Gemfibrozil

DEA Class; Rx

Common Brand Names; Lopid

Indicated for the treatment of hypercholesterolemia or hyperlipoproteinemia and hypertriglyceridemia as an adjunct to diet.

Hypersensitivity

Severe liver/renal disease

Primary biliary cirrhosis

Preexisting gallbladder disease

Coadministration with repaglinide, simvastatin, selexipag, or dasabuvir

• Dyspepsia (20%)
• 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

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

Gemfibrozil may increase enzalutamide levels when administered concomitantly, which may increase risk of seizures; if coadministration necessary, reduce enzalutamide dose

There are no adequate and well-controlled studies in pregnant women; drug should be used during pregnancy only if potential benefit justifies potential risk to fetus

It is not known whether drug is excreted in human milk; because many drugs are excreted in human milk and because of potential for tumorigenicity shown for drug in animal studies, a decision should be made whether to discontinue nursing or to discontinue drug, taking into account the importance of the drug to the mother