm Hg, P=0.013).
  • ADRB1 haplotypes predicted response; Gly49Arg389/Ser49Arg389 haplotype pairs demonstrated a 5.7-fold greater DBP reduction than Ser49Gly389 homozygotes (16.11 vs. 2.83 mm Hg, P=0.0055).
  • No association was found between ADRB2 polymorphisms and carvedilol response.

Conclusions:

  • ADRB1 polymorphisms are important determinants of diastolic blood pressure response to carvedilol in essential hypertension.
  • This study provides evidence for the pharmacogenetic influence of ADRB1 on carvedilol efficacy.
  • ADRB2 polymorphisms do not appear to influence carvedilol's antihypertensive effect.
Abstract

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