Back D J, Breckenridge A M, Crawford F E, MacIver M, Orme M L, Rowe P H
Drugs. 1981 Jan;21(1):46-61. doi: 10.2165/00003495-198121010-00003.
Large interindividual differences occur in the plasma concentration of contraceptive steroids. With the present tendency to decrease the dose of progestagen and oestrogen any factor which reduces the bioavailability of the lower dose preparations becomes very important. The possibility that other drugs and environmental chemicals may interact with contraceptive steroids is currently being investigated. Clinical reports suggest that the most important interacting drugs are the antituberculosis agent rifampicin, anticonvulsants and antibiotics. In the case of the first two, evidence is available suggesting that microsomal enzyme induction, either in the liver or the gut wall, is the operative mechanism. Antibiotics interfere with the pharmacokinetics of contraceptive steroids by interfering with their enterohepatic circulation in animal species: whether this is operative in man is still unclear. Other environmental and constitutional factors such as smoking, variations in diet, and concurrent disease may alter the disposition of contraceptive steroids and affect response accordingly. Additional studies are needed to estimate the significance of such interactions.
避孕药类固醇的血浆浓度存在很大的个体差异。随着目前降低孕激素和雌激素剂量的趋势,任何降低低剂量制剂生物利用度的因素都变得非常重要。目前正在研究其他药物和环境化学物质与避孕药类固醇相互作用的可能性。临床报告表明,最重要的相互作用药物是抗结核药利福平、抗惊厥药和抗生素。就前两者而言,有证据表明,肝脏或肠壁中的微粒体酶诱导是其作用机制。抗生素通过干扰动物体内避孕药类固醇的肠肝循环来干扰其药代动力学:这在人类中是否起作用尚不清楚。其他环境和体质因素,如吸烟、饮食变化和并发疾病,可能会改变避孕药类固醇的处置并相应影响反应。需要进行更多研究来评估此类相互作用的重要性。