Simvastatin tablets p / o 20mg, No. 30 Vertex
Expiration Date: 05/2027
Russian Pharmacy name:
Симвастатин таблетки п/о 20мг, №30 Вертекс
primary hypercholesterolemia (type IIa and IIb) with ineffectiveness of diet 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 a special diet and physical activity.
Coronary heart disease:
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 atherosclerosis, reduce the risk of revascularization procedures.
Before starting treatment with Simvastatin, the patient should be prescribed a standard cholesterol cholesterol diet, which should be followed throughout the course of treatment.
Simvastatin should be taken orally 1 time / day in the evening with plenty of water. The time of taking the drug should not be associated with food intake.
The recommended dose of Simvastatin for the treatment of hypercholesterolemia varies from 10 to 80 mg 1 time / day in the evening.
The recommended starting dose for patients with hypercholesterolemia is 10 mg. The maximum daily dose is 80 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 / day.
In patients with homozygous hereditary hypercholesterolemia, the recommended daily dose of Simvastatin is 40 mg 1 time / 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 with coronary artery disease (IHD) or a high risk of developing IHD, the effective doses of Simvastatin are 20-40 mg / day. Therefore, the recommended starting dose for such patients is 20 mg / 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 / 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 must be reduced.
In elderly patients and in patients with mild or moderate renal failure, changes in the dosage of the drug are not required.
In patients with chronic renal failure (creatinine clearance less than 30 ml / min) or receiving cyclosporine, danazol, gemfibrozil or other fibrates (except fenofibrate), niacin in lipid-lowering doses (1 g / day) in combination with simvastatin, the maximum recommended dose of simvastatin is not should exceed 10 mg / day.
For patients taking amiodarone or verapamil at the same time as simvastatin, the daily dose should not exceed 20 mg.
Active ingredient: simvastatin - 20 mg
Excipients : lactose (milk sugar), microcrystalline cellulose, povidone (polyvinylpyrrolidone), citric acid, ascorbic acid, butylhydroxyanisole, corn starch, calcium stearate, hypromellose (hydroxypropyl methylcellulose), macrogol 4000, talc dioxide.
liver disease in the active phase, a persistent increase in the activity of liver enzymes of unknown etiology;
diseases of skeletal muscles (myopathy);
age up to 18 years (efficacy and safety have not been established);
hypersensitivity to simvastatin or to other components of the drug (including hereditary lactose intolerance), as well as to other statin drugs (MMC-CoA reductase inhibitors) in history.
It is prescribed with caution to patients who abuse alcohol, patients after organ transplantation, who are undergoing immunosuppressive therapy (due to the increased risk of rhabdomyolysis and renal failure); in conditions that can lead to the development of severe renal insufficiency, such as arterial hypotension, acute infectious diseases of a 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 unclear etiology; epilepsy.
Film-coated tablets of white or almost white color, round, biconvex.
Composition:
Active ingredient: simvastatin - 10 mg
Excipients : lactose (milk sugar), microcrystalline cellulose, povidone (polyvinylpyrrolidone), citric acid, ascorbic acid, butylhydroxyanisole, corn starch, calcium stearate, hypromellose (hydroxypropyl methylcellulose), macrogol 4000, talc dioxide.
Film-coated tablets of white or almost white color, round, biconvex.
Composition:
Active ingredient: simvastatin - 20 mg
Excipients : lactose (milk sugar), microcrystalline cellulose, povidone (polyvinylpyrrolidone), citric acid, ascorbic acid, butylhydroxyanisole, corn starch, calcium stearate, hypromellose (hydroxypropyl methylcellulose), macrogol 4000, talc dioxide.
Clinical and pharmacological group: Lipid-lowering drug
Pharmaco-therapeutic group: Lipid-lowering agent - HMG-CoA reductase inhibitor
pharmachologic effect
A lipid-lowering agent, obtained synthetically from the fermentation product of Aspergillus terreus, is an inactive lactone; it undergoes hydrolysis in the body to form 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 for the formation of mevalonate from HMG-CoA. Since the conversion of HMG-CoA to mevalonate is an early stage in cholesterol synthesis, 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 is involved in many synthesis processes in the body.
Causes a decrease in blood plasma triglycerides (TG), low density lipoprotein (LDL), very low density lipoprotein (VLDL) and total cholesterol (in cases of heterozygous familial and nonfamilial forms of hypercholesterolemia, with mixed hyperlipidemia, when high cholesterol is a risk factor) ... Increases high-density lipoprotein (HDL) and decreases the LDL / HDL ratio and total cholesterol / HDL.
