Skip to Content

Gemfibrozil

Medically reviewed by Drugs.com. Last updated on Jun 20, 2019.

Pronunciation

(jem FI broe zil)

Index Terms

  • Cl-719

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Lopid: 600 mg [scored]

Generic: 600 mg

Brand Names: U.S.

  • Lopid

Pharmacologic Category

  • Antilipemic Agent, Fibric Acid

Pharmacology

The exact mechanism of action of gemfibrozil is unknown, however, several theories exist regarding the VLDL effect; it can inhibit lipolysis and decrease subsequent hepatic fatty acid uptake as well as inhibit hepatic secretion of VLDL; together these actions decrease serum VLDL levels; increases HDL-cholesterol; the mechanism behind HDL elevation is currently unknown

Absorption

Well absorbed

Metabolism

Hepatic via oxidation to two inactive metabolites; undergoes enterohepatic recycling

Excretion

Urine (~70% primarily as conjugated drug); feces (6%)

Onset of Action

May require several days

Time to Peak

Serum: 1 to 2 hours

Half-Life Elimination

1.5 hours

Protein Binding

99%

Use: Labeled Indications

Treatment of hypertriglyceridemia in Fredrickson types IV and V hyperlipidemia for patients who are at greater risk for pancreatitis and who have not responded to dietary intervention; to reduce the risk of CHD development in Fredrickson type IIb patients without a history or symptoms of existing CHD who have not responded to dietary and other interventions (including pharmacologic treatment) and who have decreased HDL, increased LDL, and increased triglycerides

Contraindications

Hypersensitivity to gemfibrozil or any component of the formulation; hepatic or severe renal dysfunction; primary biliary cirrhosis; preexisting gallbladder disease; concurrent use with dasabuvir, repaglinide, selexipag, or simvastatin.

Canadian labeling: Additional contraindications (not in the US labeling): Renal dysfunction; concurrent use with cerivastatin; pregnancy; breastfeeding.

Documentation of allergenic cross-reactivity for fibrates is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Dosing: Adult

Hyperlipidemia/hypertriglyceridemia: Oral: 600 mg twice daily 30 minutes before breakfast and dinner. Note: Discontinue if lipid response is inadequate after 3 months of therapy.

Dosing: Geriatric

Refer to adult dosing.

Administration

Administer 30 minutes prior to breakfast and dinner.

Dietary Considerations

Before initiation of therapy, patients should be placed on a standard cholesterol-lowering diet for 3 to 6 months and the diet should be continued during drug therapy. Administer 30 minutes prior to breakfast and dinner

Storage

Store at 20°C to 25°C (68°F to 77°F). Protect from light and moisture.

Drug Interactions

Acipimox: May enhance the myopathic (rhabdomyolysis) effect of Fibric Acid Derivatives. Monitor therapy

Alitretinoin (Systemic): CYP2C8 Inhibitors (Strong) may increase the serum concentration of Alitretinoin (Systemic). Management: Consider reducing the alitretinoin dose to 10 mg when used together with strong CYP2C8 inhibitors. Monitor for increased alitretinoin effects/toxicities if combined with a strong CYP2C8 inhibitor. Consider therapy modification

Amodiaquine: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Amodiaquine. Avoid combination

Apalutamide: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Apalutamide. Monitor therapy

Asunaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Asunaprevir. Avoid combination

AtorvaSTATin: Gemfibrozil may enhance the myopathic (rhabdomyolysis) effect of AtorvaSTATin. Gemfibrozil may increase the serum concentration of AtorvaSTATin. Avoid combination

Bexarotene (Systemic): Gemfibrozil may increase the serum concentration of Bexarotene (Systemic). Avoid combination

Bile Acid Sequestrants: May decrease the absorption of Fibric Acid Derivatives. Management: Separate doses by at least 2 hours to minimize this interaction; fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant. Exceptions: Colesevelam. Consider therapy modification

Chenodiol: Fibric Acid Derivatives may diminish the therapeutic effect of Chenodiol. Management: Monitor clinical response to chenodiol closely when used together with any fibric acid derivative. Monitor therapy

Ciprofibrate: May enhance the adverse/toxic effect of Fibric Acid Derivatives. Avoid combination

Colchicine: Fibric Acid Derivatives may enhance the myopathic (rhabdomyolysis) effect of Colchicine. Monitor therapy

CycloSPORINE (Systemic): May enhance the nephrotoxic effect of Fibric Acid Derivatives. Fibric Acid Derivatives may decrease the serum concentration of CycloSPORINE (Systemic). Management: Careful consideration of the risks and benefits should be undertaken prior to use of this combination; extra monitoring of renal function and cyclosporine concentrations will likely be required. Adjustment of cyclosporine dose may be necessary. Consider therapy modification

