Drugs that Reduce Elevated Blood Lipids
Statins: This is an important class of drugs which reduce formation of cholesterol by blocking enzyme (HMG COA-Reductase). Different statins differ in their potency and maximum reduction in lipid levels. In general LDL-cholesterol is reduced by 30-35% by comparable doses. HDL-cholesterol (good effect) increases by 5-15% and triglycerides reduce by 10-30%. If cholestyramine is used together, LDL-cholesterol may further reduce to 60-70% of pretreatment levels. The statins are preferably taken at night cholesterol forming enzyme has maximal activity at this time. Various drugs available are:
Adverse Effects: Mild adverse effects are nausea, headache, bowel upset and sleep disturbance. Muscle pain may occur rarely (in lout of 1000 patients). Actual myopathy may occur if Gemfibrozil or other drugs (erythromycin. ketoconazole or cyclosporine) are also taken. Liver enzymes may also increase in blood.
The 4-S Study: Scandinavian Simvastatin Survival Study (4-S) included 4444 patients with heart disease and raised serum cholesterol (> 212 mg %). Simvastatin was given to them for 6 years. The overall death rate was reduced by 30%, deaths due to heart attack were reduced by 42% and due to strokes by 30% (A remarkable feat!). Similar or larger benefits are reported by other statins in many studies. There are additional benefits of statins such as improvement in blood flow, prevention of clot formation and rupture of atheroma. Therefore statins should be used to full extent.
Combinations (Statin + Other Drugs)
A number of other drugs are combined to achieve greater cholesterol reduction [nicotinic acid + Simvastatin (SIMVOTIN TAB)] or to check atherosclerosis [Atorvastatin + Methylcobalamin + Folic acid + Vit. B6 (ATHERO CHECK tab)].
The Fibrates (Fibric Acid Derivatives)
This is another important class of drugs. Their use results in a fall in triglycerides by 20-25%, cholesterol (LDL-C) by 10-15% and, an increase in HDL-C by 10-15% and these effects are due to activation of fat metabolizing enzyme (lipo-protein lipase) and less formation of triglycerides by liver. These drugs are effective when triglycerides and cholesterol are raised. Drugs available are given in table on page 30.
Resins: Cholestyramine (Questran) and Colestipol (Colestid)
These resins bind with bile acids in the small bowel and thus allow unabsorbed bile salts and cholesterol to pass into stools. Liver tries to make more bile salts from its cholesterol and therefore levels of LDL-C decrease. Cholestyramine is given in a dose of 4 g three times a day. The granules should be made into a paste before taking. Dry powder is difficult to swallow. These drugs are unpalatable and can cause a lot of bowel upset (gases, heart burn, constipation, nausea). Loss of fat soluble vitamins can cause deficiency symptoms of Vitamin A, D, E and K. A number of drugs (warfarin, statins, digoxin) are poorly absorbed if taken together. Therefore, resins are useful as adjuncts only.
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