Simvastatin

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

It lowers the content of "bad" cholesterol (LDL) in the blood and promotes the production of "good" (HDL), protects blood vessels, has antioxidant effect.

It is prescribed for an increased risk of heart attack, stroke, with coronary heart disease, atherosclerosis. Usually it is prescribed after first-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 lipoproteins (LDL) in the blood.

Produced in tablet form. The tablet contains the active ingredient Simvastatin. Dosage of the active substance: 10, 20, 40, 80 mg.

Clinical and pharmacological group

Lipid-lowering drug.

Terms of sale from pharmacies

It is possible to buy under the prescription of the doctor.

Price

How much does Simvastatin cost in pharmacies? The average price is at the level of55 rubles.

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Composition and form of release

Dosage form - tablets coated with a film membrane: round (tablets 10, 20 and 40 mg) or oblong (80 mg) form, on both sides convex, light pink (10 and 20 mg) or pink (40 and 80 mg) color, on one side engraving "A on the other - "01 "02 "03" or "04" (respectively tablets in a dose of 10, 20, 40 or 80 mg); Two layers are visible on the cross-section - a white core surrounded by a pink envelope 10 pieces. 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, butylhydroxyanisole, magnesium stearate, citric acid monohydrate.

pharmachologic effect

The active component is produced synthetically by fermentation of Aspergillus terreus. The active substance is an inactive lactone, which, as a result of hydrolysis in the human body, passes into the 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 takes an active part in many synthesis processes in the human body.

Against the background of taking simvastatin, the level of triglycerides, total cholesterol, "bad" and "very bad" cholesterol (LDL and VLDL) decreases. The effect of the medication is manifested after 15 days of treatment, and becomes noticeable by laboratory parameters after 1-1.5 months. Cholesterol reducing effect persists throughout the course of treatment. After discontinuation of therapy, the cholesterol level gradually returns to its original value.

Pharmacokinetics

After oral administration, simvastatin is almost completely absorbed. The period of reaching the maximum concentration in the blood plasma is from, to, hours. After 12 hours, its content in the blood decreases by 90%.

Bioavailability of the drug is less than 5%.

Binding to plasma proteins is approximately 95%.

It enters the body in an inactive form, in the tissues it is hydrolyzed into beta-hydroxy acid and inactive metabolites.

Metabolised 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 hours.

Through the intestine in the form of metabolites up to 60% of the dose received, through the kidneys - 10-15%.

Indications for use

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

Indications for the use of simvastatin are:

1. With primary hypercholesterolemia of types IIa and IId, if no cholesterol-containing diet or other Non-pharmacological measures were ineffective, and the risk of coronary atherosclerosis is great.
2. With combined hypercholesterolemia and hypertriglyceridemia, which are not adjusted by diet and exercise.
3. In ischemic heart disease, to slow the development of coronary artery atherosclerosis, to prevent vascular and cardiac disease, to reduce the risk caused by revascularization procedures.

Contraindications

Absolute:

• Myopathy;
• Pregnancy period;
• The period of breastfeeding;
• Diseases of the liver in the acute phase, persistent increase in liver transaminase activity of unknown origin;
• Lactose intolerance, glucose-galactose malabsorption, deficiency of lactase enzyme;
• 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 safety and efficacy of the drug are not established);
• Hypersensitivity to the main or auxiliary components of the drug or other drugs of the statin series in the anamnesis.

Relative (use simvastatin with caution):

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

Intended use for pregnancy and lactation

Simvastatin is contraindicated in carrying a pregnancy, tk. can cause various abnormalities in newborns. During treatment, contraception is mandatory.

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

Dosage and route of administration

As indicated in the instructions for use, the time of taking the drug should not be associated with eating. Duration of the drug is determined individually by the attending physician.

• Simvastatin should be taken 1 time per day in the evening, with plenty of water.

Before the treatment with simvastatin, the patient should be prescribed a standard hypocholesterolemic diet, which should be observed throughout the course of treatment.

Cardiac ischemia

In the treatment of patients with coronary heart disease (CHD) or a high risk of developing coronary artery disease, 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 done at intervals of 4 weeks, if necessary, the dose can be increased to 40 mg per day (2 tablets of 20 mg of simvastatin).

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 should be reduced.

Hypercholesterolemia

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

If the drug is ineffective at a dose of 40 mg, it 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 the significant risk of myopathy.

The dosage of Simvastatin 80 mg should be used only in those patients who did not reach the target LDL concentration with a dose of 40 mg.

The recommended initial dose of the drug for patients with hypercholesterolemia is 10 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 at 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 a day in the evening or 80 mg in 3 divided doses (20 mg in the morning, 20 mg in the afternoon and 40 mg in the evening). Such patients are recommended to use simvastatin in combination with other lipid-lowering therapy (for example, apheresis of LDL).

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. Further increase in dose in such situations is not recommended.

In case of violations of kidney function

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

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

In patients with mild or moderate renal insufficiency, dose adjustment is not required.

