Different phenotypes of the NAT2 gene influences hydralazine antihypertensive response in patients with resistant hypertension

Pharmacogenomics. 2014 Feb;15(2):169-78. doi: 10.2217/pgs.13.202.

Abstract

Aim: Hydralazine, a vasodilator used in resistant hypertension (RH) treatment is metabolized by an acetylation reaction mediated by N-acetyltransferase 2, the activity of which depends on NAT2 polymorphisms. Our aim was to evaluate whether different acetylation phenotypes influenced the antihypertensive effect of hydralazine in patients with RH.

Patients & methods: DNA samples from 169 RH patients using hydralazine were genotyped by sequencing the NAT2 coding region, and acetylation phenotypes were defined.

Results: Sixty-five patients (38.5%) were intermediate, 60 (35.5%) slow and 21 (12.4%) fast acetylators. Twenty-three (13.6%) patients were indeterminate. Upon association analysis, only slow acetylators had significant blood pressure reductions after hydralazine use, with mean 24-h systolic and diastolic blood pressure reductions of 9.2 and 5.5 mmHg. Four patients presented hydralazine adverse effects resulting in drug withdrawal, three of them were slow acetylators.

Conclusion: The slow acetylation phenotype, determined by polymorphisms within NAT2, influenced both the antihypertensive and adverse effects of hydralazine in RH.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation / drug effects
  • Adult
  • Aged
  • Antihypertensive Agents / administration & dosage*
  • Arylamine N-Acetyltransferase / genetics*
  • Blood Pressure / drug effects
  • Female
  • Humans
  • Hydralazine / administration & dosage*
  • Hypertension / drug therapy*
  • Hypertension / pathology
  • Male
  • Middle Aged
  • Phenotype
  • Polymorphism, Genetic

Substances

  • Antihypertensive Agents
  • Hydralazine
  • Arylamine N-Acetyltransferase
  • NAT2 protein, human