Simor coated pills 20mg N30
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Active ingredients
Simvastatin
Release form
Pills
Composition
1 tablet contains: Active ingredient: simvastatin 20 mg.
Pharmacological effect
The lipid-lowering agent, obtained synthetically from the fermentation product Aspergillus terreus, is an inactive lactone, undergoes hydrolysis in the body to form a hydroxy-acid derivative. The active metabolite inhibits 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA reductant / HMG co-reduction. catalyzing the initial reaction of the formation of mevalonate from HMG-CoA. Since the transformation of HMG-CoA into mevalonat is an early stage of cholesterol synthesis, the use of simvastatin does not cause the accumulation of potentially toxic sterols in the body. HMG-CoA is easily metabolized to acetyl-CoA, which is involved in many processes of synthesis in the body. Lowers triglycerides (TG), low density lipoproteins (LDL), very low density lipoproteins (VLDL) and total cholesterol in plasma (in cases of heterozygous familial and non-familial forms of hypercholesterolemia, with mixed hyperlipidemia, when elevated cholesterol is a risk factor). Increases the content of high-density lipoprotein (HDL) and reduces the ratio of LDL / HDL and total cholesterol / HDL. The effect begins - 2 weeks from the start of treatment, the maximum therapeutic effect is achieved after 4-6 weeks. The effect persists with continued treatment; at the termination of therapy the content of cholesterol gradually returns to the original level.
Pharmacokinetics
Simvastatin absorption is high. After ingestion, the maximum plasma concentration is reached after about 1.3-2.4 hours and decreases by 90% after 12 hours. Communication with plasma proteins is 95%. Metabolized in the liver, has the effect of first passing through the liver (hydrolyzes with the formation of the active derivative of beta-hydroxy acid, and other active and inactive metabolites are found). The elimination half-life of active metabolites is 1.9 hours. It is mainly excreted with feces (60%) as metabolites. About 10% -15% excreted by the kidneys in an inactive form.
Indications
Primary hypercholesterolemia (type H a and M b) with the ineffectiveness of dietary therapy with low cholesterol and other non-drug measures (exercise and weight loss) in patients with an increased risk of coronary atherosclerosis. Combined hypercholesterolemia and hypertriglyceridemia,not corrected by special diet and exercise. Ischemic heart disease. To prevent myocardial infarction, to reduce the risk of death, reduce the risk of cardiovascular disorders (stroke or transient ischemic attacks), slow the progression of atherosclerosis of the coronary vessels, reduce the risk of revascularization procedures.
Contraindications
Hypersensitivity to simvastatin or to other components of the drug, as well as to other statin drugs (HMG-CoA reductase inhibitors) in history. Liver disease in the active phase, a persistent increase in the activity of “liver” enzymes of unknown etiology. Porphyria. Skeletal muscle disease ( myopathy). Age up to 18 years (efficacy and safety have not been established). With caution prescribed to patients: Alcohol abusers. After organ transplantation. Who are treated with immunosuppressants (in zi with an increased risk of rhabdomyolysis and renal failure). Arterial hypotension. Acute infectious diseases of severe course. Severe metabolic and endocrine disorders. Disorders of water and electrolyte balance. Surgical interventions (including dental) or trauma. Patients with low or high tone skeleton. muscles of unknown etiology. In epilepsy.
