This document discusses anti-hyperlipidemic drugs, which lower lipid and lipoprotein levels in the blood to prevent cardiovascular disease. It describes 5 classes of these drugs: statins, bile acid sequestrants, fibrates, nicotinic acid, and ezetimibe. Statins like lovastatin work by inhibiting HMG-CoA reductase to reduce cholesterol synthesis. Fibrates activate lipoprotein lipase to lower triglycerides. Bile acid sequestrants form insoluble complexes with bile acids to increase their excretion.

1. Anti-hyperlipidemic drugs
These are drugs which lower the levels of
lipids and lipoproteins in blood. The
hypolipidaemic drugs have attracted
considerable attention because of their
potential to prevent cardiovascular disease by
retarding the accelerated atherosclerosis in
hyperlipidaemic individuals.

2. Lipoproteins are of 4 types:
 High density lipoprotein
(HDL)
 Low density lipoprotein
(LDL)
 Intermediate density
lipoprotein (IDL)
 Very low density lipoprotein
(VLDL)

3. CLASSIFICATION:
1. HMG-CoA reductase inhibitors (Statins):
Lovastatin, Simvastatin, Pravastatin, Atorvastatin,
Rosuvastatin, Pitavastatin
2. Bile acid sequestrants (Resins): Cholestyramine,
Colestipol
3. Lipoprotein lipase activators (PPARα activators,
Fibrates): Clofibrate, Gemfibrozil, Bezafibrate,
Fenofibrate.
4. Lipolysis and triglyceride synthesis inhibitor:
Nicotinic acid.
5. Sterol absorption inhibitor: Ezetimibe.

5. Lovastatin:
• It is the first clinically used statin; is lipophilic and
given orally in the precursor lactone form.
Absorption is incomplete and first pass
metabolism is extensive. Metabolites are
excreted mainly in bile. The t½ is short (1–4
hours).
• competitively inhibit conversion of 3-Hydroxy-3-
methyl glutaryl coenzyme A (HMG-CoA) to
mevalonate (rate limiting step in CH synthesis) by
the enzyme HMG-CoA reductase

7. Adverse effects:
All statins are remarkably well tolerated;
Gastrointestinal complaints and headache are usually mild.
Rashes and sleep disturbances are uncommon.
Rise in serum transaminase can occur, but liver damage is rare.
Monitoring of liver function is recommended.
Uses: Statins are the first choice drugs for primary
hyperlipidaemias with raised LDL and total CH levels, with or
without raised TG levels, as well as for secondary (diabetes,
nephrotic syndrome) hypercholesterolaemia

8. . Lipoprotein lipase activators (PPARα
activators, Fibrates):
• The fibrates (isobutyric acid derivatives) primarily
activate lipoprotein lipase which is a key enzyme in
the degradation of VLDL resulting in lowering of
circulating TGs. This effect is exerted through
peroxisome proliferator-activated receptor α (PPARα)
that is a gene transcription regulating receptor
expressed in liver, fat and muscles. Activation of
PPARα enhances lipoprotein lipase synthesis and
fatty acid oxidation.

9. Clofibrate

10. BILE ACID SEQUESTRANTS (Resins):
Cholestyramine and Colestipol:
• Mechanism of actions:
•They are insoluble non-absorbable basic anion exchange
resins which bind with bile acids and form insoluble
complexes in the intestine which gets excreted in faces.
• Adverse Drug Reactions:
 Head ache, Vomiting
 Constipation, Heart burn are common
• Therapeutic Uses:
 Cholestyramine is used as an anti-hyperlipidaemic in
children and
• pregnant women.
 It is also used in treating pruritus associated with biliary
cirrhosis and cholestatic jaundice.