Simvastatin

Simvastatin (lat. Simvastatin) is a first-generation drug from the group of statins.

It lowers the blood content of "bad" cholesterol (LDL) and contributes to the development of "good" (HDL), protects blood vessels, has an antioxidant effect.

Appointed at increased risk of heart attack, stroke, coronary heart disease, atherosclerosis. It is usually prescribed after high-priority measures, including a change in diet, weight loss and increased physical activity, do not lead to a decrease in the level of total cholesterol and low-density lipoprotein (LDL) in the blood.

Available in tablet form. The tablet contains the active component Simvastatin. Dosages of the active substance: 10, 20, 40, 80 mg.

Clinico-pharmacological group

Lipid-lowering drug.

Terms of sale from pharmacies

You can buy by prescription.

Price

How much is simvastatin in pharmacies? The average price is at the level of 55 rubles.

Composition and release form

Dosage form - tablets, film-coated: round (tablets 10, 20 and 40 mg) or oblong (80 mg) forms, convex on both sides, light pink (10 and 20 mg) or pink (40 and 80 mg) color , on one side, the engraving “A”, on the other - “01”, “02”, “03” or “04” (respectively, tablets in a dose of 10, 20, 40 or 80 mg); The cross section shows two layers - a white core surrounded by a pink shell (10 each in blisters, in a cardboard bundle of 1, 3, 5 or 10 blisters).

  • Active substance: simvastatin, in 1 tablet - 10, 20, 40 or 80 mg.

Auxiliary components: microcrystalline cellulose, lactose monohydrate, ascorbic acid, pregelatinized starch, butyl hydroxyanisol, magnesium stearate, citric acid monohydrate.

Pharmachologic effect

The active ingredient is produced synthetically during the fermentation of Aspergillus terreus. The active substance is an inactive lactone, which as a result of hydrolysis in the human body turns into a hydroxy acid derivative. The main metabolite inhibits a specific enzyme that catalyzes the formation of mevalonate from HMG-CoA. This reaction underlies the early synthesis of cholesterol, which allows Simvastatin to prevent the accumulation of toxic forms of sterols. HMG-CoA can be easily metabolized to acetyl-CoA, which is actively involved in many synthesis processes in the human body.

While taking Simvastatin, triglycerides, total cholesterol, "bad" and "very bad" cholesterol (LDL and VLDL) are reduced. The effect of the drug appears after 15 days of treatment, and becomes noticeable by laboratory parameters after 1-1.5 months. Cholesterol lowering effect persists throughout the entire course of treatment. After cessation of therapy, cholesterol levels gradually return to their original level.

Pharmacokinetics

After oral administration, simvastatin is almost completely absorbed. The period of reaching the maximum plasma concentration is from 1.3 to 2.4 hours. After 12 hours, its content in the blood is reduced 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, is hydrolyzed in tissues to beta-hydroxy acid and inactive metabolites.

Metabolized in the liver as a result of the effect of the first passage through the liver with the participation of isoenzyme CYP3A4, CYP3A5, CYP3A7.

T1/2 (half-life) of active metabolites - 1.9 hours.

Up to 60% of the received dose is excreted through the intestine as metabolites, and 10-15% through the kidneys.

Indications for use

Simvastatin can be both the active substance of other drugs, and an independent medicine aimed at reducing the concentration in the blood of a number of fats.

Indications for use Simvastatin such:

  1. In cases of primary hypercholesterolemia of types IIa and IId, if a diet that does not contain cholesterol or other non-drug measures was ineffective, and the risk of coronary atherosclerosis is high.
  2. With combined hypercholesterolemia and hypertriglyceridemia, which are not corrected by diet and exercise.
  3. In ischemic heart disease, to slow the development of atherosclerosis of the coronary vessels, to prevent vascular and heart diseases, to reduce the risk caused by revascularization procedures.

Contraindications

Absolute:

  • Myopathy;
  • Gestation period;
  • Breastfeeding period;
  • Liver diseases in the acute phase, a persistent increase in the activity of liver transaminases of unknown origin;
  • Lactose intolerance, glucose-galactose malabsorption, deficiency of the enzyme lactase;
  • The simultaneous use of cytochrome P450 3A4 inhibitors (for example, ketoconazole, erythromycin, itraconazole, telithromycin, clarithromycin, HIV protease inhibitors and nefazodone);
  • Children and adolescents under 18 years of age (since the safety and efficacy of the drug have not been established);
  • Hypersensitivity to the main or auxiliary components of the drug or other means of a statin series in the anamnesis.

