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Antihyperlipidemic agents

This document discusses antihyperlipidemic agents used to treat hyperlipidemia, a condition of high lipid levels in the blood. It begins by defining hyperlipidemia and describing its causes such as diet, genetics, and medical conditions. It then covers the main classes of antihyperlipidemic drugs like HMG CoA inhibitors, fibrates, bile acid sequesterants, and their mechanisms and examples like lovastatin, atorvastatin, clofibrate, and cholestyramine. The document concludes by explaining how these drugs work to lower lipid levels through inhibiting cholesterol synthesis and absorption or increasing lipid catabolism.

Education◦
ANTIHYPERLIPIDEMIC AGENTS BY SWATHI KENCHA
INTRODUCTION • What is hyperlipidemia? • A condition in which there are high levels of fat particles(lipids) deposited in the blood. • Elevated plasma levels of lipids are deposited in the form of lipoproteins. Eg: lipids like cholesterol and triglycerides. • These lipids can deposit in blood vessel walls and restrict blood flow. • This creates a risk of heart attack & stroke.
CAUSES OF HYPERLIPIDEMIAS • Diet & Hereditary factors • Hypothyroidism • Nephrotic syndrome • Anorexia nervosa • Systemic lupus erythematousus • Obesity,Alcohol consumption & smoking • Diabetes • Pregnancy • Obstructive liver disease, Acute hepatitis
SYMPTOMS OF HYPERLIPIDMIA
ANTIHYPERLIPIDEMICS • The clinically important lipoproteins are HDL,LDL and VLDL . • Antihyperlipidemics are the drugs used to reduce the deposited levels of cholesterol and other lipoproteins from the blood plasma .
CLASSIFICATION • HMG CoA Inhibitors – Lovastatin,Atorvastatin • Fibrates – Clofibrate,Fenofibrate • Bile acid sequesterants – Cholestyramine,colestipol • LDL Oxidation inhibitors –Probucol • Pyridine derivatives –Nicotinamide,Nicotinic acid • Cholesterol absorption inhibitors –Ezetimibe • Miscellaneous –β-sitosterol,Dextrothyroxine
LOVASTATIN Uses:HMG CoA reductase inhibitor Side effects – Headache,Myositis,nausea,sleep disturbance, contraindications in pregnancy
ATORVASTATIN Uses:HMG CoA reductase inhibitor It prevents ischemia by inhibiting both deposition of lipids and decreases inflammation
CLOFIBRATE Uses:Reduces VLDL To treat hyperlipoproteinemia.
FENOFIBRATE Uses:Reduces the fatty substances like Cholesterol and VLDL Increases the amounts of HDL
CHOLESTYRAMINE Uses: To treat type II a hyperlipoproteinemia.
COLESTIPOL Uses:Reduces cholesterol levels To treat Type II hyperlipoproteinemias.
PROBUCOL Uses:It is used to treat high cholesterol levels in the blood Anticholesteremic drug with antioxidant and anti- inflammatory properties.
Nicotinamide & Nicotinic acid Uses:In high doses reduces low density lipoprotein,cholesterol and increases the amount of HDL in blood
EZETIMIBE Uses:It inhibits the cholesterol absorption in the body So it reduces the amount of cholesterol
β-Sitosterol & Dextrothyroxine Uses:Dextrothyroxine is a thyroid hormone having antihyperlipidemic activity. β-Sitosterol reduces cholesterol levels
MECHANISMS • Lovastatin regulates cholesterol synthesis in the liver by inhibiting microsomal reduction of 3-hydroxy 3-methyl glutaryl CoA (HMG Co A) catalyzed by HMGCoA reductase. • Colestyramine & Colestepol – The reduction in the amounts of reabsorbed bile acids results in increased catabolism of cholesterol in bile acids in the liver.Then it decreases concentration of bile acids.
• Fibrates inhibit triglyceride synthesis ,reduces VLDL release into circulation.This drug increases lipoprotein lipase activity,which catabolises the chylomicrons and VLDL.
• Probucol lowers the levels of cholesterol in the blood by increasing the rate of LDL catabolism.Probucol is a powerful antioxidant which inhibits the oxidation of cholesterol. • Nicotinic acid and Nicotinamide inhibits a hormone- sensitive lipase in adipose tissue which reduces the breakdown of triglycerides to free fatty acids,and the transport of free fatty acids to the liver. • Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine.
THANK YOU ALL