Leskol - instructions for use, reviews, analogs and forms of release (capsules 20 mg, 40 mg and tablets 80 mg Forte) drug for the treatment of hypercholesterolemia and hyperlipidemia in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Leskol. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Leskol in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Leskola in the presence of existing structural analogues. Use for the treatment of hypercholesterolemia (high cholesterol in the blood) and hyperlipidemia in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Leskol - a hypolipidemic agent from the group of statins, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A-reductase (HMG-CoA reductase). According to the principle of competitive antagonism, the statin molecule binds to that part of the coenzyme A receptor where this enzyme is attached. Another part of the statin molecule inhibits the conversion of hydroxymethylglutarate to mevalonate, an intermediate in the synthesis of the cholesterol molecule. Inhibition of HMG-CoA reductase activity results in a series of consecutive reactions that result in a decrease in intracellular cholesterol and a compensatory increase in the activity of low-density lipoprotein receptors (LDL receptors) and, accordingly, acceleration of catabolism of cholesterol in the form of low-density lipoproteins (Xc-LDL ).

The hypolipidemic effect of fluvastatin (the active substance of Lescoll) is associated with a decrease in the total cholesterol level due to X-LDL. The decrease in LDL is dose-dependent and has a non-linear, but an exponential nature.

Statins do not affect the activity of lipoprotein and hepatic lipases,do not have a significant effect on the synthesis and catabolism of free fatty acids, so their effect on triglyceride levels (TG) is secondary and mediated through their main effects on lowering the level of LDL-C. The moderate decrease in TG levels in statin therapy appears to be due to the expression of the receptor (apo E) receptors on the surface of hepatocytes involved in the catabolism of intermediate-density lipoproteins (ALTs), of which about 30% of TG is involved.

In addition to lipid-lowering effects, statins have a positive effect on endothelial dysfunction (preclinical signs of early atherosclerosis), on the vascular wall, atheroma state, improve the rheological properties of blood, and possess antioxidant, antiproliferative properties.

Composition

Fluvastatin + excipients.

Pharmacokinetics

The maximum concentration of fluvastatin depends on the dosage form taken, the time taken to eat, the fat content of the food, the duration of the drug intake, and the individual metabolic features. Binding to plasma proteins - more than 98%. Leskol undergoes intensive metabolism at the "first pass" through the liver before entering the systemicblood flow. In patients with hepatic insufficiency, there is a possibility of cumulation of the drug. It is excreted as metabolites through the biliary tract (93%), with urine (6%), unchanged - 2%. The fluvastatin biotransformation pathway is not associated with the isoenzymes of the cytochrome P450 system, and the metabolism remains virtually unchanged under the action of drugs that affect this enzyme system. The main components circulating in the blood: fluvastatin and the pharmacologically inactive metabolite N-desisopropyl-propionic acid. Hydroxylated metabolites have pharmacological activity, but they do not enter the systemic circulation.

Indications

• primary hypercholesterolemia in the absence or inadequate effectiveness of diet therapy, including pure hypercholesterolemia;
• mixed hyperlipidemia.

Forms of release

Capsules 20 mg and 40 mg.

Tablets coated with a coating, 80 mg (Lescola Forte).

Instructions for use and dosing regimen

Inside, regardless of food intake, swallowing whole, with a glass of water, once a day. Since fluvastatin does not interact with substances that are substrates for the isoenzyme CYP3A4, its interaction with grapefruit juice is not expected.There was no decrease in the hypolipidemic effect of fluvastatin when administered during the evening meal or 4 hours after it.

Since the maximum lipid-lowering effect of the drug develops by the 4th week, the first revision of the dose of the drug is carried out depending on the effect achieved, with an interval of at least 4 weeks. The therapeutic effect of Lescola is preserved with its long-term use.

Before starting treatment, the patient should be transferred to a standard hypocholesterol diet. The diet should be followed and during the entire treatment period.

The initial recommended dose is 40 mg (1 capsule of Lescol 40 mg) or 80 mg (2 capsules of Lescol 40 mg or 1 tablet Lescola Forte 80 mg) once a day. In mild cases of the disease, a sufficient dose of fluvastatin 20 mg (1 capsule of Lescol 20 mg) may be sufficient. The initial dose should be selected individually, taking into account the initial level of cholesterol / LDL and the stated goal of therapy.

For patients with coronary heart disease after balloon angioplasty, the recommended initial dose is 80 mg per day.

Leskol is effective when used as a monotherapy. There are data confirming its effectiveness and safety when combined with nicotinic acid, colestyramine or fibrates.

Children and teenagers under 18 years of age

Within 6 months prior to the beginning of therapy with Lescola in children and adolescents older than 9 years, one should adhere to the standard hypocholesterol diet, which must be followed during the entire treatment period. The recommended average dose is 20-40 mg orally once a day, usually in the evening. Initial doses should be selected individually according to the baseline cholesterol level and treatment goals. The use of fluvastatin simultaneously with nicotinic acid, colestyramine or fibrates in children and adolescents has not been studied.

