Simvastol

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Simvastol: 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. Drug interactions
10. Analogs
11. Terms and conditions of storage
12. Terms of dispensing from pharmacies
13. Reviews
14. Price in pharmacies

Latin name: Simvastol

ATX code: C10AA01

Active ingredient: Simvastatin (Simvastatin)

Producer: Gedeon Richter Romania, SA (Romania)

Description and photo update: 2019-12-08

Simvastol is a hypolipidemic agent, an inhibitor of HMG-CoA reductase.

Release form and composition

Dosage form of Simvastol - film-coated tablets: round, biconvex, white tablet core with a uniform structure, pink (10 mg dose), yellow (20 mg dose) or brown (40 mg dose) shell (14 pcs. In blister, in a cardboard box 1 or 2 blisters).

1 film-coated tablet contains:

active substance: simvastatin - 10, 20 or 40 mg;
auxiliary components: pregelatinized starch, lactose monohydrate, ascorbic acid, microcrystalline cellulose PH101, butylhydroxyanisole, citric acid monohydrate, magnesium stearate;
film sheath pink / yellow / brown: Opadry II 33G24737 (lactose monohydrate, hypromellose, titanium dioxide, glycerol triacetate, macrogol, iron dye red oxide, iron oxide black dye, aluminum varnish based on indigo carmine dye) / Opadry II 39G22514 (triacetin, titanium dioxide, macrogol, lactose monohydrate, dye iron oxide yellow, dye iron oxide red, dye iron oxide black) / Opadry II 33G26729 (titanium dioxide, macrogol, hypromellose, dye iron oxide yellow, glycerol triacetate, dye iron oxide red, lactose monohydrate, iron dye black oxide).

Pharmacological properties

Pharmacodynamics

Simvastol is a lipid-lowering drug of artificial origin, which is obtained from the fermentation product of Aspergillus terreus. Simvastatin, the active substance of the drug, belongs to inactive lactones and is metabolized in the body to form a hydroxy acid derivative. The active metabolite inhibits the action of 3-hydroxy-3-methyl-glugaryl-CoA reductase (HMG-CoA reductase), an enzyme responsible for the conversion of HMG-CoA into mevalonate. This process represents an early stage in cholesterol synthesis.

Simvastatin treatment does not lead to the accumulation of potentially toxic sterols in the body. In metabolic processes, HMG-CoA is easily converted into acetyl-CoA, which is involved in many synthesis processes in the body.

Simvastatin is the cause of a decrease in the concentration in blood plasma of triglycerides, low density lipoprotein (LDL), very low density lipoprotein (VLDL) and total cholesterol (this is true for cases of heterozygous non-familial and familial types of hypercholesterolemia, as well as in mixed hyperlipidemia, when high cholesterol levels are considered risk factor).

Simvastol increases high-density lipoprotein (HDL) levels and decreases the total cholesterol / HDL and LDL / HDL ratio. The first results of treatment become noticeable 2 weeks after the start of taking the drug, and the maximum therapeutic effect is observed after 4-6 weeks. The effect of Simvastol continues during regular therapy, after its withdrawal, the cholesterol concentration gradually returns to its original values.

Pharmacokinetics

The absorption of simvastatin in the body is quite high. After oral administration, the maximum plasma level is observed after about 1.3-2.4 hours, decreasing by 90% after 12 hours. The substance binds to blood plasma proteins by about 95%.

Simvastatin is metabolized in the liver, there is a "first pass" effect through the liver, which consists in hydrolysis of the compound with the formation of an active metabolite - beta-hydroxy acid. Other active and inactive derivatives have also been identified. The half-life of active metabolites is 1.9 hours. Simvastatin is excreted mainly in feces (60%) in the form of metabolites. Approximately 10-15% is excreted in the urine in an inactive form.

Indications for use

hypercholesterolemia: primary (types IIa and IIb) in patients with an increased risk of developing coronary atherosclerosis in the absence of the effect of non-pharmacological treatments such as diets low in cholesterol, exercise, and weight loss; in combination with hypertriglyceridemia, which cannot be corrected by diet therapy and physical activity;
ischemic heart disease: prevention of myocardial infarction, reducing the risk of death, slowing the progression of atherosclerosis of the coronary arteries, lowering the risk of revascularization, reducing the risk of stroke, transient ischemic attacks and other cardiovascular disorders.

Contraindications

myopathy;
active phase of liver disease, sustained increase in the activity of liver enzymes of unknown etiology;
hereditary lactose intolerance;
a history of hypersensitivity to other HMG-CoA reductase inhibitors (statin drugs);
the period of pregnancy and breastfeeding;
children and adolescents up to 18 years old;
individual intolerance to the components of the drug.

