Lovastatin - instructions for use, dose, side effects, contraindications

Active substanceLovastatinLovastatin

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Dosage form: & nbsppills

Composition:Each tablet contains: active substance lovastatin 20 mg, and Excipients: Lactose monohydrate, microcrystalline cellulose, starch prezhelatizirovaniy, butylhydroxyanisole, ascorbic acid, citric acid, magnesium stearate, indigo carmine.

Description:Tablets are light blue with marbling, round, biconvex, with a risk on one side.

Pharmacotherapeutic group:Lipid-lowering agent - inhibitor

ATX: & nbsp

C.10.A.A.02 Lovastatin

C.10.A.A Inhibitors of HMG-CoA reductase

Pharmacodynamics:

Gipolipidemicheskoe means, violates the early stages of the synthesis of cholesterol in the liver (in the stage of levan acid). The body forms a free beta-hydroxy acid, which competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A reductase and gives its conversion to mevalonate, resulting in decreased cholesterol synthesis, increasing its catabolism.Reduces the blood levels of very low density lipoproteins, low-density lipoproteins and triglycerides, moderately increases the high-density lipoprotein content. Significantly reduces the amount of apoprotein B (which is part of low-density lipoproteins) and other circulating components of low-density lipoproteins.

The expressed therapeutic effect is manifested within 2 weeks, and the maximum - in 4-6 weeks from the start of treatment.

Lovastatin is effective in primary hypercholesterolemia in patients with uncomplicated compensated insulin-dependent (type I) and non-insulin-dependent (type II) diabetes mellitus.

Pharmacokinetics:

In the gastrointestinal tract is absorbed slowly and not completely - about 30% of the dose taken, taking an empty stomach reduces absorption by 30%. The maximum concentration in the blood plasma is observed after 2-4 hours, then the level in the blood plasma rapidly decreases, making after 24 hours 10% of the maximum. Connection with blood plasma proteins - 95%. The clearance of lovastatin and its active metabolites with a single appointment for the night is achieved on the 2-3 day of therapy and 1.5 times higher than after a single dose.

Penetrates through the blood-brain barrier and placental barrier.

It is subjected to intensive metabolism during the "first passage" through the liver, is oxidized to beta-hydroxy acid, its 6-hydroxy derivative and other metabolites, some of which are pharmacologically active (blocking 3-hydroxy-3 methylglutaryl coenzyme A-reductase).

The half-life is 3 hours. Output through the intestine - 83%, kidneys 10%.

Indications:

Primary hypercholesterolemia with a high content of LDL type IIa and IIb (not corrected by special diet and exercise), combined hypercholesterolemia and hypertriglyceridemia.

Treatment of coronary atherosclerosis in patients with ischemic heart disease in order to slow its progression.

Contraindications:

Hypersensitivity to the drug, liver disease in the acute phase. An increase in the activity of "liver" transaminases (unknown etiology), the general severe condition of the patient, pregnancy, lactation, age under 18 (safety and efficacy not established).

Carefully:With liver diseases (in the anamnesis), chronic alcoholism, transplantation, organs,concomitant immunosuppressive therapy, chronic renal failure, urgent surgical manipulations (including dental), with simultaneous admission with gemfibrozil and other fibrates, niacin (more than 1 g / day) because of the risk of myopathy.

Dosing and Administration:

Inside, with food, with hypercholesterolemia, the initial dose is 10-20 mg once a day, in the evening (cholesterol is synthesized mainly at night), with atherosclerosis - 20-40 mg / day. If necessary, increase the dose every 4 weeks. The maximum daily dose is 80 mg for 1 or 2 doses (during breakfast and dinner).

Before the appointment, as well as during the application of the drug, the patient should be assigned a standard diet-lowering cholesterol.

