HMG-coA reductase inhibitors

HMG-coA reductase inhibitors, also known as statins, are a class of drugs that are used primarily to help reduce the body’s natural production of cholesterol. These drugs work by interrupting specific metabolic pathways, effectively blocking the HMG-coA enzyme that causes the body to produce cholesterol.

Most of the cholesterol and other lipids found in the body form as a result of a chemical metabolic process known as the mevalonate process. During this process, an intermediate coenzyme called HMG-coA is converted into cholesterol through a catalytic conversion made possible by the HMG-coA reductase enzyme. HMG-coA reductase inhibitors work by preventing HMG-coA reductase from catalyzing HMG-coA into cholesterol. In essence, these statin drugs act as a roadblock in the mevalonate pathway, inhibiting the catalytic action of HMG-coA reductase.

HMG-coA reductase inhibitors generally are prescribed in those individuals who have high levels of the cholesterol known as LDL, or low-density lipoproteins, which cannot be reduced through diet alone. LDL has been linked to a high risk of heart disease and stroke.

Some studies have indicated regular use of HMG-coA reductase inhibitors can reduce LDL levels by 18% to 55% in some patients, and increase HDL levels by 5% - 15%. Additional research has indicated these drugs may help the body reabsorb cholesterol that has accumulated on artery walls. For these reasons, physicians often prescribe these HMG-coA reductase inhibitors in patients who are at increased risk for heart disease from genetic or other factors. These drugs are also frequently prescribed for men and women who have had heart attacks, to help prevent the occurrence of a subsequent attack.

In addition to lowering LDL, research has indicated HMG-coA reductase inhibitors may employ other mechanisms to aid in the prevention of atherosclerosis. Even in individuals without high cholesterol, these drugs have been associated with a decreased risk of stroke and heart attack. More recent research has linked these drugs with a significant reduction in the risk of prostate cancer, prostate enlargement, impotence and incontinence in older male patients.

HMG-coA reductase inhibitor drugs are divided into two main groups: those which are derived through fermentation of foods, such as rice and yeast, and those which are synthetically manufactured. A third group relies on a combination of an HMG-coA reductase inhibitor agent and a secondary agent, which may help improve the efficacy profile or result in a reduction of potential side effects.

The following is a list of generic and trade names of statin medications currently available:

Fermentation-derived agents
· Lovastatin, sold under the trade names Mevacor, Altocor, and Altoprev
· Pravastatin, sold under the trade names Pravachol, Selektine, and Lipostat
· Simvastatin, sold under the trade names Zocor and Lipex
· Mevastatin; this agent is associated with a large number of side effects, and is not currently being marketed; however, it is used in the production of pravastatin

Synthetic agents
· Atorvastatin, sold under the trade names Lipitor and Torvast
· Fluvastatin, sold under the trade names Lescol and Lescol XL
· Pitavastatin, sold under the trade names Livalo and Pitava
· Rosuvastatin, sold under the trade name Crestor
· Cerivastatin, sold under the trade names Lipobay and Baycol, was withdrawn from the market in 2001 due to serious side effects

Combination agents
· Simvastatin and Ezetimibe, sold under the trade name Vytorin
· Lovastatin and Niacin extended release, sold under the trade name Advicor
· Atorvastatin and Amlodipine, sold under the trade name Caduet
· Simvastatin and Niacin extended release, sold under the trade name Simcor

Adverse effects

Most HMG coA reductase inhibitors are well tolerated. Serious but rare side effects include liver damage and musculoskeletal pain or damage. In 2001, drugs derived from the HMG-coA reductase inhibitor cerivostatin were recalled due to a serious risk of rhabdomyolosis, a condition which causes the rapid breakdown of skeletal muscle tissue. Both pravastatin and fluvastatin involve less muscle penetration, and hence are associated with the lowest risk of this condition. Combining HMG-coA reductase inhibitors with fibrates, another class of cholesterol drugs, can increase the risk for rhabdomyolosis significantly. Because grapefruit and grapefruit products can inhibit the metabolism of HMG-coA reductase inhibitors and other statins, most patients are advised to avoid these products while undergoing statin therapy.

Search for HMG-coA reductase inhibitor Drug Prices

Back To Prescription Drug Information Main Page