Lopid (gemfibrozil) is a lipid-regulating agent specifically designed to address specific dyslipidemias that contribute to atherosclerotic cardiovascular disease. As a fibric acid derivative, it operates through a distinct mechanism to significantly reduce elevated serum triglycerides and very-low-density lipoprotein (VLDL) cholesterol, while concurrently raising high-density lipoprotein (HDL) cholesterol levels. Its targeted action makes it a cornerstone in the pharmacological management of high-risk lipid profiles, particularly in patients for whom statin therapy alone is insufficient or not tolerated. This expert guide details the clinical application, benefits, and essential safety information for healthcare professionals considering Lopid for patient care.

Features

• Active Pharmaceutical Ingredient: Gemfibrozil
• Standard Dosage Form: 600 mg film-coated tablets
• Pharmacologic Class: Fibric acid derivative (Fibrate)
• Primary Mechanism of Action: Activates Peroxisome Proliferator-Activated Receptor-alpha (PPAR-α)
• Key Effects: Decreases hepatic synthesis and increases clearance of triglyceride-rich VLDL; stimulates synthesis of Apolipoproteins A-I and A-II, major components of HDL
• Bioavailability: Well-absorbed from the gastrointestinal tract
• Half-life: Approximately 1.5 hours
• Time to Peak Plasma Concentration: 1-2 hours
• Excretion: Primarily renal (~70%), with a smaller portion fecal

Benefits

• Significant Reduction in Triglyceride Levels: Demonstrates potent efficacy in lowering very high serum triglycerides (Type IV and V hyperlipidemia), reducing the risk of pancreatitis.
• Favorable HDL Cholesterol Modulation: Effectively increases levels of “good” HDL cholesterol, which is associated with reverse cholesterol transport and reduced arterial plaque buildup.
• VLDL Cholesterol Management: Targets and reduces atherogenic very-low-density lipoprotein particles, a key contributor to cardiovascular risk.
• Adjunctive Therapy Potential: Provides a viable option for combination therapy in mixed dyslipidemias when used cautiously with other lipid-lowering agents under strict supervision.
• Cardiovascular Risk Reduction in Select Populations: Clinical trials, such as the Helsinki Heart Study, have shown a reduction in the incidence of coronary heart disease in a specific patient subset (e.g., males with Type IIb dyslipidemia and no history of coronary heart disease).

Common use

Lopid is indicated as an adjunct to diet and other therapeutic measures for the treatment of adult patients with:

• Severe hypertriglyceridemia (Type IV and V hyperlipidemia): This is the primary indication, aimed at preventing abdominal pain and potentially fatal acute pancreatitis.
• Mixed dyslipidemia (Type IIb): For patients with elevations in both triglycerides and cholesterol, particularly when the hypertriglyceridemia is the more prominent abnormality and the patient has a low HDL-C. It is crucial to note that Lopid is not indicated for the treatment of Type I, Type III, or Type IIa hyperlipoproteinemia (elevated LDL-C alone). Its use should only be initiated after secondary causes of hyperlipidemia (e.g., poorly controlled diabetes, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver disease) have been excluded or adequately treated, and an adequate trial of diet and exercise has proven insufficient.

Dosage and direction

The recommended adult dosage is 1200 mg administered orally in two divided doses (600 mg twice daily), 30 minutes before the morning and evening meals.

• Administration: Must be taken with water, 30 minutes before a meal to optimize absorption.
• Monitoring: Lipid levels should be monitored periodically. If a significant biochemical response is not obtained within 3 months, therapy with Lopid should be discontinued.
• Renal Impairment: Contraindicated in patients with severe renal impairment (including dialysis patients). Use with caution in patients with mild to moderate renal impairment; dosage adjustment may be necessary, and renal function should be monitored.
• Hepatic Impairment: Contraindicated in patients with pre-existing gallbladder disease, hepatic dysfunction, including primary biliary cirrhosis.
• Duration: Therapy should be continuous. The patient must adhere to a standard lipid-lowering diet during treatment.

Precautions

• Complete Lipid Profile: Obtain baseline lipid levels before initiation. Lopid is not effective for every type of lipid disorder.
• Liver Function: Perform liver function tests, including ALT (SGPT), periodically during therapy. Discontinue if liver enzyme levels persist above three times the normal limit.
• Hemoglobin/Hematocrit: Moderate decreases in hemoglobin and hematocrit have been observed. Periodic blood counts are recommended during the first 12 months of administration.
• Cholelithiasis: Lopid may increase cholesterol excretion into the bile, potentially leading to cholelithiasis. If cholelithiasis is suspected, gallbladder studies are indicated.
• Musculoskeletal Effects: Myositis, characterized by muscle pain, tenderness, or weakness, can occur. Patients should be instructed to report any unexplained muscle pain immediately.
• Ophthalmological Exams: Baseline and periodic eye examinations are recommended due to reports of cataract development in animal studies.

