Lopid 300 mg Tablets

Brand Name

This medication is marketed under the trade name Lopid, a label well-known among healthcare professionals for its role in lipid management.

International Nonproprietary Name (INN)

The active ingredient is identified globally as gemfibrozil, ensuring its consistent recognition across medical practices worldwide.

Form of Release

The drug is available as film-coated tablets, designed for oral administration and offered in specific strengths to meet therapeutic needs. This tablet form provides ease of use and maintains stability under standard storage conditions.

Composition

Gemfibrozil serves as the primary active substance, engineered to influence lipid metabolism within the body. Supporting this are inactive ingredients such as microcrystalline cellulose, pregelatinized starch, sodium starch glycolate, and magnesium stearate, which contribute to the tablet’s structure and dissolution properties. The film coating, typically composed of hydroxypropyl methylcellulose, polyethylene glycol, and titanium dioxide, enhances swallowability and protects the active component from environmental degradation. Each element is carefully selected to optimize the therapeutic action of gemfibrozil without altering its effectiveness.

Pharmacologic Properties

Pharmacodynamics

This medication functions as a fibric acid derivative, primarily targeting lipid metabolism to exert its therapeutic effects. It activates peroxisome proliferator-activated receptor-alpha (PPAR-alpha), which upregulates lipoprotein lipase activity and enhances the breakdown of triglycerides in very-low-density lipoproteins (VLDL). This reduces circulating triglyceride levels while increasing high-density lipoprotein (HDL) cholesterol by promoting apolipoprotein A-I and A-II synthesis. It also modestly lowers low-density lipoprotein (LDL) cholesterol in some patients by reducing hepatic VLDL production. Effects typically manifest within days to weeks, with peak lipid changes occurring after one to two months of consistent use. This mechanism addresses dyslipidemia by shifting lipid profiles toward a less atherogenic state, supporting cardiovascular risk reduction.

Pharmacokinetics

Following oral administration, the drug absorbs efficiently from the gastrointestinal tract, with bioavailability nearing 100% when taken with food, which enhances uptake. Peak plasma concentrations occur within one to two hours. Gemfibrozil binds approximately 97% to plasma proteins, primarily albumin, and distributes widely into tissues like the liver, where it exerts its primary effects. It undergoes extensive hepatic metabolism via glucuronidation, forming a major glucuronide conjugate that retains some activity. Elimination occurs predominantly through urine, with about 70% excreted as metabolites and less than 6% unchanged, while the remainder exits via feces. The half-life averages one to two hours, though active metabolites may prolong its effects. Renal or hepatic impairment can alter clearance, requiring careful monitoring.

Indications for Use

This medication is prescribed for conditions involving abnormal lipid levels. It is primarily indicated for severe hypertriglyceridemia, reducing elevated triglyceride levels to lower the risk of pancreatitis in patients unresponsive to diet alone. It also treats mixed dyslipidemia, particularly in those with low HDL cholesterol and high triglycerides, often as an adjunct to statins when tolerated. In patients with coronary heart disease risk, it may reduce cardiovascular events by improving lipid profiles, especially when triglycerides exceed safe thresholds. Its use extends to cases where dietary and lifestyle changes fail to achieve adequate lipid control, offering a targeted approach to managing these metabolic disorders and their associated complications.

Contraindications

Certain conditions preclude the use of this drug to prevent serious health risks. Hypersensitivity to gemfibrozil or any tablet component prohibits its administration, as reactions could range from mild rashes to anaphylaxis. Severe hepatic dysfunction, including cirrhosis or active liver disease, contraindicates it due to its extensive liver metabolism and potential for toxicity. It is avoided in severe renal impairment, particularly with creatinine clearance below 30 mL/min, as reduced clearance heightens adverse effect risks. Pre-existing gallbladder disease or a history of gallstones rules it out, given its association with increased biliary cholesterol secretion. Concurrent use with certain statins like simvastatin or repaglinide is also prohibited due to heightened myopathy or hypoglycemia risks.

Method of Administration and Dosage

How to Take

Tablets are taken orally, ideally 30 minutes before meals to optimize absorption, typically before breakfast and dinner. Swallowing them whole with water ensures proper delivery to the stomach. Consistent timing each day maintains steady blood levels for effective lipid control.

