Sharma Abhisheak, Jaiswal Swati, Shukla Mahendra, Ravindrachary Kondagudur, Lal Jawahar
* Pharmacokinetics & Metabolism Division, CSIR-Central Drug Research Institute , Lucknow , India.
Eur J Contracept Reprod Health Care. 2015 Jun;20(3):231-5. doi: 10.3109/13625187.2015.1017756. Epub 2015 Mar 23.
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.
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.
Coadministration of atorvastatin or rosuvastatin may increase the systemic availability of centchroman in blood, but it does not affect the pharmacodynamic profile of centchroman.
Atorvastatin or rosuvastatin may be prescribed with centchroman without compromising the contraceptive efficacy of centchroman.
本研究旨在调查阿托伐他汀或瑞舒伐他汀与非甾体类女性口服避孕药炔雌醚同时使用时，对其药代动力学和药效学特征的影响。
采用大鼠模型预测炔雌醚与阿托伐他汀或瑞舒伐他汀之间的药代动力学药物-药物相互作用。采用干血斑采样技术，随后进行液相色谱-串联质谱检测，以分析药代动力学相互作用研究样本。对精子阳性的雌性大鼠研究了炔雌醚在联合或不联合使用阿托伐他汀或瑞舒伐他汀时的抗着床避孕活性。
阿托伐他汀或瑞舒伐他汀与炔雌醚同时使用可能会增加炔雌醚在血液中的全身可用性，但不影响炔雌醚的药效学特征。
阿托伐他汀或瑞舒伐他汀可与炔雌醚联合使用，而不会影响炔雌醚的避孕效果。
