by G. Lee

Created on: October 01, 2007

Statins, also known as HMG-CoA reductase inhibitors, are the first line treatment for low-density lipoprotein cholesterol (LDL-C) lowering. LDL-C are known as the "bad" cholesterol, and high levels of these cholesterol in the blood is undesirable. Among the most common statins available commercially are pravastatin, simvastatin, atorvastatin and fluvastatin. Statins have been proven to reduce the risk of heart attacks and strokes in patients, as well as reduce the need for revascularization procedures in those that are at high risk of cardiovascular diseases. Statins are also likely to have other beneficial effects besides cholesterol reduction, such as anti-inflammatory effects.

Basically, statins work by inhibiting 3-hydroxy-3-methylglutaryl coenzyme A, the rate limiting enzyme in hepatic cholesterol synthesis. The cholesterol synthesis inhibition reverses the inhibitory effect of elevated hepatic cholesterol on LDL receptor synthesis. Hence, there will be a marked increase in the number of cell-surface receptors synthesized, which will promote the uptake of circulating LDL-C by the liver and enhance the hepatic uptake of very-low-density lipoprotein cholesterol (VLDL-C) and VLDL remnants. Normally LDL-C levels will be reduced by 20 to 50% in total. There are also studies that show that statins can reduce hepatic lipoprotein synthesis and may raise high-density lipoprotein cholesterol (HDL-C), the "good" cholesterol, in some patients.

Statins are primarily indicated as an adjunctive therapy to diet for the treatment of hypercholesterolemia and mixed hyperlipidemia once any secondary causes have been identified and treated. Statins are also used for the secondary prevention of heart attacks where the total cholesterol level of a patient exceeds 4.0 mmol/L. Those at high risk of coronry heart diseases with or without hypercholesterolemia, such as diabetics, can also be initiated on statins. The use of statins as a cholesterol-lowering agent is contraindicated in patients who have the following conditions: active liver disease, unexplained persistent liver function test (LFT) elevations, pregnancy or lactation.

Different statins vary in their ability to inhibit HMG-CoA reductase; hence the dosage for each different statin varies as well. For example, atorvastatin is available in 10mg, 20mg, 40mg and 80mg tablet forms while fluvastatin is only available in 20mg and 40mg capsule forms. Statins are to be taken once daily preferably in the evening because the liver

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