It is recommended to prescribe Simvastol with caution for: chronic alcoholism; simultaneous therapy with immunosuppressants after organ transplantation (increased risk of renal failure and rhabdomyolysis); a history of liver disease; decreased or increased tone of skeletal muscles, of unknown etiology; epilepsy; conditions that contribute to the development of severe renal dysfunction, such as arterial hypotension, severe acute infectious diseases, severe metabolic and endocrine disorders, imbalance in water and electrolyte balance, trauma and surgery (including dental surgery).

Instructions for the use of Simvastol: method and dosage

Simvastol tablets are taken orally, 1 time per day in the evening, washed down with a sufficient amount of water, at different times with meals.

Before starting therapy, the patient is prescribed a standard hypocholesterol diet, which he must follow throughout the course of treatment.

The doctor prescribes the dose and period of use of the drug individually.

Recommended dosage of Simvastol:

hypercholesterolemia: the initial dose is 10 mg for 4 weeks, then, if necessary, the dose can be increased to 20 mg, in most cases it is optimal. The selection of a clinically effective dose is performed by increasing the previous dose by 10 mg with an interval of 4 weeks, but not exceeding 80 mg;
homozygous hereditary hypercholesterolemia: once a day in the evening - 40 mg or 80 mg in 3 divided doses (in the morning and afternoon, 20 mg, and in the evening, 40 mg);
ischemic heart disease (treatment and prevention): the initial dose is 20 mg for 4 weeks, then, taking into account the clinical course of the disease, the dose can be gradually increased to 40 mg at intervals of 4 weeks. Patients with low-density lipoprotein (LDL) levels below 75 mg / dL and total cholesterol levels below 140 mg / dL need a dose reduction.

With mild to moderate renal failure and elderly patients, dose adjustment is not required.

In the case of simultaneous administration of verapamil or amiodarone, the daily dose of Simvastol should be no more than 20 mg.

In chronic renal failure of severe degree with creatinine clearance (CC) below 30 ml / min and / or concomitant therapy with danazol, cyclosporine, gemfibrozil or other fibrates (with the exception of fenofibrate), nicotinic acid in lipid-lowering doses (1 g per day and above) is recommended do not exceed the daily dose of simvastatin more than 10 mg.

Side effects

from the digestive system: nausea, vomiting, possible abdominal pain, diarrhea, constipation, pancreatitis, flatulence, increased activity of hepatic transaminases, creatine phosphokinase (CPK), alkaline phosphatase, hepatitis;
from the nervous system: violation of taste, headache, insomnia, asthenic syndrome, dizziness, muscle cramps, peripheral neuropathy, paresthesia, blurred vision;
from the musculoskeletal system: weakness, muscle cramps, myopathy, myalgia; rarely - rhabdomyolysis;
allergic reactions: urticaria, fever, shortness of breath, lupus-like syndrome, angioedema, vasculitis, arthritis, polymyalgia rheumatica;
dermatological reactions: skin hyperemia, photosensitivity; rarely - itchy skin, rash, dermatomyositis, alopecia;
laboratory parameters: increased ESR (erythrocyte sedimentation rate), thrombocytopenia, eosinophilia;
others: anemia, palpitations, hot flashes, decreased potency; against the background of rhabdomyolysis - acute renal failure.

Overdose

The cases of Simvastol overdose known to specialists (the maximum dose taken was 450 mg) were not accompanied by the manifestation of specific symptoms. As a treatment, gastric lavage and intake of activated charcoal are recommended. They also prescribe symptomatic therapy and constantly monitor the content of CPK in the blood serum and the function of the kidneys and liver.

If the patient develops myopathy with rhabdomyolysis and acute renal failure (severe but rare side effect), the drug should be discontinued and the patient should be given sodium bicarbonate and a diuretic by intravenous infusion. If necessary, hemodialysis is performed.

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

special instructions

According to the instructions, Simvastol should not be prescribed to patients with an increased risk of rhabdomyolysis and renal failure. The risk factors for these pathologies include an acute form of severe infection, arterial hypotension, planned major surgery, trauma, and severe metabolic disorders.

The use of the drug is not indicated for hypertriglyceridemia of type I, IV and V.

