Medicinal chemistry||B.Pharmacy||Rguhs ||Antihyperlipedemic agents

1. ANTIHYPERLIPIDEMIC
AGENTS BY
SWATHI KENCHA

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

4. SYMPTOMS OF HYPERLIPIDMIA

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.

20. THANK YOU ALL