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Antihyperlipidemic drugs play a critical role in lowering elevated lipid levels in the blood, primarily combating hyperlipidemia, a major contributor to atherosclerosis and coronary heart diseases. The treatment strategies focus on dietary management by reducing fat and cholesterol intake, enhancing cholesterol excretion, and inhibiting cholesterol biosynthesis. Key drug classes include HMG-CoA reductase inhibitors (statins) like Lovastatin and Simvastatin, bile acid-binding resins like Cholestyramine, and fibrate derivatives such as Gemfibrozil and Fenofibrate. Understanding their mechanisms is vital for effective treatment.
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Cardiovascular agents Antihyperlipidemic Drugs
Elevated concentration of lipids in blood (Hyperlipidemia), is the major cause of atherosclerosis and coronary heart diseases. Cholesterol esters and triglycerides are the constituents of lipids, so decreasing fat and cholesterol intake (diet control) and enhancing cholesterol excretion in addition to inhibition of cholesterol biosynthesis are the main aspects of the treatment strategy.
Antihypercholesterolemic This group includes HMG-CoA reductase inhibitors and bile acid binding resins. Bile Acid Binding Resins Cholestyramine It is a non-absorbable strongly basic anion exchange resin that exchange chlorides for bile acids and increases its fecal excretion.
HMG-CoA Reductase The reduction of 3-hydroxy 3-methylgluteryl-CoA by the enzyme HMG-CoA reductase
Statins 1-Lovastatin , Simvastatin
Antihypercholesterolemic and antihypertriglyceridemic drugs Fibric acid derivatives The prototype drug of this group is Clofibrate. These drugs are mainly used for hypertriglyceridemia or marked HDL deficiency. They activate lipoprotein lipase (LPL) therepy promote delivery of TGs to the adipose tissue. Fibrates also decrease cholesterol levels by inhibiting its biosythesis at step before HMg-CoA formation.Gemfibrozil and Fenofibrate are other examples of this class.
Clofibrate Ethyl -p-chlorophenoxy-isobutyrate Gemfibrozil 5-(2,5-Dimethylphenoxy)2,2-dimethyl-pentanoic acid
Fenofibrate Isopropyl -(4-(p-chlorobenzoyl)phenoxy)-isobutyrate Nicotinic acid It inhibits lipolysis in adipose tissue and activates the action of lipoprotein lipase.
Probucol Probucol is an antioxidant drug that can reduce both LDL and HDL levels
Dextrothyroxine-sodium thyroxine has the ability to decrease cholesterol level by enhancing cholesterol conversion to bile acid through stimulation of 7- -cholesterol hydroxylase.