Product Type: Medicines
Active ingredients: simvastatin
Manufacturer: Zentiva K.S.
Country of Origin: Czech Republic Pharmacotherapeutic group: lipid-lowering agent - HMG-CoA reductase inhibitor
Packing: 28 tablets per pack
Storage Temperature: 2 ° C to 25 ° C
Keep away from children: Yes
The tablets, film-coated from white to almost white, are oblong, biconvex, with a notch on both sides and engraved with "SVT" and "40" on one side.
Hypolipidemic drug from the group of statins. Simvastatin is obtained synthetically from a fermentation product of Aspergillus terreus. It is an inactive lactone, in the body it undergoes hydrolysis with the formation of a hydroxy acid derivative. The active metabolite inhibits HMG-CoA reductase, an enzyme that catalyzes the initial formation of mevalonate from HMG-CoA. Since the conversion of HMG-CoA to mevalonate is an early stage in the synthesis of cholesterol, the use of simvastatin does not cause the accumulation of potentially toxic sterols in the body. HMG-CoA is easily metabolized to acetyl-CoA, which is involved in many synthesis processes in the body. It causes a decrease in plasma concentrations of TG, LDL, VLDL and total cholesterol (in cases of heterozygous familial and non-familial forms of hypercholesterolemia, with mixed hyperlipidemia, when high cholesterol is a risk factor). Increases HDL concentration and decreases the ratio of LDL / HDL and total cholesterol / HDL. The onset of the manifestation of the effect is 2 weeks after the start of administration, the maximum therapeutic effect is achieved after 4-6 weeks. The effect persists with continued treatment, with the cessation of therapy, the concentration of cholesterol gradually returns to its original level. Pharmacokinetics Absorption of simvastatin is high. After oral administration, the maximum plasma concentration is reached after about 1.3-2.4 hours and decreases by 90% after 12 hours. Communication with plasma proteins is about 95%. It is metabolized in the liver, has the effect of "first passage" through the liver (it is hydrolyzed to form an active derivative: beta-hydroxyacids, other active and inactive metabolites have been detected). The half-life of active metabolites is 1.9 hours. It is excreted mainly with feces (60%) in the form of metabolites. About 10-15% is excreted by the kidneys in an inactive form.
Hypersensitivity to simvastatin or to other components of the drug, as well as to other statin drugs (HMG-CoA reductase inhibitors) in history. Liver diseases in the active phase, a persistent increase in the activity of “liver” transaminases in blood plasma of unclear origin (more than 3 times in comparison with the upper limit of normal (AHP)). Concomitant treatment with potent inhibitors of the CYP3A4 isoenzyme (for example, itraconazole, voriconazole, ketopazole, posaconazole, HIV protease inhibitors, erythromycin, clarithromycin, telithromycin, nefazodone and drugs containing cobicistat) (see Interactions with Other Medicines) Special instructions"). Concomitant treatment with gemfibrozil, cyclosporine or danazole (see sections "Interaction with other medicines", "Special instructions"), Pregnancy or the period of breastfeeding. Age up to 18 years (with the exception of children and adolescents with heterozygous familial hypercholesterolemia) (see section "Indications for use"). Hereditary lactose intolerance, lactase deficiency, glucose-galactose malabsorption. WARNING: Use with caution in patients who abuse alcohol; patients after organ transplantation who are being treated with immunosuppressants (due to the increased risk of rhabdo myolysis and renal failure); in conditions that can lead to the development of severe renal failure, such as arterial hypotension, severe acute infectious diseases, severe metabolic and endocrine disorders, water-electrolyte imbalances, surgical interventions (including dental) or injuries; patients with reduced or increased tone of skeletal muscles of unknown etiology; while taking with fibrates, excluding gemfibrozil (see section "Contraindications), nicotinic acid in low-dose reducing doses (more than 1 g per day), colchicine, amiodarone, dronedarone, verapamil, amlodipine, diltiazem, fusidic acid, grapefruit; in severe renal failure (creatinine clearance (CC) less than 30 ml / min).