Brand and Other Names:Lopid
- Classes: Fibric Acid Agents
Dosing & Uses
Dosage Forms & Strengths
600 mg PO q12hr
Administration: 30 min before morning & evening meals
Monitor: Serum lipoproteins
May be beneficial for prophylaxis of cardiovascular events in at-risk patients, even if patients have normal levels of cholesterol.
- Adverse drug reactions from overdose may include peripheral neuropathy, diarrhea, increased K+, myopathy, rhabdomyolysis, acute renal failure, elevated LFT's, eye lens opacities
- Treatment is supportive
- Mild to moderate: Use caution, if baseline serum creatine in patient is >2mg/dL; deterioration of renal function reported in such patients
- Severe: Contraindicated
Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
Abdominal pain (10%)
Atrial fibrillation (1%)
Rhabdomyolysis (especially with admin with statin)
Severe liver/renal disease
Primary biliary cirrhosis
Preexisting gallbladder disease
Coadministration with repaglinide, simvastatin, or dasabuvir
If response inadequate after 3 months, discontinue gemfibrozil
Risk for myopathy/rhabdomyolysis increases with renal impairment
Risk for myopathy/rhabdomyolysis increases with concurrent HMG-CoA reductase inhibitors use (eg, atorvastatin, pravastatin)
If coadministered with anticoagulants, reduce anticoagulant dose and monitor prothrombin time until stabilized
Coadministration with bile acid resin binding agents decreases gemfibrozil AUC by 30%
May increase risk of malignancy
Rule out secondary causes of hyperlipidemia prior to initiating therapy; discontinue if lipid response not seen
Use with caution in patients taking warfarin; adjustments in warfarin may be required
Cases of cholelithiasis reported with gemfibrozil therapy; gemfibrozil may increase cholesterol excretion into bile; if cholelithiasis suspected, perform gallbladder studies; discontinue therapy if gallstones found
Coadministration with repaglinide shown to increase repaglinide plasma concentrations (8-fold increase); prolongs hypoglycemic effect; may result in severe hypoglycemia
Gemfibrozil inhibits CYP2C8 enzyme activity; may increase exposure of CYP2C8 substrates; consider dose reduction of CYP2C8 substrates when administered concomitantly
Gemfibrozil may increase exposure of OATP1B1 drug substrates when administered concomitantly; consider dose reduction of OATP1B1 substrates when administered concomitantly
Myopathy, including rhabdomyolysis, reported with chronic administration of colchicine at therapeutic doses; use caution, especially in the elderly and patients with renal dysfunction
Rarely, severe anemia, leukopenia, thrombocytopenia, and bone marrow hypoplasia reported; periodic blood counts are recommended during first 12 months of therapy
Elevations in serum transaminases seen with use; periodic liver function studies recommended; therapy should be terminated if abnormalities persist
Worsening renal insufficiency upon addition of therapy in individuals with baseline plasma creatinine >2.0 mg/dL reported; in such patients, consider the use of alternative therapy against risks and benefits of a lower dose of metformin
Pregnancy & Lactation
Pregnancy category: C
Lactation: Not recommended
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Inhibits peripheral lipolysis; decreases hepatic uptake of free fatty acids, which may in turn inhibit secretion of VLDL; may increase HDL-cholesterol (mechanism unknown)
Peak serum time: 1-2 hr
Protein bound: 99%
Half-life: 1.5 hr
Excretion: Urine (70%); feces (6%)
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