The beginning of the manifestation of the effect - after 2 weeks from the start of admission, the maximum therapeutic effect is achieved after 4-6 weeks. The effect persists with continued treatment, with discontinuation of therapy, the cholesterol content gradually returns to the initial level.
Pharmacokinetics
The absorption of simvastatin is high. After oral administration, Cmax in blood plasma is reached after about 1.3-2.4 hours and decreases by 90% after 12 hours. Plasma protein binding is about 95%.
It is metabolized in the liver, has a 'first pass' effect through the liver (it is hydrolyzed to form an active derivative: beta-hydroxy acids, other active as well as inactive metabolites have been found). T1 / 2 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 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 a special diet and physical activity.
Coronary heart disease:
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 atherosclerosis, reduce the risk of revascularization procedures.
Dosage regimen
Before starting treatment with Simvastatin, the patient should be prescribed a standard cholesterol cholesterol diet, which should be followed throughout the course of treatment.
Simvastatin should be taken orally 1 time / day in the evening with plenty of water. The time of taking the drug should not be associated with food intake.
The recommended dose of Simvastatin for the treatment of hypercholesterolemia varies from 10 to 80 mg 1 time / day in the evening.
The recommended starting dose for patients with hypercholesterolemia is 10 mg. The maximum daily dose is 80 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 / day.
In patients with homozygous hereditary hypercholesterolemia, the recommended daily dose of Simvastatin is 40 mg 1 time / 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 with coronary artery disease (IHD) or a high risk of developing IHD, the effective doses of Simvastatin are 20-40 mg / day. Therefore, the recommended starting dose for such patients is 20 mg / 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 / 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 must be reduced.
In elderly patients and in patients with mild or moderate renal failure, changes in the dosage of the drug are not required.
In patients with chronic renal failure (creatinine clearance less than 30 ml / min) or receiving cyclosporine, danazol, gemfibrozil or other fibrates (except fenofibrate), niacin in lipid-lowering doses (1 g / day) in combination with simvastatin, the maximum recommended dose of simvastatin is not should exceed 10 mg / day.
For patients taking amiodarone or verapamil at the same time as simvastatin, the daily dose should not exceed 20 mg.
Side effect
From the digestive system: possible abdominal pain, constipation, flatulence, nausea, diarrhea, pancreatitis, vomiting, hepatitis, increased activity of liver enzymes, alkaline phosphokinase and creatine phosphokinase (CPK).
From the side of the central nervous system: asthenic syndrome, headache, dizziness, insomnia, muscle cramps, paresthesias, peripheral neuropathy, blurred vision, impaired taste.
Allergic and immunopathological reactions: angioedema, polymyalgia rheumatica, vasculitis, thrombocytopenia, increased ESR, fever, arthritis, urticaria, photosensitivity, skin flushing, hot flashes, shortness of breath, lupus-like syndrome, eosinophilia.
Dermatological reactions: rarely skin rash, pruritus, alopecia, dermatomyositis.
From the musculoskeletal system: myopathy, myalgia, muscle cramps, weakness; rarely, rhabdomyolysis.
Others: anemia, palpitations, acute renal failure (due to rhabdomyolysis), decreased potency.
Contraindications for use
liver disease in the active phase, a persistent increase in the activity of liver enzymes of unknown etiology;
diseases of skeletal muscles (myopathy);
age up to 18 years (efficacy and safety have not been established);
hypersensitivity to simvastatin or to other components of the drug (including hereditary lactose intolerance), as well as to other statin drugs (MMC-CoA reductase inhibitors) in history.
It is prescribed with caution to patients who abuse alcohol, patients after organ transplantation, who are undergoing immunosuppressive therapy (due to the increased risk of rhabdomyolysis and renal failure); in conditions that can lead to the development of severe renal insufficiency, such as arterial hypotension, acute infectious diseases of a 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 unclear etiology; epilepsy.
Application during pregnancy and lactation
Simvastatin is contraindicated in pregnant women. There are several reports of the development of abnormalities in newborns whose mothers took simvastatin.
Women of childbearing age taking simvastatin should avoid conception. If, during the course of treatment, pregnancy does occur, Simvastatin should be canceled, and the woman should be warned of the possible danger to the fetus.
