Prolactin levels: sex differences in the effects of risperidone, 9-hydroxyrisperidone levels, CYP2D6 and ABCB1 variants

Pharmacogenomics. 2018 Jul 1;19(10):815-823. doi: 10.2217/pgs-2018-0053. Epub 2018 Jun 19.

Abstract

Aim: The role of sex on the association of plasma prolactin levels with risperidone (R) and 9-hydroxyrisperidone (9-OHR) concentrations is investigated.

Methods: Plasma R and prolactin concentrations, CYP2D6 and exon 21 and 26 ABCB1 gene variants were studied in 110 patients.

Results: In females, a 1 ng/ml increase in R levels was associated with a significant 1.02% increase in prolactin levels. In males, a 1 ng/ml increase in 9-OHR levels was associated with a significant 1.18% increase in prolactin levels. ABCB1 haplotype 12 had significant but opposite effects in males and females. In the combined sample, 9-OHR, but not R levels had significant effects on prolactin levels.

Conclusion: Genes had sex-specific effects on risperidone-associated prolactin elevations.

Keywords: 9-hydroxyrisperidone; ABCB1; CYP2D6; p-glycoprotein; prolactin; risperidone; sex.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B / genetics
  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Adult
  • Cytochrome P-450 CYP2D6 / genetics*
  • Female
  • Genetic Association Studies
  • Genotype
  • Haplotypes / genetics
  • Humans
  • Male
  • Middle Aged
  • Paliperidone Palmitate / blood
  • Prolactin / blood*
  • Prolactin / genetics
  • Risperidone / blood*
  • Risperidone / therapeutic use
  • Sex Characteristics

Substances

  • ABCB1 protein, human
  • ATP Binding Cassette Transporter, Subfamily B
  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Prolactin
  • Cytochrome P-450 CYP2D6
  • Risperidone
  • Paliperidone Palmitate