Zokor

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

Zokor: instructions for use and reviews

1. Release form and composition
2. Pharmacological action
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: Zocor

ATX code: C10AA01

Active ingredient: Simvastatin (Simvastatin)

Producer: Merck Sharp & Dohme BV (Netherlands)

Description and photo update: 2019-06-08

Prices in pharmacies: from 159 rubles.

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Zokor is a hypolipidemic drug.

Release form and composition

Produced in the form of coated tablets: oval, smooth on one side, on the other side - engraving "MSD 735" (light pink tablets) or engraving "MSD 740" (yellowish brown tablets) (14 pcs. In blisters, 1 or 2 blisters in a cardboard box).

The active substance is simvastatin:

1 light pink tablet - 10 mg;
1 yellowish brown tablet - 20 mg

Excipients: ascorbic acid, butylhydroxyanisole, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, citric acid, magnesium stearate.

Shell composition: hydroxypropyl cellulose, talc, methyl hydroxypropyl cellulose, titanium dioxide, iron oxide yellow and iron oxide red dyes.

pharmachologic effect

According to the instructions, Zokor is characterized by a pronounced lipid-lowering effect. The tablets contain the active ingredient simvastatin, which, upon hydrolysis, turns into active compounds. Its metabolite inhibits the enzyme HMG-CoA reductase, which is involved in cholesterol biosynthesis at the initial stage.

As a result, the use of the drug helps to reduce the total concentration of cholesterol in the body, as well as the level of cholesterol bound by low and very low density lipoproteins. The concentration of cholesterol in the plasma of triglycerides also decreases.

At the same time, when taking Zokor, the content of cholesterol bound by high density lipoproteins significantly increases. The drug is used for various types of hyperlipidemia, including non-familial, familial, heterozygous. It is also prescribed for mixed types of hyperlipidemia in cases where diet fails to normalize plasma lipid concentrations.

Plasma lipid levels decrease 14 days after starting therapy. Their number reaches a minimum at 4-6 weeks of treatment. With further administration of the drug, this result remains.

After completion of therapy, the values of total plasma cholesterol gradually return to the initial values, which were determined before the start of the drug.

Pharmacodynamics and pharmacokinetics

The maximum concentration of simvastatin metabolites in the blood is recorded 1.3–2.4 hours after taking one dose of Zokor. Approximately 85% of the active substance contained in the tablets is absorbed in the body when taken orally.

During treatment with the drug, a higher level of simvastatin is noted in the liver compared to other tissues. As a result of the effect of the "first passage" of a substance through the liver, it is metabolized, after which the drug itself and its metabolites are excreted from the body with bile.

Taking Zokor does not depend on food intake, which does not affect the pharmacokinetics of the drug. Long-term therapy does not lead to the accumulation of simvastatin in body tissues.

Indications for use

Zokor is prescribed to patients with coronary artery disease (CHD) or a predisposition to this disease, as well as to patients with a high risk of CHD (including hyperlipidemia), for example, patients with diabetes mellitus, patients with peripheral vascular disease, stroke or other cerebrovascular diseases history. The purpose of the drug:

Reducing the risk of mortality due to coronary heart disease;
Reducing the risk of developing serious coronary or vascular complications such as stroke, nonfatal myocardial infarction, coronary death;
Reducing the risk of hospitalization for angina attacks;
Reducing the likelihood of surgery due to the need to restore peripheral blood flow or other types of non-coronary revascularization.

Also, the listed categories of patients are prescribed the drug in case of need for revascularization surgery.

In addition, Zokor is prescribed for hypercholesterolemia - as an addition to the diet in cases where dietary nutrition and other non-drug methods of treatment are not enough. The purpose of the drug:

Treatment of type IV hyperlipidemia according to the Fredrickson classification (hypertriglyceridemia);
Treatment of primary hyperlipidemia of type III in accordance with the Fredrickson classification (dysbetalipoproteinemia);
Reducing elevated levels of total cholesterol, low-density lipoprotein (LDL) cholesterol, apolipoprotein B and triglycerides;
Increased high-density lipoprotein (HDL) cholesterol in patients with primary hypercholesterolemia, including type IIa hyperlipidemia according to Fredrickson's classification (heterozygous familial hypercholesterolemia) or type IIb hyperlipidemia according to Fredrickson's classification (mixed hypercholesterolemia);
Reducing the ratio of total cholesterol in relation to HDL cholesterol, as well as LDL cholesterol to HDL cholesterol;
Reducing elevated levels of total cholesterol, LDL cholesterol and apolipoprotein B in patients with homozygous familial hypercholesterolemia (in addition to diet and other treatments).