Simvastol treatment should be accompanied by monitoring of liver function. Studies of the activity of liver enzymes are carried out before starting the use of the drug and regularly during therapy: 2 times every 6 weeks, then every 8 weeks until the end of the first year, then - once every six months. A liver function test should be performed with each dose increase, and with a daily intake of 80 mg, every 12 weeks. A transient increase in the level of liver enzymes is possible at the beginning of therapy. If the activity of transaminases exceeds 3 times the initial level and maintains a steady increase, the pills should be discontinued.

Patients with hypothyroidism and / or kidney disease (including nephrotic syndrome) with high cholesterol levels are advised to first treat the underlying disease.

In addition to monotherapy, the use of the drug is indicated in combination with bile acid sequestrants.

It is recommended to avoid the simultaneous use of large amounts (more than 250 ml) of grapefruit juice, since the severity of side effects of simvastatin may increase.

Against the background of the use of Simvastol, the development of myopathy, rhabdomyolysis and renal failure is possible. Symptoms of these pathologies include the appearance of muscle soreness, unexplained pain, lethargy or muscle weakness, accompanied by general malaise or fever. The risk of developing myopathy increases with the simultaneous administration of fibrates (fenofibrate, gemfibrozil), nefazodone, cyclosporine, macrolides (clarithromycin, erythromycin), HIV protease inhibitors (ritonavir), antifungal agents of the azole group (itraconazole, ketoconazole). In addition, the likelihood of developing myopathy is higher in patients with severe renal failure. When prescribing a drug, the doctor should warn the patient about the possibility of this disease, its symptoms and the need to immediately contact a specialist when they develop.

In patients with suspected or diagnosed myopathy, withdrawal of Simvastol is required.

Patients of childbearing age need to use reliable contraceptives during the entire period of taking the drug. If pregnancy occurs during treatment, the drug is discontinued, and the woman should be warned of the possible risk to the fetus.

Cancellation of lipid-lowering drugs during pregnancy does not significantly affect the result of long-term therapy of primary hypercholesterolemia.

With the appearance of myalgia, myasthenia gravis and / or a pronounced increase in CPK activity, the use of Simvastol should be discontinued.

If the next dose is accidentally missed, it should be taken as soon as you remember, provided that this does not mean taking two doses at the same time.

With severe renal failure, treatment should be carried out with monitoring of renal function.

The patient should follow a cholesterol diet before starting therapy and during the entire period of taking Simvastol.

The effect of the drug on the patient's ability to drive vehicles and mechanisms has not been established.

Drug interactions

The increase in the risk of myopathy is influenced by the simultaneous use of cytostatics, fibrates, immunosuppressants, nefazodone, erythromycin, clarithromycin, antifungal agents of the azole group, HIV protease inhibitors, high doses of nicotinic acid, telithromycin, in addition, at high doses of simvastatin - cyclosporin, danazol amiodarone, verapamil, diltiazem.

The bioavailability of simvastatin is reduced by colestipol and colestyramine, therefore, with concomitant therapy, in order to achieve an additive effect, Simvastol should be taken no earlier than 4 hours after the indicated funds.

The drug increases the level of digoxin in the blood plasma.

Simvastatin increases the effect of oral anticoagulants (including phenprocoumon, warfarin) and the risk of bleeding, therefore, before starting combined treatment, it is necessary to determine the patient's blood clotting parameters and regularly monitor them in the initial period of therapy. After reaching a stable level of prothrombin time, they switch to a standard treatment with anticoagulants. When you change the dose of the drug or stop taking it, you should use the above scheme for monitoring prothrombin time.

With monotherapy, Simvastol has no effect on laboratory parameters of prothrombin time and on an increased risk of bleeding.

Grapefruit juice significantly increases the inhibitory activity against HMG-CoA reductase in blood plasma.

Analogs

Simvastol analogs are: Aterostat, Holvasim, Vasilip, Simgal, Avestatin, Simplakor, Vero-Simvastatin, Simvor, Aktalipid, Sincard, Zokor Forte, Simlo, Zovatin, Simvakard, Levomir, Simvastatin, Ovenkor, Simvakor, Simvakor, Zovat

Terms and conditions of storage

Store at temperatures up to 25 ° C. Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Simvastol

According to reviews, Simvastol is quite successfully used according to indications. This effective and inexpensive drug allows you to reduce the concentration of cholesterol in hypercholesterolemia and minimize the risk of developing complications from the cardiovascular system.

The price of Simvastol in pharmacies

The approximate price for Simvastol 10 mg is 180-216 rubles. (per pack of 28 tablets). The cost of tablets with a dosage of 20 mg is on average 280-320 rubles. (the package contains 28 tablets).

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!