There are no data on the excretion of simvastatin in breast milk. If it is necessary to prescribe Simvastatin during lactation, it should be borne in mind that many drugs are excreted in breast milk, and there is a threat of severe reactions, therefore, breastfeeding while taking the drug is not recommended.
Application for violations of liver function
At the beginning of therapy with Simvastatin, a transient increase in the level of hepatic enzymes is possible. Before starting therapy and then regularly conduct a study of liver function (monitor the activity of liver enzymes every 6 weeks during the first 3 months, then every 8 weeks during the remaining first year, and then once every 6 months), as well as with increasing doses, liver function test. When the dose is increased to 80 mg, a test must be performed every 3 months. With a persistent increase in transaminase activity (3 times compared to the initial level), Simvastatin should be discontinued.
Application for impaired renal function
In patients with mild or moderate renal failure, changes in the dosage of the drug are not required.
In patients with chronic renal failure (creatinine clearance less than 30 ml / min) or receiving cyclosporine, danazol, gemfibrozil or other fibrates (except fenofibrate), niacin in lipid-lowering doses (1 g / day) in combination with simvastatin, the maximum recommended dose of simvastatin is not should exceed 10 mg / day.
Application in children
Contraindicated in children under 18 years of age.
Use in elderly patients
In elderly patients, changes in the dosage of the drug are not required.
special instructions
At the beginning of therapy with Simvastatin, a transient increase in the level of hepatic enzymes is possible. Before starting therapy and then regularly conduct a study of liver function (monitor the activity of liver enzymes every 6 weeks during the first 3 months, then every 8 weeks during the remaining first year, and then once every 6 months), as well as with increasing doses, liver function test. When the dose is increased to 80 mg, a test must be performed every 3 months. With a persistent increase in transaminase activity (3 times compared to the initial level), Simvastatin should be discontinued.
Simvastatin, like other HMG-CoA reductase inhibitors, should not be used with an increased risk of rhabdomyolysis and renal failure (against the background of severe acute infection, arterial hypotension, planned major surgery, trauma, severe metabolic disorders).
Cancellation of lipid-lowering drugs during pregnancy does not significantly affect the results of long-term treatment of primary hypercholesterolemia.
Due to the fact that HMG-CoA reductase inhibitors inhibit cholesterol synthesis, and cholesterol and other products of its synthesis play an essential role in the development of the fetus, including the synthesis of steroids and cell membranes, simvastatin can have an adverse effect on the fetus when administered to pregnant women (women of reproductive age should avoid conception). If pregnancy occurs during treatment, the drug should be canceled, and the woman should be warned of the possible danger to the fetus.
The use of Simvastatin is not recommended in women of childbearing age who do not use contraceptives.
In patients with an underactive thyroid gland (hypothyroidism) or some kidney disease (nephrotic syndrome), if the cholesterol level is high, the underlying disorder should be treated first.
Simvastatin is prescribed with caution to persons who abuse alcohol and / or have a history of liver disease.
Before and during treatment, the patient should be on a cholesterol-free diet.
Simultaneous intake of grapefruit juice can increase the severity of side effects associated with taking Simvastatin, so you should avoid taking them at the same time.
Simvastatin is not indicated in cases where there is type I, IV and V hypertriglyceridemia.
Simvastatin treatment 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 Simvastatin: fibrates (gemfibrozil, fenofibrate), cyclosporine, nefazadone, macrolides (erythromycin, clarithromycin), antifungal agents from the azole group (ketoconazole, itraconazole) and HIV proteases (ritonavir). The risk of developing myopathy is also increased in patients with severe renal failure.
All patients starting Simvastatin 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 to immediately consult a doctor in case of unexplained pain, muscle soreness, lethargy or muscle weakness, especially if this is accompanied by malaise or fever. Drug therapy should be discontinued immediately if myopathy is diagnosed or suspected.
In order to diagnose the development of myopathy, it is recommended to regularly measure the value of CPK.
When treating with Simvastatin, an increase in the content of serum CPK is possible, which should be taken into account in the differential diagnosis of chest pain. The criterion for discontinuation of the drug is an increase in the content of CPK in the blood serum by more than 10 times relative to the upper limits of the norm. In patients with myalgia, myasthenia gravis and / or a pronounced increase in CPK activity, treatment with the drug is discontinued.
The drug is effective both as monotherapy and in combination with bile acid sequestrants.
If the current dose is missed, the drug must be taken as soon as possible. If it is time for the next dose, do not double the dose.
Patients with severe renal impairment are treated under the control of renal function.
