Simvastatin tabs 20mg #30

Instruction for Simvastatin

You can buy Simvastatin here

Simvastatin is a lipid-lowering drug, an inhibitor of HMG-CoA reductase (3-hydroxy-3-methyl-glutaryl-CoA reductase).

Release form and composition

Simvastatin is available in the form of film-coated tablets: round, biconvex, from yellow to light yellow, the core is white or almost white (at a dose of 10 mg, 20 mg or 40 mg - in blisters: 7, 10 , 14, 20, 30 or 50 pcs., In a cardboard box 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 packs; 10 pcs. In blisters, in a cardboard box 1, 3, 5 or 10 blisters; in polymer jars: 10, 15, 20, 30, 40, 50, 60, 70, 80, 90, 100 pcs., in a cardboard box 1 can; 20 or 30 pcs. in dark glass jars , in a cardboard box 1 can; 20 or 30 pcs. in polymer bottles, in a cardboard box 1 bottle; at a dose of 10 mg or 20 mg - in blisters: 15 pcs., in a cardboard box 1 or 2 packages; 10 pcs., In a cardboard box 100, 200, 300, 400 or 500 packs; 500, 1000 or 2000 pcs. In polymer cans, in a cardboard box 1, 2, 3, 4, 5 or 6 cans).
1 coated tablet contains:
    active substance: simvastatin - 10 mg, 20 mg or 40 mg;
    auxiliary components: lactose monohydrate, ascorbic acid, citric acid, potato starch, butylhydroxyanisole, microcrystalline cellulose, colloidal silicon dioxide (aerosil), magnesium stearate, talc;
    shell composition: opadry II - partially hydrolyzed polyvinyl alcohol, macrogol (polyethylene glycol 3350), titanium dioxide (E171), iron dye oxide II yellow (E172), aluminum varnish based on sunset yellow dye (E110), aluminum varnish based on quinoline dye yellow (E104), indigo carmine-based aluminum varnish (E132), talc.

Pharmacodynamics

Simvastatin is a lipid-lowering drug obtained as a result of synthetic transformation from the fermentation product of Aspergillus terreus. The active substance, being an inactive lactone, is converted in the body by hydrolysis into a hydroxy acid derivative. The active metabolite inhibits the HMG-CoA reductase enzyme, which catalyzes the initial reaction for the formation of mevalonate from HMG-CoA. The conversion of HMG-CoA to mevalonate is an early stage in the synthesis of cholesterol; therefore, the use of simvastatin does not contribute to the accumulation of potentially toxic sterols in the body. HMG-CoA is easily metabolized to acetyl-CoA, which is involved in many synthesis processes in the body.
The action of simvastatin inhibits the synthesis of cholesterol in the liver and causes the appearance on the surface of cells of an increased number of low density lipoprotein (LDL) receptors, this provides an increase in the capture and catabolism of LDL. As a result, the level of triglycerides (TG), LDL and very low density lipoproteins (VLDL), total cholesterol decreases in blood plasma.
While taking Simvastatin, the content of high density lipoproteins (HDL) increases, decreasing the ratio: LDL and HDL, total cholesterol and HDL. Simvastatin does not cause gene mutation.
The therapeutic effect begins to appear after 14 days of therapy, the maximum effect is achieved after 28–42 days and lasts throughout the entire period of use of the tablets. After stopping treatment, cholesterol levels gradually return to baseline levels.

Pharmacokinetics

After oral administration, simvastatin is almost completely absorbed. The period of reaching the maximum concentration in blood plasma is from 1.3 to 2.4 hours. After 12 hours, its content in the blood decreases by 90%.
The bioavailability of the drug is less than 5%.
Plasma protein binding is approximately 95%.
It enters the body in an inactive form, in tissues it is hydrolyzed into beta-hydroxy acid and inactive metabolites.
It is metabolized in the liver as a result of the effect of the first passage through the liver with the participation of the isoenzyme CYP3A4, CYP3A5, CYP3A7.
T1 / 2 (half-life) of active metabolites - 1.9 hours.
Up to 60% of the dose is excreted through the intestine in the form of metabolites, and 10–15% through the kidneys.

