Coadministration of HMG-CoA reductase inhibitors, atorvastatin and rosuvastatin, does not affect contraceptive efficacy of centchroman

Eur J Contracept Reprod Health Care. 2015 Jun;20(3):231-5. doi: 10.3109/13625187.2015.1017756. Epub 2015 Mar 23.

Abstract

Objective: The study aimed to investigate the effect of concomitant use of atorvastatin or rosuvastatin on the pharmacokinetic and pharmacodynamic profile of centchroman, a non-steroidal female oral contraceptive.

Methods: A rat model was used to predict pharmacokinetic drug-drug interactions between centchroman and atorvastatin or rosuvastatin. A dried blood spot sampling technique followed by liquid chromatography-tandem mass spectrometry detection was employed for analysis of the pharmacokinetic interaction study samples. Sperm-positive female rats were investigated for postcoital contraceptive activity of centchroman with or without coadministration of atorvastatin or rosuvastatin.

Results: Coadministration of atorvastatin or rosuvastatin may increase the systemic availability of centchroman in blood, but it does not affect the pharmacodynamic profile of centchroman.

Conclusion: Atorvastatin or rosuvastatin may be prescribed with centchroman without compromising the contraceptive efficacy of centchroman.

Keywords: Dried blood spot; Drug interaction; Liquid chromatography–tandem mass spectrometry; Ormeloxifene.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Atorvastatin / administration & dosage
  • Atorvastatin / pharmacology*
  • Centchroman / administration & dosage
  • Centchroman / pharmacokinetics*
  • Chromatography, High Pressure Liquid
  • Contraceptives, Oral / administration & dosage
  • Contraceptives, Postcoital, Synthetic / administration & dosage
  • Contraceptives, Postcoital, Synthetic / pharmacokinetics*
  • Female
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / administration & dosage
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Rosuvastatin Calcium / administration & dosage
  • Rosuvastatin Calcium / pharmacology*

Substances

  • Contraceptives, Oral
  • Contraceptives, Postcoital, Synthetic
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Centchroman
  • Rosuvastatin Calcium
  • Atorvastatin