Vazilip - instructions for use, reviews, analogs and formulations (10 mg, 20 mg and 40 mg tablets) of statin drugs for the treatment of hypercholesterolemia and the reduction of elevated cholesterol in adults, children and pregnancy

In this article, you can read the instructions for using the drug Wazilip. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of the statin Vasilip in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Wazilip in the presence of existing structural analogues. Use to treat hypercholesterolemia and reduce elevated cholesterol in adults, children, as well as during pregnancy and lactation.

Wazilip - a hypolipidemic drug (statin).

The active substance of the drug Vazilip is simvastatin, the main effect of which is a decrease in the total cholesterol (total Xc) and low-density lipoprotein (LDL-C) cholesterol in blood plasma. It is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid (early stage of Xc synthesis). Simvastatin reduces the concentration of total Xc, Xc-LDL and triglycerides (TG). The Xc content of very low density lipoproteins (Xc-VLDL) also decreases, while the high-density lipoprotein (Xc-HDL) cholesterol content moderately increases. Reduces the total content of cholesterol and LDL in cases of heterozygous family and non-family forms of cholesterolemia, with mixed hyperlipidemia, when elevated Xc content is a risk factor. The drug reduces the level of total Xc and Xc-LDL in patients with IHD, reducing the risk of myocardial infarction and death for these patients.

Simvastatin also significantly reduces the content of apolipoprotein B, moderately increases the concentration of Xc-HDL and reduces plasma concentrations of TG.As a result of these effects of simvastatin, the ratio of total Xc to total XC-HDL and Xc-LDL decreases to Xc-LBV.

Anti-atherosclerotic effect of simvastatin is a consequence of the drug on the walls of blood vessels and components. Simvastatin alters the metabolism of macrophages, inhibiting the activation of macrophages and the destruction of atherosclerotic plaques. The drug inhibits the synthesis of isoprenoids, which are growth factors in the proliferation of smooth muscle cells of the inner shell of vessels. The action of simvastatin improves the endothelium-dependent dilatation of blood vessels.

Therapeutic effect occurs after 2 weeks, the maximum effect is observed after 4-6 weeks of treatment.

Composition

Simvastatin + excipients.

Pharmacokinetics

Simvastatin is presented in an inactive lactone form, which is relatively well absorbed (from 61% to 85%) from the digestive tract. Bioavailability is less than 5%. Simultaneous food intake does not affect the absorption of the drug. With prolonged intake of cumulation of the drug in the body does not occur. Binding to blood plasma proteins - 98%. Metabolised in the liver, subjected to the effect of "first passage" through the liver (basically hydrolyzed into its active form beta-hydroxy acid).It is mainly excreted through the intestine (60%) in the form of metabolites. About 13% is excreted by the kidneys in an inactive form.

Indications

Hypercholesterolemia:

• primary hypercholesterolemia or mixed dyslipidemia (in addition to diet and in the ineffectiveness of other non-pharmacological activities (physical activity and weight loss));
• homozygous hereditary hypercholesterolemia (in addition to a special diet and lipid-lowering therapy (for example, LDL apheresis) or in the inefficiency of these measures).

Prevention of cardiovascular diseases:

• reduction of cardiovascular mortality and morbidity in patients with clinical manifestations of atherosclerotic cardiovascular diseases or diabetes mellitus, with normal or elevated cholesterol levels and as an additional measure to correct other risk factors and cardioprotective therapy.

Forms of release

Tablets coated with 10 mg, 20 mg and 40 mg.

Instructions for use and dosing regimen

Inside, once in the evening. The recommended dose of simvastatin varies from 5 mg to 80 mg once a day in the evening. Most often, the initial dose of the drug is 10 mg.Changes (selection) of the dose should be carried out at intervals of not less than 4 weeks. The maximum daily dose is 80 mg. The maximum daily dose is recommended only for patients with severe hypercholesterolemia or a high risk of cardiovascular complications. Duration of the drug is determined individually by the attending physician.

Hypercholesterolemia

The patient should observe a standard hypocholesterol diet throughout the entire period of treatment with Vasilip. The recommended initial dose of the drug for patients with hypercholesterolemia is 10 mg. With the aim of a more pronounced decrease in the level of X-LDL (more than 45%), treatment can be started from 20-40 mg per day (once in the evening).

