Anti-Hyperlipidemic Agents

Anti-hyperlipidemic agents lower blood lipid levels to prevent cardiovascular diseases like heart attack and atherosclerosis.

• Anti-hyperlipidemic agents are medications designed to manage abnormal lipid levels in the blood, thereby reducing the risk of atherosclerosis, coronary artery disease, and related cardiovascular events.

Pathophysiology of Hyperlipidemia

• Hyperlipidemia involves elevated levels of lipids (cholesterol and triglycerides) in the blood, which can lead to the formation of fatty deposits (plaques) in arteries.
• This process narrows and hardens arteries (atherosclerosis), increasing the risk of heart attacks, strokes, and peripheral vascular disease.

Classification of Anti-Hyperlipidemic Agents

• Anti-hyperlipidemic drugs are classified based on their primary mechanism of action:

1. Fibrates

   • Mechanism of Action:
     • Fibrates activate peroxisome proliferator-activated receptors (PPAR-α), leading to increased oxidation of fatty acids in the liver and muscle. This results in decreased triglyceride levels and, to a lesser extent, increased high-density lipoprotein (HDL) cholesterol.
   • Common Drugs:
     • Clofibrate
   • Uses:
     • Primarily used to reduce triglyceride levels.
     • Can also modestly increase HDL cholesterol.
   • Side Effects:
     • Gastrointestinal disturbances (e.g., abdominal pain, nausea).
     • Increased risk of gallstones.
     • Myopathy, especially when combined with statins.

2. Statins

   • Mechanism of Action:
     • Statins inhibit HMG-CoA reductase, the key enzyme in cholesterol synthesis in the liver. This leads to decreased low-density lipoprotein (LDL) cholesterol levels and upregulation of LDL receptors, enhancing clearance of LDL from the bloodstream.
   • Common Drugs:
     • Lovastatin
   • Uses:
     • Lowering LDL cholesterol.
     • Reducing the risk of cardiovascular events (e.g., myocardial infarction, stroke).
     • Stabilizing atherosclerotic plaques.
   • Side Effects:
     • Myalgia and myopathy.
     • Elevated liver enzymes.
     • Increased risk of diabetes mellitus.
     • Gastrointestinal issues (e.g., constipation, diarrhea).

3. Bile Acid Sequestrants

   • Mechanism of Action:
     • These agents bind bile acids in the intestine, preventing their reabsorption. The liver responds by converting more cholesterol into bile acids, thereby lowering circulating cholesterol levels.
   • Common Drugs:
     • Cholestyramine
     • Colestipol
   • Uses:
     • Lowering LDL cholesterol.
     • Reducing triglyceride levels.
     • Increasing HDL cholesterol (to a minor extent).
   • Side Effects:
     • Gastrointestinal disturbances (e.g., constipation, bloating).
     • Interference with the absorption of fat-soluble vitamins (A, D, E, K).
     • May bind other medications, reducing their efficacy.

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