Controlled-release drug delivery technology has had a significant effect on the pharmacotherapy of cardiovascular diseases. Oral and transcutaneous controlled-release systems allow relatively short-acting drugs to be administered once or twice daily with comparable therapeutic efficacy and fewer adverse reactions compared with standard formulations. They can provide decreased fluctuations in drug concentrations in plasma while possibly reducing the total amount of drug necessary for a clinical response. Techniques include the diffusion, bioerosion or degradation, and generation of osmotic pressure in orally active and transcutaneous drug delivery systems. Calcium-channel blocking agents, nitrates, beta-blocking agents, antiarrhythmic agents, clonidine, and nicotinic acid can be administered by these techniques, which have greatly influenced the application of these drugs in clinical practice.