Class: Fibric acid derivative
- Tablets, oral 600 mg
Decreases blood levels of triglycerides and VLDL by decreasing their production. Also decreases cholesterol and increases HDL.
Bioavailability is 100%. T max is 1 to 2 h.Food
Maximum rate of absorption and a 50% to 60% increase in C max when administered 30 min before meals versus with meals or fasting.
Protein binding is high.
Mainly undergoes oxidation to form a hydroxymethyl and a carboxyl metabolite.
Plasma half-life is 1.5 h, biological half-life is longer because of enterohepatic circulation and reabsorption in the GI tract. Approximately 70% excreted in urine (less than 2% as unchanged); 6% excreted in feces.
Indications and Usage
Treatment of hypertriglyceridemia in adult patients with type IV or V hyperlipidemia that presents risk of pancreatitis and does not respond to diet; reduction of coronary heart disease risk in type IIb patients who have low HDL levels (in addition to elevated LDL and triglycerides) and have not responded to other measures.
Concurrent use with repaglinide; hepatic or severe renal impairment, including primary biliary cirrhosis; hypersensitivity to gemfibrozil; preexisting gallbladder disease.
Dosage and AdministrationAdults
PO 600 mg twice daily 30 min before morning and evening meals.
Store at room temperature in a tightly closed container.
Drug InteractionsBexarotene, loperamide, montelukast, tiagabine
Plasma concentrations of these agents may be elevated, increasing the pharmacologic effects and risk of adverse reactions. Monitor the clinical response and for adverse reactions. Adjust the dose of these agents as needed.Colestipol
Gemfibrozil pharmacologic effect may be decreased. Separate administration times by at least 2 h.Cyclosporine
Cyclosporine pharmacologic effect may be decreased. Monitor whole blood cyclosporine concentrations. Adjust the dose of cyclosporine as indicated and observe the patient for signs of toxicity or rejection when gemfibrozil therapy is stopped or started, respectively.HMG-CoA reductase inhibitors (eg, lovastatin)
Increases risk of rhabdomyolysis. If combined use cannot be avoided, frequently monitor for symptoms and signs of rhabdomyolysis and myopathy. If myositis is suspected or diagnosed, discontinue gemfibrozil treatment.Oral anticoagulants (eg, warfarin)
Anticoagulant effect may be increased. Monitor coagulation parameters. Adjust the anticoagulant dose as needed.Repaglinide
Repaglinide plasma concentrations may be greatly increased and prolonged, increasing the risk of severe and protracted hypoglycemia. Coadministration is contraindicated.Sulfonylureas (eg, glyburide)
Increased hypoglycemic effects may occur. Monitor blood glucose concentrations when gemfibrozil is started or stopped. Adjust the sulfonylurea dose accordingly.Thiazolidinediones (eg, pioglitazone)
The risk of hypoglycemia and other adverse reactions (eg, peripheral edema) may be increased. Monitor blood glucose concentrations and for adverse reactions when gemfibrozil is stopped or started. Adjust the thiazolidinedione dose accordingly.
Fatigue; headache; vertigo.
Abdominal pain; acute appendicitis; constipation; diarrhea; dyspepsia; nausea; vomiting.
Anemia; bone marrow hypoplasia; eosinophilia; leukopenia.
Cholestatic jaundice; elevated LFT results.
Muscle pain or weakness; myositis; rhabdomyolysis; taste perversions.
Category B .
Safety and efficacy not established.
Drug may increase cholesterol excretion into the bile, leading to cholelithiasis.
- Inform patient of the need to restrict dietary intake of fats; teach patient dietary restrictions to follow.
- Emphasize importance of the following increased cardiac risk factors: smoking, alcohol consumption, lack of exercise.
- Instruct patient to report the following symptoms to health care provider: abdominal pain, persistent nausea and vomiting, bleeding, and irregular heartbeat.
- Advise patient that drug may cause dizziness or blurred vision and to use caution while driving or performing other tasks requiring mental alertness.
Copyright © 2009 Wolters Kluwer Health.
More about gemfibrozil
- Other brands: Lopid