Precautionary measures
Application in violation of the function of the liverWith caution prescribed to persons who have a history of liver disease. Use in violation of renal functionPatients with severe renal insufficiency, treatment is carried out under the control of renal function. At the beginning of therapy with the Simvor, a transient increase in the level of “liver” enzymes is possible. Before starting therapy and then regularly conduct a study of the liver function (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 half a year), as well as with increasing doses should be a test to determine the function of the liver. If you increase the dose to 80 mg, you need to test every 3 months. With a persistent increase in the activity of transaminases (3 times compared with the initial level), the use of the Character should be stopped. Simore, like others.HMG-CoA reductase inhibitors should not be used with an increased risk of developing rhabdomyolysis and renal failure (against the background of severe acute infection, arterial hypotension, planned major surgery, trauma, severe metabolic disorders). Canceling hypolipidemic agents during pregnancy has no significant effect on the results of long-term treatment of primary hypercholesterolemia. Grapefruit juice contains one or more components that inhibit CYP3A4 and may increase plasma concentrations Blood agents metabolized 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, consuming a large volume of juice (more than 1 liter per day) while taking simvastatin significantly increases the level of inhibitory activity against HMG-CoA reductase in plasma. In this regard, it is necessary to avoid the consumption of grapefruit juice in large quantities. In patients with low thyroid function (hypothyroidism) or in the presence of certain kidney diseases (nephrotic syndrome), when the level of cholesterol increases, you should first treat the underlying disease that caused hypercholesterolemia. Treat with caution prescribed to persons who abuse alcohol. Before the start and during treatment, the patient must be on a cholesterol diet. Taking grapefruit juice at the same time can increase the severity of side effects associated with the reception of the character, so you should avoid their simultaneous reception. In patients with myalgia, myasthenia and / or a pronounced increase in the activity of CPK, treatment with the drug is discontinued. Simvor is not shown in cases where there is hypertriglyceridemia I, IV and V types. Treatment with Simor can cause myopathy, leading to rhabdomyolysis and renal failure. The risk of this pathology increases in patients receiving one or more of the following drugs simultaneously with Simvor: fibrates (gemfibrozil, fenofibrate), cyclosporine, nefazadone, macrolides (erythromycin, clarithromycin), antifungal agents from the azoles group (ketoconazole, itraconazole) and HIV protease inhibitors (ritonavir).The risk of myopathy development also increases in patients with severe renal insufficiency. All patients starting therapy with Simvor, 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 treatment to the doctor in case of unexplained pain, pain muscle weakness or muscle weakness, especially if accompanied by malaise or fever. Drug therapy should be immediately discontinued if myopathy is diagnosed or assumed. In order to diagnose the development of myopathy, it is recommended to regularly measure CPK values. When treatment with Simvor, the serum CPK content may increase, which should be taken into account in the differential diagnosis of chest pain. CK in the serum is more than 10 times relative to the upper limits of the norm. It is effective both in the form of monotherapy and in combination with s estrantami bile kislot.V case of missing current drug dose must be taken as soon as possible. If it is time to take the next dose, do not double the dose. The duration of use of the drug is determined by the attending physician individually. The effect on the ability to drive and work with mechanismsOn adverse effect of the Character on the ability to drive and work with mechanisms was not reported.
Use during pregnancy and lactation
Simor is contraindicated in pregnant women. There are several reports of the development of anomalies in newborns whose mothers took simvastatin. Women of childbearing age who take simvastatin should avoid conception. If, in the course of treatment, the pregnancy has nevertheless arrived, the Simvor should be canceled, and the woman should be warned about the possible danger to the fetus. There is no data on the release of simvastatin with mother's milk. If necessary, the appointment of a character during lactation should take into account that many drugs are excreted in breast milk, and there is a risk of severe reactions, so breastfeeding while taking the drug is not recommended.
