Zocor - lipid-lowering agent.
Release form and composition
The drug is available in the form of tablets:
- Zocor 10 mg and 20 mg (in blisters of 14 pcs.);
- Zokor Forte 40 mg (in blisters of 14 pcs.).
The active ingredient of the drug is simvastatin.
Auxiliary components of tablets: butylhydroxyanisol, pregelatinized starch, ascorbic acid, microcrystalline cellulose, magnesium stearate, lactose monohydrate, citric acid;
The composition of the shell: talc, hydroxypropylcellulose, methylhydroxypropylcellulose, titanium dioxide, dye.
Indications for use
Zocor is prescribed to patients with peripheral vascular diseases, ischemic heart disease (IHD), predisposition to it, as well as people who are at risk of developing IHD, including patients with diabetes, patients with stroke and other cerebrovascular diseases.
The purpose of Zocor in this case:
- Prevention of hospitalization for angina attacks;
- Reducing the risk of developing severe vascular and / or coronary complications, including nonfatal myocardial infarction, stroke, coronary death;
- Prevention of surgery to restore peripheral blood flow and other types of non-coronary revascularization;
- Reducing the risk of the need for surgical intervention for the restoration of coronary blood flow (coronary artery bypass surgery, percutaneous transluminal coronary angioplasty);
- Reducing mortality from coronary artery disease.
In patients with coronary artery disease with increased cholesterol, Zocor can slow the development of coronary artery disease and prevent complications associated with it.
Zokor is also prescribed for hypercholesterolemia in those cases when only diet and other non-drug therapies were not enough. In particular, it is shown:
- To reduce elevated levels of total cholesterol, low density lipoprotein (LDL), apolipoprotein B, triglycerides;
- To reduce elevated levels of total cholesterol, LDL and apolipoprotein B in patients with homozygous familial hypercholesterolemia;
- When hypertriglyceridemia (type IV hyperlipidemia in accordance with the classification of Fredrickson);
- With primary dysbetalipoproteinemia (type III hyperlipidemia according to the Fredrickson classification);
- To increase high-density lipoproteins (HDL) in patients with primary hypercholesterolemia (including Type IIa hyperlipidemia according to Fredrickson classification) and with mixed hypercholesterolemia (Type IIb hyperlipidemia according to Fredrickson classification);
- To reduce the ratio of total cholesterol to HDL, as well as LDL with respect to HDL.
Patients with diabetes mellitus Zokor is prescribed to reduce the risk of developing peripheral vascular complications, including the formation of trophic ulcers, the need for revascularization or amputation of the lower extremities.
Zokor is not prescribed:
- In the case of known hypersensitivity to simvastatin or any auxiliary component of the drug;
- Patients with liver disease in the active phase or a persistent increase in plasma transaminases of unknown etiology;
- During pregnancy;
- During the period of breastfeeding;
- Children up to 18 years.
Careful observation during treatment is necessary:
- Patients who underwent rhabdomyolysis during the previous therapy with simvastatin or had a complicated history (for example, suffered from renal failure);
- People who, before the start of treatment, abused alcohol;
- Patients with sustained elevated serum transaminase levels (if this indicator is 3 times higher than the upper normal range, the drug should be immediately discontinued);
- Patients with severe renal insufficiency (it is not recommended to exceed the daily dose of 10 mg).
Dosing and Administration
Prior to starting Zocor, the patient is prescribed a standard hypocholesterol diet, which the patient must follow and the entire course of treatment.
The dose is selected individually, if necessary, its increase is done gradually - at intervals of at least 4 weeks. The maximum allowable daily dosage is 80 mg. Take the drug should be once a day, in the evening.
As a rule, average therapeutic doses are:
- For patients with coronary artery disease and high risk of its development, including patients with diabetes mellitus, with peripheral vascular diseases, stroke or other cerebrovascular diseases - 40 mg;
- When hypercholesterolemia (not included in the above risk categories) - 20 mg. If you need a significant decrease in LDL (more than 45%), the dose is increased to 40 mg. With mild to moderate hypercholesterolemia, 10 mg is usually sufficient.
With homozygous familial hypercholesterolemia, 40 mg once daily or 80 mg in 3 divided doses may be administered: 20 mg in the morning and afternoon, then 40 mg in the evening.
Zokor is used as a single agent, and in combination with bile acid sequestrants.
Patients receiving lipid-lowering doses of niacin (> 1 g / day) or cyclosporin, gemfibrozil, danazol, or other fibrates (except fenofibrate), Zokor is prescribed in a daily dose of 10 mg.
For patients taking verapamil or amiodarone, the maximum dose of Zocor is 20 mg.
Patients with moderate renal insufficiency do not need to adjust the dose of simvastatin. In severe renal failure, it is not recommended to take more than 10 mg / day. If there is a need for higher doses, treatment should be carried out under special supervision.
Basically, Zokor is well tolerated. Side effects, if they occur, are usually expressed weakly and are transient.
Possible adverse reactions due to taking Zocor:
- Abdominal pain, constipation / diarrhea, nausea and / or vomiting, flatulence, rarely - pancreatitis, hepatitis, jaundice;
- Asthenia, headache, dizziness, peripheral neuropathy;
- Myalgia, rarely - myopathy / rhabdomyolysis;
- Skin rash, pruritus, dermatomyositis, alopecia;
- Anemia, paresthesia, muscle cramps, general malaise;
- Lupus-like syndrome, angioedema, rheumatic polymyalgia, eosinophilia, thrombocytopenia, increased ESR, vasculitis, arthritis, photosensitization, urticaria, fever, arthralgia, shortness of breath, skin hyperemia.
There are also separate reports on the development of a persistent and pronounced increase in the level of transaminases, an increase in the activity of gamma-glutamyltranspeptidase, alkaline phosphatase, reatinphosphokinase.
Like other inhibitors of GM-CoA reductase, Zocor can cause myopathy, manifested by muscle pain, tenderness, general weakness, and an increase in creatine phosphokinase (10 or more times the upper limit of the norm). In some cases, myopathy can manifest itself as rhabdomyolysis, sometimes fatal.
The risk of myopathy / rhabdomyolysis increases with simultaneous use of:
- powerful inhibitors of CYP3A4, including clarithromycin, ketoconazole, itraconazole, erythromycin, HIV protease inhibitors, telithromycin, nefazodone;
- other lipid-lowering agents that are not potent inhibitors of CYP3A4, but can cause myopathy when taken as monodrugs, these include gemfibrozil and other fibrates (except fenofibrate), lipid-lowering doses of niacin;
- cyclosporine, danazol;
- amiodarone, verapamil;
It is important to note that grapefruit juice contains several components that inhibit CYP3A4 and are able to increase the concentration of drugs metabolized by CYP3A4 in the blood. When using 1 cup of juice per day, this effect is minimal and has no clinical significance, however, it increases significantly with the consumption of more than 1 liter of grapefruit juice per day. This should be taken into account during the period of treatment with Zokor.
When taken in a dose of 20 mg or more, simvastatin potentiates the effect of coumarin anticoagulants and increases the risk of bleeding. For this reason, the prothrombin time should be determined before the start of Zocor's administration, quite often at the beginning of therapy and periodically during the entire treatment.
Atherostat, Aktalipid, Vasilip, Avestatin, Zorstat, Simvalimit, Simvakard, Simvastatin, Ovenkor, Simvastol, Holvasim, Simgal, Simvor, Simlo.
Terms and conditions of storage
Store Zokor should be in a dry, dark place at temperatures up to 30 ºС. Shelf life - 2 years.