Indications for use

    primary hypercholesterolemia: type IIa, type IIb or mixed according to Fredrickson's classification, heterozygous familial and non-familial - in the absence of a clinical effect from diet therapy with low cholesterol levels, exercise and non-drug measures to reduce body weight in patients with an increased risk of developing coronary atherosclerosis;
    a combined form of hypercholesterolemia and hypertriglyceridemia, which cannot be corrected with a special diet and physical activity;
    coronary heart disease - for secondary prevention of myocardial infarction, slowing the progression of coronary atherosclerosis, reducing the risk of cardiovascular disorders (transient ischemic attacks or stroke), death, revascularization procedures.

Contraindications

    acute phase of liver disease, sustained increase in the activity of hepatic transaminases of unknown etiology;
    myopathy and other diseases of skeletal muscles;
    simultaneous use of itraconazole, ketoconazole, HIV protease inhibitors, erythromycin, clarithromycin, telithromycin, nefazodone and other inhibitors of cytochrome P450 3A4 (isoenzyme CYP3A4);
    lactase deficiency, glucose-galactose malabsorption syndrome, lactose intolerance;
    period of pregnancy;
    breast-feeding;
    age under 18;
    an indication of a history of established hypersensitivity to statin drugs (HMG-CoA reductase inhibitors);
    individual intolerance to the components of the drug.
According to the instructions, Simvastatin should be prescribed with caution in case of alcoholism, a history of liver disease, impaired renal function, severe renal failure with creatinine clearance (CC) less than 30 ml / min, uncontrolled epilepsy, severe disturbances in water and electrolyte balance, arterial hypotension, pronounced endocrine and metabolic disorders, severe acute infections (sepsis), acute necrosis of skeletal muscles, myopathy, major surgery, trauma, concomitant therapy with fibrates (except fenofibrate), gemfibrozil, nicotinic acid (when using lipid-lowering doses - more than 1 g per day), cyclosporine, amiodarone, diltiazem, verapamil, when taken simultaneously with grapefruit juice, if the patient is over 65 years old (especially for women).

Instructions for use: method and dosage

Simvastatin treatment should be carried out against the background of adherence to a standard hypocholesterol diet during the entire course of therapy.
The tablets are taken orally with plenty of water.
Taking Simvastatin is not associated with food intake.
The doctor prescribes the duration of the course of treatment individually.
Recommended dosage:
    hypercholesterolemia: 5 to 80 mg. The initial dose is 10 mg once a day (in the evening) for 28 days. Then, based on the research results, the optimal dose is selected, reducing the initial dose to 5 mg or increasing it. In most patients, the therapeutic effect is provided by taking the drug in a dose of up to 20 mg. In the absence of a clinical effect while taking Simvastatin at a dose of 40 mg, one should consider switching to another means of lipid-lowering therapy, since doses of more than 40 mg lead to a significant increase in the risk of myopathy. A dose of 80 mg can be used only if there is no target LDL concentration when taking 40 mg of simvastatin;
    homozygous hereditary hypercholesterolemia: 40 mg once a day (in the evening) or at a dose of 80 mg per day, divided into 3 doses (Simvastatin 20 mg in the morning, 20 mg in the afternoon and 40 mg in the evening). The use of the drug is recommended in combination with LDL apheresis or other lipid-lowering therapy;
    ischemic heart disease (including patients with or without hyperlipidemia): the initial dose is Simvastatin 20 mg once a day (in the evening). If necessary, the dose can be increased to 40 mg. To change (select) the dose, an interval of 28 days of therapy should be observed. The basis for reducing the dose of the drug is the content of LDL less than 75 mg / dl, and total cholesterol - less than 140 mg / dl.
Recommended dosage for patients on concomitant therapy with the following drugs:
    cyclosporine, danazol, nicotinic acid in a lipid-lowering (more than 1000 mg per day) dose, gemfibrozil and other fibrates (except fenofibrate): the maximum daily dose is 10 mg;
    diltiazem: no more than 40 mg per day;
    amiodarone, verapamil: no more than 20 mg per day.
For elderly patients and with mild to moderate renal failure, dose adjustment is not required.
With severe renal failure (CC less than 30 ml / min) Simvastatin should be taken in a dose of no more than 10 mg per day. If it is necessary to take the drug in higher doses, careful monitoring of the patient's condition should be ensured.

