Anti-Hyperlipidemic Drugs

• Learn about Anti-Hyperlipidemic Drugs including statins, fibrates, and other agents used to manage cholesterol and triglycerides.
• Hyperlipidemia involves elevated levels of lipids in the blood, increasing the risk of atherosclerosis, coronary artery disease, and stroke.
• Anti-Hyperlipidemic Drugs aim to lower lipid levels, particularly low-density lipoprotein (LDL) cholesterol, and raise high-density lipoprotein (HDL) cholesterol.

Major Classes of Anti-Hyperlipidemic Drugs

1. Statins (HMG-CoA Reductase Inhibitors)

• Examples: Atorvastatin, Simvastatin, Rosuvastatin
• MOA: Inhibit HMG-CoA reductase, reducing cholesterol synthesis and upregulating LDL receptors for clearance.
• Benefits: Lower LDL, reduce cardiovascular risks, and stabilize plaques.
• Side Effects: Myopathy, rhabdomyolysis, elevated liver enzymes, GI disturbances.
• Considerations: Monitor liver enzymes and use cautiously in liver disease.

2. Ezetimibe

• Example: Ezetimibe (Zetia)
• MOA: Blocks cholesterol absorption in the intestine by inhibiting NPC1L1 protein.
• Benefits: Lowers LDL; effective alone or with statins.
• Side Effects: Diarrhea, abdominal pain, elevated liver enzymes.
• Considerations: Often combined with statins for enhanced LDL reduction.

3. Bile Acid Sequestrants

• Examples: Cholestyramine, Colestipol, Colesevelam
• MOA: Bind bile acids, promoting cholesterol conversion to bile acids and reducing LDL.
• Benefits: Lower LDL; may increase HDL slightly.
• Side Effects: GI issues (constipation, bloating), increased triglycerides, impaired vitamin absorption.
• Considerations: Separate dosing from other medications and supplement fat-soluble vitamins if needed.

4. Fibrates

• Examples: Gemfibrozil, Fenofibrate
• MOA: Activate PPAR-α, enhancing fatty acid oxidation and lipase activity to lower triglycerides and increase HDL.
• Benefits: Reduce triglycerides and raise HDL.
• Side Effects: Myopathy (especially with statins), gallstones, elevated liver enzymes.
• Considerations: Monitor liver and kidney function; caution with statin combinations.

5. Niacin (Vitamin B3)

• Example: Niacin (Nicotinic Acid)
• MOA: Reduces VLDL synthesis, lowering LDL and triglycerides while raising HDL.
• Benefits: Improves overall lipid profile.
• Side Effects: Flushing, hyperglycemia, hyperuricemia, hepatotoxicity.
• Considerations: Aspirin can reduce flushing; monitor liver function at high doses.

6. PCSK9 Inhibitors

• Examples: Alirocumab, Evolocumab
• MOA: Monoclonal antibodies inhibiting PCSK9, promoting LDL receptor recycling and LDL clearance.
• Benefits: Marked LDL reduction; effective in familial hypercholesterolemia or statin intolerance.
• Side Effects: Injection site reactions, nasopharyngitis, neurocognitive effects.
• Considerations: Given via subcutaneous injection, often combined with other therapies.

7. Omega-3 Fatty Acid Derivatives

• Examples: Icosapent Ethyl (Vascepa)
• MOA: Decrease triglyceride synthesis and VLDL production while promoting fatty acid oxidation.
• Benefits: Lower triglycerides and reduce cardiovascular risk.
• Side Effects: GI issues, elevated liver enzymes.
• Considerations: May complement statin therapy for comprehensive lipid management.

Clinical Considerations:

• Risk Assessment: Based on factors like LDL levels, cardiovascular risk, and presence of diabetes or existing atherosclerosis.
• Combination Therapy: May be necessary for optimal lipid control.
• Monitoring: Regular lipid panels, liver function tests, and assessment for muscle symptoms.
• Lifestyle Modifications: Diet, exercise, and smoking cessation are fundamental alongside pharmacotherapy.

Thank you for reading from Firsthope's notes, don't forget to check YouTube videos!