With violations of liver function

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

With caution: liver disease in the anamnesis.

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: developed hypersensitivity syndrome - urticaria, dermatomyositis, dyspnea, flushing of the skin to the skin of the face, rheumatic polymyalgia, lupus-like syndrome, vasculitis, eosinophilia, thrombocytopenia, increased ESR (erythrocyte sedimentation rate), arthralgia, arthritis, photosensitivity, angioedema;
2. On the part of the digestive system: dyspepsia, abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting, pancreatitis, hepatitis, Cholestatic jaundice, impaired liver function, increased activity of alkaline phosphatase, hepatic transaminases, creatine phosphokinase;
3. From the central nervous system and sensory organs: weakness, insomnia, taste disorders, headache, violation memory, asthenia, paresthesia, dizziness, muscle cramps, peripheral neuropathy, myasthenia gravis, blurred vision perception;
4. From the musculoskeletal system: myalgia, myopathy, rhabdomyolysis, muscle cramps;
5. Dermatological reactions: skin itching, rashes, alopecia;
6. Other: acute renal failure (due to rhabdomyolysis), palpitations, anemia, decreased potency.

Overdose

Prolonged use of the drug increases the likelihood of side effects.

In case of an overdose (simultaneous administration of the drug in a dosage significantly exceeding the recommended by experts), it is necessary to rinse the stomach, take activated charcoal. It is necessary to monitor the level of CK in the blood serum.

special instructions

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

1. Before starting the use of this drug, the patient must always observe a special diet with a reduced content of fats and carbohydrates for a certain period of time. When taking Simvastatin, patients are not advised to abuse grapefruit juice and citrus fruits, as this leads to an increased risk of side effects.
2. At the beginning of therapy, the drug Simvastatin should be checked every month for the level of hepatic enzymes in the patient. If the test results for a long time remain unsatisfactory, then the drug is stopped.
3. If a history of the patient has a disease or functional disorders of the liver, you should consult a doctor and take tests before starting therapy. The same goes for people 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 appearance of the first symptoms of this complication or the prerequisites for the development of myopathy, treatment with the drug is immediately stopped.
5. The drug is administered with caution to people with chronic kidney disease. In the case of a risk of developing renal failure in a patient, the drug is not treated with the drug.
6. Patients suffering from thyroid gland diseases, in particular, its hypofunction, should start a course of therapy for the underlying disease before starting the administration of Simvastatin tablets.
7. The drug should be taken at 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 of the next appointment has already arrived, the dose of the drug is not double.

Data on the effect of the drug on the ability to manage the patient's motor transport or complex technology is not provided, so during the reception of tablets Simvastatin should be abandoned driving car.

Interaction with other drugs

Myopathy can be caused by the following medicines:

• antimycotics (Itraconazole, ketoconazole);
• fibrates;
• immunosuppressants;
• Telithromycin;
• Nefazodone;
• HIV protease inhibitors;
• Erythromycin;
• large doses of nicotinic acid;
• Clarithromycin.

High doses of simvastatin and the joint administration of Danazol and Cyclosporine may lead to rhabdomyolysis. The drug is able to potentiate the effect of oral forms of anticoagulants (Warfarin, Fenprokumone), increase the risk of bleeding. The drug increases the concentration of digoxin.

Reviews

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

1. Sofia. The most affordable drug for all their statins. Packages in 80-90 rubles is enough for a month. Take it must be a long time, or at least courses, so that expensive drugs I can not afford, and simvastatin - just right. Although there is nausea and dizziness, but after my course, cholesterol returned to normal.
2. Valentina. To me of 76 years, the therapist is appointed Simvastatinum on 20 mg 1tab. at night after the first pill pains in the intestines began, I on the second day still drank a pill and the pain intensified. She stopped taking the pain after three days, the pain was very strong. Of course, she did not drink any more.
3. Natalia. The doctor prescribed atorvastatin or rosuvastatin, but after learning the prices for them I decided to study the question and ventured to buy simvastatin. List of pobochek, of course upsetting, but there's nothing to do. At first it seemed to me that it was bad for him, but I did not give up and after the 3rd pill it stopped. After two months of taking the test, the cholesterol dropped!

The doctors' opinions are divided. Some believe that the drug belongs to the "old guard" and outlived itself, given the severity of adverse reactions, and appearance on the pharmaceutical market of atorvastatin and rosuvastatin, which relate to the preparation of a new generation. Others note that the drug successfully reduces cholesterol and serves as an excellent means of preventing atherosclerosis.

Analogues

Simvastatin as an active substance is part of many medicines:

1. Avestatin,
2. Atorvastatin,
3. Simva Hexala,
4. Aktalipida,
5. Zokora,
6. Simlo,
7. Wazilip,
8. Zorstata,
9. Ovenkor,
10. Atherostat,
11. The symbol,
12. Simgala,
13. Simvilimita,
14. Holvasima,
15. Zovatina.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Simvastatin tablets are dispensed from pharmacies only on prescription. The drug should be stored out of the reach of children cool place.

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

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