Side effects

    from the central nervous system and sensory organs: weakness, insomnia, taste disturbance, headache, memory impairment, asthenia, paresthesia, dizziness, muscle cramps, peripheral neuropathy, myasthenia gravis, blurred visual perception;
    from the digestive system: dyspepsia, abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting, pancreatitis, hepatitis, cholestatic jaundice, liver dysfunction, increased activity of alkaline phosphatase, hepatic transaminases, creatine phosphokinase;
    from the musculoskeletal system: myalgia, myopathy, rhabdomyolysis, muscle cramps;
    dermatological reactions: pruritus, rash, alopecia;
    allergic and immunopathological reactions: extensive hypersensitivity syndrome - urticaria, dermatomyositis, shortness of breath, flushing of the face, polymyalgia rheumatica, lupus-like syndrome, vasculitis, eosinophilia, thrombocytopenia, increased ESR (erythrocyte sedimentation rate, arthritis
    others: acute renal failure (due to rhabdomyolysis), palpitations, anemia, decreased potency.

Overdose

Symptoms: the characteristic symptoms have not been established even while taking simvastatin in a single dose of 450 mg.
Treatment: there is no specific antidote, therefore, if a high dose of the drug is accidentally ingested, the stomach should be immediately flushed or induced vomiting to prevent the absorption of simvastatin. Further, the appointment of activated carbon, laxatives, symptomatic therapy is carried out. It is necessary to ensure careful monitoring of renal and liver function, the level of concentration of creatine phosphokinase in the blood serum, general measures aimed at maintaining vital functions, monitoring the patient's condition. In the case of the development of myopathy with acute renal failure and rhabdomyolysis, intravenous (IV) drip of sodium bicarbonate and a diuretic is required. With the development of hyperkalemia, the patient is prescribed intravenous calcium chloride or calcium gluconate, in severe cases the use of hemodialysis is indicated.

Special instructions

The initiation of therapy with Simvastatin may be accompanied by a transient increase in the level of hepatic enzymes.
The study of liver function should be carried out before starting the use of the drug, then regular monitoring of the activity of liver enzymes is required. During the first three months, studies are carried out with an interval of 1.5 months, then every 2 months until the end of the first year of therapy, then once every 6 months. The state of liver function should be monitored with each increase in the dose of the drug. When using 80 mg per day, the test should be performed at intervals of 3 months. If the level of transaminase activity is 3 times higher than the initial one and remains stable, Simvastatin should be discontinued.
It is important to take into account that the use of simvastatin in severe acute infection, arterial hypotension, severe metabolic disorders, trauma, and extensive surgical intervention increases the risk of rhabdomyolysis and renal failure.
If an increase in cholesterol levels is observed against the background of hypothyroidism (decreased thyroid function) or kidney disease (including nephrotic syndrome), then primary therapy should involve treatment of the underlying disease.
The use of simvastatin is associated with the risk of developing myopathy, leading to rhabdomyolysis and renal failure. The likelihood of myopathy increases with severe renal failure or concomitant use of fibrates (gemfibrozil, fenofibrate), cyclosporine, nefazodone, macrolides (clarithromycin, erythromycin), azole antifungals (ketoconazole, itraconazole), ritonavir inhibitors, and others. In addition, predisposing factors for the development of myopathy include the patient's age over 65, female sex, renal failure, and uncontrolled hypothyroidism. Patients should be informed that if they feel unwell or have a fever accompanied by unexplained pain, soreness and / or weakness in the muscles, they should consult a doctor.
The simultaneous use of grapefruit juice may have an effect on an increase in the severity of side effects of simvastatin.
In case of hypertriglyceridemia of I, IV and V types, the use of the drug is not indicated.
For the timely diagnosis of the development of myopathy, regular studies are required to determine the rate of creatine phosphokinase in the blood serum; if it is more than 10 times the upper limit of the norm, then Simvastatin should be canceled.
The clinical efficacy of the drug has been established both in monotherapy and in combination with bile acid sequestrants.
If you accidentally skip taking the current dose, the pill should be taken as soon as you remember, if this does not correspond to taking two doses at the same time.

