Medostatin - 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

Excipients:

Lactose Monohydrate 146 mg

Pregelatinized starch 27 mg

Microcrystalline cellulose 10 mg

Butylhydroxyanisole 0.04 mg

Magnesium stearate 1.0 mg

Indigokarmin (indigotin E 132) 0.1 mg

Description:Round, flat blue tablets with separating risk on one side. Minor inclusions are possible.

Pharmacotherapeutic group:Hypolipidemic agent - inhibitor of HMG-CoA reductase

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 mevalonic acid). In the body it forms a free beta-hydroxy acid, which competitively inhibits 3-hydroxy-3-methylglutaryl coenzyme A-reductase and breaks its transformation into mevalonate, as a result of which the synthesis of cholesterol decreases, its catabolism increases.Reduces the concentration of triglycerides (TG), low density lipoprotein (JIPP) and very low density lipoproteins (VLDL) in the blood. Significantly reduces the amount of apoprotein B (which is part of low-density lipoproteins) and other circulating components of low-density lipoproteins. Moderately increases the concentration of high-density lipoproteins (HDL).

The expressed therapeutic effect is manifested during 2 weeks of therapy, 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 1) and non-insulin-dependent (type 2) diabetes mellitus.

Pharmacokinetics:

In the gastrointestinal tract (GIT) is absorbed slowly and not completely - about 30% of the dose taken internally, taking an empty stomach reduces absorption by 30%. The maximum concentration in the blood plasma is achieved in 2-4 hours after taking the drug, after 2-3 days, on the condition of daily intake, an equilibrium concentration is achieved. The connection with blood plasma proteins is more than 95%, penetrates through the blood-brain and placental barriers.

Lovastatin is hydrolyzed in the liver with the formation of an active beta-hydroxy acid, its 6-hydroxy derivative and other metabolites, some of which are pharmacologically active (blocking 3-hydroxy-3-methylglutaryl coenzyme A-reductase). Metabolized by the isoenzyme CYP3A4.

The clearance of lovastatin and its active metabolites with a single admission for the night is reached on the 2-3 day of therapy and is 1.5 times higher than after a single dose at a different time of day.

The half-life is 3 hours. 83% are excreted through the intestine and 10% by the kidneys.

Indications:

Primary hypercholesterolemia with high concentration of LDL type IIa and IIb according to Fredriksen classification (not corrected by special diet and exercise), combined hypercholesterolemia and hypertriglyceridemia.

In patients with ischemic heart disease in order to slow the progression of coronary atherosclerosis.

Contraindications:Hypersensitivity to the components of the drug; liver disease in the active phase; increased activity of "liver" transaminases (unclear etiology); use in women of reproductive age not using reliable methods of contraception; pregnancy orpregnancy planning; the period of breastfeeding; the general severe condition of the patient; age under 18 years (safety and efficacy not established); simultaneous administration of potent inhibitors of the isoenzyme CYP3A4 (incl. itraconazole, ketoconazole, posaconazole, HIV protease inhibitors, bocepprir, telaprevir, erythromycin, clarithromycin, telithromycin and nefazodone); simultaneous reception of gemfibrozil, cyclosporine; lactose intolerance, lactase deficiency, glucose-galactose malabsorption; grapefruit juice - more than 1 liter per day.

Carefully:Liver diseases (history), alcohol abuse, patients after organ transplantation who undergo immunosuppressive therapy (increased risk of rhabdomyolysis and renal insufficiency), surgical interventions (including dental), while taking with gemfibrozil and other fibrates, nicotinic acid in lipid-lowering doses (more than 1 g / day) because of the risk of myopathy.

Pregnancy and lactation:The drug is contraindicated during pregnancy and during breastfeeding.

Dosing and Administration:

The drug is taken once a day in the evening (cholesterol is synthesized mostly at night) during meals. During treatment with Honey, it is necessary to follow the standard cholesterol reducing diet.

Hypercholesterolemia

The initial dose of 10 (1/2 tablet 20 mg) - 20 mg / day. If necessary, increase the dose (1 every 4 weeks). The maximum daily dose of 80 mg in one session or in two meals (during breakfast and dinner).

If the plasma concentration of total cholesterol is reduced to 140 mg / 100 ml (3.6 mmol / L) or LDL-cholesterol to 75 mg / 100 ml (1.94 mmol / l), the dose should be reduced. At simultaneous appointment of Medostatin with immunosuppressant drugs, fibrates, nicotinic acid in lipid-lowering doses (more than 1 g / day), Danazol, Diltiazem, Verapamil, and also with pronounced chronic renal failure (creatinine clearance <30 ml / min), the maximum daily dose should not exceed 20 mg. With the simultaneous appointment of Medostatin with Amiodarone, the maximum daily dose should not exceed 40 mg.

