Skip to main content

Gemfibrozil (Monograph)

Brand name: Lopid
Drug class: Fibric Acid Derivatives
VA class: CV350
Chemical name: 5-(2,5-Dimethylphenoxy)-2,2-dimethylpentanoic acid
Molecular formula: C15H22O3
CAS number: 25812-30-0

Medically reviewed by on Jul 17, 2023. Written by ASHP.


Antilipemic agent; fibric acid derivative.

Uses for Gemfibrozil

Prevention of Cardiovascular Events

Adjunct to dietary therapy to reduce the risk of developing CHD in patients with type IIb hyperlipoproteinemia without clinical evidence of CHD (primary prevention) who have an inadequate response to dietary management, weight loss, exercise, and drugs known to reduce LDL-cholesterol and increase HDL-cholesterol (e.g., bile acid sequestrants, niacin) and who have low HDL-cholesterol concentrations in addition to elevated LDL-cholesterol and triglycerides.

Potential benefit unlikely to outweigh potential risks in patients with type IIa hyperlipoproteinemia and elevations of LDL-cholesterol only (because of toxicity, including malignancy, gallbladder disease, abdominal pain leading to appendectomy and other abdominal surgeries, and increased incidence of noncardiovascular and all-cause mortality, associated with the chemically and pharmacologically similar drug clofibrate [no longer commercially available in US]).

Manufacturer states that gemfibrozil is not indicated for use in the management of patients with low HDL-cholesterol as their only lipid abnormality (isolated low HDL-cholesterol).

Reduction of recurrent coronary events [off-label], including death from coronary causes, MI, and stroke in men with clinical evidence of CHD who have low HDL-cholesterol and moderately elevated LDL-cholesterol concentrations.

AHA/ACC cholesterol management guideline states that lifestyle modification is the foundation of cardiovascular risk reduction. If pharmacologic therapy is needed, statins are first-line drugs of choice because of their demonstrated benefits in reducing risk of atherosclerotic cardiovascular disease (ASCVD). Nonstatin drugs may be considered as adjunctive therapy in certain high-risk patients, but other drugs (e.g., ezetimibe) are generally recommended. Although fibrates have mild LDL-lowering effects, randomized controlled studies do not support their use as add-on therapy to statins.

If fibrate therapy is necessary in a statin-treated patient, AHA/ACC states that it is safer to use fenofibrate than gemfibrozil because of lower risk of severe myopathy.


Adjunct to dietary therapy in the management of severe hypertriglyceridemia in patients at risk of developing pancreatitis (typically those with serum triglyceride concentrations >2000 mg/dL and elevated concentrations of VLDL-cholesterol and fasting chylomicrons) who do not respond adequately to dietary management.

Also may be used in patients with triglyceride concentrations of 1000–2000 mg/dL who have a history of pancreatitis or of recurrent abdominal pain typical of pancreatitis; however, efficacy in patients with type IV hyperlipoproteinemia and triglyceride concentrations >1000 mg/dL who exhibit type V patterns subsequent to dietary or alcoholic indiscretion has not been adequately studied.

Manufacturer states that gemfibrozil is not indicated for use in patients with type I hyperlipoproteinemia who have elevated triglyceride and chylomicron concentrations but normal VLDL-cholesterol concentrations.

Effective in a very limited number of patients with type III hyperlipoproteinemia [off-label] to decrease elevated triglyceride and cholesterol concentrations associated with this disorder.

Gemfibrozil Dosage and Administration



Oral Administration

Administer orally twice daily, 30 minutes before the morning and evening meals.



Prevention of Cardiovascular Events

600 mg twice daily.

Monitor lipoprotein concentrations periodically. Discontinue therapy in patients who fail to achieve an adequate response after 3 months of therapy.


600 mg twice daily.

Monitor lipoprotein concentrations periodically. Discontinue therapy in patients who fail to achieve an adequate response after 3 months of therapy.

Cautions for Gemfibrozil





May increase cholesterol excretion in bile, resulting in cholelithiasis. Cholecystitis and cholelithiasis reported. Discontinue therapy if gallbladder studies indicate the presence of gallstones.

Musculoskeletal Effects

Use may be associated with myositis. Myalgia, myopathy, myasthenia, painful extremities, arthralgia, synovitis, and rhabdomyolysis reported. Myopathy, rhabdomyolysis, and other complications also reported in patients receiving gemfibrozil concomitantly with certain other antilipemic agents.

Monitor creatine kinase (CK, creatine phosphokinase, CPK) concentrations in patients reporting adverse musculoskeletal effects. Discontinue therapy if myositis is suspected or diagnosed.

