Elevated total and LDL cholesterol levels in patients with primary hypercholesterolemia, in which nonpharmacologic therapies were ineffective.
Composition:
1 tabl powl. contains 10 mg or 20 mg Simvastatin (and 30.85 mg or 61.69 mg lactose).
Action:
HMG-CoA reductase inhibitor. The mechanism of action of the drug is to reduce hepatic cholesterol biosynthesis by competitive and reversible inhibition of HMG-CoA reductase, the enzyme responsible for the initial stage of cholesterol biosynthesis - the conversion of HMG-CoA to mevalonic acid. Reduction in cholesterol biosynthesis results in the activation of hepatic (and other) LDL receptors, leading to increased catabolism of LDL cholesterol. It also moderately reduces triglycerides and increases HDL-C levels. The effect of the drug on the concentration of lipids is observed after 2 weeks of use, the maximum effect of action after 4-6 weeks. The preparation is an inactive prodrug. The drug is well absorbed from the digestive tract. A significant uptake is in the liver (first-pass effect). The maximum concentration of the active form is reached after about 1-2h after administration. Simvastatin and its active metabolites bind to proteins in over 95%. About 13% is excreted in the urine and about 60% in the faeces.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Active liver disease or persistent, unexplained elevation of blood transaminases. Concomitant administration of potent CYP3A4 inhibitors such as Itraconazole, ketoconazole, HIV protease inhibitors, Erythromycin, Clarithromycin, telithromycin and nefazodone. Pregnancy. Breastfeeding period.
Precautions:
Caution in patients with predisposing factors for rhabdomyolysis (creatine kinase activity should be determined before starting treatment in the following cases: older age (> 70 years), renal dysfunction, refractory or untreated hypothyroidism, individual or family history of hereditary disorders on the part of the muscular system, patients who have had muscle fibrates toxic in the past, addiction to alcohol). The indications for discontinuation of treatment are: diagnosis or suspicion of myopathy, finding increased creatine kinase (5-fold compared to the norm), increase in transaminases in the blood (3-fold compared to the norm) or the presence of predisposing factors for the development of renal failure caused by rhabdomyolysis . Treatment with simvastatin should be discontinued a few days before the planned major surgery or if it is necessary to undergo internist or surgical treatment. Use with caution in patients with a history of liver disease and in people who abuse alcohol. The preparation contains lactose, patients with rare hereditary lactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose, should not take the drug.
Pregnancy and lactation:
Do not use in pregnant women, those planning pregnancy or those who are suspected of being pregnant, as mother's treatment with simvastatin may reduce the fetus concentration of mevalonate, which is a precursor to cholesterol biosynthesis. It is not known whether simvastatin or its metabolites are excreted in human milk - do not use during breast-feeding due to the possibility of serious side effects in the infant.
Side effects:
Rare: anemia, headache, paresthesia, dizziness, peripheral neuropathy, constipation, abdominal pain, flatulence, indigestion, diarrhea, nausea, vomiting, pancreatitis, hepatitis, jaundice, rash, pruritus, alopecia, myopathy, rhabdomyolysis , muscle pain, muscle spasms, weakness, symptoms of hypersensitivity syndrome (angioneurotic edema, lupus-like syndrome, rheumatoid type muscle pain, dermatomyositis, vasculitis, thrombocytopenia, eosinophilia, accelerated OB, arthritis, arthralgia, urticaria, hypersensitivity to light , fever, redness, difficulty in breathing, feeling unwell),increase in transaminases (ALT, AST, GGT), increase in ALP, increase in CK activity in the blood.
Dosage:
Orally. Initially 10 mg once a day in the evening; the dose can be gradually increased, at 4-week intervals, up to a maximum dose of 40 mg daily in the evening. The patient should use a standard low-cholesterol diet, which should be continued during treatment. The drug is not recommended in children and adolescents.
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