Influence on the ability to drive vehicles and complex mechanisms

During the period of treatment, it is recommended to be careful when working with complex mechanisms and driving vehicles.

Application during pregnancy and lactation

The use of Simvastatin during gestation and lactation is contraindicated.
Cancellation of a lipid-lowering agent during pregnancy does not significantly affect the results of long-term therapy of primary hypercholesterolemia.
The use of simvastatin in women of childbearing age should take place against the background of the use of reliable methods of contraception. Conception should not be allowed during the period of drug treatment.
If pregnancy occurs during the period of taking the drug, then immediate cancellation of simvastatin is required, the woman should be informed about the risk of developing fetal abnormalities.
If it is necessary to use simvastatin during lactation, breastfeeding should be discontinued.

Childhood use

Due to the lack of information on the efficacy and safety of the use of simvastatin in children, the prescription of the drug for the treatment of patients under the age of 18 is contraindicated.

With impaired renal function

Simvastatin should be used with caution in case of impaired renal function, severe renal failure (CC less than 30 ml / min).
No dose adjustment is required for mild to moderate renal impairment.
With severe renal failure (CC less than 30 ml / min), you should take no more than 10 mg of simvastatin per day. If it is necessary to take the drug in higher doses, careful monitoring of the patient's condition should be ensured.

For violations of liver function

The appointment of the drug is contraindicated during the acute phase of liver diseases, a persistent increase in the activity of liver enzymes of unknown etiology.

Use in the elderly

The drug should be used with caution to treat patients over the age of 65, especially women.
Elderly patients do not need dose adjustment.

Drug interactions

With the simultaneous use of Simvastatin:
    fibrates (except fenofibrate), nicotinic acid at a dose of more than 1000 mg per day, amlodipine: increase the risk of myopathy and rhabdomyolysis;
    ketoconazole, itraconazole, erythromycin, clarithromycin, telithromycin, nefazodone, HIV protease inhibitors (inhibitors of the cytochrome CYP3A4 isoenzyme): contribute to a clinically significant increase in the risk of myopathy and rhabdomyolysis, should not be prescribed during therapy with simvastatin;
    cyclosporine, verapamil, diltiazem: should be prescribed with caution due to the risk of myopathy and rhabdomyolysis;
    indirect anticoagulants coumarin derivatives (including warfarin): in a daily dose of 20-40 mg simvastatin potentiates the action of coumarin anticoagulants, causing an increase in prothrombin time and the international normalized ratio (careful monitoring of these parameters is required before starting therapy, during the entire period of drug use and after its withdrawal );
    cholestyramine, colestipol: contribute to a decrease in the bioavailability of simvastatin, therefore, it should be taken 4 hours after taking these drugs, an additive effect is possible;
    digoxin: the concentration of digoxin in the blood plasma increases;
    grapefruit juice: Drinking more than 1 liter of juice per day can cause a clinically significant increase in the activity of HMG-CoA reductase inhibitors.

Terms and conditions of storage

Keep out of the reach of children.
Store at temperatures up to 25 ° C, protected from light and moisture.
Shelf life is 2 years.

Reviews

Reviews of Simvastatin are mostly positive. Patients and some doctors point to the effectiveness of the drug in lowering cholesterol levels and preventing atherosclerosis, an affordable price, ease of use, and good tolerance.
Another part of doctors gives preference to new generation drugs, the side effects of which are less pronounced.
While taking the drug in chronic pancreatitis, there is an increase in the frequency of exacerbations of the disease.

Terms of sell

You don't need a prescription to buy Simvastatin.