Drug therapy may need to be initiated when target lipid levels are not achieved with diet alone. Most patients with a genetic form of hyperlipidaemia will need to take drugs in addition to following a diet. The effects of diet and drugs are independent and additive; consumption of an appropriate diet can reduce the dose of drug required. Drug therapy may also be of value in patients with established coronary artery disease; recent trials have demonstrated that the progression of atherosclerotic lesions can be halted or even regress with substantial lowering of plasma lipid levels. A complete review of the available lipid-lowering drugs and their indications, dosages, and side effects is beyond the scope of this chapter. An understanding of their mechanisms of action is, however, useful and provides important insights into their use.