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CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, PLAIN › Fibrates
gemfibrozil
C10AB04
Adult Dosing
- Primary hypertriglyceridemia: 600 mg orally twice daily, administered 30 minutes before the morning and evening meals
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of adult patients with very high serum triglyceride elevations (Fredrickson Type IV and V hyperlipidemia) who present a risk of pancreatitis and do not respond adequately to a determined dietary effort
Mechanism of Action
- Fibric acid derivative that acts as a peroxisome proliferator-activated receptor alpha (PPAR-alpha) agonist, downregulating hepatic apo C-III expression and increasing apo A-I and apo A-II levels, which decreases very low-density lipoprotein (VLDL) production and increases VLDL clearance via lipoprotein lipase
Contraindications
- Pre-existing gallbladder disease
- Severe hepatic dysfunction
- Severe renal dysfunction
- Concomitant use with simvastatin
- Concomitant use with repaglinide
- Hypersensitivity to gemfibrozil
Adverse Reactions
- Dyspepsia
- Abdominal pain
- Diarrhea
- Nausea
- Fatigue
- Headache
- Eczema
- Rash
- Myopathy
- Cholelithiasis
- Elevated liver transaminases
Drug Interactions
- HMG-CoA reductase inhibitors (statins): increased risk of myopathy and rhabdomyolysis
- Repaglinide: significantly increased exposure and risk of severe hypoglycemia
- Coumarin anticoagulants (warfarin): potentiation of anticoagulant response, requiring close monitoring of INR
- Bile acid sequestrants: may bind gemfibrozil and reduce its absorption
- OATP1B1 substrates: gemfibrozil inhibits hepatic uptake transporters, increasing systemic exposure of certain drugs
Curated Content: Needs Vetting Before Put to Clinical Use