Dosing and uses of Lopid (gemfibrozil)
Adult dosage forms and strengths
tablet
- 600mg
Hypertriglyceridemia, Hypercholesterolemia
600 mg PO q12hr
Administration: 30 min before morning & evening meals
Dosing Considerations
Monitor: Serum lipoproteins
May be beneficial for prophylaxis of cardiovascular events in at-risk patients, even if patients have normal levels of cholesterol.
Overdose management
- 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
Dosing Modifications
Renal impairment
- Mild to moderate: Use caution, if baseline serum creatine in patient is >2mg/dL; deterioration of renal function reported in such patients
- Severe: Contraindicated
Hepatic impairment
- Contraindicated
Pediatric dosage forms and strengths
Safety and efficacy not established
Lopid (gemfibrozil) adverse (side) effects
>10%
Dyspepsia (20%)
1-10%
Abdominal pain (10%)
Atrial fibrillation (1%)
Diarrhea (7%)
Fatigue (4%)
N/V (3%)
Eczema (2%)
Rash (2%)
Vertigo (2%)
Constipation (1%)
Headache (1%)
<1%
Myalgia
Rhabdomyolysis (especially with admin with statin)
Acute appendicitis
Cholelithiasis
Angioedema
Hypokalemia
Eosinophilia
Myopathy
Synovitis
Taste disturbance
Xerostomia
Flatulence
Rash
Warnings
Contraindications
Hypersensitivity
Severe liver/renal disease
Primary biliary cirrhosis
Preexisting gallbladder disease
Coadministration with repaglinide, simvastatin, or dasabuvir
Cautions
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 and lactation
Pregnancy category: C
Lactation: Not recommended
Pregnancy categories
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.
Pharmacology of Lopid (gemfibrozil)
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)
Absorption
Peak serum time: 1-2 hr
Distribution
Protein bound: 99%
Metabolism
Enterohepatic circulation
Elimination
Half-life: 1.5 hr
Excretion: Urine (70%); feces (6%)