If the concentration of total cholesterol in the blood plasma drops to 140/100 ml (3.6 mmol / L) or low-density lipoprotein cholesterol to 75 mg / 100 mg (1.94 mmol / L), the dose should be reduced. With simultaneous appointment with drugs that suppress immunity, as well as with severe chronic renal failure (creatinine clearance <30 ml / min.), Fibrates, niacin, the daily dose should not exceed 20 mg.

Side effects:

From the digestive tract: heartburn, nausea, diarrhea, constipation, flatulence, abdominal pain, dry mouth, taste disorder, anorexia, gastralgia, cholestatic jaundice, hepatitis, acute pancreatitis.

From the central nervous system: dizziness, headache, general weakness, convulsions, insomnia paresthesia, mental disorders.

From the musculoskeletal system: myalgia, myositis, myopathy, rhabdomyolysis (in patients receiving simultaneously ciclosporin, gemfibrozil or nicotinic acid), arthralgia.

From the hematopoiesis: hemolytic anemia, leukopenia, thrombocytopenia.

From the sense organ: "fog" before the eyes, clouding of the lens, cataracts, atrophy of the optic nerve.

Laboratory indicators: an increase in the activity of "hepatic" transaminases, an increase in the activity of creatinine phosphokinase, alkaline phosphatase, bilirubin, eosinophilia, an increase in ESR, a positive test for antinuclear antibodies.

Allergic reactions: urticaria, Quincke's edema, toxic epidermal necrolysis, skin itch, rash.

Other: decreased potency,acute renal failure (due to rhabdomyolysis) chest pain, palpitations.

Overdose:The firm does not have information about the symptoms of overdose.

Interaction:

Immunosuppressants, gemfibrozil, a nicotinic acid, cyclosporins, erythromycins increase the risk of rhabdomyolysis, acute renal failure.

Strengthens the anticoagulant effect of indirect anticoagulants and the risk of bleeding. Regular prothrombin time control is necessary.

Kolestyramin and colestipol reduce bioavailability (the use of lovastatin is possible 4 hours after taking these drugs, with an additive effect noted).

Cyclosporine increases the plasma level of lovastatin metabolites.

Fibrates, a nicotinic acid, intraconazole and other antifungal agents of the azole group, erythromycin increase the risk of myopathy.

Grapefruit juice in large quantities increases the maximum concentration in the blood plasma and AUC of lovastatin and the risk of myopathy (their simultaneous use is not recommended).

Special instructions:

Patients should be warned that in case of unexplained pain in the muscles, tenderness and weakness of the muscles (especially when combined with a fever), they should consult a doctor.

In the case of a persistent elevation in the blood transaminases and / or creatine phosphokinase, drug withdrawal is indicated.

Therapy should be interrupted for a long time or discontinued if the patient's general serious condition is due to some disease.

With prolonged therapy, biochemical control of liver function is indicated. The activity of transaminases is determined before the start of treatment, every 8 weeks during the first year of therapy, then at least once every six months.

Patients who have a daily dose of 80 mg should be examined once every three months. When the activity of transaminases increases, the study should be repeated and subsequently carried out more often. In case of an increase in transaminase levels, especially when the upper limit of the norm is exceeded 3 times, the drug should be canceled,

If the current dose is skipped, the drug should be taken as soon as possible. If the time of the next dose has come, do not increase the dose.

During the treatment, patients should be on a standard diet with low cholesterol.

Form release / dosage:Tablets of 20 mg.

Packaging:10 tablets per blister. 2 blisters together with instructions for use in a cardboard box.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001669

Date of registration:16.06.2006 / 23.12.2009

Expiration Date:16.06.2011

The owner of the registration certificate:REPLEK FARM Skopje, OOOREPLEK FARM Skopje, OOO Macedonia

Manufacturer: & nbsp

REPLEK PHARM, Ltd. Macedonia

Representation: & nbspREPLECK FARM LTD SCOPJEREPLECK FARM LTD SCOPJERussia

Information update date: & nbsp12.04.2018

Illustrated instructions

Instructions

Lovastatin (Lovastatin)