In patients with homozygous hereditary hypercholesterolemia, the recommended daily dose of Vasilip is 40 mg 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); these patients are recommended to use Vasilip in combination with other lipid-lowering therapy (for example, apheresis of LDL).

Prevention of cardiovascular diseases

In patients with a high risk of coronary heart disease, with or without hyperlipidemia, effective doses of Vasilip 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. If the LDL content is less than 75 mg / dL (1.94 mmol / L), the total Xc content is less than 140 mg / dL (3.6 mmol / L), the dose of the drug should be reduced.

Concomitant therapy

The drug Vazilip is effective in monotherapy or in combination with bile acid sequestrants (for example, colestyramine and colestipol). In patients treated with cyclosporine, gemfibrozil, other fibrates or nicotinic acid (more than 1 g per day), the recommended initial dose is 5 mg, the maximum daily dose of Vasilip is 10 mg. Further increase in dose in such situations is not recommended.

In patients who are simultaneously receiving Amiodarone or verapamil, daily doses of Vasilip should not exceed 20 mg.

In elderly patients and in patients with moderate renal insufficiency, dosage adjustment is not required.

Side effect

• constipation, diarrhea;
• abdominal pain;
• flatulence;
• dyspepsia;
• nausea, vomiting;
• pancreatitis;
• hepatitis;
• jaundice;
• headache;
• paresthesia;
• dizziness;
• peripheral neuropathy;
• asthenia;
• insomnia;
• convulsions;
• blurred vision;
• a violation of taste sensations;
• myopathy;
• myalgia;
• muscle cramps;
• developed syndrome of hypersensitivity (angioedema, lupus-like syndrome, rheumatic polymyalgia, dermatomyositis, vasculitis, thrombocytopenia, eosinophilia, increased ESR, arthritis, arthralgia, urticaria, photosensitivity, fever, flushing of the skin, shortness of breath and severe weakness);
• skin rash;
• itching;
• alopecia;
• anemia;
• palpitation;
• acute renal failure (due to rhabdomyolysis);
• decreased potency.

Contraindications

• liver disease in the active phase or persistent increase in hepatic transaminase activity of unclear etiology;
• simultaneous administration of inhibitors of the isoenzyme CYP3A4 (eg, itraconazole, ketoconazole, HIV protease inhibitors, erythromycin, clarithromycin, telithromycin and nefazodone);
• pregnancy;
• lactation period (breastfeeding);
• age under 18 years (efficacy and safety of use not studied);
• hypersensitivity to simvastatin and other components of the drug.

Application in pregnancy and lactation

The drug is contraindicated in pregnancy. There was no evidence of an increase in the incidence of congenital malformations in children of women taking Vasilip or another HMG-CoA reductase inhibitor. When a pregnant woman receives simvastatin, a decrease in the fetal levels of mevalonate, which is a precursor of the biosynthesis of Xs, is possible. The abolition of hypolipidemic drugs during pregnancy does not have a significant effect on the results of the short-term risk associated with primary hypercholesterolemia.

Simvastatin should not be used in pregnant women, in women planning pregnancy, or with suspected pregnancy. If during pregnancy pregnancy occurs, the drug should be canceled, and the woman is warned about possible danger to the fetus.

During the period of treatment with the drug Vazilip, women of reproductive age should use reliable contraceptives.

It is not known whether the drug is excreted into breast milk, so the therapy with Vasilip during breastfeeding is contraindicated.

Application in elderly patients

In elderly patients, dosage adjustment is not required.

Use in children

Contraindicated in children and adolescents under the age of 18 years (efficacy and safety of use not studied).

special instructions

In patients with reduced thyroid function (hypothyroidism) or in the presence of certain kidney diseases (nephrotic syndrome) with an increase in Xc level, the underlying underlying disease should first be treated.

Patients with severe renal failure are treated with renal function.

