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Statins - HMG-CoA reductase inhibitors
Cholesterol is a waxy, fatlike substance that your body needs to function normally. Cholesterol is naturally present in cell walls or membranes everywhere in the body, including the brain, nerves, muscles, skin, liver, intestines, and heart. Your body uses cholesterol to produce many hormones, vitamin D, and the bile acids that help digest fat. Several drugs and diseases can bring about high cholesterol, but for most people, a high-fat diet, obesity, a sedentary lifestyle, smoking, excessive alcohol consumption, or inherited risk factors are the main causes. Why is high cholesterol a health risk? Having high cholesterol is a risk factor for heart disease. A healthy artery has a smooth, even surface. When too much cholesterol builds up in the wall of your arteries thick deposits, called plaque, form. The buildup of plaque narrows the artery, so your heart must work harder to force blood through. Plaques can limit or block the blood flow in the artery. They can also rupture and form blood clots. When either happens in a major artery supplying the heart or brain, the blood flow can be completely blocked. The result can be a heart attack or stroke. Statins (HMG-CoA reductase inhibitors) Statin drugs (HMG-CoA reductase inhibitors) are a class of hypolipidemic agents. Statins inhibit the enzyme HMG-CoA reductase, which controls the rate of cholesterol production in the body. These drugs lower cholesterol by slowing the production of cholesterol and by increasing the liver's ability to remove the “bad” cholesterol (low-density lipoprotein) already in the blood. Statins are used to lower cholesterol levels in people at risk for cardiovascular disease because of hypercholesterolemia (high cholesterol). Statin drugs are considered a first-line therapy for the treatment of high cholesterol. The drugs in this class are associated with few side effects and are the most effective drugs for lowering total and LDL cholesterol levels. Statins have been studied extensively and overall have been proven to decrease the risk of heart attack, stroke, and other coronary artery diseases that are related to high cholesterol levels. They also modestly increase the “good” cholesterol (high-density lipoprotein) and decrease total cholesterol and triglycerides. Statins are medications available only by prescription (Rx). In comparison to other classes of cholesterol lowering drugs, the statins are the most effective for lowering LDL. Statins produce about a 25% to 55% reduction in levels of LDL cholesterol, a 5% to 15% increase in HDL cholesterol levels, and a 10% to 25% reduction in triglyceride levels. The relative efficacy of the statins for lowering LDL cholesterol and triglyceride levels is as follows: rosuvastatin has the most potent effect, followed by atorvastatin, simvastatin, pravastatin, lovastatin, and fluvastatin. The ability to lower LDL cholesterol levels is usually the most important factor to consider when choosing a statin, but other considerations include a patient's level of coronary heart disease risk, differences in side effects, drug interactions, cost, results of clinical trials, and the time of day a dose should be taken. The first results can be seen after one week of use and the effect is maximal after four to six weeks. Comparison of effects on Cholesterol levels
The statins are well tolerated with mild upper GI disturbances, myalgias and sleep disturbances as the most common side effects (10%). Serious side effects (contact your doctor as soon as possible):
Less serious side effects (usually do not need medical attention):
Pregnancy: Pregnancy Category X. Statin drugs are contraindicated during pregnancy and in nursing mothers. Interesting Facts
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