Glucuronidation is a major metabolic pathway for a large number of drugs in humans. Conjugation of drugs and other chemicals with glucuronic acid is catalyzed by the multigene UDP-glucuronosyltransferase family. It is believed that a number (unspecified at present) of glucuronosyltransferase isozymes, which probably differ in terms of substrate specificity and regulation, contribute to drug glucuronidation. Factors known to influence the pharmacokinetics of glucuronidated drugs in man, presumably via an effect on specific glucuronosyltransferases, include age (especially the neonatal period), cigarette smoking, diet, certain disease states, coadministered drugs, ethnicity, genetics and hormonal effects.