Lescol

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

Therapeutic effect is observed after 14 days with a peak intensity occurring after 1 month of the course. In the case of regular use of the drug, the effect persists for a long time.

[1]

Indications Leskola

It is used in adults with such disorders:

• primary hypercholesterolemia, or dyslipidemia of a mixed nature (subspecies 2a, as well as 2b according to Fredrickson) - while this therapy is carried out together with a diet;
• coronary atherosclerosis in people with coronary artery disease and the primary stage of hypercholesterolemia (even with weak intensity) - to slow the progression of the disease;
• people with coronary artery disease after percutaneous TBCA - to conduct secondary prevention of dangerous manifestations associated with cardiovascular disease (myocardial infarction, revascularization of a coronary nature or ARIA).

For a child of 9 years old, the drug is used in combination with a diet in the case of a heterozygous family of hypercholesterolemia.

Release form

The release of the drug is sold in tablets - 7 pieces inside the cellular packaging; in the box - 1 or 2 such packages.

[2], [3]

Pharmacodynamics

Component fluvastatin acts as a racemate of 2 separate erythro-enantiomers, among which one always demonstrates therapeutic effect. With a weakening of cholesterol binding, a decrease in its number inside liver cells occurs, and with it a compensatory increase in endings active relative to LDL is noted. Their hepatocyte uptake is also increasing, which leads to a decrease in plasma cholesterol values.

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

In persons with coronary artery disease, against the background of which hypercholesterolemia appears, the daily dosage of 40 mg in 2.5 years of use causes a marked inhibition of the progression of coronary atherosclerosis. The introduction of Lescola during ischemic 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 BCC or heart attack is reduced by 31% when using drugs.

[4], [5], [6], [7],

Pharmacokinetics

After ingestion, fluvastatin is absorbed completely and at high speed (60-90%). When taken with food, this process slows down insignificantly. The level of bioavailability of the drug is 24%. With intra plasma protein, over 98% of fluvastatin is synthesized. Synthesis rate in this case is not tied to the level of fluvastatin, plasma values of warfarin, glyburide and salicylic acid.

The metabolism of fluvastatin mostly takes place inside the liver.

Excretion is carried out by the intestine (93%), and another 6% of the substance is excreted through the kidneys. Unchanged fluvastatin is only 2% of the excreted volume.

[8], [9], [10]

Dosing and administration

Tablets can be used without reference to food intake. The standard size of the initial portion is 80 mg. In the case of the development of mild symptoms of the disease, you can take only 20 mg of the drug. It is necessary to select the initial dosage personally, taking into account the initial values of LDL / cholesterol and the goal of the treatment being performed.

The lipid-lowering effect reaches its maximum by the end of the 4th week of therapy. At this stage, the first revision of the portion size is carried out, which takes into account the effect of medication. The entire period of therapy is necessary to adhere to the cholesterol diet.

[17], [18], [19]

Use Leskola during pregnancy

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

Women living in reproductive age need to use reliable contraception. If pregnancy occurs during therapy, the medication should be immediately withdrawn.

[11], [12], [13]

Contraindications

The main contraindications:

• severe intolerance associated with elements of the drug;
• severe forms of hepatopathology;
• persistent increase in serum transaminase levels, which has an unknown nature.

Extremely carefully the drug is administered with such violations:

• a history of hepatopathology;
• alcohol abuse;
• predisposition to the development of rhabdomyolysis;
• muscular diseases of hereditary nature;
• history of toxic lesion of the musculoskeletal structure associated with the introduction of other statins or fibrates.

[14], [15], [16]

Side effects Leskola

Among the side effects:

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

Overdose

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

Symptomatic actions are performed that support vital body functions.

[20], [21], [22]

Interactions with other drugs

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

Gall-acid sequestrants can synthesize fluvastatin, due to which it is necessary to observe a minimum of 4-hour interval between the administration of Kolestiramine and Lescol.

Rifampicin can reduce fluvastatin's bioavailability by about 50%, which requires a change in the portion of Lescol in case of using such a combination.

[23], [24], [25], [26]

Storage conditions

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

[27]

Shelf life

Lescol can be used for a 36-month term since the sale of the drug substance.

[28],

Application for children

It can not be appointed to persons under the 9th anniversary.

[29], [30],

Reviews

Leskol receives good reviews from doctors - he is considered a very effective drug, always allowing to achieve a positive therapeutic dynamics. The portion and the scheme of therapy should be selected personally, taking into account the indicators of cholesterol.

Of the minuses, the cost of the medicine is rather high, which is not always convenient and affordable for patients, because it needs to be taken for quite a long time.

[31], [32], [33],