Cholesterol is present in tissues and in plasma either as free cholesterol or as storage form.Cholesterol synthesis is extramitochondrial.

Biosynthesis of cholesterol is divided into five steps. a) Biosynthesis of mevalonate from Acetyl CoA two molecules of acetyl-CoA condense to form acetoacetyl-CoA catalyzed by cytosolic thiolase. Acetoacetyl-CoA condenses with a further molecule of acetyl-CoA catalyzed by HMG-CoA synthase to form HMG-CoA, which is reduced to mevalonate by NADPH catalyzed by HMG-CoA reductase.This is an integral part in the regulation of cholesterol synthesis in that is the site of action of HMG-CoA reductase inhibitors (statins) a class of drugs which are used to lower cholesterol levels.

Some of the drugs that act as anti-cholesterol drugs function through different ways as shown below: They mainly function through blocking the formation of cholesterol at different stages of the biosynthetic pathway e.g. Statins drugs such as atorvastatin, simvastatin, and pravastatin inhibit HMG-CoA reductase thus up regulating LDL receptors.Statins inhibit HMG-CoA reductase in part by mimicking the structure of mevalonate thus inhibit cholesterol synthesis. Cholesterol absorption inhibitor drugs such as Zetia or ezetimibe lowers cholesterol by preventing absorption of cholesterol in the small intestine. Selective cholesterol inhibitors

are effective in lowering LDL cholesterol but have modest effects in lowering triglycerides and raising HDL cholesterol. Resins or bile acid binding drugs such as cholestarymine resin act by blocking the reabsorption of bile acids i.e. through preventing their digestion; this causes an increase in bile acid synthesis in the liver. In response the liver makes more bile which increases cholesterol excretion and up regulates the LDL receptors. Thus lowering the plasma cholesterol in circulation in the blood stream. Hypocholesterolemic agents such as sitosterol acts by blocking the absorption of cholesterol from the gastrointestinal tract. Aspirin is considered as a drug with capability properties of lowering cholesterol levels by preventing the formation of plaque caused by deposition of cholesterol in the blood vessels of the heart i.e. leading to reduction in arteriosclerosis. Aspirin has its disadvantage in that it acts like an anti-coagulant thus preventing platelet aggregation.