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Pronunciation:

(jem FI broe zil)

U.S. Brand Names:

Lopid®

Synonyms:

Cl-719

Generic Available:

Yes

Canadian Brand Names:

Apo-Gemfibrozil®; Gen-Gemfibrozil; Lopid®; Novo-Gemfibrozil; Nu-Gemfibrozil; PMS-Gemfibrozil

Use:

Treatment of hypertriglyceridemia in types IV and V hyperlipidemia for patients who are at greater risk for pancreatitis and who have not responded to dietary intervention

Pregnancy Risk Factor:

Lactation:

Excretion in breast milk unknown/contraindicated

Contraindications:

Hypersensitivity to gemfibrozil or any component of the formulation; significant hepatic or renal dysfunction; primary biliary cirrhosis; pre-existing gallbladder disease

Warnings/Precautions:

Possible increased risk of malignancy and cholelithiasis. No evidence of cardiovascular mortality benefit. Anemia and leukopenia have been reported. Elevations in serum transaminases can be seen. Discontinue if lipid response not seen. Be careful in patient selection; this is not a first- or second-line choice. Other agents may be more suitable. Adjustments in warfarin therapy may be required with concurrent use. Use caution when combining gemfibrozil with HMG-CoA reductase inhibitors (may lead to myopathy, rhabdomyolysis). Renal function deterioration has been seen when used in patients with a serum creatinine >2.0 mg/dL. Safety and efficacy in pediatric patients have not been established.

Adverse Reactions:

>10% Gastrointestinal: Dyspepsia (20%)

1% to 10%:

Central nervous system: Fatigue (4%), vertigo (2%), headache (1%)

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

Gastrointestinal: Abdominal pain (10%), diarrhea (7%), nausea/vomiting (3%), constipation (1%)

<1% or case reports with probable causation (limited to important or life-threatening): Alkaline phosphatase increased, anemia, angioedema, arthralgia, bilirubin increased, blurred vision, bone marrow hypoplasia, cataracts, cholelithiasis, cholecystitis, cholestatic jaundice, creatine phosphokinase increased, depression, dermatitis, dermatomyositis/polymyositis, dizziness, eosinophilia, exfoliative dermatitis, headache, hypoesthesia, hypokalemia, impotence, intracranial hemorrhage, laryngeal edema, leukopenia, libido decreased, myalgia, myasthenia, myopathy, nephrotoxicity, paresthesia, peripheral neuritis, peripheral vascular disease, pruritus, rash, Raynaud's phenomenon, rhabdomyolysis, somnolence, synovitis, taste perversion, transaminases increased, urticaria, vasculitis

Reports where causal relationship has not been established: Weight loss, extrasystoles, pancreatitis, hepatoma, colitis, confusion, seizure, syncope, retinal edema, decreased fertility (male), renal dysfunction, positive ANA, drug-induced lupus-like syndrome, thrombocytopenia, anaphylaxis, vasculitis, alopecia, photosensitivity

Overdosage/Toxicology:

Symptoms of overdose include abdominal pain, diarrhea, nausea, and vomiting. Treatment is supportive.

Drug Interactions:

Substrate of CYP3A4 (minor); Inhibits CYP1A2 (moderate), 2C8/9 (strong), 2C19 (strong)

Bexarotene's serum concentration is significantly increased; avoid concurrent use.

Chlorpropamide: May increase risk of hypoglycemia.

Cyclosporine's blood levels may be reduced; monitor cyclosporine levels and renal function.

CYP1A2 substrates: Gemfibrozil may increase the levels/effects of CYP1A2 substrates. Example substrates include aminophylline, fluvoxamine, mexiletine, mirtazapine, ropinirole, theophylline, and trifluoperazine.

CYP2C8/9 substrates: Gemfibrozil may increase the levels/effects of CYP2C8/9 substrates. Example substrates include amiodarone, fluoxetine, glimepiride, glipizide, nateglinide, phenytoin, pioglitazone, rosiglitazone, sertraline, and warfarin.

CYP2C19 substrates: Gemfibrozil may increase the levels/effects of CYP2C19 substrates. Example substrates include citalopram, diazepam, methsuximide, phenytoin, propranolol, and sertraline.

Furosemide: Increased blood levels of both in hypoalbuminemia.

Glyburide (and possibly other sulfonylureas): The hypoglycemic effects may be increased.

HMG-CoA reductase inhibitors (atorvastatin, fluvastatin, lovastatin, pravastatin, simvastatin) may increase the risk of myopathy and rhabdomyolysis. The manufacturer warns against the concurrent use of lovastatin (if unavoidable, limit lovastatin to <20 mg/day). Combination therapy with statins has been used in some patients with resistant hyperlipidemias (with great caution).

