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Gemfibrozil

Gemfibrozil is a fibrate medication primarily used to manage hypertriglyceridemia and mixed dyslipidemia. This article details its mechanism of action, clinical uses, dosing guidelines, side effects, precautions, drug interactions, and generic/brand names, referencing the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.

Gemfibrozil activates peroxisome proliferator-activated receptor alpha (PPAR-α), a nuclear receptor that regulates lipid metabolism. This activation:

  1. Reduces Triglycerides: Enhances lipoprotein lipase activity, accelerating the breakdown of triglyceride-rich very-low-density lipoproteins (VLDL) and chylomicrons.
  2. Modifies Cholesterol Profile:
    • Increases high-density lipoprotein (HDL) cholesterol by stimulating apolipoprotein A-I and A-II synthesis.
    • Shifts low-density lipoprotein (LDL) particles to larger, less atherogenic forms (Lippincott Textbook of Pharmacology).
  1. Hypertriglyceridemia:
    • Management of severe hypertriglyceridemia (Fredrickson type IV/V) to prevent acute pancreatitis.
  2. Mixed Dyslipidemia:
    • Adjunctive therapy in patients with combined elevations of triglycerides and LDL cholesterol, particularly when statins are contraindicated or ineffective (BNF).
  3. Primary Prevention:
    • May reduce cardiovascular risk in select patients with type 2 diabetes and dyslipidemia (Lange Basic & Clinical Pharmacology).
  • Adults:
    • Standard Dose: 600 mg twice daily, taken 30 minutes before morning and evening meals.
  • Renal Impairment:
    • Contraindicated in severe renal impairment (eGFR <30 mL/min/1.73m²).
    • Use with caution in moderate renal impairment (eGFR 30–60 mL/min/1.73m²).
  • Administration:
    • Administer with water before meals to enhance absorption.
    • Avoid concurrent bile acid sequestrants (e.g., cholestyramine); separate doses by 2 hours.
  • Common (≥1%):
    • Gastrointestinal disturbances (dyspepsia, abdominal pain, diarrhoea).
    • Headache, fatigue, or dizziness.
  • Serious (Rare):
    • Myopathy/Rhabdomyolysis: Increased risk with concurrent statins.
    • Cholelithiasis: Due to increased biliary cholesterol excretion.
    • Hepatotoxicity: Discontinue if ALT/AST >3× upper limit of normal (ULN).

Pancreatitis: Linked to rapid triglyceride reduction

  • Contraindications:
    • Severe hepatic or renal impairment.
    • Gallbladder disease, primary biliary cirrhosis.
    • Hypersensitivity to fibrates.
  • Pregnancy/Lactation:
    • Avoid in pregnancy (Category C: potential fetal risk) and breastfeeding (excretion in milk unknown).
  • Monitoring:
    • Baseline liver function tests (LFTs) and renal function: Repeat LFTs every 3–6 months.
    • Lipid Profile: Assess efficacy after 3 months.

Creatine Kinase (CK): Check if myalgia or muscle weakness occurs

  1. Statins (e.g., simvastatin, atorvastatin): ↑ Risk of myopathy (avoid combination if possible).
  2. Warfarin: Gemfibrozil ↑ anticoagulant effect (monitor INR closely).
  3. CYP2C8/CYP2C9 Substrates (e.g., repaglinide, sulfonylureas): ↑ Drug levels (risk of hypoglycaemia).
  4. Cyclosporine: ↑ Risk of nephrotoxicity.
  • Generic Name: Gemfibrozil.
  • Brand Names:
    • UK: Lopid.

US: Lopid, Jezil

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