drugs

LOPID ® Gemfibrozil

LOPID ® is a Gemfibrozil based drug

THERAPEUTIC GROUP: Ipolipemizzanti - Fibrati

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications LOPID ® Gemfibrozil

LOPID ® reducing the blood level of triglycerides and normalizing that of cholesterol, is indicated in the therapeutic treatment of dyslipidemias in which the non-pharmacological approach (hypolipidic diet and physical activity) has not guaranteed satisfactory results.

LOPID ® can be used in the treatment of hypercholesterolemia as a replacement or statin replacement therapy.

Mechanism of action LOPID ® Gemfibrozil

The active ingredient of LOPID ® gemfibrozil, is a derivative of fibric acid. Taken orally, gemfibrozil is totally absorbed in the gastro-intestinal tract, and distributed through blood bound to plasma proteins.

Although the mechanism of action has not yet been definitively clarified, it is possible that the therapeutic activity of this active ingredient is linked to the activation of the PPAR receptor, mainly in the liver, with the following:

  1. Reduction of blood triglyceride levels;
  2. Reduction of blood levels of VLDL cholesterol, hence LDL;
  3. Increased blood levels of HDL cholesterol.

The therapeutic potential of lipid normalizer plays an important preventive role for the development of atherosclerosis and associated cardiovascular diseases.

After its action, gemfibrozil is metabolized in the liver through carboxylation and hydroxylation reactions, and eliminated mainly through the urine.

Studies carried out and clinical efficacy

ANTIPERTENSIVE ACTION OF GEMFIBROZIL

In addition to the lipid-lowering effects of gemfibrozil, recent studies have also shown a diminishing effect on blood pressure values. In vitro and in vivo investigations have allowed us to understand the biological basis of this effect. Indeed, it appears that gemfibrozil can act selectively on smooth muscles, facilitating relaxation, which results in an important effect not only on blood pressure levels but also on gastro-intestinal motility. This research can therefore justify the greater incidence of side effects in the gastro-intestinal tract.

2. GEMFIBROZIL: NOT JUST HYPOLYPHEZISM

The lipid-lowering therapeutic properties of gemfibrozil are now known, but more and more studies are aimed at clarifying the complex pharmacodynamic characteristics of this molecule. New evidence, in fact, also suggests a regulatory role in inflammation, activation of T lymphocytes, cell-cell contact and oxidative stress processes.

3. PRAVASTATINA vs GEMFIBROZIL

All-Italian study showing the different therapeutic efficacy of statins and fibrates. In particular, the effects of therapeutic doses of pravastatin and gemfibrozil were studied - in a double-blind experiment - with the following results.

Pravastatin was more effective in reducing LDL cholesterol levels than gemfibrozil (30% compared to 23%), while gemfibrozil was more effective than pravastatin in reducing triglyceride levels (37% compared to 5%) and in the 'increase HDL cholesterol levels (13% compared to 5%).

Method of use and dosage

LOPID ® gemfibrozil 600/900 mg coated tablets: two 600mg tablets per day are recommended, taken at least 30 minutes before meals.

The dosage can be corrected depending on the case and normalized on 900mg / day in case of good lipid control.

Both before and during the therapeutic intervention, it is necessary to follow a hypolipid dietary regime and healthy lifestyle habits.

IN ANY CASE, BEFORE TAKING LOPID ® Gemfibrozil, THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.

Warnings LOPID ® Gemfibrozil

Drug treatment with LOPID ® should be considered only after following healthy lifestyle and eating habits for at least a quarter. Hypolipid diet, controlled physical activity and reduced alcohol consumption are the first precautions to be observed in the presence of dyslipidemia.

If these measures, pursued for at least 3 months, do not guarantee satisfactory results, the association with a gemfibrozil drug therapy is indicated. In this case, given the inhibitory activity on the enzyme HMG-CoA reductase, and the possibility of developing liver disease and myopathies, it would be advisable - before and throughout the treatment - to monitor some laboratory parameters (transaminases and creatinkinase), indicative of the state of liver and muscle health.

The therapy should be suspended, or never started, in the case of plasma transaminase concentrations 3 times higher than the normal range, with an increase in the level of cratinkinase accompanied by muscle pain, myalgia, fatigue and persistent fatigue, in case of peptic ulcer, of cholelithiasis and reduced kidney function.

Although no cases are described in the literature in which genfibrozil has reduced the cognitive abilities of the patient, the presence of vertigo and dizziness, frequently felt in the initial phase of treatment, could alter the normal ability to drive vehicles and use machinery.

PREGNANCY AND BREASTFEEDING

The absence of studies concerning the safety of gemfibrozil taken during pregnancy and the importance of lipids in correct embryonic, fetal and neonatal development suggest avoiding the use of this drug during the entire period of pregnancy and lactation.

Interactions

Gemfibrozil, when taken concomitantly with oral anticoagulants, could determine an increase in the biological efficacy of these drugs, with possible bleeding complications. In this case it would be advisable to constantly monitor the prothrombin time and adjust the anticoagulant dosage.

The lipid-lowering activity of LOPID ® could instead be enhanced by the concomitant administration of other drugs, such as statins (HMG-CoA reductase inhibitors), for which - in addition to an increased efficacy due to synergy - a increased side effects.

Particularly harmful, with serious events of myopathy, myositis and rhabdomyolysis. The association between gemfibrozil and cerivastatin was found.

Gemfibrozil also appears to increase the hypoglycemic effect of repaglinide, with possible glycemic drops, even serious ones.

Contraindications LOPID ® Gemfibrozil

LOPID ® is contraindicated in cases of severe hepatic and renal insufficiency, and in the case of cholelithiasis or hypersensitivity to one of its components.

LOPID ® should not be taken concurrently with cerivastatin or repaglinide.

Undesirable effects - Side effects

The most common side effects described following LOPID ® therapy were all transient and clinically insignificant. Among the most common reactions there were gastro-intestinal disorders, dyspepsia, abdominal pains, nausea, diarrhea, dizziness and fatigue.

Other reactions, even more serious, were recorded only in a few cases and in particular categories of patients at risk, with involvement of the musculoskeletal, visual and hepatic apparatus.

Note

LOPID ® is salable only under medical prescription.