Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers

Pharmacogenomics. 2013 Jul;14(10):1203-14. doi: 10.2217/pgs.13.106.

Abstract

Aim: Clinical trials with healthy volunteers are a useful model for evaluating safety and tolerability, without the interference of concomitant diseases and drugs. The present study aims to improve our understanding of antipsychotic-related adverse reactions (ARs) and their possible association with common genetic variants of pharmacodynamic proteins such as neurotransmitter receptors/transporters.

Materials & methods: A total of eight polymorphisms located in seven pharmacodynamic-related genes (SCL6A4, MDR1, 5HT2A, DRD2, DRD3, COMT and GRIN2B) were genotyped in a cohort of 211 healthy volunteers who received a single dose of risperidone (1 mg), olanzapine (5 mg) or quetiapine (25 mg).

Results: Interestingly, a significant association was found between the incidence of neurological ARs and specific polymorphisms in key genes (DRD2 and SCL6A4).

Conclusion: Genetic variants in pharmacodynamic genes could represent valuable markers of AR risk and antipsychotic safety. Original submitted 7 February 2013; Revision submitted 3 June 2013.

Publication types

  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antipsychotic Agents / administration & dosage
  • Antipsychotic Agents / adverse effects*
  • Antipsychotic Agents / pharmacokinetics
  • Benzodiazepines / administration & dosage
  • Benzodiazepines / adverse effects
  • Benzodiazepines / pharmacokinetics
  • Biomarkers, Pharmacological
  • Dibenzothiazepines / administration & dosage
  • Dibenzothiazepines / adverse effects
  • Dibenzothiazepines / pharmacokinetics
  • Drug-Related Side Effects and Adverse Reactions / genetics*
  • Drug-Related Side Effects and Adverse Reactions / pathology
  • Female
  • Genotype
  • Healthy Volunteers
  • Humans
  • Huntingtin Protein
  • Male
  • Nerve Tissue Proteins / genetics*
  • Olanzapine
  • Quetiapine Fumarate
  • Receptors, Dopamine D2 / genetics*
  • Risperidone / administration & dosage
  • Risperidone / adverse effects
  • Risperidone / pharmacokinetics

Substances

  • Antipsychotic Agents
  • Biomarkers, Pharmacological
  • DRD2 protein, human
  • Dibenzothiazepines
  • HTT protein, human
  • Huntingtin Protein
  • Nerve Tissue Proteins
  • Receptors, Dopamine D2
  • Benzodiazepines
  • Quetiapine Fumarate
  • Risperidone
  • Olanzapine