In patients with diabetes mellitus, Zokor reduces the risk of developing peripheral complications of vascular origin (including the likelihood of trophic ulcers, revascularization and amputation of the lower extremities).

In patients with ischemic heart disease, accompanied by high cholesterol levels, the drug can reduce the risk of developing coronary atherosclerosis, incl. the appearance of complications and new injuries.

Contraindications

Absolute:

Persistent increase in the level of hepatic transaminases in blood plasma of unclear etiology;
Active liver disease;
Pregnancy and the period of its planning;
Lactation;
Individual hypersensitivity to drug components.

Due to insufficient data on the safety of the use of simvastatin in pediatrics, it is not recommended to prescribe the drug to children.

Relative:

History of rhabdomyolysis;
Diabetes;
A steady increase in the level of serum transaminases (if the upper norm is exceeded by 3 times, the drug is canceled);
Severe renal failure (creatinine clearance less than 30 ml / minute);
Alcohol abuse.

Instructions for use of Zokor: method and dosage

Before using Zokor, the patient is prescribed a standard hypocholesterol diet, which must be followed throughout the course of treatment.

The daily dose of the drug (from 5 to 80 mg) should be taken in 1 dose in the evening.

During the titration period, the dose should be increased at least at 4-week intervals. The maximum allowable daily dose is 80 mg.

Recommended doses:

Patients with coronary artery disease or a high risk of its development: 40 mg 1 time per day. Drug therapy begins at the same time as diet and exercise therapy;
Patients with hypercholesterolemia (not included in the risk groups for IHD): the initial dose is 20 mg per day. In some cases (if a decrease in LDL levels by more than 45% is required), an initial dose of 40 mg may be prescribed. With a mild to moderate form of hypercholesterolemia, therapy can be started with a daily dose of 10 mg, if necessary, it is gradually increased;
Patients with homozygous familial hypercholesterolemia: 40 mg once a day or 80 mg in 3 divided doses - 20 mg in the morning and afternoon and 40 mg in the evening. In this case, Zokor can be prescribed as a monopreparation or in addition to another method of therapy that lowers cholesterol levels (for example, LDL plasmapheresis).

Zokor is used as monotherapy or in combination with bile acid sequestrants. In this case, a correction of its dose is required depending on the drugs used simultaneously:

Danazol, cyclosporin, gemfibrozil, other fibrates (with the exception of fenofibrate), niacin in lipid-lowering doses (> 1000 mg / day): the daily dose of Zokor is 10 mg;
Verapamil, amiodarone: the daily dose should not exceed 20 mg.

Patients with moderate renal impairment do not need to adjust the dose. Patients with severe renal insufficiency (creatinine clearance less than 30 ml / minute) are not recommended to exceed the daily dose of 10 mg. If such a need is justified, the treatment should be carried out under particularly careful medical supervision.

Side effects

Digestive system: dyspepsia (diarrhea, nausea and vomiting); rarely - pancreatitis, jaundice, hepatitis;
Central nervous system: vertigo, peripheral neuropathy;
Musculoskeletal system: myalgia; rarely - rhabdomyolysis;
Allergic and immunopathological reactions: lupus-like syndrome, angioedema, polymyalgia rheumatica, increased ESR, eosinophilia, arthritis, thrombocytopenia, arthralgia, vasculitis, urticaria, skin hyperemia, photosensitization, shortness of breath, fever, general malaise;
Dermatological reactions: skin rash, itching, dermatomyositis, alopecia;
Others: muscle cramps, paresthesias, general malaise, anemia;
Laboratory indicators: increased levels of transaminases, alkaline phosphatase and gamma-glutamyl transpeptidase, creatine phosphokinase.

