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

One tablet, coated, contains the active substance simvastatin 10 or 20 mg and excipients: butyl hydroxy anisole, ascorbic acid, lactose, citric acid, pregelatinized starch, microcrystalline cellulose, magnesium stearate, corn starch, hydroxypropylmethylcellulose, castor oil, polyethylene glycol -4000, titanium dioxide, talc.

Description:

Round biconvex tablets, coated with a white coating.

Pharmacotherapeutic group:Hypolipidaemic agent - HMG-CoA reductase inhibitor

ATX: & nbsp

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

C.10.A.A.01 Simvastatin

Pharmacodynamics:

A hypolipidemic agent obtained synthetically from a fermentation product Aspergillus terreus, is an inactive lactone, in the body is metabolized with the formation of a hydroxy-acid derivative. The active metabolite inhibits 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA reductase), an enzyme that catalyzes the initial reaction of mevalonate formation from HMG-CoA. Since the conversion of HMG-CoA to mevalonate is an early stage in the synthesis of cholesterol, the use of simvastatin does not cause the accumulation of potentially toxic sterols in the body. HMG-CoA is readily metabolized to acetyl-CoA, which participates in many synthesis processes in organism.

It causes a decrease in the plasma levels of triglycerides (TG), Low-density lipoprotein (LPSNT), very low density lipoproteins (VLDL) and total cholesterol (in cases of heterozygous familial and non-family forms of hypercholesterolemia, with mixed hyperlipidemia, when elevated cholesterol is a risk factor).

Increases of high density lipoprotein (HDL) and reduces the ratio of LDL / HDL and total cholesterol / HDL.

The onset of the effect is 2 weeks after the start of the treatment, the maximum therapeutic effect is achieved after 4-6 weeks. The effect persists with the continuation of treatment, with the cessation of therapy, the cholesterol content gradually returns to the baseline level.

Pharmacokinetics:

Absorption of simvastatin is high. After oral administration, the maximum concentration in the blood plasma is reached after approximately 1.3 - 2.4 hours and decreases by 90% after 12 hours. The connection with plasma proteins is about 95%.

Metabolised in the liver, has the effect of "first passage" through the liver (hydrolyzed to form an active derivative: beta-hydroxy acid, other active as well as inactive metabolites were found). The half-life of active metabolites is 1.9 hours.

It is excreted mainly with feces (60%) in the form of metabolites. About 10 - 15% is excreted by the kidneys in an inactive form

Indications:

Hypercholesterolemia:

primary hypercholesterolemia (type IIa and IIb) with ineffectiveness of diet with lowthe content of cholesterol and other non-medicamentous measures (physical activity and weight loss) in patients with an increased risk of coronary atherosclerosis;
combined hypercholesterolemia and hypertriglyceridemia, not corrected by special diet and exercise.

Cardiac ischemia:

- for the prevention of myocardial infarction, to reduce the risk of death, reduce the risk of cardiovascular disorders (stroke or transient ischemic attacks), slow the progression of coronary artery atherosclerosis, reduce the risk of revascularization procedures.

Contraindications:

hypersensitivity to simvastatin or other components preparation, as well as to other drugs of the statin series (inhibitors of HMG-CoA reductase) in the history;

liver disease in the active phase, persistent increase in the activity of "liver" enzymes of unclear etiology;
porphyria;
diseases of skeletal muscles (myopathy);
age to 18 years (effectiveness and safety not established)

Carefully:

With caution appoint patients who abuse alcohol, patients after organ transplantation,who undergo immunosuppressant therapy (due to an increased risk of rhabdomyolysis and renal insufficiency); at conditions that can lead to the development of severe renal function deficiency, such as arterial hypotension, acute infectious diseases of severe course, severe metabolic and endocrine disorders, disturbances in water and electrolyte balance, surgical interventions (including dental), or trauma; patients with decreased or increased tone of skeletal muscles of unknown etiology; epilepsy.

Pregnancy and lactation:

Ovénkor is contraindicated in pregnancy. There are several reports of the development of anomalies in newborns whose mothers were taking simvastatin.

Women of childbearing age who receive simvastatin, should avoid conception. If during the treatment the pregnancy does occur, the Ovencor should be canceled, and the woman should be warned about the possible danger to the fetus.

Data on the isolation of simvastatin with mother's milk are absent. If it is necessary to appoint an Ovencor in the period of breastfeeding,that many drugs are excreted in breast milk, and there is a threat of severe reactions, so breast-feeding during the drug is not recommended.

Dosing and Administration:

Before treatment with Ovencor, the patient should be given a standard hypocholesterol diet, which should be observed throughout the course of treatment.

Ovenkor should be taken orally 1 time per day in the evening, with enough water.

The time of taking the drug should not be associated with eating.

Recommended dose of Ovecor for treatment hypercholesterolemia varies from 10 to 80 mg once a day in the evening. The recommended initial dose of the drug for patients with hypercholesterolemia is 10 mg. The maximum daily dose - 80 mg.