Effect on Morbidity and Mortality

Effect on cardiovascular mortality not established. Because gemfibrozil is chemically, pharmacologically, and clinically similar to other fibric acid derivatives, some adverse effects of clofibrate (no longer commercially available in the US) such as increased incidence of cholelithiasis, cholecystitis requiring surgery, postcholecystectomy complications, malignancy, pancreatitis, appendectomy, gallbladder disease, and increased overall mortality may also apply to gemfibrozil, and the usual precautions associated with fibrate therapy should be observed.


Possible subcapsular bilateral and unilateral cataracts.

Sensitivity Reactions

Hypersensitivity Reactions

Angioedema, laryngeal edema, urticaria, rash, dermatitis, and pruritus reported.

Major Toxicities

Hematologic Effects

Mild decreases in hemoglobin, hematocrit, and leukocyte counts reported; these counts usually normalize during long-term therapy. Severe anemia, leukopenia, thrombocytopenia, and bone marrow hypoplasia have occurred rarely; eosinophilia also reported.

Monitor blood cell counts periodically during the first 12 months of therapy.

General Precautions

Hepatic Effects

Possible elevations in serum concentrations of aminotransferase (i.e., AST, ALT), LDH, bilirubin, and alkaline phosphatase. Serum aminotransferase concentrations usually return slowly to pretreatment values following discontinuance of gemfibrozil. Cholestatic jaundice reported.

Perform liver function tests periodically. Discontinue therapy if abnormalities persist.


Carcinogenicity (e.g., hepatic tumors, Leydig cell tumors) demonstrated in animals.

Specific Populations


Category C.


Not known if gemfibrozil is distributed into milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established.

Renal Impairment

Possible exacerbation of renal insufficiency in patients with baseline Scr >2 mg/dL. Consider use of alternative antilipemic therapy against the risks and benefits of a lower dose of gemfibrozil.

Common Adverse Effects

GI disturbances (e.g., dyspepsia, abdominal pain, diarrhea, nausea, vomiting, constipation, acute appendicitis, gallbladder surgery), adverse CNS effects (headache, hypesthesia, paresthesias, dizziness, somnolence, peripheral neuritis, depression), fatigue, eczema, vertigo, taste perversion, blurred vision, decreased libido, impotence.

Drug Interactions

Specific Drugs




β-Adrenergic blocking agents

Possible increase in serum triglyceride and decreases in HDL-cholesterol concentrations

Anticoagulants, oral (e.g., warfarin)

Potentiation of anticoagulant effects

Use with caution; reduce anticoagulant dosage to maintain PT at desired level to prevent bleeding complications; monitor PT frequently until stabilized


Potential increase in serum triglyceride concentrations

HMG-CoA reductase inhibitors (statins)

Increased risk of adverse musculoskeletal effects (e.g., myopathy, rhabdomyolysis)


Possible decrease in HDL- and LDL-cholesterol concentrations


Increased repaglinide concentrations and half-life, resulting in enhanced and prolonged blood glucose-lowering effects; potential for severe hypoglycemia

Do not initiate repaglinide in patients receiving gemfibrozil, and vice versa

Monitor blood glucose and reduce repaglinide dosage as required if drugs already used concomitantly

Patients receiving gemfibrozil concomitantly with repaglinide should not receive itraconazole

Thiazide diuretics

Possible increase in total cholesterol and triglyceride concentrations

Gemfibrozil Pharmacokinetics



Rapidly and completely absorbed from the GI tract.

Peak plasma concentrations occur within 1–2 hours. Plasma concentrations do not appear to correlate with therapeutic response.


Rate and extent of absorption increased when administered 30 minutes before meals.



Highest tissue concentrations observed in the liver and kidneys in animals.

Gemfibrozil crosses the placenta; not known if it is distributed into milk.

Plasma Protein Binding

About 95%.



Appears to be metabolized in the liver to 4 major metabolites produced via 3 metabolic pathways. A phenol derivative (metabolite I) is pharmacologically active.

Elimination Route

Excreted in urine (70%) in the form of metabolites and in feces (approximately 6%).


1.3–1.5 hours.





20–25°C. Protect from light and humidity.

Actions and Spectrum

Advice to Patients


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name



Dosage Forms


Brand Names



Tablets, film-coated

600 mg*

Gemfibrozil Tablets



AHFS DI Essentials™. © Copyright 2024, Selected Revisions July 26, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Off-label: Use is not currently included in the labeling approved by the US Food and Drug Administration.

Reload page with references included