The duration of the use of the drug is determined by the attending physician individually.
Influence on the ability to drive vehicles and use mechanisms
ќ неблагопри¤тном вли¤нии препарата на способность управл¤ть автомобилем и работе с механизмами не сообщалось.
ѕередозировка
Ќи в одном из известных нескольких случаев передозировки (максимально прин¤та¤ доза 450 мг) специфических симптомов вы¤влено не было.
Ћечение: вызвать рвоту, прин¤ть активированный уголь, провести симптоматическую терапию. —ледует контролировать функции печени и почек, уровень ‘ в сыворотке крови. ѕри развитии миопатии с рабдомиолизом и острой почечной недостаточности (редкий, но т¤желый побочный эффект) следует немедленно прекратить прием препарата и ввести больному диуретик и натри¤ бикарбонат (внутривенна¤ инфузи¤). ѕри необходимости показан гемодиализ. –абдомиолиз может вызывать гиперкалиемию, которую можно устранить в/в введением кальци¤ хлорида или кальци¤ глюконата, инфузией глюкозы с инсулином, использованием калиевых ионообменников или, в т¤желых случа¤х, с помощью гемодиализа.
Ћекарственное взаимодействие
?итостатики, противогрибковые средства (кетоконазол, итраконазол), фибраты, высокие дозы никотиновой кислоты, иммунодепрессанты, эритромицин, кларитромицин, телитромицин, ингибиторы ¬»„-протеазы, нефазодон повышают риск развити¤ миопатии.
?иклоспорин или даназол: риск развити¤ миопатии/рабдомиолиза увеличиваетс¤ при совместном назначении циклоспорина или даназола с высокими дозами симвастатина.
?ругие гиполипидемические средства, способные вызывать развитие миопатии: риск развити¤ миопатии повышаетс¤ при совместном назначении других гиполипидемических средств, которые не ¤вл¤ютс¤ мощными ингибиторами CYP3ј4, но способные вызвать миопатию в услови¤х монотерапии. “акие как гемфиброзил и другие фибраты (кроме 1 г фенофибрата), а также ниацин (никотинова¤ кислота) в дозе более 1 г/сутки.
јмиодарон и верапамил: риск развити¤ миопатии увеличиваетс¤ при совместном приеме амиодарона или верапамила с высокими дозами симвастатина.
?илтиазем: риск развити¤ миопатии незначительно увеличиваетс¤ у пациентов, получающих дилтиазем одновременно с симвастатином в дозе 80 мг.
—имвастатин потенцирует действие пероральных антикоагул¤нтов (напр., фенпрокумон, варфарин) и увеличивает риск возникновени¤ кровотечений, что требует необходимости проведени¤ контрол¤ показателей свертываемости крови до начала лечени¤, а также достаточно часто в начальный период терапии. ак только достигаетс¤ стабильный уровень показател¤ протромбинового времени или ћеждународное Ќормализованное ќтношение (ћЌќ), его дальнейший контроль следует проводить с интервалами, рекомендуемыми дл¤ пациентов, получающих терапию антикоагул¤нтами. ѕри изменении дозировки или прекращении приема симвастатина также следует проводить контроль протромбинового времени или ћЌќ по вышеизложенной схеме.
“ерапи¤ симвастатином не вызывает изменений протромбинового времени и риска кровотечений у пациентов, не принимающих антикоагул¤нты.
ѕовышает уровень дигоксина в плазме крови.
олестирамин и колестипол снижают биодоступность (применение симвастатина возможно через 4 ч после приема указанных лекарственных средств, при этом отмечаетс¤ аддитивный эффект).
—ок грейпфрута содержит один или более компонентов, которые ингибируют CYP3ј4 и могут повышать концентрацию в плазме крови средств, метаболизирующихс¤ CYP3ј4. ”величение активности ингибиторов vћv- ој-редуктазы после употреблени¤ 250 мл сока в день ¤вл¤етс¤ минимальным и не имеет клинического значени¤. ќднако потребление большого объема сока (более 1 литра в день) при приеме симвастатина значительно увеличивает уровень ингибирующей активности в отношении vћv- ој-редуктазы в плазме крови. ¬ св¤зи с этим необходимо избегать потреблени¤ сока грейпфрута в больших количествах.
”слови¤ хранени¤
In a dry, out of reach of children, protected from light, at a temperature not exceeding 25 ? C.
Shelf life
Shelf life is
2 years.
Terms of sale
The drug is available with a prescription.