Oral hypoglycaemic drugs, sulphonylureas and biguanides, occupy an important place in the treatment of Type II (non-insulin-dependent) diabetic patients who fail to respond satisfactorily to diet therapy and physical exercise. Although the precise mechanisms of action of these compounds are still poorly understood, there is sufficient agreement that sulphonylureas have both pancreatic and extrapancreatic effects, whereas biguanides have predominantly extrapancreatic actions. By using labelled compounds or measuring the circulating concentrations, the main pharmacokinetic properties of oral hypoglycaemic agents have been assessed and, in some cases, their pharmacokinetic-pharmacodynamic relationships have been evaluated. A correlation between diabetes control and plasma sulphonylurea or biguanide concentrations is generally lacking at the steady-state, with the possible exception of long-acting agents; after either oral or intravenous dosing, the reduction of plasma glucose is usually related to the increased circulating drug concentrations. The toxic effects of oral hypoglycaemic drugs are more frequent in the elderly and in the presence of conditions that may lead to drug accumulation or potentiation (increased dosage, use of long-acting compounds, hepatic and renal disease, interaction with other drugs); however, a relationship between toxic effects and drug plasma levels has been reported only for biguanides.