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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:
- Reduces Triglycerides: Enhances lipoprotein lipase activity, accelerating the breakdown of triglyceride-rich very-low-density lipoproteins (VLDL) and chylomicrons.
- 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).
- Hypertriglyceridemia:
- Management of severe hypertriglyceridemia (Fredrickson type IV/V) to prevent acute pancreatitis.
- Mixed Dyslipidemia:
- Adjunctive therapy in patients with combined elevations of triglycerides and LDL cholesterol, particularly when statins are contraindicated or ineffective (BNF).
- 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
- Statins (e.g., simvastatin, atorvastatin): ↑ Risk of myopathy (avoid combination if possible).
- Warfarin: Gemfibrozil ↑ anticoagulant effect (monitor INR closely).
- CYP2C8/CYP2C9 Substrates (e.g., repaglinide, sulfonylureas): ↑ Drug levels (risk of hypoglycaemia).
- Cyclosporine: ↑ Risk of nephrotoxicity.
- Generic Name: Gemfibrozil.
- Brand Names:
- UK: Lopid.
US: Lopid, Jezil