CYP2C8 Substrates (High risk with Inhibitors): CYP2C8 Inhibitors (Strong) may decrease the metabolism of CYP2C8 Substrates (High risk with Inhibitors). Consider therapy modification

Dabrafenib: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Dabrafenib. Avoid combination

Dasabuvir: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Dasabuvir. Avoid combination

Desloratadine: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Desloratadine. Monitor therapy

Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix. Avoid combination

Eluxadoline: Gemfibrozil may increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with gemfibrozil and monitor patients for increased eluxadoline effects/toxicities. Consider therapy modification

Enzalutamide: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Enzalutamide. Management: Avoid concurrent use of strong CYP2C8 inhibitors and enzalutamide if possible. If the combination must be used, reduce enzalutamide to 80 mg once daily. Consider therapy modification

Ezetimibe: Gemfibrozil may enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Gemfibrozil may increase the serum concentration of Ezetimibe. Avoid combination

Fluvastatin: Gemfibrozil may enhance the myopathic (rhabdomyolysis) effect of Fluvastatin. Avoid combination

Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Grazoprevir. Avoid combination

Imatinib: Gemfibrozil may decrease serum concentrations of the active metabolite(s) of Imatinib. Specifically N-desmethylimatinib concentrations may be decreased. Gemfibrozil may decrease the serum concentration of Imatinib. Monitor therapy

Lovastatin: Gemfibrozil may enhance the myopathic (rhabdomyolysis) effect of Lovastatin. Gemfibrozil may increase the serum concentration of Lovastatin. More specifically, gemfibrozil may increase the serum concentrations of lovastatin acid (active form of parent drug). Avoid combination

Montelukast: Gemfibrozil may increase the serum concentration of Montelukast. Monitor therapy

OATP1B1/1B3 (SLCO1B1/1B3) Substrates: Gemfibrozil may increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates. See separate drug interaction monographs for agents listed as exceptions. Exceptions: AtorvaSTATin; Eluxadoline; Ezetimibe; Fluvastatin; Pitavastatin; Pravastatin; Repaglinide; Rosuvastatin; Simvastatin. Monitor therapy

Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir. Specifically, the serum concentrations of dasabuvir may increase significantly. Avoid combination

Pioglitazone: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Pioglitazone. Management: Limit pioglitazone adult maximum dose to 15 mg/day when used in combination with any strong CYP2C8 inhibitor. Consider therapy modification

Pitavastatin: Gemfibrozil may enhance the myopathic (rhabdomyolysis) effect of Pitavastatin. Gemfibrozil may increase the serum concentration of Pitavastatin. Avoid combination

Pravastatin: Gemfibrozil may enhance the myopathic (rhabdomyolysis) effect of Pravastatin. Gemfibrozil may increase the serum concentration of Pravastatin. Avoid combination

Raltegravir: May enhance the myopathic (rhabdomyolysis) effect of Fibric Acid Derivatives. Monitor therapy

Repaglinide: Gemfibrozil may increase the serum concentration of Repaglinide. The addition of itraconazole may augment the effect of gemfibrozil on repaglinide. Avoid combination

Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentrations of the active metabolite(s) of Revefenacin. Avoid combination

Rosuvastatin: Gemfibrozil may enhance the myopathic (rhabdomyolysis) effect of Rosuvastatin. Gemfibrozil may increase the serum concentration of Rosuvastatin. Management: If possible, avoid concomitant use of rosuvastatin with gemfibrozil. If concomitant can not be avoided, limit rosuvastatin to 10 mg/day (US recommendation) or 20 mg/day (Canadian recommendation). Monitor for signs/symptoms of rhabdomyolysis. Avoid combination

Selexipag: CYP2C8 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Selexipag. CYP2C8 Inhibitors (Strong) may increase the serum concentration of Selexipag. Avoid combination

Simvastatin: Gemfibrozil may enhance the myopathic (rhabdomyolysis) effect of Simvastatin. Gemfibrozil may increase the serum concentration of Simvastatin. Concentrations of the active simvastatin acid metabolite may also be increased by gemfibrozil. Avoid combination

Sulfonylureas: Fibric Acid Derivatives may enhance the hypoglycemic effect of Sulfonylureas. Monitor therapy

Thiazolidinediones: Gemfibrozil may decrease the metabolism of Thiazolidinediones. Management: Limit pioglitazone maximum adult dose to 15 mg/day, and consider dose reduction of rosiglitazone, when used in combination with gemfibrozil. Consider therapy modification

