Zomepirac has been shown to be rapidly and completely absorbed after oral administration to man. Urinary excretion is the principal route for removal of zomepirac and its metabolites in man and in animals. Zomepirac is highly bound to plasma protein. The pharmacokinetics of zomepirac after single and multiple doses in man can be adequately described by a two-compartment oral absorption model. There is a linear relationship between dose and peak plasma concentration, AUC, and urinary excretion of zomepirac. The bioavailability of zomepirac was unaffected by single or repeated doses of antacid. The rhesus monkey has been shown to be a good predictive animal model for zomepirac's metabolism and pharmacokinetics in man, with glucuronidation found to be the principal route of metabolism in both species.