Lescol

Lescol is an effective hypolipidemic drug that actively slows down the activity of HMG-CoA reductase. Its main active element is the substance fluvastatin, which has an artificial hypocholesterolemic effect. Due to its action, HMG-CoA is transformed into mevalonate, which effectively suppresses intrahepatic cholesterol binding.

The therapeutic effect is observed after 14 days with peak intensity occurring after 1 month of the course. In case of regular intake of the drug, the effect lasts for a long time.

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Indications Leskola

It is used in adults for the following disorders:

• primary hypercholesterolemia, or mixed dyslipidemia (subtype 2a, as well as 2b according to Fredrickson) - in this case, therapy is carried out together with diet;
• coronary atherosclerosis in individuals with coronary heart disease and primary hypercholesterolemia (even of low intensity) – to slow down the progression of the disease;
• people with coronary artery disease after percutaneous TBCA – to carry out secondary prevention of dangerous manifestations associated with the cardiovascular system (myocardial infarction, coronary revascularization or SCD).

For children over 9 years old, the medication is used in combination with diet in the case of a familial type of heterozygous hypercholesterolemia.

Release form

The drug is released in tablets - 7 pieces in a cell package; in a box - 1 or 2 such packages.

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Pharmacodynamics

The component fluvastatin is a racemate of two separate erythro-enantiomers, one of which always demonstrates a therapeutic effect. When cholesterol binding is weakened, its number inside liver cells decreases, and at the same time, a compensatory increase in the endings active with respect to LDL is noted. Their hepatocyte capture also increases, which leads to a decrease in plasma cholesterol values.

In individuals with a mixed form of primary dyslipidemia (subtypes 2A and 2B according to Fredrickson), in the case of using the drug in a dose of 80 mg per day, the level of TG in the plasma decreases by 25%.

In people with coronary heart disease, against the background of which hypercholesterolemia appears, a daily dose of 40 mg for 2.5 years of use causes a noticeable slowdown in the progression of the coronary type of atherosclerosis. The introduction of Lescol during coronary heart disease reduces the likelihood of a dangerous 1st cardiovascular reaction (myocardial infarction, SCD, the need for urgent revascularization or coronary bypass surgery).

The probability of sudden cardiac death or heart attack is reduced by 31% when using the drug.

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Pharmacokinetics

After oral administration, fluvastatin is completely and rapidly absorbed (60-90%). When taken with food, this process slows down insignificantly. The bioavailability of the drug is 24%. Over 98% of fluvastatin is synthesized with intraplasmic protein. The synthesis rate in this case is not tied to the level of fluvastatin, plasma values of warfarin, glyburide and salicylic acid.

Fluvastatin metabolism processes occur mainly within the liver.

Excretion occurs via the intestines (93%), and another 6% of the substance is excreted via the kidneys. Unchanged fluvastatin accounts for only 2% of the excreted volume.

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Dosing and administration

The tablets can be taken without reference to food intake. The standard size of the initial portion is 80 mg. In case of development of mild symptoms of the disease, only 20 mg of the drug can be taken. The initial dosage must be selected individually, taking into account the initial values of LDL/cholesterol and the purpose of the treatment.

The hypolipidemic effect reaches its maximum by the end of the 4th week of therapy. At this stage, the first revision of the portion size is performed, taking into account the medicinal effect. It is necessary to adhere to a hypocholesterol diet throughout the entire period of therapy.

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Use Leskola during pregnancy

Lescol use leads to a decrease in the production of cholesterol and other bioactive components. Such an effect can be harmful to the fetus and infant, which is why the drug is not used during breastfeeding and pregnancy.

Women of reproductive age should use reliable contraception. If pregnancy occurs during therapy, the drug should be discontinued immediately.

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Contraindications

Main contraindications:

• severe intolerance associated with elements of the drug;
• severe forms of hepatopathologies;
• persistent increase in serum transaminase values of unknown origin.

The medication is administered with extreme caution in the following disorders:

• presence of a history of hepatopathologies;
• alcohol abuse;
• predisposition to the development of rhabdomyolysis;
• muscle-affecting diseases of a hereditary nature;
• history of toxic musculoskeletal injury associated with the administration of other statins or fibrates.

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Side effects Leskola

Side effects include:

• lesions affecting the central nervous system: dysesthesia, insomnia, hypoesthesia, as well as paresthesia and headaches;
• disorders associated with digestive function: nausea, dyspepsia, abdominal pain, hepatitis and pancreatitis;
• problems with the functioning of blood vessels: vasculitis;
• disorders of hematopoiesis: thrombocytopenia;
• lesions of subcutaneous tissues with the epidermis: dermatitis, urticaria, bullous type of exanthema and eczema;
• Musculoskeletal symptoms: myalgia, rhabdomyolysis, muscle weakness, lupus-like manifestations, myositis and myopathy.

Overdose

Intoxication with the drug may lead to potentiation of negative symptoms.

Symptomatic actions are performed to support vital body functions.

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Interactions with other drugs

The drug is carefully combined with niacin and fibrates, cyclosporine and fluconazole.

Bile acid sequestrants can synthesize fluvastatin, which is why it is necessary to maintain at least a 4-hour interval between the administration of cholestyramine and Lescol.

Rifampicin may reduce the bioavailability of fluvastatin by approximately 50%, requiring a change in the dosage of Lescol when using such a combination.

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Storage conditions

Lescol must be stored at a maximum temperature of 30°C.

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Shelf life

Lescol can be used for a period of 36 months from the date of sale of the medicinal substance.

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Application for children

Should not be administered to persons under 9 years of age.

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Reviews

Lescol receives good reviews from doctors - it is considered a very effective medicine, always allowing to achieve positive therapeutic dynamics. The dose and treatment regimen should be selected individually, taking into account cholesterol levels.

The disadvantages include the rather high price of the drug, which is not always convenient and affordable for patients, because it must be taken for quite a long time.

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