Treprostinil: CYP2C8 Inhibitors (Strong) may increase the serum concentration of Treprostinil. Management: Reduce the initial treprostinil extended release tablet dose to 0.125 mg twice daily, titrating by 0.125 mg twice daily every 3 to 4 days. No preemptive dose adjustment is recommended for other treprostinil products. Consider therapy modification

Ursodiol: Fibric Acid Derivatives may diminish the therapeutic effect of Ursodiol. Monitor therapy

Vitamin K Antagonists (eg, warfarin): Fibric Acid Derivatives may enhance the anticoagulant effect of Vitamin K Antagonists. Consider therapy modification

Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Voxilaprevir. Avoid combination

Adverse Reactions

>10%: Gastrointestinal: Dyspepsia (20%)

1% to 10%:

Cardiovascular: Atrial fibrillation (1%)

Central nervous system: Fatigue (4%), vertigo (2%)

Dermatologic: Eczema (2%), skin rash (2%)

Gastrointestinal: Abdominal pain (10%), nausea and vomiting (3%)

<1%, postmarketing and/or case reports (probable causation): Anemia, angioedema, arthralgia, blurred vision, bone marrow depression, cholecystitis, cholelithiasis, cholestatic jaundice, decreased libido, depression, dermatitis, dermatomyositis, dizziness, drowsiness, dysgeusia, eosinophilia, exfoliative dermatitis, headache, hypoesthesia, hypokalemia, impotence, increased creatine phosphokinase, increased serum alkaline phosphatase, increased serum bilirubin, increased serum transaminases, laryngeal edema, leukopenia, limb pain, myalgia, myasthenia, myopathy, nephrotoxicity, paresthesia, peripheral neuritis, polymyositis, pruritus, Raynaud phenomenon, rhabdomyolysis, synovitis, urticaria

Reports where causal relationship has not been established: Alopecia, anaphylaxis, cataract, colitis, confusion, extrasystoles, hepatic neoplasm, intracranial hemorrhage, lupus-like syndrome, pancreatitis, peripheral vascular disease, positive ANA titer, reduced fertility (male), renal insufficiency, retinal edema, seizure, skin photosensitivity, syncope, thrombocytopenia, vasculitis, weight loss

Warnings/Precautions

Concerns related to adverse effects:

• Cholelithiasis: May increase risk of cholelithiasis; discontinue if gallstones are found upon gallbladder studies.

• Elevated transaminases: Elevations in serum transaminases may be seen with use; periodic monitoring recommended.

• Hematologic effects: May cause mild decreases in hemoglobin, hematocrit, and WBC upon initiation which usually stabilizes with long-term therapy. Anemia, leukopenia, thrombocytopenia, and bone marrow hypoplasia have rarely been reported. Periodic monitoring recommended during the first year of therapy.

• Malignancy: Possible increased risk of malignancy.

• Myopathy/rhabdomyolysis: Has been associated with rare myositis or rhabdomyolysis; patients should be monitored closely. Patients should be instructed to report unexplained muscle pain, tenderness, weakness, or brown urine.

Disease-related concerns:

• Renal impairment: Use with caution in patients with mild-to-moderate renal impairment; contraindicated in patients with severe impairment. Deterioration has been seen when used in patients with a serum creatinine >2 mg/dL.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Other warnings/precautions:

• Appropriate use: Secondary causes of hyperlipidemia should be ruled out prior to therapy. Be careful in patient selection, this is not a first- or second-line choice; other agents may be more suitable. Discontinue if lipid response not seen.

Monitoring Parameters

Serum cholesterol, LFTs periodically, CBC periodically (first year)

Pregnancy Considerations

Gemfibrozil crosses the placenta (Tsai 2004).

Triglyceride concentrations increase during pregnancy as required for normal fetal development. When increases are greater than expected, supervised dietary intervention should be initiated. In women who develop very severe hypertriglyceridemia and are at risk for pancreatitis, use of gemfibrozil beginning in the second trimester is one intervention that may be considered (Avis 2009; Berglund 2012; Jacobson 2015; Wong 2015).

Patient Education

What is this drug used for?

• It is used to lower bad cholesterol and raise good cholesterol (HDL).

• It is used to lower triglycerides.

Frequently reported side effects of this drug

• Heartburn

• Abdominal pain

• Diarrhea

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

• Gallstones like pain in the upper right abdominal area, right shoulder area, or between the shoulder blades; jaundice; or fever with chills.

• Infection

• Muscle pain

• Muscle weakness

• Urinary retention

• Change in amount of urine passed

• Severe loss of strength and energy

• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Hide