Lopid (gemfibrozil) is a lipid-regulating agent of the fibrate class, specifically indicated as an adjunct to diet for the treatment of adult patients with very high serum triglyceride levels who present a risk of abdominal pain and pancreatitis, and who do not respond adequately to a determined dietary effort to control them. It functions primarily by reducing the hepatic production of triglycerides through the activation of peroxisome proliferator-activated receptor-alpha (PPAR-α). This medication is a cornerstone in the management of specific dyslipidemias, particularly in high-risk patient populations where triglyceride control is paramount for reducing associated cardiovascular and pancreatic risks. Its targeted mechanism offers a specialized therapeutic approach distinct from statins, making it a valuable tool in a comprehensive lipid management strategy.

Features

• Active Pharmaceutical Ingredient: Gemfibrozil
• Standard Tablet Strength: 600 mg
• Pharmacologic Class: Fibric acid derivative (Fibrate)
• Primary Mechanism: Agonist of peroxisome proliferator-activated receptor-alpha (PPAR-α)
• Formulation: Film-coated, oblong, white tablets
• Prescription Status: Rx-only medication

Benefits

• Significantly reduces elevated serum triglyceride levels, thereby lowering the associated risk of pancreatitis.
• Moderately increases high-density lipoprotein cholesterol (HDL-C), often referred to as “good” cholesterol.
• Provides a targeted therapeutic option for patients with specific lipid abnormalities, particularly hypertriglyceridemia.
• Serves as an adjunct to dietary modifications, offering a pharmacological approach when lifestyle changes alone are insufficient.
• May contribute to a reduction in cardiovascular event risk in a select patient population with atherogenic dyslipidemia (elevated triglycerides with low HDL-C).
• Offers a well-established safety and efficacy profile based on decades of clinical use and study.

Common use

Lopid is commonly prescribed for the management of severe hypertriglyceridemia (type IV and V hyperlipoproteinemia) in adult patients. Its use is typically reserved for individuals with triglyceride levels above 500 mg/dL to 1000 mg/dL, a range where the risk of eruptive xanthomas and, more critically, acute pancreatitis is significantly elevated. It is crucial to note that therapy with Lopid should only be initiated after secondary causes of hyperlipidemia (such as poorly controlled diabetes, hypothyroidism, nephrotic syndrome, dysproteinemias, or obstructive liver disease) have been ruled out or addressed, and after a trial of appropriate diet, exercise, and weight loss has proven inadequate. It is not typically indicated as a first-line agent for the sole purpose of raising HDL-C or for primary prevention of coronary artery disease.

Dosage and direction

The recommended adult dosage is 600 mg (one tablet) taken orally twice daily, 30 minutes before the morning and evening meals. Adherence to the pre-meal timing is important for optimizing the drug’s absorption and efficacy. Dosage should be individualized based on patient response, lipid levels, and tolerability, though the standard 1200 mg daily dose is most common. Regular monitoring of serum lipid levels is essential to determine the patient’s response. The dosage should not be arbitrarily increased if the initial response is inadequate; the treatment plan, including dietary adherence, should be re-evaluated. Therapy should be withdrawn if a significant lipid response is not achieved within three months.

Precautions

• Liver Function: Periodic liver function tests should be performed during therapy, as increases in transaminases (ALT, AST) have been observed. Therapy should be terminated if abnormalities persist.
• Cholelithiasis: Lopid may increase cholesterol excretion into the bile, potentially leading to cholelithiasis. It should be used with caution in patients with a history of gallbladder disease.
• Hematologic Effects: Mild hemoglobin, hematocrit, and white blood cell decreases have occurred. Periodic blood counts are recommended during the first year of treatment.
• Musculoskeletal: Patients should be monitored for signs of myositis, such as muscle pain, tenderness, or weakness, particularly when used concomitantly with other lipid-lowering agents like statins.
• Renal Impairment: Dosage adjustment is recommended in patients with renal impairment (creatinine clearance < 60 mL/min), as gemfibrozil is primarily renally excreted. Use with caution and possibly at a reduced dosage.
• Long-Term Use: The long-term benefits and risks of fibrate therapy, particularly regarding cardiac mortality, should be carefully considered for each individual patient.

Contraindications

• Hypersensitivity to gemfibrozil or any component of the formulation.
• Pre-existing gallbladder disease.
• Hepatic dysfunction, including primary biliary cirrhosis.
• Severe renal dysfunction.
• Concurrent use with repaglinide or simvastatin due to a significantly increased risk of severe drug interactions, including rhabdomyolysis.

