Simvatin

Simvatin is a lipid-lowering drug that reduces the values of serum triglycerides and cholesterol.

The drug reduces the likelihood of developing major vascular complications and the need for revascularization in the area of non-coronary and peripheral vessels. It also reduces the risk of major coronary disorders and the need for coronary revascularization (PTCA and AS), and reduces the likelihood of stroke. In addition, the drug reduces overall mortality, reducing mortality associated with coronary heart disease, and reduces the number of hospitalizations due to angina pectoris. [1]

The drug lowers the proportions of LDL-C / HDL-C and the proportion of total cholesterol / HDL-C. [2]

Indications Simvatin

It is used in people with a high likelihood of coronary artery disease (with or without hyperlipidemia) - for example, in diabetics, persons with a history of stroke or other cerebrovascular diseases, as well as in patients with peripheral vascular lesions or coronary artery disease.

It is prescribed as a dietary supplement to reduce the increased level of total cholesterol, triglycerides, LDL-C and apo B, and in addition to increase the level of HDL-C in people with primary form of hypercholesterolemia (familial type of hypercholesterolemia of a heterozygous nature or mixed type of hypercholesterolemia) - in situations where only diet and the use of other non-drug methods of therapy are ineffective.

The drug is used for hypertriglyceridemia and the primary form of dysbetalipoproteinemia.

In addition, it can be used in the form of supplementing the diet and other methods of therapy in individuals with a familial type of homozygous hypercholesterolemia - to reduce the increased level of total cholesterol, LDL-C and apolipoprotein B.

Release form

The release of the medication is sold in tablets - 10 pieces inside a blister pack. The pack contains 3 such packages.

Pharmacodynamics

Simvastatin is a cholesterol-lowering substance. It slows down the action of HMG-CoA reductase (an enzyme involved in intrahepatic cholesterol binding).

The drug reduces the values of total intrahepatic cholesterol, plasma triglycerides and LDL cholesterol. Along with this, the level of VLDL-C decreases, as well as a moderate increase in the HDL-C level. [3]

In addition, the drug improves the activity of the vascular endothelium of the circulatory system, has antioxidant properties and suppresses cell migration and proliferation during atherosclerotic processes.

Pharmacokinetics

Simvastatin, which is an inactive lactione, is quite well absorbed inside the gastrointestinal tract and is transformed into its active drug variety.

With the 1st intrahepatic passage, over 79% of the absorbed substance is retained inside the liver and undergoes metabolic processes.

Excretion is mainly carried out with feces and bile.

The drug effect develops within a period of 14 days with the achievement of the maximum effect after 1-2 months from the start of treatment.

Dosing and administration

The size of daily portions of drugs is within 10-80 mg; the medicine is taken in the evening, once a day. When choosing a dosage, it can be adjusted at intervals of at least 1 month. Changes are carried out until the maximum rate per day is reached - 80 mg.

Use in persons with ischemic heart disease or a high probability of developing this disease.

The size of the standard initial dosage for the specified group of patients is 40 mg, with 1 dose per day (in the evening). Medication therapy can be started at the same time as physical therapy and diet.

People with hypercholesterolemia who are not included in the risk groups described above.

Before starting therapy, a standard hypocholesterol diet is carried out, which is also observed throughout the entire period of the treatment cycle.

The starting serving per day is often 20 mg, taken once in the evening. Individuals who need a significant (over 45%) lowering of LDL values can be prescribed an initial dose of 40 mg.

In people with mild to moderate hypercholesterolemia, Simvatin is used at an initial dosage of 10 mg. Correction of portions, if necessary, is carried out according to the scheme described above.

Individuals with a familial type of homozygous hypercholesterolemia.

Given the data from controlled clinical testing, for patients with this type of disease, you should use daily servings of 40 mg (1 time in the evening) or 80 mg (divided into 3 uses - 20 mg each morning and afternoon, as well as 40 mg in the evening).

In these patients, the medication is used as an adjunct to another therapy regimen that lowers the cholesterol value (for example, the LDL-plasmapheresis procedure), or without other therapy when it is not available.

Combined schemes.

