Unfractionated heparin (UFH) is widely used to both treat and prevent venous thromboembolism. More recently, UFH has been used to prevent death and myocardial infarction in patients with unstable angina or acute myocardial infarction and acute occlusion in those undergoing percutaneous coronary revascularization. However, its poor bioavailability (when administered in low doses subcutaneously), its mechanism of clearance, and its short half-life make its anticoagulant activity difficult to predict and maintain. To overcome these limitations, low-molecular-weight heparins (LMWHs) have been developed that have greater bioavailability and a longer half-life in plasma. Because LMWHs provide more predictable anticoagulant activity compared with subcutaneous UFH, it is not necessary to monitor the activated partial thromboplastin time during treatment. These newer agents are as effective as UFH in the prophylaxis and treatment of thromboembolic and cardiac disorders and, by allowing shorter hospital stays, are more cost effective. Thus LMWHs offer clear pharmacokinetic advantages over UFH. More studies are needed to determine the extent to which clinically available LMWHs can be used in place of UFH.