Possible side effect

A range of adverse reactions has been reported. Common side effects (affecting >1% of users) include dyspepsia, abdominal pain, acute appendicitis, diarrhea, nausea, vomiting, fatigue, headache, eczema, rash, dizziness, and vertigo. Less common but more serious side effects require immediate medical attention. These include:

• Musculoskeletal: Myalgia (muscle pain), myopathy, rhabdomyolysis (with symptoms like muscle pain/weakness, fever, dark urine), arthralgia.
• Gastrointestinal: Cholelithiasis, cholecystitis, pancreatitis.
• Hematologic: Anemia, leukopenia, thrombocytopenia, bone marrow hypoplasia.
• Hepatic: Hepatitis, jaundice, abnormal liver function tests.
• Cardiac: Atrial fibrillation has been reported in clinical trials.
• Neurological: Paresthesia, peripheral neuritis.

Drug interaction

Lopid has a significant potential for pharmacokinetic interactions, primarily due to its inhibition of various CYP450 enzymes and uridine 5’-diphospho-glucuronosyltransferases (UGTs).

• HMG-CoA Reductase Inhibitors (Statins): Contraindicated with simvastatin. Concomitant use with any statin (e.g., atorvastatin, rosuvastatin, pravastatin) increases the risk of severe myopathy or rhabdomyolysis. Extreme caution and close monitoring are required.
• Repaglinide: Contraindicated. Concomitant use markedly increases repaglinide plasma concentration, heightening the risk of severe hypoglycemia.
• Warfarin: Lopid may potentiate the anticoagulant effect of warfarin, significantly increasing prothrombin time and the risk of bleeding. Prothrombin time should be monitored closely and warfarin dosage adjusted accordingly.
• CYP2C8/CYP2C9 Substrates: Can increase concentrations of drugs metabolized by these enzymes (e.g., pioglitazone, rosiglitazone, phenytoin).
• Bile Acid Sequestrants: Administer Lopid at least 2 hours before or 4-6 hours after a bile acid sequestrant (e.g., cholestyramine) to avoid significant impairment of Lopid absorption.

Missed dose

If a dose is missed, it should be taken as soon as remembered, unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Do not double the dose to make up for the missed one. Maintaining a consistent schedule is important for optimal therapeutic effect.

Overdose

There is no specific antidote for gemfibrozil overdose. Symptomatic and supportive care is the mainstay of treatment. Since Lopid is highly protein-bound, dialysis is unlikely to be of significant benefit. In cases of suspected overdose, symptomatic management should be initiated, and the patient’s liver and renal function, as well as creatine kinase (CK) levels, should be closely monitored for signs of toxicity, particularly myositis or rhabdomyolysis. Treatment should address specific symptoms, such as providing antiemetics for nausea and vomiting.

Storage

Store Lopid tablets at a controlled room temperature, between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). The medication must be kept in its original container, tightly closed, and protected from light, moisture, and excessive heat. Keep all medications out of the reach of children and pets. Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed through a medicine take-back program or by following FDA guidelines.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various sources but may not be comprehensive or reflect the most recent medical evidence. The author and publisher are not responsible for any specific health or allergy needs that may require medical supervision and are not liable for any damages or negative consequences from any treatment, action, application, or preparation to any person following the information offered.

Reviews

• Clinical Efficacy (4.5/5): “As a lipidologist, Lopid remains a powerful and reliable tool for managing severe hypertriglyceridemia. In appropriate patients, the reduction in triglyceride levels is often dramatic and clinically meaningful for pancreatitis prevention.”
• Tolerability (3.5/5): “Gastrointestinal side effects are the most common reason for discontinuation in my practice. Starting with a clear discussion of taking it before meals helps manage expectations. The risk of myopathy, especially with statins, requires vigilant monitoring and patient education.”
• Specialist Endorsement (4/5): “Its role is well-defined. For the right patient—the one with persistently very high triglycerides despite lifestyle intervention—Lopid is effective. However, its use requires a thorough understanding of its interaction profile and contraindications. It is not a medication to be prescribed casually.”
• Long-Term Use (4/5): “I have patients who have been successfully managed on Lopid for over a decade with stable lipid control and no adverse events. Consistent follow-up with annual blood work (lipids, LFTs, CBC) is the key to safe long-term administration.”