Simvastatin
Simvastatin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Simvastatin
ATX code: C10AA01
Active ingredient: simvastatin (simvastatin)
Manufacturer: ZENTIVA (Czech Republic), Vertex JSC, ALSI Pharma CJSC, Severnaya Zvezda CJSC, Atoll LLC (Russia)
Description and photo updated: 2018-26-11
Prices in pharmacies: from 30 rubles.
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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., 1 can in a cardboard box; 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), dye iron oxide II yellow (E172), aluminum varnish based on the dye sunset yellow (E110), aluminum varnish based on the quinoline dye yellow (E104), indigo carmine-based aluminum varnish (E132), talc.
Pharmacological properties
Pharmacodynamics
Simvastatin is a hypolipidemic drug obtained as a result of a 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 enzyme HMG-CoA reductase, 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 the 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.
T 1/2 (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, not amenable to correction with a special diet and physical activity;
- ischemic 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 up to 18 years;
- 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 violations of 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 women).
Instructions for the use of Simvastatin: method and dosage
Simvastatin treatment should be carried out against the background of 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, you 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 only be used 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
- on the part of the central nervous system and sensory organs: weakness, insomnia, taste disturbance, headache, memory impairment, asthenia, paresthesia, dizziness, muscle cramps, peripheral neuropathy, myasthenia gravis, blurred vision;
- 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: skin itching, rash, alopecia;
- allergic and immunopathological reactions: extensive hypersensitivity syndrome - urticaria, dermatomyositis, shortness of breath, flushing to the skin of the face, rheumatic polymyalgia, lupus-like syndrome, vasculitis, eosinophilia, thrombocytopenia, increased ESR (erythrocyte sedimentation rate, arthritis), arthralnsitis
- 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 has been accidentally ingested, the stomach should be immediately washed out or induced vomiting to prevent the absorption of simvastatin. Next, they prescribe activated carbon, laxatives, symptomatic therapy. Careful monitoring of renal and liver function, serum creatine phosphokinase levels, general measures aimed at maintaining vital functions, monitoring of the patient's condition should be ensured. In the case 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 hypertriglyceridemia of types I, IV and V, the use of the drug is not indicated.
For the timely diagnosis of the development of myopathy, regular studies are required to determine the serum creatine phosphokinase index; 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 is contraindicated during gestation and lactation.
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.
Pediatric use
Due to the lack of information on the efficacy and safety of the use of simvastatin in children, prescribing 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
It is contraindicated to prescribe the drug during the acute phase of liver disease, 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 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 the indicated funds, 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.
Analogs
Simvastatin analogs are: Aterostat, Vazilip, Simgal, Zokor, Ovenkor, Akorta, Atomax, Pravastatin, Simvastol, Lipitor.
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.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Simvastatin
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.
Price for Simvastatin in pharmacies
The price of Simvastatin for a package containing 30 tablets at a dose of 10 mg can range from 34 to 123 rubles, at a dose of 20 mg - from 121 rubles. You can buy a package containing 20 tablets at a dose of 20 mg for 243 rubles.
Simvastatin: prices in online pharmacies
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Drug name Price Pharmacy |
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Simvastatin 10 mg film-coated tablets 30 pcs. RUB 30 Buy |
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Simvastatin 10 mg film-coated tablets 30 pcs. 34 rbl. Buy |
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Simvastatin 20 mg film-coated tablets 30 pcs. RUB 44 Buy |
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Simvastatin 20 mg film-coated tablets 30 pcs. RUB 50 Buy |
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Simvastatin 20 mg film-coated tablets 30 pcs. RUB 55 Buy |
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Simvastatin 10 mg film-coated tablets 30 pcs. RUB 62 Buy |
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Simvastatin 20 mg film-coated tablets 30 pcs. RUB 65 Buy |
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Simvastatin tablets p.o. 10mg 30 pcs. ALSI 73 rbl. Buy |
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Simvastatin tablets p.p. 20mg 30 pcs. 79 RUB Buy |
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Simvastatin tablets p.o. 20mg 30 pcs. 92 RUB Buy |
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Simvastatin Alkaloid 20 mg film-coated tablets 28 pcs. 92 RUB Buy |
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Simvastatin 40 mg film-coated tablets 30 pcs. 93 rbl. Buy |
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Simvastatin 10 mg film-coated tablets 28 pcs. 93 rbl. Buy |
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Simvastatin tablets p.o. 10mg 30 pcs. 94 r Buy |
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Simvastatin tab. p.p. 10 mg 28 pcs. RUB 97 Buy |
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Simvastatin tablets p.o. 20mg 30 pcs. Ozone RUB 99 Buy |
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Simvastatin 20 mg film-coated tablets 28 pcs. 119 RUB Buy |
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Simvastatin 10 mg film-coated tablets 30 pcs. 120 RUB Buy |
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Simvastatin tab. p.p. 20 mg 28 pcs. 123 r Buy |
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Simvastatin Alkaloid tablets p.o. 10mg 28 pcs. 134 r Buy |
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Simvastatin Alkaloid 10 mg film-coated tablets 28 pcs. 134 r Buy |
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Simvastatin 20 mg film-coated tablets 30 pcs. RUB 138 Buy |
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Simvastatin 20 mg film-coated tablets 20 pcs. 148 RUB Buy |
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Simvastatin Zentiva 10 mg film-coated tablets 28 pcs. RUB 165 Buy |
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Simvastatin tablets p.o. 10mg 30 pcs. RUB 186 Buy |
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Simvastatin Zentiva 20 mg film-coated tablets 28 pcs. 275 RUB Buy |
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Simvastatin Zentiva 40 mg film-coated tablets 28 pcs. 433 r Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