Coronary atherosclerosis

The initial dose of 20-40 mg / day. If necessary, increase the dose (1 every 4 weeks). The maximum daily dose of 80 mg in one session or in two meals (during breakfast and dinner).

Side effects:

From the digestive system: heartburn, nausea, diarrhea, constipation, flatulence, vomiting, dryness of the oral mucosa, abdominal pain, taste disorder, anorexia, gastralgia (pain in the stomach), cholestatic jaundice, hepatitis, impaired liver function, acute pancreatitis.

From the central nervous system: dizziness, headache, general weakness, convulsions, insomnia, paresthesia, peripheral neuropathy, memory loss, mental disorders (including anxiety).

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

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

Allergic reactions: when taking statins described a syndrome that can include hemolytic anemia, leukopenia, thrombocytopenia, eosinophilia, increased erythrocyte sedimentation rate (ESR), positive test results for antinuclear antibodies, urticaria, skin rash, angioedema, toxic epidermal necrolysis, skin itching.

Laboratory indicators: increased activity of "hepatic" transaminases, increased activity of creatine phosphokinase (CK), bilirubin.

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

Overdose:

Several cases of accidental administration of excessively large doses of the drug have been described, but no specific symptoms have been observed in patients.

Treatment: symptomatic, it is necessary to induce vomiting, rinse the stomach, the purpose of activated charcoal is indicated, control of liver function and activity of CKF is necessary. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

Immunosuppressants, potent inhibitors of the isoenzyme CYP3A4 (incl. itraconazole, ketoconazole, posaconazole, HIV protease inhibitors, bocepprir, telaprevir, erythromycin, clarithromycin, telithromycin and nefazodone), gemfibrozil, ciclosporin, a nicotinic acid in lipid-lowering doses (more than 1 g / day), colchicine, ranolazine and drugs that affect the concentration of endogenous steroid hormones increase the risk of myopathy with rhabdomyolysis and acute renal failure.

With simultaneous administration with danazol, Diltiazem, Verapamil maximum daily dosage of lovastatin should not exceed 20 mg, amiodarone - 40 mg.

At simultaneous appointment with indirect anticoagulants the anticoagulant effect and the risk of bleeding increases. Regular prothrombin time control is necessary.

Kolestyramin and colestipol reduce bioavailability (use is possible after 4 hours after taking the above drugs).

Cyclosporine can increase the plasma level of metabolites.

Grapefruit juice in large quantities (more than 1 liter / day) increases the maximum concentration (C_max) and the area under the concentration-time curve (AUC) of lovastatin and the risk of myopathies (their simultaneous use is not recommended).

Special instructions:

During the treatment period, patients should adhere to a special diet with low cholesterol concentration.

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

Medostatin treatment can cause an increase in the activity of "liver" transaminases and CK.With prolonged therapy, biochemical control of liver function is indicated. Activity of "liver" transaminases is determined before the start of treatment, every 8 weeks during the first year of therapy and further - at least 1 time in six months. When the activity of "hepatic" transaminases and CK is increased more than 3 times relative to the upper limit of the norm, the drug should be canceled.

The use of statins can lead to the development of hyperglycemia in patients with diabetes mellitus.

Hepatitis therapy may lead to the development of myopathy with rhabdomyolysis and renal failure. The risk of this pathology increases with simultaneous use with immunosuppressants, gemfibrozil, nicotinic acid in lipid-lowering doses (more than 1 g / day), cyclosporine, erythromycin and antifungal agents of the azole group (itraconazole and etc.).

If the patient's overall serious condition is due to a disease, therapy should be discontinued.

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.

Effect on the ability to drive transp. cf. and fur:Care should be taken when driving vehicles and servicing moving vehicles due to the risk of dizziness.

Form release / dosage:Tablets of 20 mg.

Packaging:

For 10 tablets in a blister of PVC / aluminum foil.

For 3 or 10 blisters together with instructions for use in a cardboard box.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012832 / 01

Date of registration:29.03.2012

Expiration Date:Unlimited

The owner of the registration certificate:Medocemi Co., Ltd.Medocemi Co., Ltd. Cyprus

Manufacturer: & nbsp

MEDOCHEMIE, Ltd. Cyprus

Representation: & nbspMEDOKEMI LTD. MEDOKEMI LTD. Cyprus

Information update date: & nbsp26.04.2018

Illustrated instructions

Instructions

Medostatin® (Medostatin®)