Relative (Simvastatin is used with caution):

  • Alcoholism;
  • Severe violations of water and electrolyte balance;
  • Injuries;
  • Extensive surgical interventions;
  • Uncontrolled epilepsy;
  • Hypotension;
  • Acute skeletal muscle necrosis;
  • History of liver disease;
  • Severe renal failure;
  • Impaired renal function;
  • Pronounced metabolic and endocrine disorders;
  • Severe acute infections (eg, sepsis);
  • Advanced age (especially women over 65);
  • Simultaneous use with cyclosporine, verapamil, amiodarone, nicotinic acid in doses of more than 1 g per day, gemfibrozil and other fibrates (with the exception of fenofibrate), diltiazem and grapefruit juice.

Appointment during pregnancy and lactation

Simvastatin is contraindicated in pregnancy, because able to cause various developmental abnormalities in newborns. During treatment, the use of contraception.

There is no data on the penetration of the active substance into breast milk. Nevertheless, it is important to remember that there is a high risk of Simvastatin's influence on the health of the child.

Dosage and method of use

As indicated in the instructions for use while taking the drug should not be associated with food intake. The duration of the drug is determined by the attending physician individually.

  • Simvastatin should be taken orally once a day in the evening, drinking plenty of water.

Before treatment with simvastatin, the patient should be prescribed a standard hypocholesterol diet, which should be followed during the entire course of treatment.

Coronary heart disease

When treating patients with ischemic heart disease (IHD) or at high risk of developing IHD, with or without hyperlipidemia, effective doses of Simvastatin are 20, 40 mg per day. Therefore, the recommended initial dose in such 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 (2 tablets of 20 mg of the drug simvastatin).

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 should be reduced.

Hypercholesterolemia

The recommended dose of Simvastatin for the treatment of hypercholesterolemia varies from 5 to 80 mg once daily in the evening.

With the ineffectiveness of the drug in a dose of 40 mg is recommended to switch to another type of lipid-lowering therapy. The use of the drug in a dose of more than 40 mg increases a significant risk of myopathy.

The dose of Simvastatin 80 mg should be used only in those patients who have not reached the target concentration of LDL when using a dose of 40 mg.

The recommended starting dose for patients with hypercholesterolemia is 10 mg. Changes (selection) 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.

In patients with homozygous hereditary hypercholesterolemia, the recommended daily dose of Simvastatin is 40 mg (2 tablets of 20 mg once daily in the evening or 80 mg in 3 doses (20 mg in the morning, 20 mg in the afternoon and 40 mg in the evening). These patients are recommended to use Simvastatin in combination with another lipid-lowering therapy (for example, LDL apheresis).

Concomitant therapy

In patients receiving treatment with cyclosporine, danazol, gemfibrozil, other fibrates (except fenofibrate) or nicotinic acid in lipid-lowering doses (more than 1 g / day), the recommended maximum daily dose of the drug Simvastatin should not exceed 10 mg. A further dose increase in such situations is not recommended.

For violations of the kidneys

With care: severe renal failure (CC less than 30 ml / min); impaired renal function.

In patients with severe renal insufficiency (CC less than 30 ml / min), the recommended dose of the drug Simvastatin should not exceed 10 mg per day. If you need to increase the dose, careful monitoring of such patients is carried out.

Patients with mild or moderate renal insufficiency do not require dose adjustment.

With abnormal liver function

Contraindications: liver disease in the active phase, a persistent increase in liver enzymes of unknown etiology.

With caution: a history of liver disease.

Side effect

In most cases, the drug Simvastatin is well tolerated by patients, but in individuals with increased individual sensitivity to the components of tablets, side effects may occur:

  1. Allergic and immunopathological reactions: hypersensitivity syndrome developed - urticaria, dermatomyositis, dyspnea, rushes to the skin of the face, rheumatic polymyalgia, lupus-like syndrome, vasculitis, eosinophilia, thrombocytopenia, increased ESR (erythrocyte sedimentation rate), an increase in ESR (erythrocyte sedimentation rate), eosinophilia, thrombocytopenia, an increase in ESR (erythrocyte sedimentation rate
  2. On the part of the digestive system: dyspepsia, abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting, pancreatitis, hepatitis, cholestatic jaundice, abnormal liver function, increased activity of alkaline phosphatase, hepatic transaminase, creatine phosphokinase;
  3. From the central nervous system and sensory organs: weakness, insomnia, impaired taste, headache, impaired memory, asthenia, paresthesia, dizziness, muscle cramps, peripheral neuropathy, myasthenia gravis, blurred visual perception;
  4. On the part of the musculoskeletal system: myalgia, myopathy, rhabdomyolysis, muscle cramps;
  5. Dermatological reactions: pruritus, rash, alopecia;
  6. Others: acute renal failure (due to rhabdomyolysis), palpitations, anemia, a decrease in potency.

