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Fenofibrate

Fenofibrate is a lipid-lowering agent primarily used to treat 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.

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

  1. Reduces Triglycerides: Enhances lipoprotein lipase activity, increasing clearance of triglyceride-rich particles (VLDL, chylomicrons).
  2. Modifies LDL Cholesterol: Shifts LDL particles to larger, less atherogenic forms.
  3. Raises HDL Cholesterol: Stimulates apolipoprotein A-I and A-II synthesis (Lippincott Textbook of Pharmacology).
  1. Hypertriglyceridemia:
    • Management of severe hypertriglyceridemia (Fredrickson type IV/V) to prevent pancreatitis.
  2. Mixed Dyslipidemia:
    • Adjuvant therapy in patients with elevated triglycerides and low HDL cholesterol, particularly when statins are insufficient (BNF).
  3. Primary Prevention:
    • May reduce cardiovascular risk in select patients with type 2 diabetes and dyslipidemia (Lange Basic & Clinical Pharmacology).
  • Adults:
    • Standard Dose: 145 mg once daily (micronized formulation).
    • Non-Micronized Formulations: 67–200 mg daily, depending on brand.
  • Renal Impairment:
    • eGFR 30–60 mL/min: Reduce dose by 50%.
    • eGFR <30 mL/min: Contraindicated.
  • Administration:
    • Take with food to enhance absorption.

Avoid concomitant bile acid sequestrants (e.g., cholestyramine); administer 1 hour before or 4–6 hours after

  • Common (≥1%):
    • Gastrointestinal disturbances (nausea, abdominal pain, diarrhea).
    • Headache, elevated liver enzymes (ALT/AST).
  • Serious (Rare):
    • Myopathy/Rhabdomyolysis: Risk increases with concurrent statins.
    • Pancreatitis: Linked to rapid triglyceride reduction.
    • Cholelithiasis: Due to increased biliary cholesterol excretion.

Hepatotoxicity: Discontinue if ALT/AST >3× ULN

  • Contraindications:
    • Severe hepatic or renal impairment (eGFR <30 mL/min).
    • Gallbladder disease, hypersensitivity to fibrates.
    • Pregnancy/lactation (avoid unless essential; potential fetal harm).
  • Monitoring:
    • Baseline LFTs and renal function: Repeat LFTs at 3–6 months.
    • Lipid Profile: Assess efficacy at 2–3 months.
    • Muscle Symptoms: Check CK if myalgia occurs.
  1. Statins (e.g., simvastatin): ↑ Risk of myopathy (avoid combination if possible).
  2. Warfarin: Fenofibrate ↑ anticoagulant effect (monitor INR closely).
  3. Cyclosporine: ↑ Risk of nephrotoxicity.
  4. Bile Acid Sequestrants: Reduce fenofibrate absorption (dose separation required).
  • Generic Name: Fenofibrate.
  • Brand Names:
    • UK: Lipantil, Supralip.

US: Tricor, Fenoglide, Antara

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