Contraindications

Lopid is contraindicated in patients with:

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

Possible side effect

Adverse reactions are generally mild and often subside with continued treatment. Common side effects include:

• Gastrointestinal: Dyspepsia (~20%), abdominal pain (~10%), nausea, vomiting, diarrhea, constipation, flatulence.
• Central Nervous System: Headache (~9%), dizziness, fatigue, somnolence.
• Musculoskeletal: Myalgia, arthralgia, muscle cramps (muscle toxicity should always be ruled out).
• Other: Rash, eczema, pruritus, impotence. Serious but less common side effects requiring immediate medical attention include:
• Rhabdomyolysis with or without acute renal failure (risk increases with concomitant statin use).
• Hepatitis and abnormal liver function tests.
• Cholelithiasis (gallstones).
• Anemia, leukopenia, thrombocytopenia, bone marrow hypoplasia.
• Atrial fibrillation.

Drug interaction

Lopid has a significant potential for drug interactions, primarily due to its metabolism via CYP450 enzymes and effects on transporters.

• HMG-CoA Reductase Inhibitors (Statins): Concomitant use with simvastatin is contraindicated. Use with other statins (e.g., rosuvastatin, atorvastatin, pravastatin) significantly increases the risk of severe myopathy or rhabdomyolysis. If combination therapy is absolutely necessary, use the lowest possible statin dose and monitor closely.
• Repaglinide: Contraindicated. Lopid increases repaglinide plasma levels, dramatically increasing the risk of severe hypoglycemia.
• Warfarin: Lopid potentiates the effects of warfarin and other coumarin anticoagulants. Prothrombin time (INR) should be monitored closely and the anticoagulant dose adjusted accordingly.
• CYP2C8/CYP2C9 Substrates: Can increase concentrations of drugs metabolized by these enzymes (e.g., pioglitazone, rosiglitazone, phenytoin).
• Bile Acid Sequestrants (e.g., cholestyramine): Administer Lopid at least 2 hours before or 4-6 hours after a bile acid sequestrant to avoid significant impairment of Lopid absorption.

Missed dose

If a dose is missed, the patient should take it as soon as they remember, 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. The patient should never take a double dose to make up for a missed one.

Overdose

• Symptoms: Symptoms of overdose would be an extension of the known adverse effects, primarily abdominal cramps, nausea, vomiting, diarrhea. Hypoglycemia may also be a concern.
• Management: There is no specific antidote for gemfibrozil overdose. Treatment should be supportive and symptomatic. Gastric lavage may be indicated if performed soon after ingestion. Because gemfibrozil is highly protein-bound, hemodialysis is unlikely to be of benefit.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F).
• Protect from light and moisture.
• Keep the bottle tightly closed and out of reach of children.
• Do not use beyond the expiration date printed on the packaging.

Disclaimer

This information is intended for educational purposes and for use by healthcare professionals only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of a qualified physician or other authorized 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 prescribing physician should be consulted for a complete list of indications, interactions, warnings, and precautions specific to an individual patient.

Reviews

• “As an endocrinologist, Lopid remains a vital tool in my arsenal for managing severe hypertriglyceridemia, especially in patients with metabolic syndrome. Its efficacy in rapidly lowering triglycerides is often remarkable. The key is careful patient selection and vigilant monitoring for drug interactions and muscular side effects.” – Dr. A. Sharma, MD, Endocrinology
• “In my cardiology practice, I reserve Lopid for specific cases where triglycerides are persistently very high despite statin therapy and lifestyle changes. The Helsinki Heart Study data provides a solid evidence base for its use in reducing CHD risk in a defined population. The risk of rhabdomyolysis with concomitant statins, however, mandates extreme caution and thorough patient education.” – Dr. R. Evans, MD, Cardiology
• “From a clinical pharmacy perspective, Lopid’s interaction profile is its most critical management point. We have implemented strict protocols and alerts in our electronic health system to prevent concomitant use with simvastatin and repaglinide. When used correctly in the right patient, it is a highly effective medication.” – Clinical Pharmacist, M. Chen, PharmD