Dosage for Adults and Children

For adults with hypertriglyceridemia or dyslipidemia, treatment typically involves 600 mg twice daily, totaling 1200 mg per day, maintained as long as lipid goals are unmet or side effects remain tolerable. Adjustments are rare, though some may reduce to 600 mg daily if partial response suffices with dietary support. Pediatric use lacks established guidelines, but when prescribed, dosing is individualized, often starting at 10 mg per kilogram daily, divided into two doses, adjusted under specialist supervision based on lipid response and tolerance. Regular lipid profile monitoring guides therapy to balance efficacy and safety across age groups.

Dose Adjustment in Specific Conditions

Renal impairment requires caution; doses may drop to 600 mg daily if clearance falls between 30 and 60 mL/min, while it’s avoided below 30 mL/min due to accumulation risks. Mild hepatic dysfunction suggests starting at 600 mg daily with close liver function monitoring, though severe cases typically contraindicate use. Elderly patients or those with reduced metabolic capacity may also begin with 600 mg daily to minimize gastrointestinal or muscular side effects. Frequent laboratory assessments ensure dosing aligns with individual physiological needs, particularly in compromised states.

Side Effects

This medication may provoke a range of unintended reactions, though most are mild and manageable. Gastrointestinal discomfort, such as abdominal pain, nausea, or diarrhea, is common, often subsiding with continued use or meal adjustments. Fatigue, headache, or dizziness might occur, typically linked to metabolic shifts or mild dehydration. Elevated liver enzymes or muscle pain can emerge, occasionally signaling myopathy, especially with concurrent risk factors. Skin rashes or itching affect some users but rarely persist. Rarely, severe effects like gallstones, significant liver dysfunction, or rhabdomyolysis—a breakdown of muscle tissue—occur, necessitating immediate medical attention. Regular monitoring of liver, kidney, and muscle function helps detect and address these issues promptly.

Overdose

Symptoms of Overdose

Excessive intake can lead to pronounced gastrointestinal distress, including severe nausea, vomiting, or abdominal cramping, reflecting irritation from high concentrations. Muscle pain or weakness might escalate, potentially indicating early rhabdomyolysis, while dizziness or confusion could signal metabolic or circulatory disruption. Elevated liver enzymes or acute kidney injury may develop in extreme cases, posing risks if untreated. Symptoms typically surface within hours and intensify without intervention, highlighting the drug’s potent metabolic impact.

First Aid Measures

In an overdose situation, discontinue administration immediately and seek urgent medical care. If ingestion is recent, gastric lavage or activated charcoal may reduce absorption, performed under professional supervision. Supportive care, including intravenous fluids, addresses dehydration or circulatory issues, while monitoring liver and kidney function guides further management. Muscle enzyme levels should be checked to rule out rhabdomyolysis, with treatment like hydration or alkalinization if needed. Stabilization focuses on reversing acute effects and preventing organ damage until recovery.

Drug Interactions

Effects on Other Medications

This drug can alter the performance of various medications when used concurrently. It increases the risk of myopathy with statins like simvastatin or lovastatin by inhibiting their metabolism, requiring avoidance or careful monitoring with safer alternatives. It enhances the hypoglycemic effects of repaglinide or sulfonylureas, risking low blood sugar, so glucose checks are advised. Warfarin’s anticoagulant effect may intensify due to displacement from protein binding, necessitating prothrombin time adjustments. Bile acid sequestrants like cholestyramine reduce its absorption if taken together, requiring dosing separation by at least two hours. Adjustments and oversight minimize these interactions effectively.

Compatibility with Alcohol and Food

Alcohol consumption may increase triglyceride levels or gastrointestinal irritation, countering therapeutic goals, so moderation is recommended. Food, particularly meals, enhances absorption, improving efficacy, though high-fat diets might undermine lipid-lowering benefits, suggesting a balanced approach. No strict restrictions apply beyond avoiding excessive calorie intake that could elevate lipids.

Special Precautions

Use During Pregnancy and Breastfeeding

Lopid is generally avoided in pregnancy unless benefits outweigh risks, as animal studies suggest potential fetal harm, though human data are limited. It may pass into breast milk, with unknown effects on infants, so nursing mothers should consult their physician, possibly opting for alternatives to reduce exposure.

Impact on Driving and Machinery Operation

Dizziness or fatigue, particularly at initiation or with side effects, may impair driving or machinery operation. Patients should evaluate their tolerance before engaging in such activities, ensuring safety for themselves and others.

Considerations for Elderly and Pediatric Populations

Elderly individuals may require lower initial doses due to reduced renal or hepatic function, with monitoring for gastrointestinal or muscular effects. In children, its use is rare and guided by specialists, with weight-based dosing adjusted cautiously to avoid metabolic or growth impacts. Personalized care optimizes safety and efficacy across these groups.