Simvalimit

Simvalimit is a medication from the subgroup of monocomponent drugs with lipid-lowering activity; it slows down one of the reductase subtypes. The main active ingredient is simvastatin.

The administration of the drug helps to reduce the level of cholesterol with HDL and apolipoproteins, and besides, it weakens catabolism and the production of cholesterol-LDL, at the same time affecting the levels of these components inside the blood, changing the proportions of lipoproteins having different densities. [1]

Indications Simvalimit

It is used for hereditary forms of primary hypercholesterolemia of the homo- or heterozygous type, and in addition for the combined form of hyperlipidemia, which cannot be corrected by diet or other non-drug methods.

It is prescribed for coronary heart disease with symptoms of hypercholesterolemia to reduce the likelihood of coronary death, myocardial infarction (without fatal outcome), stroke and risks during the procedure of myocardial revascularization, and in addition to slow down the progression of coronary atherosclerosis.

Release form

The release of drugs is made in the form of tablets - 10 pieces inside a cell pack; inside the box - 3 such packs.

Pharmacodynamics

Simvastatin is a substance that regulates lipid levels. It is included in the subgroup of elements that slow down the HMG-CoA reductase (they are also called statins). The blockade of HMG-CoA reductase activity leads to a slowdown in the transformation of HMG CoA into mevalonic acid (a precursor of cholesterol; cholesterol binding processes are mostly realized inside the liver).

Inside the plasma, statins reduce the level of total cholesterol, as well as LDL-C and VLDL-C. At the same time, they can decrease triglyceride values and slightly increase HDL-C. In this case, the hypolipidemic effect of drugs from this category is realized using another mechanism. [2]

A decrease in intracellular cholesterol reserves inside the hepatocyte wall leads to a compensatory increase in the number of endings to LDL, and also promotes the excretion of LDL from the blood. [3]

Pharmacokinetics

Simvastatin is absorbed inside the gastrointestinal tract and, after hydrolysis processes, is transformed into an active element - β-hydroxy acid. Other metabolic products (with and without activity) are also allocated. The drug reaches plasma values of Cmax over a period of 1.3-2.4 hours.

Simvastatin has intensive metabolic processes in the 1st intrahepatic passage. Less than 5% of an orally administered portion penetrates into the circulation in the form of active metabolic components. Protein synthesis of simvastatin with β-hydroxy acid is 95%.

The drug enters the gastrointestinal tract in the form of metabolic products along with bile; excreted for the most part in the feces. About 10-15% of the dosage is excreted in the urine (most of it is in the form of metabolites that have no activity). The half-life of active metabolic elements is 1.9 hours.

Dosing and administration

Before using the medication, the patient should begin to follow a standard diet with low cholesterol levels (the regimen must be adhered to throughout the treatment cycle). It is necessary to use the drug in the evening - before dinner or with it.

Application to persons with a combined type of hyperlipidemia, a primary form of hypercholesterolemia, as well as hereditary hypercholesterolemia of a heterozygous nature.

Consume 10 mg of the substance once a day (in the evening). Correction of portions is performed at least once a month. A day can be used within 10-80 mg of the drug. Do not exceed the daily dosage of 80 mg.

Hereditary form of homozygous hypercholesterolemia.

Consume 1 time per day (in the evening) at 40 mg, or use a regimen with the intake of 80 mg, divided into 3 injections (in the morning and afternoon - 20 mg, and the remaining 40 mg - in the evening).

Introduction for ischemic heart disease.

First, you need to take 1 time per day, in the evening, 20 mg each. Then the portion is changed (at least once a month). For a day (in 1 dose), you can use no more than 80 mg.

In the case of combined use with fibrates, cyclosporine or niacin, which is used in the form of a lipid-lowering substance, Simvalimit can be taken in a portion of no more than 10 mg per day.

Lack of kidney function.

In a severe stage of violation (CC level <30 ml per minute), the initial dosage is 5 mg per day. These patients need to be closely monitored. They consume no more than 10 mg of drugs per day.

• Application for children

Use in pediatrics is prohibited because there is no reliable information regarding drug exposure and safety.

Use Simvalimit during pregnancy

Cholesterol, along with other intermediate binding elements, are components that are necessary for the development of the fetus (among other things, for the binding of cell walls and steroids). Due to the fact that statins slow down the binding of cholesterol and other bioactive cholesterol derivatives, if administered to pregnant women, they can provoke fetal development disorders. Therefore, statins are not used during pregnancy.

Statin therapy in women of childbearing age requires the use of contraception during the treatment period and for 1 month after its completion. In case of pregnancy during therapy, it is necessary to stop taking drugs.

Simvalimit is prohibited for use while breastfeeding. If there is a vital need to use the medication, it is necessary to abandon GV for the duration of therapy.

Contraindications

Among the contraindications:

• severe intolerance associated with simvastatin or other elements of the drug;
• an active form of hepatic pathology or an increase in the activity of intra-serum aminotransferases (of an unknown nature);
• porphyria.

Side effects Simvalimit

Often, among the side symptoms of the drug, disorders of the gastrointestinal tract are noted: abdominal pain, vomiting, bloating, diarrhea or constipation and nausea.

Sometimes it is possible to develop rashes, blurred vision, dizziness, dysgeusia, headaches and insomnia.

Occasionally, there is a negative effect on the muscles and liver. An increase in the activity of serum aminotransferases is possible.

There is information about the appearance of hepatitis, jaundice or pancreatitis, as well as intolerance syndrome with the occurrence of Quincke's edema.

Myopathy may develop, which manifests itself in the form of myositis, myalgia and muscle weakness, together with a simultaneous increase in CPK activity, especially in people using simvastatin in combination with fibrates, erythromycin, immunosuppressants, niacin and itraconazole.

The appearance of polyneuropathy and paresthesias is possible.

There is evidence of the development of secondary renal failure and rhabdomyolysis.

Overdose

There are isolated situations with Simvalimit poisoning, but no specific signs were found; the condition of patients has always stabilized after symptomatic procedures.

In case of an overdose, standard actions are performed (induction of vomiting, taking activated carbon, monitoring the work of important organs). In addition, kidney / liver function and serum creatine kinase values should be monitored.

Interactions with other drugs

Grapefruit juice increases the plasma levels of simvastatin.

Antibiotics erythromycin with clarithromycin, nefazodone, which is an antidepressant, antimycotics ketoconazole with itraconazole and other derivatives of triazole with imidazole, cyclosporine (immunosuppressant), antiviral drugs (slowing down the action of viral proteases) and other substances that can decrease the rate of phibracin the appearance of myopathy.

The combination of statins with anticoagulants, which are derivatives of oxycoumarin (for example, warfarin with acenocoumarol), can provoke an increase in the likelihood of bleeding and PTT.

The combination of Simvalimit with coumarin anticoagulants (for example, warfarin or acenocoumarol) or changing the portion of simvastatin requires constant monitoring of the PTV level before starting treatment and during the treatment cycle. Upon reaching stable values, then it is monitored at intervals that are prescribed to persons taking anticoagulants.

The use of the medication together with digoxin can lead to an increase in the plasma level of the latter, which can cause vomiting, nausea and arrhythmia.

Storage conditions

Simvalimite should be kept in a dark place, protected from moisture and small children. Temperature level - no more than 25 ° С.

Shelf life

Simvalimit can be used for 24 months from the date of manufacture of the medicinal product.

Analogs

Analogues of drugs are the substances Simvor, Simgal with Simvastatin, Simvastol and Vasilip with Ovenkor, and in addition Simvagexal, Zokor and Aktalipid.