Simvakor

Simvacor belongs to the subgroup of monocomponent drugs of the hypolipidemic type; the drug slows down the activity of one of the reductase subspecies. Its main active ingredient is simvastatin.

The introduction of simvastatin allows you to reduce the level of cholesterol, apolipoproteins and HDL, and in addition to reduce catabolism and the production of LDL-C. Along with this, the medication affects the indicators of the above elements inside the blood, changing the proportions of lipoproteins having different densities. [1]

Indications Simvakor

It is used in the case of dyslipidemia or hypercholesterolemia (as an addition to non-drug methods), as well as in the case of a familial form of homozygous hypercholesterolemia.

In addition, it can be prescribed to prevent the development of CVS diseases. Thanks to the use of drugs, the likelihood of death in people with CVS pathologies, diabetes mellitus and atherosclerosis decreases.

Release form

The release of a therapeutic substance is realized in tablets with a volume of 10 mg.

Pharmacodynamics

Simvastatin is an inactive lactione, a complex hydroxy acid ester capable of intrahepatic hydrolysis. As a result, a derivative is formed that has a slowing effect on the HMG-CoA reductase enzyme, which is capable of catalyzing the formation of mevalonate crystals from it, which are participants in the initial and most important stage of cholesterol formation processes.

Due to these properties, simvastatin can reduce not only increased, but also normal values of low-density cholesterol. [2]

This type of cholesterol can also be formed from cholesterol with a low level of density, and then catabolize, for the most part, with endings that have a noticeable similarity to LDL. [3]

Pharmacokinetics

Simvastatin has a high absorption rate. When using drugs, the active substance reaches the plasma level Cmax after 1.3-2.4 hours, with a subsequent decrease by 90% 12 hours after the first use. The active form of the drug inside the circulatory system is equal to 5% of the ingested portion. Protein synthesis - 95%.

The metabolic processes of Simvacor are realized inside the liver with the effect of the 1st intrahepatic passage (most of it is hydrolyzed to form the active form - β-hydroxy acids; in addition, other metabolic components are observed, both with and without therapeutic activity) and further excretion of the drug into the bile.

The term for the half-life of active metabolic elements is approximately 3 hours. The main part (60%) of the drug is excreted in the form of metabolic products with feces. Approximately 10-15% of the inactive substance is excreted through the kidneys.

Dosing and administration

The medication is taken orally, 1 time per day, before bedtime. The serving size is selected personally by the attending physician (dosage is in the range of 5-80 mg).

It is allowed to adjust the portion once a month.

The maximum allowable portion (80 mg) is administered only for severe disorders with increased blood cholesterol levels or at the risk of severe complications, as well as concomitant CVD diseases.

When using the medication, you can not reduce physical activity or stop the diet.

People with insufficient liver / kidney function do not need to change the dosage of drugs. If there is severe renal failure, use 10-20 mg of the drug.

• Application for children

You can not use the medicine in pediatrics.

Use Simvakor during pregnancy

Simvacor is prohibited from prescribing during pregnancy.

If you need to take drugs during hepatitis B, it is recommended to refuse feeding for the period of therapy.

Contraindications

The main contraindications:

• severe intolerance to the active or auxiliary elements of the drug;
• hepatic pathology;
• administration in combination with drugs that have a powerful inhibitory effect on CYP3A4 (ketoconazole with itraconazole, drugs that slow down HIV protease, posaconazole, etc.);
• combined use with cyclosporine, gemfibrozil or danazol.

Side effects Simvakor

The medication is often tolerated without complications. Sometimes manifestations of intolerance can be noted:

• depression, neuropathy, anemia, paresthesias, memory disorders and insomnia;
• bloating, vomiting, dyspepsia, pancreatitis, and nausea;
• insufficiency of hepatic function, jaundice;
• alopecia, rashes and itching;
• asthenia, myalgia and impotence;
• allergy symptoms in the form of arthritis, vasculitis, hot flashes, Quincke's edema, eosinophilia, urticaria and arthralgia;
• eating on an empty stomach can cause an increase in blood sugar levels;
• cognitive disorders.

Overdose

Poisoning with Simvacor is observed only occasionally. With the use of 3.6 g of the drug, there was no development of negative signs. In theory, a more pronounced drug overdose over a long time period can provoke a potentiation of side symptoms.

If violations occur, it is necessary to carry out gastric lavage and intake of enterosorbents.

Interactions with other drugs

Colestipol with cholestyramine reduces the bioavailability of the drug (you can start using it after 4 years from the end of the previous therapy; moreover, in this case, the development of addiction is observed).

Simvacor potentiates the medicinal activity of coumarin anticoagulants.

Administration in combination with immunosuppressants and fibric acid derivatives increases the likelihood of myopathy.

The drug potentiates the effect of indirect anticoagulants, which increases the risk of bleeding.

Antimycotics (itraconazole with ketoconazole), cytostatics, high dosage niacin, fibrates, erythromycin with immunosuppressants, protease inhibitors, and clarithromycin, when combined with medication, increase the likelihood of rhabdomyolysis.

The drug increases serum digoxin values.

Storage conditions

Simvakor must be stored at a temperature of no more than 25 ° C.

Shelf life

Simvacor is allowed to be used within an 18-month term from the date of manufacture of the therapeutic agent.

Analogs

The analogues of the medication are the drugs Vasilip, Simvastatin with Allesta, Zokor and Vasostat.