Overdose

In case of an overdose, traditional medication methods are used to overcome the consequences of intoxication of the body.

special instructions

Like all HMG-CoA reductase inhibitors, Zokor can cause myopathy, manifested by symptoms such as muscle pain, soreness or general weakness, accompanied by an increase in creatine phosphokinase (more than 10 times the upper limit of normal). Myopathy can manifest itself in the form of rhabdomyolysis, which is sometimes accompanied by acute secondary renal failure due to myoglobinuria and, in some cases, is fatal. The risk of developing myopathy increases with an increase in the concentration in blood plasma of substances that have an inhibitory effect on HMG-CoA reductase.

Some drugs used concomitantly with Zokor (especially in high doses) increase the risk of myopathy / rhabdomyolysis.

All patients who are prescribed simvastatin should be warned about the need for urgent medical attention in case of muscle weakness, muscle soreness or any unexplained pain. At the beginning of treatment and at each dose increase, it is recommended to determine the concentration of creatinine phosphokinase.

In cases where a planned surgical intervention is necessary, Zokor should be canceled several days before the operation and refrain from taking it in the postoperative period.

Before starting therapy, and in the future, in accordance with the patient's clinical parameters, it is recommended to monitor liver function. Additional studies of liver function should be carried out in patients who are planning to increase the dose of simvastatin to 80 mg / day, then 3 months after the start of the high dose of the drug, then about once every 6 months during the first year of treatment. Particular attention should be paid to patients diagnosed with elevated serum transaminase levels. This category of patients needs to be re-examined in the near future and then carried out regularly until the level of serum transaminases returns to normal. If the level rises, especially in the case of a steady increase in 3 times the upper limit of the norm, Zokor should be canceled.

Drug interactions

The following drugs, taken concomitantly with simvastatin (especially in high doses), increase the risk of myopathy / rhabdomyolysis:

Potent CYP3A4 inhibitors: clarithromycin, erythromycin, telithromycin, ketoconazole, nefazodone, itraconazole, human immunodeficiency virus protease inhibitors;
Other lipid-lowering agents that are not potent inhibitors of CYP3A4, but can cause the development of myopathy: gemfibrozil and other fibrates (with the exception of fenofibrate), niacin (nicotinic acid) in lipid-lowering doses (> 1 g / day);
Cyclosporine, Danazol;
Amiodarone, verapamil;
Diltiazem.

Simvastatin, used in a daily dose of 20-40 mg, potentiates the effect of coumarin anticoagulants and increases the risk of bleeding: prothrombin time (International Normalized Ratio) increases from an initial level of 1.7 to 1.8 in healthy volunteers, and in patients with hypercholesterolemia - from 2, 6 to 3.4. To exclude significant changes in this indicator, patients receiving coumarin anticoagulants, prothrombin time should be determined before starting Zokor use and periodically during the initial period of treatment. After the INR indicator has stabilized, its further determination should be carried out at the intervals recommended for monitoring patients undergoing anticoagulant therapy.

Grapefruit juice contains at least one component that inhibits CYP3A4 and may increase plasma levels of drugs metabolized by this enzyme. The consumption of 1 glass of juice (250 ml) per day has no clinical significance. However, with the consumption of large amounts of juice (more than 1 liter per day) during the period of simvastatin therapy, the plasma level of activity of HMG-CoA reductase inhibitors significantly increases. For this reason, large amounts of grapefruit juice should not be consumed during treatment.

Analogs

Zokor's analogues are: Simvastatin, Simvastatin Zentiva, Avestatin, Simvakard, Simlo, Aterostat, Levomir, Vabadin, Simgal, Zovatin, Simvor.

Terms and conditions of storage

Store at temperatures up to 30 ºC out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Zokor

There are numerous reviews of Zokora, confirming the effectiveness of the drug. Its active ingredient actually helps to significantly lower cholesterol levels. However, in order to obtain the expected result, it is recommended to use the drug strictly for the period specified by the attending physician. Patients also note positive results when using simvastatin for prophylactic purposes.

Zokor price in pharmacies

The price for Zokor 20 mg (for a pack of 28 tablets) is on average 720-800 rubles. You can buy the drug in a dose of 10 mg in pharmacies for about 440–500 rubles (28 pcs per pack).

Zokor: prices in online pharmacies

Drug name

Price

Pharmacy

Zokor 10 mg film-coated tablets 28 pcs.

159 r

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Zokor 20 mg film-coated tablets 28 pcs.

307 r

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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!