Interactions between clinically used drugs and oral contraceptives

Environ Health Perspect. 1994 Nov;102 Suppl 9(Suppl 9):35-8. doi: 10.1289/ehp.94102s935.

Abstract

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).

MeSH terms

  • Animals
  • Contraceptives, Oral / metabolism*
  • Drug Interactions
  • Enzyme Induction / drug effects
  • Enzyme Inhibitors / pharmacology
  • Estrogens / blood
  • Female
  • Humans
  • Hydroxylation / drug effects
  • Liver Circulation / drug effects
  • Mice
  • Pharmaceutical Preparations / metabolism*
  • Phenobarbital / metabolism
  • Rats
  • Rifampin / metabolism

Substances

  • Contraceptives, Oral
  • Enzyme Inhibitors
  • Estrogens
  • Pharmaceutical Preparations
  • Rifampin
  • Phenobarbital