Dosage and administration
Before starting treatment with the Simvor, the patient should be prescribed a standard hypocholesterol diet, which should be followed during the entire course of treatment. Simvor should be taken 1 time per day in the evening, drinking plenty of water. The drug intake time should not be associated with food intake. varies from 10 to 80 mg once daily in the evening. The recommended initial dose for patients with hypercholesterolemia is 10 mg. The maximum daily dose is 8 0 mg. Changes (selection) of the dose should be carried out at intervals of 4 weeks. In most patients, the optimal effect is achieved when taking the drug in doses up to 20 mg per day. Patients with homozygous hereditary hypercholesterolemia. Patients with homozygous hereditary hypercholesterolemia have a recommended daily dose of 40 mg once daily in the evening or 80 mg in three doses (20 mg in the morning, 20 mg in the afternoon and 40 mg in the evening). (IHD) or at high risk of developing IHD, effective doses of Symbol are 20–40 mg per day. Therefore, the recommended initial dose in these 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 content of LDL 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 must be reduced. Elderly patients or those with mild to moderate renal insufficiency. The dosage of the drug is not required to be changed. In patients with chronic renal failure, patients with chronic renal insufficiency (creatinine clearance less than 30 ml / min) or receiving cyclosporine, fibrates, danazol, gemfibrozil or other fibrates (except fenofibrate), niacin in doses reducing lipids (less than 1 g / day), the maximum recommended dose of a character should not exceed 10 mg per day. The daily dose of the Symbol in patients taking amiodarone or verapamil simultaneously with it should not exceed 20 mg.
Side effects
Digestive system. Possible abdominal pain, constipation, flatulence, nausea, diarrhea, pancreatitis, vomiting, hepatitis, increased activity of "liver" enzymes, alkaline phosphatase and creatine phosphokinase (CPK). 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, photosensitization, skin flushing, hot flashes, shortness of breath, lupus-like syndrome, eosinophilia. Dermatological reactions: Rare skin rash, itching, alopecia, dermatomyositis. On the part of the musculoskeletal systemMyopathy, myalgia, muscle cramps, weakness.Redko - rhabdomyolysis. Others Anemia, palpitations, acute renal failure (due to rhabdomyolysis), reduced potency.
Overdose
Symptoms: In none of the known several cases of overdose (maximum dose of 450 mg), no specific symptoms were identified. Treatment: induce vomiting, take activated charcoal. Symptomatic therapy. Liver and kidney functions, serum CK levels should be monitored. When myopathy develops with rhabdomyolysis and acute renal failure (a rare but serious side effect), the drug should be stopped immediately and a diuretic and sodium bicarbonate should be given to the patient (intravenous infusion). If necessary, hemodialysis is indicated. Rhabdomyolysis can cause hyperkalemia, which can be eliminated by intravenous administration of calcium chloride and calcium gluconate, infusion of glucose with insulin, the use of potassium ion exchangers, or in severe cases by hemodialysis.
Interaction with other drugs
Cytostatics, antifungal agents (ketoconazole, itraconazole), fibrates, high doses of nicotinic acid, immunosuppressants, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors, nefazodone increase the risk of myopathy. or danazol with high doses of simvastatin. Other lipid-lowering drugs that can cause the development of myopathy: the risk of myopathy increases with the joint appointment of others Other hypolipidemic agents that are not potent inhibitors of CYP3A4, but that can cause myopathy under monotherapy, such as gemfibrozil and other fibrates (except fenofibrate), and niacin (nicotinic acid) in a dose of more than 1 g per day. Amiodarone and verapamil: risk development of myopathy increases with co-administration of amiodarone or verapamil with high doses of simvastatin. Diltiazem: the risk of myopathy slightly increases in patientsreceiving diltiazem simultaneously with simvastatin in a dose of 80 mg. Simvastatin potentiates the action of oral anticoagulants (eg, fenprokumon, warfarin) and increases the risk of bleeding, which requires the need to monitor blood clotting indicators before the start of treatment, as well as quite often in the initial period of therapy. Once a stable level of the prothrombin time or the International Normalized Attitude (MHO) is reached, its further monitoring should be carried out at intervals recommended for patients receiving anticoagulant therapy. When changing the dosage or discontinuation of simvastatin, the prothrombin time or MHO should also be monitored according to the above scheme. Simvastatin therapy does not cause changes in the prothrombin time and the risk of bleeding in patients not taking anticoagulants. Increases the level of digoxin in the blood plasma. simvastatin may be 4 hours after taking these drugs, while there is an additive syndrome).