Simvatin is effective both in monotherapy and in combination with bile acid sequestrants.

People who use cyclosporine or gemfibrozil with other fibrates, or lipid-lowering dosages (≥1 g per day) of niacin together with medication, should not be administered more than 10 mg of drugs per day.

Individuals using verapamil or amiodarone should have a maximum daily serving size of 20 mg.

• Application for children

There is no information regarding the therapeutic effect and safety when using the drug in children, which is why it is not prescribed in pediatrics.

Use Simvatin during pregnancy

It is impossible to use Simvatin for HB or pregnancy.

Contraindications

Among the contraindications:

• severe intolerance to any of the elements of the medication;
• active phase of liver disease;
• developing for an unexplained reason, an increase in the values of serum transaminases.

Side effects Simvatin

Often, the medication is tolerated without complications, but at times side symptoms appear:

• epidermal and allergic disorders: itching, epidermal rash and alopecia;
• digestive problems: nausea, dyspepsia, bloating, constipation, vomiting, diarrhea, abdominal pain and pancreatitis. Occasionally jaundice or hepatitis develops;
• disorders in the work of the NA: paresthesias, headaches, polyneuropathy, dizziness, asthenia and convulsions;
• signs associated with the activity of ODA: myalgia. Rhabdomyolysis or myopathy is rare;
• lesions of the circulatory system: anemia;
• others: occasionally vasculitis, arthralgia, rheumatic polymyalgia and arthritis appear, in addition to this, urticaria, fever, photophobia, angioedema, blood flushes to the face and lupus-like syndrome occur. In addition, malaise, dyspnea, eosinophilia, thrombocytopenia, and increased ESR levels occasionally develop.

Overdose

Several situations were recorded with poisoning with simvastatin substances (with the maximum dosage used being 0.45 g), but the patients did not show specific complications and signs.

Overdose requires symptomatic action.

Interactions with other drugs

The metabolic processes of simvastatin are carried out with the participation of CYP3A4, but it does not have an inhibitory effect on this enzyme. In this regard, the introduction of drugs does not change the plasma values of drugs, whose metabolic processes occur under the influence of CYP3A4. Drugs that strongly inhibit the activity of CYP3A4 increase the likelihood of myopathy, since they slow down the elimination of simvastatin. These include ketoconazole with itraconazole, cyclosporine, HIV protease inhibitors, clarithromycin with erythromycin, and nefazodone.

Concomitant use with ritonavir may increase the serum values of simvastatin.

The likelihood of myopathy increases in the case of the use of lipid-lowering drugs, which are not potent inhibitors of the action of CYP3A4, but can provoke the appearance of myopathy in the case of monotherapy. Among them are gemfibrozil with other fibrates and lipid-lowering portions of niacin (> 1 g per day).

Verapamil with amiodarone can also increase the likelihood of myopathy; however, other Ca channel blocking agents do not have a similar effect.

The composition of grapefruit juice contains 1 or more elements that inhibit the effect of CYP3A4 and can increase the plasma level of drugs, which are metabolized with the participation of this substance. When drinking juice in a low dosage (1 glass with a volume of 0.25 liters per day) leads to a minimal effect (an increase in the activity of HMG-CoA reductase by 13%), which has no clinical significance. But when it is used in large portions (over 1 liter per day), the intraplasmic activity of drugs that slow down HMG-CoA reductase increases significantly. Because of this, while using simvastatin, you need to stop consuming large amounts of grapefruit juice.

In people using coumarin anticoagulants, it is necessary to determine the PTT value before starting therapy, and also regularly monitor it at the initial stage of treatment to make sure that there are no significant deviations in the new PTT values. After stabilization of this indicator, the new PTT values are checked at the frequency usually prescribed during therapy with the introduction of coumarin anticoagulants.

This procedure is repeated in case of cancellation of taking Simvatin or correction of its portion.

Storage conditions

Simvatin must be kept out of the reach of children. Temperature level - maximum 30 ° C.

Shelf life

Simvatin is used within a 3-year period from the date of manufacture of the medicinal substance.

Analogs

Analogues of drugs are the medicines Vasostat, Simvastatin with Vasilip, Zokor and Allesta.