Simvacor

Simvacor is a subgroup of monocomponent hypolipidemic medications; the drug slows down the activity of one of the reductase subtypes. Its main active ingredient is simvastatin.

The introduction of simvastatin allows to reduce the level of cholesterol, apolipoproteins and HDL, and also to reduce the catabolism and production of LDL-C. At the same time, the drug affects the levels of the above elements in the blood, changing the proportions of lipoproteins with different densities. [ 1 ]

Indications Simvacor

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

In addition, it can be prescribed to prevent the development of cardiovascular diseases. Thanks to the use of drugs, the likelihood of a fatal outcome in people with cardiovascular pathologies, diabetes mellitus and atherosclerosis is reduced.

Release form

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

Pharmacodynamics

Simvastatin is an inactive lactone, a hydroxy acid ester capable of intrahepatic hydrolysis. As a result, a derivative is formed that has a retarding effect on the enzyme HMG-CoA reductase, 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 elevated but also normal values of low-density lipoprotein cholesterol. [ 2 ]

This type of cholesterol can also be formed from low-density cholesterol and then catabolized, mostly with endings that have a noticeable similarity to LDL. [ 3 ]

Pharmacokinetics

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

Metabolic processes of Simvacor are realized inside the liver with the effect of the first intrahepatic passage (the majority is hydrolyzed with the formation of the active form - β-hydroxy acid; in addition, other metabolic components are observed, both with and without therapeutic activity) and further excretion of the drug into the bile.

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

Dosing and administration

The medication is taken orally, once a day, before bedtime. The portion size is selected by the attending physician (dosage within 5-80 mg).

The portion can be adjusted once a month.

The maximum permissible dose (80 mg) is administered only in severe cases of the disorder with increased blood cholesterol levels or with the risk of severe complications, as well as concomitant cardiovascular diseases.

When using the medicine, you should not reduce physical activity or stop your diet.

People with liver/kidney failure do not need to change the dosage of the drug. If renal failure is observed in a severe form, 10-20 mg of the drug is used.

• Application for children

The medicine cannot be used in pediatrics.

Use Simvacor during pregnancy

Simvacor is contraindicated during pregnancy.

If you need to take medications while breastfeeding, it is recommended to stop breastfeeding during the therapy period.

Contraindications

Main contraindications:

• severe intolerance to the active substance or auxiliary elements of the drug;
• liver pathologies;
• administration in combination with drugs that have a strong inhibitory effect on CYP3A4 (ketoconazole with itraconazole, drugs that inhibit HIV protease, posaconazole, etc.);
• combined use with cyclosporine, gemfibrozil or danazol.

Side effects Simvacor

Often the medication is tolerated without complications. Sometimes intolerance may occur:

• depression, neuropathy, anemia, paresthesia, memory disorders and insomnia;
• bloating, vomiting, dyspepsia, pancreatitis and nausea;
• liver failure, 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;
• consumption on an empty stomach may cause an increase in blood sugar levels;
• cognitive disorders.

Overdose

Poisoning with Simvacor is observed only once. When using 3.6 g of the drug, no negative symptoms were observed. In theory, a more pronounced overdose of the drug over a long period of time can provoke a potentiation of side effects.

If any disturbances occur, gastric lavage and enterosorbents should be performed.

Interactions with other drugs

Colestipol with colestyramine reduces the bioavailability of the drug (it can be used after 4 years from the end of the previous therapy; in addition, in this case, addiction develops).

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.

Antifungal agents (itraconazole with ketoconazole), cytostatics, niacin in high doses, fibrates, erythromycin with immunosuppressants, protease inhibitors, and clarithromycin when combined with the drug increase the likelihood of rhabdomyolysis.

The drug increases serum digoxin levels.

Storage conditions

Simvacor should be stored at a temperature of no more than 25°C.

Shelf life

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

Analogues

Analogues of the drug are the drugs Vasilip, Simvastatin with Allesta, Zocor and Vasostat.