LOVINACOR ® is a lovastatin-based drug
THERAPEUTIC GROUP: Lipid-lowering agents - HMG-CoA reductase inhibitors
Indications LOVINACOR ® Lovastatin
LOVINACOR® is indicated in the treatment of primary hypercholesterolemia, heterozygous familial hypercholesterolemia and mixed dyslipidemia, in case of failure of dietary therapy and other non-pharmacological lipid-lowering measures.
The administration of LOVINACOR ® can also be recommended in case of high cardiovascular risk with hypercholesterolemia not corrected by the diet.
Mechanism of action LOVINACOR ® Lovastatin
The lovastatin contained in LOVINACOR ® is found in the form of an inactive lactone, therefore biologically not functioning. Taken orally and absorbed in the gastro-intestinal tract, the drug is mainly concentrated in the liver, where it is hydrolyzed into its active form of hydroxy-acid (effective in inhibiting the hepatic enzyme HMG-CoA reductase). The inhibitory action on this enzyme materializes in the reduction of 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, ensuring a more intense uptake of cholesterol, therefore also a significant drop in 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.
About 24 hours after its intake, lovastatin is eliminated mainly by the liver.
Studies carried out and clinical efficacy
1. THE EFFECTIVENESS OF LOVASTATINE ON WOMEN WITH HYPERCHOLESTEROLEMIA
Ann Intern Med. 1993 Jun 1; 118: 850-5.
Efficacy and tolerability of lovastatin in 3390 women with moderate hypercholesterolemia.
Bradford RH, Downton M, Chremos AN, Langendörfer A, Stinnett S, Nash DT, Mantell G, Shear CL.
This study, conducted on about 3390 women with mild primary hypercholesterolemia, showed how the administration of 20 or 40 mg of lovastatin per day can promote a drop in LDL cholesterol from 24 to 40%, triglycerides from 9 to 18%, and a increase in HDL cholesterol from 7 to 9%.
2. LOVASTATINE IN THE PREVENTION OF CARDIOVASCULAR RISK
Am J Cardiol. 2001 May 1; 87: 1074-9.
Air Force / Texas Coronary Atherosclerosis Prevention Study (AFCAPS / TEXCAPS): additional perspectives on tolerability of long-term treatment with lovastatin.
Downs JR, Clearfield M, Tyroler HA, Whitney EJ, Kruyer W, Langendorfer A, Zagrebelsky V, Weis S, Shapiro DR, Beere PA, Gotto AM.
Very important study that shows the effectiveness of treatment with lovastatin in the prevention of cardiovascular diseases. More precisely, both the 20 mg and 40 mg doses have guaranteed a reduction in the incidence of heart and coronary diseases, neoplastic diseases and mortality. total, in the face of clinically insignificant side effects.
3. STATINS AND CANCER
Beijing By Xue Xue Bao. 2010 Aug 18; 42: 391-5.
Effects of clinically effective dose of lovastatin on prostate cancer PC3 cells
Yang L, Wang Y, Lv TJ, Zhou LQ, Jin J.
The study of the anticancer potential of statins is still open, and in the literature there are numerous and conflicting results in this regard. One of the most important limitations is the contrast in findings during the transition from cell cultures, and animal models, to human clinical practice. For example, this study shows the ability of lovastatin - at therapeutic doses used in clinical practice - to inhibit growth of prostate cancer cells in vitro Although these results seem somewhat encouraging, there is still a lack of noteworthy clinical trials.
Method of use and dosage
LOVINACOR ® 10/20/40 mg tablets of lovastatin: The intake of this drug should only be recommended after a period, at least three months, of a low-fat diet and controlled physical activity.
In the absence of an effective therapeutic response, drug therapy with LOVINACOR ® should be initiated by taking one 10mg tablet daily, possibly in the evening during dinner.
If this dosage is ineffective, your doctor may increase the dose up to 40mg daily. This corrective intervention is to be considered only after 4 weeks from the beginning of therapy with lovastatin, the period necessary to achieve the maximum lipid-lowering efficacy of LOVINACOR ®.
Dose adjustment may be required in case of concomitant therapy with lipid-lowering drugs or in case of renal insufficiency.
IN ANY CASE, BEFORE TAKING LOVINACOR ® Lovastatin - YOU MUST BE REQUIRED AND CHECK FROM YOUR DOCTOR.
Warnings LOVINACOR ® Lovastatin
As mentioned, the drug therapy of hypercholesterolemia represents a phase subsequent to dietary and lifestyle adjustment. Consequently, all non-pharmacological interventions aimed at counteracting this condition should also be maintained during therapy with LOVINACOR ®.
Before and during the intake of lovastatin it is advisable to monitor the liver function and the plasma level of transaminases, in order to avoid the onset of liver disease. In fact, if the blood concentrations of liver enzymes exceed the normal ones by 3 times, it is advisable to immediately discontinue drug therapy.
In addition to transaminases, the doctor should investigate the presence of muscle pathologies, previous myopathies or conditions predisposing to damage to skeletal muscle (advanced age or concomitant administration of particular drugs). All this in order to minimize the risk of rhabdomyolysis described after taking lovastatin. In these at-risk patient groups, serum creatinkinase levels should be monitored continuously.
In healthy patients, however, it would be advisable to ascertain the absence of symptoms related to muscle damage - such as asthenia, persistent fatigue and muscle pain - and then possibly investigate them through appropriate haematoclinical investigations.
Long-term therapy with LOVINACOR ®, albeit only in exceptional cases, has been associated with interstitial lung disease, characterized by dyspnoea, 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 glucose / galactose intolerance and malabsorption, or from lactase enzymatic deficiency.
Although dizziness is described as one of the side effects associated with lovastatin therapy, LOVINACOR ® does not appear to interfere with the normal ability to drive and use machines.
PREGNANCY AND BREASTFEEDING
Given the importance of cholesterol in the stages of embryonic and fetal development, the administration of LOVINACOR ® during pregnancy is strictly contraindicated.
It is also advisable to discontinue breastfeeding during therapy, given the absence of studies characterizing 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 ®
Particularly:
- Taking cytochrome 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 by increasing incidence of side effects, including serious ones;
- The concomitant administration of fibrates, niacin and other lipid-reducing drugs could cause an increase in biological activity, with an increase in the risk of rhabdomyolysis and myopathies;
Finally, lovastatin - like other statins - could lead to an increase in prothrombin time, thus enhancing the therapeutic effects of oral anticoagulants.
Contraindications LOVINACOR ® Lovastatin
LOVINACOR ® is contraindicated in case of a previous history of myopathy or predisposition to the development of this pathology, in case of liver disease in the active phase, 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 after taking lovastatin are generally not clinically relevant and transient.
The most common adverse reactions included 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 predisposed to certain pathologies. In these cases. however, the suspension of therapy with LOVINACOR ® ensured a rapid restoration of normal functions.
Note
LOVINACOR ® can only be sold under medical prescription.
The information on LOVINACOR ® Lovastatin 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.
