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Antihyperlipidemic agents - Comment

2. 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.
3. 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
5. 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 .
6. 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
7. LOVASTATIN Uses:HMG CoA reductase inhibitor Side effects – Headache,Myositis,nausea,sleep disturbance, contraindications in pregnancy
8. ATORVASTATIN Uses:HMG CoA reductase inhibitor It prevents ischemia by inhibiting both deposition of lipids and decreases inflammation
9. CLOFIBRATE Uses:Reduces VLDL To treat hyperlipoproteinemia.
10. FENOFIBRATE Uses:Reduces the fatty substances like Cholesterol and VLDL Increases the amounts of HDL
11. CHOLESTYRAMINE Uses: To treat type II a hyperlipoproteinemia.
12. COLESTIPOL Uses:Reduces cholesterol levels To treat Type II hyperlipoproteinemias.
13. PROBUCOL Uses:It is used to treat high cholesterol levels in the blood Anticholesteremic drug with antioxidant and anti- inflammatory properties.
14. Nicotinamide & Nicotinic acid Uses:In high doses reduces low density lipoprotein,cholesterol and increases the amount of HDL in blood
15. EZETIMIBE Uses:It inhibits the cholesterol absorption in the body So it reduces the amount of cholesterol
16. β-Sitosterol & Dextrothyroxine Uses:Dextrothyroxine is a thyroid hormone having antihyperlipidemic activity. β-Sitosterol reduces cholesterol levels
17. 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.
18. • Fibrates inhibit triglyceride synthesis ,reduces VLDL release into circulation.This drug increases lipoprotein lipase activity,which catabolises the chylomicrons and VLDL.
19. • 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.

Posted by :  peter88 Post date :  2020-10-19 22:54
Category :  Health & Medicine Views :  217

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