Comprehensive overview of Antihyperlipidemic Drugs

Antihyperlipidemic Drugs

Classification, Pharmacokinetics, Mechanism of Action, Indications, Adverse Effects, Contraindications, and Drug Interactions

Introduction to Antihyperlipidemic Drugs

• Used to lower lipid levels in the blood
• Aim to prevent cardiovascular diseases
• Act on different pathways involved in lipid metabolism

Classification of Antihyperlipidemic Drugs

1. Statins (HMG-CoA reductase inhibitors)
   Eg. Simvastatin, Atorvastatin
2. Fibrates (PPAR-α activators)
   Clofibrate, Gemfibrozil
3. Bile Acid Sequestrants (Resins)
   Colestipol
4. Inhibitor of Triglyceride Synthesis
   Nicotinic Acid (Niacin)
5. Other Agents
   Omega Fatty Acids

Mechanism of Action of Statins
Inhibit HMG-CoA reductase enzyme

• Reduce cholesterol synthesis in the liver
• Increase LDL receptor expression → enhanced LDL clearance
• Decrease plasma LDL and total cholesterol levels

Indications of Statins

• Hypercholesterolemia
• Prevention of cardiovascular diseases
• Post-myocardial infarction patients

Adverse Effects of Statins

• Muscle pain (myopathy, rhabdomyolysis in severe cases)
• Hepatotoxicity (monitor liver enzymes)
• Gastrointestinal disturbances

Contraindications of Statins

• Pregnancy and lactation
• Active liver disease
• Drug interactions (e.g., CYP3A4 inhibitors increase statin levels)

Mechanism of Action of Fibrates

• Activate PPAR-α receptors
• Increase lipoprotein lipase activity → enhances triglyceride breakdown
• Decrease VLDL and increase HDL levels

Contraindications of Fibrates

• Hypertriglyceridemia
• Type III hyperlipoproteinemia

Adverse Effects of Fibrates

• Gallstone formation
• Myopathy (increased risk when combined with statins)
• Gastrointestinal disturbances

Contraindications of Fibrates

• Severe hepatic or renal dysfunction
• Gallbladder disease
• Drug interactions (increased risk of myopathy with statins)

Mechanism of Action of Bile Acid Sequestrants

• Bind bile acids in the intestine → prevent reabsorption
• Increase conversion of cholesterol to bile acids → lowers LDL levels

Indications of Bile Acid Sequestrants

• Hypercholesterolemia (adjunct therapy)
• Used in patients who cannot tolerate statins

Adverse Effects of Bile Acid Sequestrants

• Constipation and bloating
• Interference with fat-soluble vitamin absorption (A, D, E, K)

Contraindications of Bile Acid Sequestrants

• Bowel obstruction
• Severe hypertriglyceridemia

Mechanism of Action of Nicotinic Acid (Niacin)

• Inhibits triglyceride synthesis in the liver
• Reduces VLDL and LDL levels
• Increases HDL levels

Indications of Nicotinic Acid

• Hypertriglyceridemia
• Combined hyperlipidemia

Adverse Effects of Nicotinic Acid

• Flushing and itching (prostaglandin-mediated, reduced by aspirin)
• Hepatotoxicity
• Hyperuricemia (may exacerbate gout)

Contraindications of Nicotinic Acid

• Peptic ulcer disease
• Severe liver disease
• Gout

Role of Omega Fatty Acids in Lipid Management

• Reduce triglyceride levels
• Anti-inflammatory properties
• Cardioprotective effects

Presentation for Antihyperlipidemic Drugs

                                                                      END OF THE CHAPTER

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