Bolt H M
Institut fur Arbeitsphysiologie an der Universität Dortmund, Germany.
Environ Health Perspect. 1994 Nov;102 Suppl 9(Suppl 9):35-8. doi: 10.1289/ehp.94102s935.
Metabolism of contraceptive compounds may be influenced by various drugs. Of clinical importance is induction by barbiturates, by diphenylhydantoin, and especially by rifampicin, of enzymes that are responsible for degradation of estrogens. The major target is the hepatic microsomal estrogen-2-hydroxylase (cytochrome P450 3A4). Another type of interaction of drugs with disposition and effectiveness of estrogens is impairment of their enterohepatic circulation. This may be due to absorption of biliary estrogen conjugates (e.g., by cholestyramine) or to insufficient cleavage of the conjugate by intestinal bacteria, the latter being observed after administration of antibiotics (e.g., ampicillin, neomycin).
避孕药化合物的代谢可能会受到多种药物的影响。具有临床重要性的是巴比妥类药物、苯妥英,尤其是利福平对负责雌激素降解的酶的诱导作用。主要靶点是肝微粒体雌激素-2-羟化酶(细胞色素P450 3A4)。药物与雌激素的处置和有效性的另一种相互作用类型是其肠肝循环受损。这可能是由于胆汁雌激素结合物的吸收(例如通过考来烯胺)或肠道细菌对结合物的裂解不足所致,后者在使用抗生素(例如氨苄西林、新霉素)后可见。