Gemfibrozil

Pronunciation: jem-FYE-broe-zil
Class: Fibric acid derivative

Trade Names

Lopid
- Tablets, oral 600 mg

Pharmacology

Decreases blood levels of triglycerides and VLDL by decreasing their production. Also decreases cholesterol and increases HDL.

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Pharmacokinetics

Absorption

Bioavailability is 100%. T _max is 1 to 2 h.

Maximum rate of absorption and a 50% to 60% increase in C _max when administered 30 min before meals versus with meals or fasting.

Distribution

Protein binding is high.

Metabolism

Mainly undergoes oxidation to form a hydroxymethyl and a carboxyl metabolite.

Elimination

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.

Contraindications

Concurrent use with repaglinide; hepatic or severe renal impairment, including primary biliary cirrhosis; hypersensitivity to gemfibrozil; preexisting gallbladder disease.

Dosage and Administration

PO 600 mg twice daily 30 min before morning and evening meals.

Storage/Stability

Store at room temperature in a tightly closed container.

Drug Interactions

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.

Gemfibrozil pharmacologic effect may be decreased. Separate administration times by at least 2 h.

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.

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.

Anticoagulant effect may be increased. Monitor coagulation parameters. Adjust the anticoagulant dose as needed.

Repaglinide plasma concentrations may be greatly increased and prolonged, increasing the risk of severe and protracted hypoglycemia. Coadministration is contraindicated.

Increased hypoglycemic effects may occur. Monitor blood glucose concentrations when gemfibrozil is started or stopped. Adjust the sulfonylurea dose accordingly.

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.

Adverse Reactions

Cardiovascular

Atrial fibrillation.

CNS

Fatigue; headache; vertigo.

Dermatologic

Eczema; rash.

EENT

Blurred vision.

GI

Abdominal pain; acute appendicitis; constipation; diarrhea; dyspepsia; nausea; vomiting.

Genitourinary

Impotence.

Hematologic

Anemia; bone marrow hypoplasia; eosinophilia; leukopenia.

Hepatic

Cholestatic jaundice; elevated LFT results.

Metabolic

Mild hyperglycemia.

Miscellaneous

Muscle pain or weakness; myositis; rhabdomyolysis; taste perversions.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Cholelithiasis

Drug may increase cholesterol excretion into the bile, leading to cholelithiasis.

Patient Information

• 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.