Treatment with Vasilip, like other inhibitors of GMC-CoA reductase, can cause myopathy, sometimes resulting in rhabdomyolysis with or without renal failure, due to myoglobinuria. The risk of myopathy increases with an increase in the dose of simvastatin and in patients with severe renal insufficiency. In the treatment with simvastatin, it is possible to increase the content of serum CK, which should be taken into account in the differential diagnosis of chest pain and after intensive physical exertion.

Before starting therapy with Vasilip or increasing its dose, patients should be informed of the risk of developing myopathy and the need to consult a doctor immediately if there is an unexplainedpain, tension or weakness in the muscles, especially if it is accompanied by a malaise or fever. The baseline level of CKD should be determined before the start of therapy in the following situations:

• in elderly patients;
• with kidney damage;
• with decompensated hypothyroidism;
• with a burdened family history of hereditary muscle diseases;
• if there is a history of toxic effects on the muscles of statins or fibrates;
• at abusing alcohol.

It is necessary to evaluate the possible risk and the expected benefit and during the clinical monitoring recommended on the background of therapy. If initially the level of CK is significantly increased (more than 5 times with respect to IGN), the measurement should be repeated after 5-7 days to confirm the results. With a significant initial increase in the level of CK (more than 5 times relative to IGN), the drug should not be prescribed.

Before and during the course of treatment, the patient should be on a hypocholesterol diet.

During treatment with Vasilip, when muscle pain, weakness, or seizures appear, it is necessary to determine the level of CK. The criterion for the discontinuation of the drug is an increase in the serum levels of CK in more than 5 times relative to IGN.If the muscle symptoms are severe and cause discomfort, even if the CK level is less than 5 times the VGN, it may be necessary to stop treatment. If suspected of myopathy, therapy should be discontinued, regardless of the cause of myopathy.

If the symptoms disappear and the content of CPK returns to normal, reintroduction of a statin or an alternative drug of the same class in a minimal clinically effective dose and under careful medical supervision is possible. Therapy with Vasilip should be temporarily stopped a few days before major surgical interventions.

Patients with severe renal failure are treated with renal function.

Measures to reduce the risk of myopathy caused by drug interactions

The risk of myopathy and rhabdomyolysis increases significantly with the simultaneous use of simvastatin and potent inhibitors of CYP3A4 (eg, itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors, nefazodone), gemfibrozil or cyclosporine. The risk of myopathy and rhabdomyolysis also increases with the combined use of fibrates and high doses of nicotineacid (more than 1 g per day) or with simultaneous therapy with amiodarone or Verapamil with high doses of simvastatin. The risk also increases somewhat with the simultaneous administration of diltiazem and high doses of simvastatin (80 mg). Therefore, the use of simvastatin concomitantly with itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors and nefazodone is contraindicated. If you can not refuse therapy with the listed inhibitors of CYP3A4, you should refrain from prescribing simvastatin. Simvastatin should also be combined with caution with some other, less potent inhibitors of CYP3A4: cyclosporine, verapamil and diltiazem.

Avoid simultaneous administration of Wazilip and grapefruit juice.

In patients taking ciclosporin, gemfibrozil or high doses of nicotinic acid (more than 1 g per day), the daily dose of simvastatin should not exceed 10 mg.

Simultaneous appointment of simvastatin and gemfibrozil is possible only in those cases when the expected benefit significantly exceeds the potential risk of such a drug combination.The benefits of combined use of simvastatin 10 mg per day and other fibrates (other than fenofibrate), nicotinic acid (more than 1 g per day) or cyclosporine should be carefully weighed against the potential risk of such combinations.

There is a risk of myopathy in the appointment of fenofibrate and simvastatin alone, so caution is needed when taking this combination at the same time.

When taking simvastatin at doses exceeding 20 mg per day, simultaneous administration of amiodarone or verapamil should be avoided, unless the expected benefit exceeds the potential risk of myopathy.

Effects on the liver

Treatment with Vasilip can cause an increase in the activity of hepatic enzymes in the blood serum. This increase is usually insignificant and clinically insignificant. After the drug is discontinued, transaminase levels usually slowly decrease to the baseline level. Nevertheless, before the treatment begins, it is necessary to conduct a study of liver function in the future (to monitor the activity of hepatic transaminases every 6 weeks for the first 3 months, then every 8 weeks for the remaining first year, and then once every six months).If it is necessary to increase the dose to 80 mg, it is necessary to monitor liver function before increasing the dose, 3 months after the increase and then periodically (for example, every 6 months) during the first year of treatment. If the activity of ACT and / or ALT in the blood serum increases by a factor of 3 with respect to VGN, treatment with simvastatin should be stopped.