Repaglinide: Gemfibrozil may increase the serum concentration of repaglinide (prolonged, severe hypoglycemia has been reported). The addition of itraconazole may augment the effects of gemfibrozil on repaglinide. Consider alternative therapy.

Rifampin: Decreased gemfibrozil blood levels.

Warfarin: Hypoprothrombinemic response increased; monitor INRs closely when gemfibrozil is initiated or discontinued.

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol to decrease triglycerides.

Mechanism of Action:

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

Pharmacodynamics/Kinetics:

Onset of action: May require several days

Absorption: Well absorbed

Protein binding: 99%

Metabolism: Hepatic via oxidation to two inactive metabolites; undergoes enterohepatic recycling

Half-life elimination: 1.4 hours

Time to peak, serum: 1-2 hours

Excretion: Urine (70% primarily as unchanged drug)

Dosage:

Adults: Oral: 1200 mg/day in 2 divided doses, 30 minutes before breakfast and dinner

Hemodialysis: Not removed by hemodialysis; supplemental dose is not necessary

Monitoring Parameters:

Serum cholesterol, LFTs

Dietary Considerations:

Before initiation of therapy, patients should be placed on a standard cholesterol-lowering diet for 3-6 months and the diet should be continued during drug therapy.

Patient Education:

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Should be taken 30 minutes before meals. Take with milk or meals if GI upset occurs. Avoid alcohol. Follow dietary recommendations of prescriber. You will need check-ups and blood work to assess effectiveness of therapy. You may experience loss of appetite and flatulence (small, frequent meals may help); or diarrhea (buttermilk, boiled milk, or yogurt may help). Report severe stomach pain, nausea, vomiting; headache; persistent diarrhea; or vision changes. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Do not breast-feed.

Anesthesia and Critical Care Concerns/Other Considerations:

Gemfibrozil increases HDL, decreases total cholesterol and triglycerides. A recent study (HIT), showed that gemfibrozil therapy resulted in a significant reduction in the risk of major cardiovascular events in patients with low HDL-cholesterol. These findings suggest that the rate of coronary events is reduced by raising HDL-cholesterol levels and lowering triglyceride levels. The treatment of low HDL in the general population, is not established.

Cardiovascular Considerations:

Fibric acids decrease triglycerides (TGs) by 20% to 50%, and increase HDL-cholesterol (HDL-C) by 10% to 35%. They decrease LDL-cholesterol (LDL-C) by 5% to 20%, however, LDL-C actually may increase by 10% to 30% when fibrates are initiated in patients with high TGs (>400 mg/dL).

A recent study (VA-HIT) showed that gemfibrozil therapy resulted in a significant reduction in the risk of major cardiovascular events in patients with CHD and isolated low HDL-C 40 mg/dL (average: 32 mg/dL) with LDL-C 140 mg/dL (average: 111 mg/dL) and TGs 300 mg/dL (average: 161 mg/dL) (Rubins, 1999). These findings suggest that the rate of coronary events is reduced by raising HDL-cholesterol levels in patients with isolated low HDL-C levels. The treatment of isolated low HDL-C in the general population is usually reserved for patients at high risk for developing CAD with therapy focused on addressing the other risk factors. At present, minimal if any, data are available on how to use medications in patients with low HDL-C and no risk factors.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

May rarely cause sedation or depression

Mental Health: Effects on Psychiatric Treatment:

None reported

Dosage Forms:

Tablet [film coated]: 600 mg

International Brand Names:

Afibrozil® (PL); Apo-Gemfibrozil® (CA, NZ); Ausgem® (AU); Bisil® (TH); Bolutol® (ES); Boluzin® (YU); Brozil YSP® (SG); Chem mart Gemfibrozil® (AU); Chlorestrol® (TH); DBL Gemfibrozil® (AU); Decrelip® (ES); Delipid® (BD); Deopid® (TH); Dropid® (TH); Dubrozil® (ID); Elmogan® (HK, HR, SI); Fetinor® (ID); Fibralip® (ID); Fibrocit® (IT); Gedum® (AR); Gemd YSP® (SG); Gemfi 1A Pharma® (DE); Gemfibral® (PL); Gemfibril® (TH); Gemfibrozil-BC® (AU); Gemfibrozil DOC® (IT); Gemfibrozil EG® (IT); Gemfibrozil® (GB); Gemfibrozil GEA® (SE); Gemfibrozil Indo Farma® (ID); Gemfibrozil Merck® (IT); Gemfibrozilo Bayvit® (ES); Gemfibrozilo Bexal® (ES); Gemfibrozilo® (CL, EC); Gemfibrozilo Genfar® (EC); Gemfibrozilo MK® (CO, DO, GT, HN, PA, SV); Gemfibrozilo Ur® (ES); Gemfibrozil-ratiopharm® (IT); Gemfibrozil R.O.® (AR); Gemfibrozil Teva® (IT, TH); Gemhexal® (AU); Gemizol® (NZ); Gemlipid® (IT); Genfibrozila® (BR); Gen-Gemfibrozil (CA); Genlip® (IT); Genozil® (IT); GenRX Gemfibrozil® (AU); Gevilon® (CH, CZ, DE, FI, PL, RO); Gozid® (TH); Grifogemzilo® (CL); Healthsense Gemfibrozil® (AU); Hidil® (SG, TH); Hipolixan® (AR); Hypofil® (ID); Innogem® (CZ, HU, RO); Ipolipid® (BG, CY, CZ, HK, JO, RO, RU, SG, SK); Jezil® (AU); Lanaterom® (ID); Lapibroz® (ID); Lifibron® (ID); Lipazil® (AU); Lipidys® (TH); Lipigem® (PL); Lipira® (ID); Lipison® (SG, TH); Lipitrop® (ID); Lipofor® (CY, SG); Lipogen® (IT); Lipoite® (PT); Lipolo® (TH); Lipotril® (CL); Lipox Gemfi® (DE); Lipozid® (IT); Lipozil® (GT, HN, PL, SV, TH); Lipur® (FR); Litarek® (ES); Locholes® (TH); Lochol® (ID); Lokoles® (ID); Lopid® (AR, AU, BE, BR, CA, CL, CO, CY, DK, EG, ES, FI, GB, HK, ID, IE, IN, IT, JO, KW, LB, LU, MX, NL, NZ, PT, SE, SG, TH, TR, ZA); Lowdown® (TH); Lowlip® (ID); Low-Lip® (JO, RO); Manobrozil® (TH); Mariston® (TH); Minilip® (HU); Normolip® (BD, IN); Norpid® (TH); Novo-Gemfibrozil (CA); Nufalemzil® (ID); Nu-Gemfibrozil (CA); Nurital® (EC); Pharzil® (TH); Pilder® (ES); PMS-Gemfibrozil (CA); Poli-Fibrozil (TH); Polyxit® (TH); Progemzal® (ID); Recozil® (SG); Regulip® (RO); Renabrazin® (ID); SBPA Gemfibrozil® (AU); Scantipid® (ID); Sinelip® (YU); Terry White Chemists Gemfibrozil® (AU); Tiba® (TH); Trialmin® (ES); Triglizil® (CO); Zilop® (CO, ID)

References

Bermingham RP, Whitsitt TB, Smart ML, et al, "Rhabdomyolysis in a Patient Receiving the Combination of Cerivastatin and Gemfibrozil," Am J Health-Syst Pharm, 2000, 57:461-4.

Duell PB, Connor WE, and Illingworth DR, "Rhabdomyolysis After Taking Atorvastatin With Gemfibrozil,"Am J Cardiol, 1998, 81:368-9.

"Executive Summary of The Third Report of The National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, And Treatment of High Blood Cholesterol In Adults (Adult Treatment Panel III),"JAMA, 2001, 285(19):2486-97.

Frick MH, Heinonen OP, Huttunen JK, et al, "Efficacy of Gemfibrozil in Dyslipidaemic Subjects With Suspected Heart Disease. An Ancillary Study in the Helsinki Heart Study Frame Population,"Ann Med, 1993, 25(1):41-5.

Mahley RW and Bersot TP, "Drug Therapy for Hypercholesterolemia and Dyslipidemia,"Goodman and Gilman's The Pharmacological Basis of Therapeutics, 10th ed, Hardman JE and Limbird LE, eds, New York, NY: McGraw-Hill, 2001, 993-5.

Pierce LR, Wysowski DK, and Gross TP, "Myopathy and Rhabdomyolysis Associated With Lovastatin/Gemfibrozil Combination Therapy,"JAMA, 1990, 264(1):71-5.

Rubins HB, Robbins SJ, Collins D, et al, "Gemfibrozil for the Secondary Prevention of Coronary Heart Disease in Men With Low Levels of High-Density Lipoprotein Cholesterol. Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial Study Group,"N Engl J Med, 1999, 341(6):410-8.

Tal A, Rajeshawari M, and Isley W, "Rhabdomyolysis Associated With Simvastatin/Gemfibrozil Therapy,"South Med J, 1997, 90(5):546-7.

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