Changes (selection) of the dose should be carried out at intervals of 4 weeks. Have most patients the optimal effect is achieved when taking the drug in doses up to 20 mg per day.

Have patients with homozygous hereditary hypercholesterolemia the recommended daily dose of Ovencor is 40 mg once a day in the evening or 80 mg in three divided doses (20 mg in the morning, 20 mg in the afternoon and 40 mg in the evening).

In the treatment of patients from ischemic heart disease (CHD) or a high risk of CHD effective doses of Ovencor are 20-40 mg per day. Therefore, the recommended initial dose in such patients is 20 mg per day. Changes (selection) of the dose should be carried out at intervals of 4 weeks, if necessary, the dose can be increased to 40 mg per day. If the LDL content is less than 75 mg / dL (1.94 mmol / L), the total cholesterol content is less than 140 mg / dl (3.6 mmol / L), the dose of the drug should be reduced.

Have elderly patients and in patients with mild or moderate degree renal insufficiency no change in dosage is required.

In patients with chronic renal failure (creatinine clearance less than 30 ml / min) or receiving ciclosporin, danazol, gemfibrozil or other fibrates (except fenofibrate), niacin in lipid-lowering doses (≥1 g / day) in combination with simvastatinom, the maximum recommended dose of Ovencor should not exceed 10 mg per day.

For patients receiving amiodarone or verapamil simultaneously with Ovencor, the daily dose of Ovencor should not exceed 20 mg.

Side effects:

Digestive system: abdominal pain, constipation, flatulence, nausea, diarrhea, pancreatitis, vomiting, hepatitis, increased activity of "liver" enzymes, alkaline phosphokinase and creatine phosphokinase (CKF).

Nervous system and sensory organs: asthenic syndrome, headache, dizziness, insomnia, muscle cramps, paresthesia, peripheral neuropathy, blurred vision, impaired taste sensations.

Allergic and immunopathological reactions: angioedema, rheumatic polymyalgia, vasculitis, thrombocytopenia, increased ESR, fever, arthritis, urticaria, photosensitivity, skin hyperemia, hot flashes, dyspnea, lupus-like syndrome, eosinophilia.

Dermatological reactions: rarely skin rash, itching, alopecia, dermatomyositis.

From the musculoskeletal system: Myopathy, myalgia, muscle cramps, weakness; rarely rhabdomyolysis.

Other: anemia, palpitation, acute renal failure (due to rhabdomyolysis), decreased potency

Overdose:

In none of the known few cases of overdose (the maximum dose of 450 mg) specific symptoms were identified.

Treatment: induce vomiting, take Activated carbon. Symptomatic therapy. It is necessary to monitor the liver and kidney function, the level of CK in the blood serum.

With the development of myopathy with rhabdomyolysis and acute renal failure (a rare but severe side effect), the drug should be stopped immediately and the diuretic and sodium bicarbonate (intravenous infusion) administered to the patient. If necessary, hemodialysis is indicated.

Rhabdomyolysis can cause hyperkalemia, which can be eliminated by intravenous administration of calcium chloride or calcium gluconate, glucose infusion with insulin, the use of potassium ion exchangers or, in severe cases, by hemodialysis.

Interaction:

Cytostatics, antifungal agents (ketoconazole, itraconazole), fibrates, high doses of nicotinic acid, immunosuppressants, erythromycin, kparitromycin, telithromycin, HIV protease inhibitors, nefazodone increase the risk of myopathy.

Cyclosporine or danazol: The risk of myopathy / rhabdomyolysis increases with the simultaneous administration of cyclosporine or danazol with high doses of simvastatin.

Other hypolipidemic agents that can cause the development of myopathy: the risk of myopathy increases with the co-administration of other lipid-lowering drugs that are not potent inhibitors CYP3A4, but capable of causing myopathy under conditions of monotherapy. Such as gemfibrozil and other fibrates (except fenofibrate), as well as niacin (a nicotinic acid) in a dose of □ 1 g per day. Amiodarone and verapamil: The risk of myopathy increases with the joint administration of amiodarone or verapamil with high doses of simvastatin.

Diltiazem: The risk of myopathy is slightly increased in patients receiving diltiazem simultaneously with simvastatinom in a dose of 80 mg.

Simvastatin potentiates the action oral anticoagulants (eg fenprokumone, warfarin) and increases the risk of bleeding, which requires the need to monitor the coagulability of the blood before treatment, and often enough in the initial period of therapy. Once a stable prothrombin time indicator or International Normalized Ratio (MNO) is reached, its further control should be performed at intervals recommended for patients receiving anticoagulant therapy.When changing the dosage or stopping the intake of simvastatin, it is also necessary to monitor prothrombin time or INR according to the above scheme.

Therapy with simvastatin does not cause changes in prothrombin time and the risk of bleeding in patients who do not take anticoagulants.

Increases the level digoxin in the blood plasma.

Kolestyramine and colestipol reduce the bioavailability (the use of simvastatin is possible 4 hours after the administration of these drugs, with an additive effect noted).