Overdose

Long-term use of the drug increases the likelihood of side effects.

In case of overdose (simultaneous administration of the medication in a dosage much higher than recommended by specialists), it is necessary to wash the stomach, take activated charcoal. The level of serum CK should be monitored.

Special instructions

Before you start using the drug, read the specific instructions:

  1. Before using this drug, the patient must observe a special diet with a low content of fats and carbohydrates for some period of time. While taking Simvastatin, patients are advised not to abuse grapefruit juice and citrus fruits, as this increases the risk of side effects.
  2. At the beginning of therapy with Simvastatin, it is necessary to check the level of liver enzymes in a patient every 1.5 months. If the test results remain unsatisfactory for a long time, then the drug is discontinued.
  3. If the patient has a history of liver disease or functional disorders, you should consult with your doctor and pass tests before starting therapy. The same applies to persons with alcohol dependence.
  4. Patients who are recommended to increase the dose of the drug should be warned about the risk of myopathy. In the case of the first symptoms of this complication or prerequisites for the development of myopathy, treatment with the drug is immediately stopped.
  5. The drug is prescribed with caution to persons with chronic kidney disease. In the case of the risk of developing renal failure in a patient, drug treatment is not carried out.
  6. Patients suffering from diseases of the thyroid gland, in particular its hypofunction, should start a course of treatment of the underlying disease before taking Simvastatin tablets.
  7. It is desirable to take the drug at one and the same time, if for some reason the patient forgot to take the pill, it should be drunk as soon as possible, but if the time for the next dose is already ready, then the dose of the drug is not doubled.

There are no data on the effect of the drug on the ability to control the patient of a vehicle or a complicated technique, therefore, when taking Simvastatin tablets, you should refuse to drive a car.

Interaction with other drugs

The following medications can cause myopathy:

  • anti-mycotic drugs (Itraconazole, Ketoconazole);
  • fibrates;
  • immunosuppressants;
  • Telithromycin;
  • Nefazodone;
  • HIV protease inhibitors;
  • Erythromycin;
  • large doses of nicotinic acid;
  • Clarithromycin.

High dosages of simvastatin and joint administration of Danazole and Cyclosporine can lead to rhabdomyolysis. The drug is able to potentiate the effect of oral forms of anticoagulants (warfarin, Fenprokumon), increase the risk of bleeding. The drug increases the concentration of digoxin.

Reviews

We offer you to read the reviews of people who used the drug Simvastatin:

  1. Sofia. The most affordable drug of all statins. Packing 80-90 rubles enough for a month. It should be taken for a long time, or at least in courses, so I can not afford expensive drugs, and simvastatin is just right. Although there is nausea and dizzy, but after a course of cholesterol I returned to normal.
  2. Valentine. I am 76 years old, Simvastatin is prescribed as a therapist by 20mg 1tab. for the night after the first pill, pains in the intestines began, on the second day I took another pill and the pain increased. I stopped taking the pain after three days, the pain was very strong. Of course, she no longer drinks.
  3. Natalia. The doctor prescribed atorvastatin or rozuvastatin, but after learning the prices for them, I decided to study the issue and ventured to buy simvastatin. The list of side effects, of course, was frustrating, but there is nothing to do. At first it seemed to me that I felt bad from him, but I didn’t give up taking it and after the 3rd pill it stopped. After two months of admission, she passed the analysis, cholesterol dropped!

Reviews of doctors are divided. Some believe that the drug belongs to the "old guard" and has become obsolete, given the severity of adverse reactions, and the appearance on the pharmaceutical market of Atorvastatin and Rosuvastatin, which belong to the drug of a new generation. Others note that the drug successfully reduces cholesterol and is an excellent means of preventing atherosclerosis.

Analogs

Simvastatin as an active substance is included in many medicines:

  1. Avestatina,
  2. Atorvastatin,
  3. SimvaGeksala,
  4. Actalipida,
  5. Zokora
  6. Simlo
  7. Vasilip,
  8. Zorstat,
  9. Ovenkora,
  10. Atherostat,
  11. Character
  12. Simgal
  13. Simvalimita
  14. Holvasima
  15. Zovatina.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Simvastatin tablets are dispensed from pharmacies only by prescription. The drug should be kept out of the reach of children in a cool place.

The shelf life of the tablets is indicated on the package and is 2 years from the date of manufacture.

Watch the video: The Side Effects of Statins (November 2019).

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