LOPID ® is a Gemfibrozil-based drug
THERAPEUTIC GROUP: Hypolipidemics - Fibrates
Indications LOPID ® Gemfibrozil
LOPID ® by 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 add-on therapy to statins.
Mechanism of action LOPID ® Gemfibrozil
The active ingredient of LOPID ® gemfibrozil is a derivative of fibric acid.Taken orally, gemfibrozil is completely absorbed from the gastrointestinal tract and distributed through the 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 principle is linked to the activation of the PPAR receptor, mainly in the liver, resulting in:
- Reduction in blood levels of triglycerides;
- Reduction of blood levels of VLDL cholesterol, therefore LDL;
- Increased blood levels of HDL cholesterol.
The therapeutic potential of lipid normalizer plays an important preventive role for the development of atherosclerosis and associated cardio-vascular diseases.
Once its action is terminated, gemfibrozil is metabolized in the liver through carboxylation and hydroxylation reactions, and eliminated mainly in the urine.
Studies carried out and clinical efficacy
ANTI-HYPERTENSIVE ACTION OF GEMFIBROZIL
J Smooth Muscle Res. 2010; 46: 125-42.
Evidence of direct smooth muscle relaxant effects of the fibrate gemfibrozil.
Phelps LE, Peuler JD.
In addition to the lipid-lowering effects of gemfibrozil, recent studies have also shown a diminutive effect on blood pressure values. In vitro and in vivo investigations have allowed us to understand the biological basis of this effect. In fact, it seems that gemfibrozil can selectively act on smooth muscle facilitating its relaxation, which results in an important effect not only on blood pressure levels but also on gastrointestinal motility. These researches can therefore justify the higher incidence of side effects in the gastrointestinal tract.
2. GEMFIBROZIL: NOT ONLY HYPOLIPEMIZING
Immunopharmacol Immunotoxicol. 2009; 31: 339-51.
Gemfibrozil, stretching arms beyond lipid lowering.
Roy A, Pahan K.
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, in the activation of T lymphocytes, in cell-cell contact and in oxidative stress processes.
3. PRAVASTATIN vs GEMFIBROZIL
Arch Intern Med. 1991 Jan; 151: 146-52.
Pravastatin vs gemfibrozil in the treatment of primary hypercholesterolemia. The Italian Multicenter Pravastatin Study I.
Crepaldi G, Baggio G, Arca M, Avellone G, Avogaro P, Bittolo Bon G, Bompiani GD, Capurso A, Cattin L, D "Alŏ G, et al.
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 lowering LDL cholesterol levels than gemfibrozil (30% versus 23%), while gemfibrozil was more effective than pravastatin at lowering triglyceride levels (37% versus 5%) and in "increase HDL cholesterol levels (13% versus 5%).
Method of use and dosage
LOPID ® gemfibrozil 600/900 mg coated tablets:two 600mg tablets a day are recommended, taken at least 30 minutes before meals.
The dosage can be adjusted according to the case and normalized to 900mg / day in case of good lipid control.
Both before and during the therapeutic intervention, it is necessary to follow a low-fat diet and healthy lifestyle habits.
IN ANY CASE, BEFORE TAKING LOPID ® Gemfibrozil - YOU NEED THE PRESCRIPTION AND CONTROL OF YOUR DOCTOR.
LOPID ® Gemfibrozil warnings
Pharmacological treatment with LOPID ® should only be considered after following healthy lifestyle and eating habits for at least one quarter. Hypolipidic diet, controlled physical activity and reduction of alcohol consumption are the first precautions to be observed in the presence of dyslipidemias.
If these precautions, pursued for at least 3 months, do not guarantee satisfactory results, the association with a pharmacological therapy with gemfibrozil 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 during the whole treatment - to monitor some laboratory parameters (transaminases and creatinkinases), indicative of the state of health of the liver and muscles.
Therapy should be suspended, or never started, in case of plasma transaminase concentrations 3 times higher than the normal range, of an increase in the level of cratinkinase accompanied by muscle pain, myalgia, tiredness and persistent fatigue, in case of peptic ulcer, of cholelithiasis and impaired renal function.
Although no cases have been described in the literature in which genfibrozil has reduced the patient's cognitive abilities, the presence of vertigo and dizziness, frequently felt in the initial phase of treatment, could alter the normal ability to drive cars and use machines.
PREGNANCY AND BREASTFEEDING
The absence of studies regarding the safety of gemfibrozil taken during pregnancy and the importance of lipids in the 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 cause 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 dosage of anticoagulant.
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 severe events of myopathy, myositis and rhabdomyolysis. The association between gemfibrozil and cerivastatin was found.
Furthermore, gemfibrozil seems to increase the hypoglycemic effect of repaglinide, with possible glycemic drops, even severe ones.
Contraindications LOPID ® Gemfibrozil
LOPID ® is contraindicated in case of severe hepatic and renal insufficiency, and in case of cholelithiasis or hypersensitivity to one of its components.
LOPID ® should not be taken concomitantly with cerivastatin or repaglinide.
Undesirable Effects - Side Effects
The most common side effects described following LOPID ® therapy were all transient and clinically insignificant. The most common reactions included gastrointestinal disturbances, dyspepsia, abdominal pain, 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, involving the musculoskeletal, visual and hepatic systems.
Note
LOPID ® can only be sold under medical prescription.
The information on LOPID ® Gemfibrozil published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
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