ABSTRACT

This chapter discusses knowledge of the mechanism of induction. It evaluates the implications of enzyme induction to human health. Inducers interfere with the metabolism of other drugs, altering their plasma half-lives with consequent reduction in their therapeutic effect or increase in their toxicity. Enzyme inducers crossing the placenta may also stimulate the fetal metabolism of hormones which may lead to a hormonal inbalance in the neonate. In order to produce the same pharmacologic effect the dose of the drug must be increased accordingly, so that therapeutic blood levels are maintained. Inducing agents have been used therapeutically in the treatment of the various forms of hyperbilirubinemia associated with kernicterus and in the treatment of Cushing’s syndrome. The majority of studies on enzyme induction involved only the enzymes localized in the hepatic microsomes. Therefore enzyme induction by repeated sex hormones appears questionable, and it is unlikely that oral contraceptives can influence significantly the metabolism of other drugs.