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

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.Chinese 摘要目的 这项研究旨在调查同时使用阿托伐他汀或罗苏伐他汀时centchroman（一种非甾体女性口服避孕药）的药代动力学和药效情况。方法 采用大鼠模型来预测centchroman与阿托伐他汀或罗苏伐他汀之间药物相互作用的药代动力学。随后采用干燥血斑点采样技术和液相色谱串联质谱检测用于样本的药代动力学相互作用的研究分析。对精子阳性的雌性大鼠，观察centchroman同时服用/不服用阿托伐他汀或瑞舒伐他汀的事后避孕效果。结果 合用阿托伐他汀或瑞舒伐他汀可能会增加全身血液中的centchroman的生物利用率，但并不影响centchroman的药效。结论 阿托伐他汀或瑞舒伐他汀并不影响centchroman的避孕效果