Antihyperlipidemic Drugs

 

Antihyperlipidemic drugs are medications used to manage elevated levels of lipids in the blood, such as cholesterol and triglycerides, to reduce the risk of cardiovascular disease. Here are some common classes of antihyperlipidemic drugs along with examples.

1. Statins (HMG-CoA Reductase Inhibitors)

• Mechanism: Inhibit HMG-CoA reductase, an enzyme involved in cholesterol synthesis in the liver, leading to reduced cholesterol levels, especially LDL-C (low-density lipoprotein cholesterol).
• Examples:
• Atorvastatin (Lipitor)
• Simvastatin (Zocor)
• Rosuvastatin (Crestor)
• Pravastatin (Pravachol)
• Lovastatin (Mevacor)

2. Fibrates

• Mechanism: Activate peroxisome proliferator-activated receptors (PPARs), which increase the oxidation of fatty acids and reduce triglyceride levels while modestly increasing HDL-C (high-density lipoprotein cholesterol).
• Examples:
• Fenofibrate (Tricor)
• Gemfibrozil (Lopid)
• Clofibrate (Atromid-S

3. Bile Acid Sequestrants (Resins)

Mechanism: 

Bind bile acids in the intestine, preventing their reabsorption, which in turn causes

the liver uses more cholesterol to produce bile acids, reducing blood cholesterol levels.

Examples:

Cholestyramine (Questran)

Colestipol (Colestid)

Colesevelam (Welchol)

4. Niacin (Nicotinic Acid)

Mechanism

Inhibits lipolysis in adipose tissue, reducing the synthesis of VLDL (very low-density

lipoprotein) and LDL, while also increasing HDL levels.

Examples:

Niacin (Niaspan, Niacor)

Note: Niacin is often used in combination with other lipid-lowering agents.

5. Cholesterol Absorption Inhibitors

Mechanism: 

Inhibit the absorption of cholesterol from the small intestine, reducing the amount of

cholesterol that enters the bloodstream.

Example:

Ezetimibe (Zetia)

Combination: Ezetimibe + Simvastatin (Vytorin)

6. Omega-3 Fatty Acids

Mechanism:

Reduce triglyceride levels by decreasing hepatic production of triglycerides and

VLDL.

Example:

Omega-3-acid ethyl esters (Lovaza)

Icosapent ethyl (Vascepa)

7. PCSK9 Inhibitors

Mechanism:

Monoclonal antibodies that inhibit the protein PCSK9, which increases the number of

LDL receptors on the liver surface, enhancing the clearance of LDL from the bloodstream.

Example:

Alirocumab (Praluent)

Evolocumab (Repatha)

8. Selective Peroxisome Proliferator-Activated Receptor (PPAR) Agonists

Mechanism:

Specifically, activate PPAR-alpha to reduce triglycerides and increase HDL.

Example:

Pemafibrate (Parmodia)

9. Bempedoic Acid

Mechanism:

Inhibits ATP citrate lyase, an enzyme involved in cholesterol synthesis upstream of

HMG-CoA reductase, reducing LDL cholesterol levels.

Example:

Bempedoic acid (Nexletol)

10. Combination Therapies

Mechanism:

Combine drugs with complementary mechanisms to enhance lipid-lowering effects.

Example:

Ezetimibe + Atorvastatin (Liptruzet)

Simvastatin + Niacin (Simcor)

Conclusion:

These antihyperlipidemic drugs target different pathways in lipid metabolism to effectively reduce cholesterol and triglyceride levels, with the goal of reducing the risk of atherosclerosis and cardiovascular events. The choice of therapy depends on the patient's lipid profile, risk factors, and tolerance to medications.

Download PDF Here