BEZALIP ® Bezafibrate

BEZALIP ® is a drug based on Bezafibrate

THERAPEUTIC GROUP: Ipolipemizzanti - Fibrati

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

Indications BEZALIP ® Bezafibrate

The lipid-lowering action of BEZALIP ® is used in the treatment of those forms of dyslipidemia and hypercholesterolemia in which the triglyceride component is the major therapeutic problem.

BEZALIP ® should only be used in the event of failure of a non-pharmacological lipid-lowering therapy, lasting for at least 3 months. A hypolipidic diet and a healthy lifestyle should in any case also be pursued during drug therapy.

Mechanism of action BEZALIP ® Bezafibrate

BEZALIP ® provides prolonged-release bezafibrate, which absorbed at the gastro-intestinal level reaches its maximum plasma concentration after about 3-4 hours, exhibiting a bioavailability of 70% of the total dose taken.

The therapeutic action seems to be carried out mainly in the liver, where this active principle is able to activate the PPAR alpha receptor, and promote a series of intracellular events that materialize at the systemic level in:

reduction of LDL cholesterol concentrations, thanks to the inhibition of the HMG-CoA reductase enzyme and to the increased expression of lipoprotein lipase.
Increased blood concentrations of HDL cholesterol, thanks to the increased production of Apo AI and AII.
Reduction of triglycerides, thanks to the increase in oxidative processes and the reduction of VLDL production.

To these lipid-lowering effects, already protective against cardiovascular pathologies, an anti-thrombogenic action is also added, exercised through the reduction of the fibrin plasma levels and inhibition of platelet aggregation.

After a persistence in the organism of about 2-4 hours, the bezafibrate is partly metabolized in the liver via glucuronation, and consequently eliminated mainly via the kidney.

Studies carried out and clinical efficacy

THE EFFECTIVENESS OF COMBINED THERAPY

All-Italian study conducted by researchers at Federico II of Naples, which shows how the concomitant administration of bezafibrate (400mg) and fluvastatin (40mg) ensured a series of significantly more significant lipid-lowering effects compared to monotherapy, with triglyceride reduction of 38%, of LDL cholesterol by 24%, and with an increase in HDL cholesterol of 22%. Despite the combined therapy, the incidence of side effects was similar to the monotherapy group, with no case of liver disease or myopathies.

2. BEZAFIBRATO AND ATEROSCLEROSIS

The administration of bezafibrate in patients suffering from hyperglyceridemia and evident atherosclerotic plaques, guaranteed a regression of varying degrees of the aforesaid abdominal and thoracic plaques. The therapeutic action could be determined both by the lipid-lowering effects and probably by the antiplatelet and antifibrinogenic role of bezafibrate.

3. HYPOGLYCOGENIC EFFECT OF BEZAFIBRATO

In 1342 patients, suffering from type II diabetes mellitus and related dyslipidemia, 8 weeks of bezafibrate therapy guaranteed an increase in HDL cholesterol of 20%, a reduction in plasma triglycerides of 50%, total cholesterol of 12% and fasting blood sugar from 151 to 128 mg / dL. These data thus highlight the hypoglycemic role of bezafibrate, probably due to an increase in insulin sensitivity.

Method of use and dosage

BEZALIP ® 400 mg prolonged release bezafibrate coated tablets: we recommend taking one tablet a day with meals.

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

Warnings BEZALIP ® Bezafibrate

The pharmacological prescription of BEZALIP ® should take place only after a period, at least quarterly, of a hypolipidic diet and a healthy lifestyle, characterized by reduced alcohol consumption and planned physical activity.

In case of therapeutic need, before and during treatment with bezafibrate, it would be advisable to monitor the plasma levels of creatine kinase and transaminase, in order to minimize the incidence of myopathies and liver diseases. The administration of the drug should be avoided, or suspended, in case of increased concentrations of liver enzymes, in case of an increase in creatine kinase values, as well as in the presence of muscle pain, tiredness and persistent fatigue.

The drug should be withdrawn even if renal function is impaired.

BEZALIP ® among its excipients, contains lactose; therefore its intake could be followed by gastro-intestinal problems in patients suffering from glucose / galactose malabsorption and lactase deficiency.

BEZALIP ® does not seem to interfere with the ability to use machinery and drive vehicles, although among the side effects described above, especially in the early stages of therapy, there are dizziness and lightheadedness.

PREGNANCY AND BREASTFEEDING

BEZALIP ® is contraindicated in pregnancy and during lactation, given the lack of studies in the literature that characterize the activity of bezafibrate on the health of the fetus and the breast-fed newborn.

Interactions

As described for the other fibrates, also bezafibrate can interact with oral anticoagulants and determine the onset of bleeding, even serious ones; therefore, prothrombin times should be monitored.

An enhancement of the hypoglycemic abilities of the sulfonylureas and of insulin itself was observed following the concomitant use of BEZALIP ®, the pharmacological interaction could therefore determine, in these cases, the onset of hypoglycemic crises.

The increase in lipid-lowering action observed following combination therapy with statins may be used for therapeutic purposes, but could significantly increase the risk of myopathies.

Furthermore, it would be advisable to avoid the concomitant intake of drugs or compounds of various nature capable of compromising liver and kidney function.

Contraindications BEZALIP ® Bezafibrate

BEZALIP ® is contraindicated in case of hypersensitivity to one of its compounds, in case of liver and colicistica affections, in case of renal insufficiency and in case of concomitant administration of statins in patients suffering from myopathies, or with predisposition to the development of muscle pathologies skeletal.

Undesirable effects - Side effects

BEZALIP ® seems to be well tolerated, leading to clinically little relevant and transient side effects, so much so that it does not generally require the suspension of therapy.

The most common adverse reactions generally involve the gastro-intestinal apparatus, with reduced appetite and nausea, and the nervous one with vertigo and headache.

The cases of hepatomegaly, myopathies and increase in serum enzymes (creatine kinase, alkaline phosphatase, creatinine, transaminase) were decidedly more rare, but clinically more relevant, for which it was necessary to suspend therapy.