There is strong evidence to support a causal relationship between the level of circulating plasma cholesterol and the risk of clinically overt coronary heart disease (CHD) events. Current UK guidelines recommend reductions of total cholesterol levels to below 5.0 mmol/L. Statins remain the drugs of first choice for reducing low-density lipoproteins (LDL). Rosuvastatin has already been approved in the Netherlands and is likely to become more widely available in the next year. It has a potent effect in lowering LDL and it also appears to raise high-density lipoproteins (HDL). It has a similar safety profile compared with other statins.
Cholesterol absorption inhibitors are a new treatment option for the management of hypercholesterolaemia. Ezetimibe, the first drug in this class, has recently been approved for use in the US and Germany. It selectively inhibits the uptake of dietary and biliary cholesterol at the level of the enterocyte. The site of action of ezetimibe may be the ‘sterol permease’ transport protein. As monotherapy, the role of ezetimibe appears limited at present. However, in combination with a low-dose statin, significant reductions in plasma LDL levels are seen. It may also be a useful agent for patients with homozygous familial hypercholesterolaemia.
For UK healthcare professionals only