With caution, prescribe to people who abuse alcohol and / or have a history of liver disease.

Impact on the ability to drive vehicles and manage mechanisms

The adverse effect of the drug Vazilip on the ability to drive and work with machinery has not been reported. Nevertheless, it should be borne in mind that in the postmarketing use of simvastatin, isolated cases of dizziness are noted.

Drug Interactions

Pharmacodynamic interactions

Simultaneous use of simvastatin with fibrates, nicotinic acid (more than 1 g per day) increases the risk of myopathy, including rhabdomyolysis (with simultaneous use with fenofibrate - there is no evidence of an increased risk of myopathy compared with monotherapy with each drug alone).

Simultaneous use with gemfibrozil can lead to an increase in the concentration of simvastatin in the serum.

Pharmacokinetic interactions

Inhibitors of cytochrome CYP3A4 (itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors and nefazodone) involved in the metabolic conversion of simvastatin in the liver increase the risk of myopathy and rhabdomyolysis during simvastatin therapy. Simultaneous use with these drugs is contraindicated.

With caution, it is necessary to simultaneously appoint with less potent inhibitors of CYP3A4: cyclosporine, verapamil and diltiazem. The daily dose of simvastatin when taken concomitantly with cyclosporine should not exceed 10 mg. The daily dose of simvastatin against a simultaneous reception of amiodarone or verapamil should not exceed 20 mg, and 40 mg - on the background of simultaneous diltiazem administration, unless the expected benefit clearly exceeds the potential risk of myopathy and rhabdomyolysis.

Vasilip in a dose of 20-40 mg per day in volunteers and patients with hypercholesterolemia potentiates the effects of coumarin anticoagulants (eg, warfarin), in particular an increase in prothrombin time, MHO.Therefore, in patients taking coumarin anticoagulants, prothrombin time and MHO should be determined before the start of simvastatin therapy, in the initial treatment period, with a change in the dose of simvastatin or drug withdrawal. When a stable prothrombin time and MHO are reached, further monitoring should be performed at intervals recommended for patients receiving anticoagulant therapy. Therapy with simvastatin does not cause changes in prothrombin time and the risk of bleeding in patients who do not take anticoagulants.

Grapefruit juice inhibits the activity of CYP3A4. Simultaneous reception of a large amount of grapefruit juice (more than 1 liter per day) and simvastatin leads to a significant increase in the concentration in the blood plasma of simvastatin acid. Therefore, during the treatment with simvastatin should avoid the use of grapefruit juice.

Analogues of the drug Vasylip

Structural analogs for the active substance:

• Aktalipid;
• Atherostat;
• Zocor;
• Zokor forte;
• Zorstat;
• Ovenkor;
• Simva Hexal;
• Simvard;
• Simvakol;
• Simvale;
• Simvastatin;
• Simvastol;
• Symvor;
• Simgal;
• Simlo;
• Sinquard;
• Holvasim.

Analogues for the pharmacological group (statins):

• Akorta;
• Anistat;
• Apexstatin;
• Atokord;
• Atomax;
• Atorvastatin;
• Atorvox;
• Atoris;
• The Vasator;
• Vazilip;
• Cardiostatin;
• The Cross;
• Leskol;
• Leskol Fort;
• Lipobay;
• Lipon;
• Lipostat;
• Lipofford;
• Liprimar;
• Liptonorm;
• Lovacor;
• Lovastatin;
• Lovasterol;
• Mevakor;
• Medostatin;
• Mertenil;
• Ovenkor;
• Pravastatin;
• Rovacor;
• Rosart;
• Rosystark;
• Rosuvastatin;
• Rosewood;
• Rosulip;
• Roxer;
• Simvastatin;
• Simvastol;
• Tevastor;
• Torvazine;
• Torvacard;
• Tulip;
• Holvasim;
• Holletar.

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