LOVINACOR® Lovastatin

LOVINACOR ® is a drug based on lovastatin

THERAPEUTIC GROUP: Hypolipidemic - HMG-CoA reductase inhibitors

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

Indications LOVINACOR ® Lovastatina

LOVINACOR® is indicated in the treatment of primary hypercholesterolemia, heterozygous familial hypercholesterolemia and mixed dyslipidemia, in the event of failure of diet therapy and other non-pharmacological lipid-lowering measures.

The administration of LOVINACOR ® can also be recommended in case of high cardiovascular risk with incorrect hypercholesterolemia from the diet.

Mechanism of action LOVINACOR ® Lovastatin

The lovastatin contained in LOVINACOR ® is in the form of an inactive lactone, therefore biologically inoperative. Taken orally and absorbed in the gastro-intestinal tract, the drug concentrates mainly in the liver, where it is hydrolyzed in its active form of hydroxy-acid (effective in inhibiting the hepatic enzyme HMG-CoA reductase). The inhibitory action on this enzyme takes the form of a reduction in the synthesis of mevalonate, a fundamental precursor of cholesterol.

The reduced synthesis of cholesterol and associated lipoproteins acts as a positive stimulus for the expression of hepatic receptors for LDL, guaranteeing a more intense cholesterol uptake, therefore also a significant decrease in the plasma levels of this lipoprotein.

The therapeutic action of LOVINACOR ® therefore allows - by controlling the plasma values of LDL cholesterol and triglycerides - to reduce the incidence of cardiovascular events.

Approximately 24 hours after taking it, lovastatin is mainly eliminated via the liver.

Studies carried out and clinical efficacy

1 THE EFFECTIVENESS OF LOVASTATIN ON WOMEN WITH HYPERCOLESTEROLEMIA

This study of around 3390 women with mild primary hypercholesterolemia showed that administering 20 or 40 mg of lovastatin daily could promote a decrease in LDL cholesterol from 24 to 40%, in triglycerides from 9 to 18%, and a increase in HDL cholesterol from 7 to 9%.

2. THE LOVASTATIN IN THE PREVENTION OF CARDIOVASCULAR RISK

A very important study showing the effectiveness of lovastatin treatment in the prevention of cardiovascular diseases. More precisely, both the 20 mg and the 40 mg dose guaranteed a reduction in the incidence of cardiac and coronary diseases, neoplastic diseases and total mortality, compared with clinically insignificant side effects.

3. STATINE AND CANCER

The study of the antitumor potential of statins is still open, and the results in this regard are numerous and conflicting. One of the most important limitations is the contrast in the findings during the transition from cell cultures, and animal models, to human clinical practice. For example, this study shows the capacity of lovastatin - at therapeutic doses used in clinical practice - to inhibit the growth of prostate cancer cells in vitro. Although these results seem quite encouraging, noteworthy clinical trials are still lacking.

Method of use and dosage

LOVINACOR ® 10/20/40 mg lovastatin tablets : this medicine should be taken only after a period of at least a quarter of a hypolipid diet and controlled physical activity.

In the absence of an effective therapeutic response, drug therapy with LOVINACOR ® should be started by taking one 10mg tablet a day, possibly in the evening during dinner.

If this dosage is ineffective, the doctor may increase the dose up to 40mg daily. This corrective intervention is to be considered only after 4 weeks from the start of lovastatin therapy, a period necessary to achieve maximum lipid-lowering efficacy of LOVINACOR ®

An adjustment of the doses could be required in case of concomitant therapy with lipid-lowering drugs or in case of renal insufficiency.

IN ANY CASE, BEFORE TAKING LOVINACOR ® Lovastatina, THE PRESCRIPTION AND CONTROL OF ITS OWN DOCTOR IS NECESSARY.

Warnings LOVINACOR ® Lovastatina

As mentioned, the pharmacological therapy of hypercholesterolemia represents a phase following dietary and lifestyle adjustment. Consequently, all non-pharmacological interventions aimed at contrasting this condition should be maintained even during therapy with LOVINACOR ®

Before and while taking lovastatin it is advisable to monitor the liver function and the plasma level of transaminases, in order to avoid the onset of liver diseases. In fact, if the blood concentrations of liver enzymes exceed 3 times the normal ones, it is advisable to immediately stop the drug therapy.

In addition to transaminases, the doctor should investigate the possible presence of muscular pathologies, previous myopathies or conditions predisposing to damage to the skeletal muscle (advanced age or concomitant administration of particular drugs). All this in order to minimize the risk of rhabdomyolysis described after taking lovastatin. Serum creatinkinase levels should be constantly monitored in these groups of patients at risk.

In healthy patients it would still be advisable to ascertain the absence of symptoms related to muscle damage - such as fatigue, persistent fatigue and muscle pain - to eventually investigate them through appropriate hematoclinic investigations.

Long-term therapy with LOVINACOR ® although only in exceptional cases, has been associated with interstitial lung disease, characterized by dyspnea, cough, asthenia, fever and weight loss.

LOVINACOR ® contains lactose among its excipients; therefore, its intake could lead to the onset of gastro-enteric side effects of varying severity in patients suffering from intolerance and malabsorption of glucose / galactose, or from lactase enzyme deficiency.

Despite the side effects associated with lovastatin therapy, the presence of vertigo is described, LOVINACOR ® does not seem to interfere with the normal driving skills of vehicles and the use of machinery.

PREGNANCY AND BREASTFEEDING

Given the importance of cholesterol in the embryonic and fetal development phases, the administration of LOVINACOR ® during the period of pregnancy is strictly contraindicated.

It is also advisable to suspend breastfeeding during therapy, given the absence of studies that characterize the pharmacokinetic properties of the active ingredient taken with breast milk and their repercussions on the health of the newborn.

Interactions

Lovastatin is metabolised in the liver mainly by the cytochrome P450 3A4 enzyme, easily modulated by different active ingredients, which can therefore alter the normal pharmacokinetic properties of LOVINACOR ®

In particular:

Intake of CYP3A4 inhibitors (chamomile, grapefruit juice, itraconazole, ketoconazole, HIV protease inhibitors, erythromycin, clarithromycin, cyclosporine, telithromycin and nefazodone) could result in a significant increase in drug exposure, increasing the incidence of even serious side effects;
The concomitant administration of fibrates, niacin and other low-fat drugs could lead to an increase in biological activity, with an increased risk of rhabdomyolysis and myopathies;

Finally, lovastatin - like other statins - could increase prothrombin time, thus enhancing the therapeutic effects of oral anticoagulants.

Contraindications LOVINACOR ® Lovastatina

LOVINACOR ® is contraindicated in case of previous history of myopathy or predisposition to the development of this disease, in case of active liver disease, in case of hypersensitivity to the drug or to one of its components, and during the entire period of pregnancy and breastfeeding.

Undesirable effects - Side effects

The side effects described following lovastatin are generally not clinically relevant and transient.

The most common adverse reactions were asthenia, abdominal pain, constipation, nausea, cramps, myalgia and dizziness.

More important and serious side effects - such as interstitial lung disease, liver damage, neurological and musculoskeletal damage - have been described, albeit rarely, in patients at risk or with a predisposition to certain pathologies. In these cases. however, discontinuation of LOVINACOR ® therapy ensured a rapid return to normal function.