Side effect

• dyspepsia (indigestion);
• pain in the abdominal region (in the abdomen);
• nausea;
• constipation, diarrhea;
• hepatitis (inflammation of the liver);
• headache, dizziness;
• insomnia;
• sensitivity disorders - paresthesia, dysesthesia and hypoesthesia, possibly related to the underlying disease;
• rash, hives;
• eczema, dermatitis, exanthema;
• angioedema;
• thrombocytopenia;
• vasculitis (inflammation of blood vessels);
• lupus-like syndrome;
• Myalgia (pain in muscles), tenderness of muscles;
• muscle weakness;
• Myopathy (dystrophic changes in muscle tissue);
• myositis (inflammation of the muscles);
• rhabdomyolysis (destruction of cells of muscle tissue);
• increased activity of hepatic transaminases, creatine phosphokinase (CK), alkaline phosphatase (APF).

Contraindications

• active pathological process in the liver;
• persistent increase in the level of hepatic transaminases in the blood;
• renal failure (creatinine clearance (CK) less than 30 ml per minute or serum creatinine content more than 250 μmol per liter);
• violation of muscle tone of unknown origin;
• increased activity of creatine phosphokinase (CKF);
• pregnancy and lactation (the period of breastfeeding);
• hypersensitivity to fluvastatin.

Application in pregnancy and lactation

Leskol is contraindicated for use during pregnancy and lactation.

Women of childbearing age in the course of fluvastatin therapy should use reliable methods of contraception. If nevertheless, when fluvastatin treatment occurs, pregnancy should be stopped immediately.

Since HMG-CoA reductase inhibitors reduce the synthesis of cholesterol and, probably, other biologically active substances - cholesterol derivatives, when prescribing these drugs to pregnant women, they can harm the fetus.

Use in children

Contraindicated in children under 9 years.

Application in elderly patients

Efficacy and good tolerability of Lescol was demonstrated for patients aged 65 years and younger. In the age group older than 65 years, the response to treatment was more pronounced, and no data were available that would indicate a worse tolerability, was not obtained. Thus, there is no need to change the dose of the drug taking into account the age.

special instructions

They are used with caution in patients with liver diseases, chronic alcoholism, diffuse myalgia, epilepsy, and renal insufficiency.

Since fluvastatin is excreted mainly by the liver and only less than 6% of the dose received in the body is excreted in the urine, in patients with impaired renal function of any severity, there is no need to adjust the dose of the drug.

Contraindicated the use of Leskol with active liver disease or persistent increase in the concentration of serum transaminases of unknown etiology.

Drug Interactions

With simultaneous use with warfarin, its anticoagulant effect is enhanced.

With simultaneous application with colestyramin, the bioavailability of fluvastatin decreases, while the overall lipid-lowering effect is enhanced.

With simultaneous use with rifampicin, the concentration of fluvastatin in the blood plasma decreases, apparently due to the increase in its metabolism in the liver under the influence of rifampicin, which is the inducer of microsomal liver enzymes.

When used simultaneously with cyclosporine, there are reports of the development of myalgia and increased activity of CK.

When used simultaneously with cimetidine, ranitidine, omeprazole, an increase in fluvastatin absorption is possible.

Analogues of the medicinal product Leskol

Structural analogs for the active substance:

• Lescola Forte.

Analogues of Lescol on the pharmacological group (statins):

• Akorta;
• Aktalipid;
• Anistat;
• Apexstatin;
• Atherostat;
• Atokord;
• Atomax;
• Ator;
• Atorvastatin;
• Atorvox;
• Atoris;
• The Vasator;
• Vazilip;
• Vero-Simvastatin;
• Zocor;
• Zorstat;
• Cardiostatin;
• The Cross;
• Lipobay;
• Lipon;
• Lipopraim;
• Lipostat;
• Lipofford;
• Liprimar;
• Lovacor;
• Lovastatin;
• Lovasterol;
• Mevakor;
• Medostatin;
• Mertenil;
• Novostat;
• Ovenkor;
• Pravastatin;
• Reddistatin;
• Ro-statin;
• Rovacor;
• Rosart;
• Rosystark;
• Rosuvastatin;
• Rosewood;
• Rosulip;
• Rozufast;
• Roxer;
• Rustor;
• Simva Hexal;
• Simvakol;
• Simvale;
• Simvastatin;
• Simvastol;
• Symvor;
• Simgal;
• Simlo;
• Sinquard;
• Suvardio;
• TG-torus;
• Tevastor;
• Torvacard;
• Torvalip;
• Torvas;
• Tulip;
• Holvasim;
• Holletar.

Response of a therapist

I prescribe Leskol not as often as other statins. This is due, in the first place, to its rather high cost. Not every patient has this medicine on his pocket, especially since the treatment implies long-term use of tablets. But Leskol's therapeutic effect is good. Usually, one month from the beginning of the admission, when the patient gives the first control blood test for cholesterol and triglycerides, their concentration is already within the normal range.The initial dose of the drug, I select individually, depending on the initial level of cholesterol in the blood. There are, of course, cases when it is necessary to increase the daily dose. But it is always possible to achieve positive dynamics.

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