Grapefruit juice contains one or more components that inhibit CYP3A4 and can increase the concentration in the blood plasma of metabolic agents CYP3A4. The increase in the activity of HMG-CoA reductase inhibitors after consuming 250 ml of juice per day is minimal and has no clinical significance. However, consumption of a large amount of juice (more than 1 liter per day) with the use of simvastatin significantly increases the level of inhibitory activity against HMG-CoA reductase in blood plasma. In this regard, it is necessary to avoid the consumption of grapefruit juice in large quantities

Special instructions:

At the beginning of Ovencor therapy, a transient increase in the level of "liver" enzymes is possible.

Before starting therapy, continue to regularly investigate the function of baking (monitor the activity of "liver" enzymes every 6 weeks for the first 3 months, then every 8 weeks for the remaining first year, and then 1 time in six months), as well as with increasing doses Functional tests for the determination of liver function should be performed. When the dose is raised to 80 mg, a test should be performed every 3 months. With a persistent increase in transaminase activity (3-fold compared with baseline), the Ovenkor should be discontinued.

Ovenkor, like other inhibitors of HMG-CoA reductase, should not be used at an increased risk of rhabdomyolysis and renal insufficiency (against severe acute infection, arterial hypotension, planned large surgery, trauma, severe metabolic disorders).

The abolition of lipid-lowering drugs during pregnancy does not significantly affect the results of long-term treatment of primary hypercholesterolemia.

In connection with the fact that inhibitors of HMG-CoA reductase inhibit the synthesis of cholesterol,and cholesterol and other products of its synthesis play an important role in the development of the fetus, including the synthesis of steroids and cell membranes, simvastatin may have an adverse effect on the fetus when prescribing it to pregnant women (women of reproductive age should avoid conception). If during pregnancy pregnancy occurs, the drug should be canceled, and the woman is warned about possible danger to the fetus.

The use of Ovencor is not recommended in women of childbearing age who do not use contraceptives.

In patients with a reduced thyroid function (hypothyroidism) or in the presence of certain kidney diseases (nephrotic syndrome), when the level of cholesterol is increased, the underlying disease should first be treated.

Ovencor is cautiously prescribed to people who abuse alcohol and / or have a history of liver disease.

Before and during treatment, the patient should be on a hypocholesterol diet.

Simultaneous reception of grapefruit juice can increase the severity of side effects associated with taking Ovencor, so you should avoid their simultaneous intake.

In patients with myalgia, myasthenia gravis and / or a marked increase in the activity of CKK, treatment with the drug is stopped. Ovenkore is not indicated in cases where there is hypertriglyceridemia I, IV and V types.

Treatment with Ovencor can cause myopathy, leading to rhabdomyolysis and renal failure. The risk of this pathology increases in patients receiving one or more of the following medicinal products simultaneously with Ovencor: fibrates (gemfibrozil, fenofibrate), ciclosporin, nefazadone, macrolides (erythromycin, clarithromycin), antifungal agents from the group of "azoles" (ketoconazole, intraconazole) and HIV protease inhibitors (ritonavir). The risk of developing myopathy is also increased in patients with severe renal failure.

All patients starting Ovencor therapy, as well as patients who need to increase the dose of the drug, should be warned about the possibility of myopathy and the need for immediate medical attention in the event of unexplained pain, muscle soreness, lethargy or muscle weakness, especially if accompanied by malaise or fever.The drug should be discontinued immediately if myopathy is diagnosed or suspected.

In order to diagnose the development of myopathy, it is recommended that CK values be measured regularly.

In the treatment with Ovencor, an increase in the serum CKF content is possible, which should be taken into account in the differential diagnosis of chest pain. The criterion for the discontinuation of the drug is an increase in serum levels of CK in more than 10 times the upper limit of the norm.

It is effective both in the form of monotherapy, and in combination with bile acid sequestrants.

If the current dose is skipped, the drug should be taken as soon as possible. If it's time to take the next dose, do not double the dose.

Patients with severe renal failure receive treatment under the control of kidney function.

Duration of application of the drug is determined by the attending physician individually.

Effect on the ability to drive transp. cf. and fur:

The adverse effect of Ovencor on the ability to drive and work with machinery was not reported.

Form release / dosage:

The tablets covered with a cover, on 10 mg and 20 mg.

Packaging:

For 10, 30 tablets in a contour mesh box made of PVC film and aluminum foil printed lacquered.

By 10, 14, 20, 28, 30, 40, 50 or 100 tablets into a polymer container. Free space in the container is filled with cotton wool, hygroscopic.

One container or 1, 2, 3, 4, 5, 6, 8 andwhether 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

For 10 or 20 containers or 10, 20, 40, 60, 80 and 100 contour mesh packages, together with 10 instructions for use, put in a cardboard box (for hospitals).

Storage conditions:AT dry, protected from light, 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 printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000527

Date of registration:28.05.2010

Expiration Date:Unlimited

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp21.05.2017

Illustrated instructions

Instructions

Ovenkor (Ovenkor)