When administered simvastatin is well absorbed in the gastrointestinal tract (an average of 85% of the dose). In the liver biotransformation process proceeds simvastatin in which the inactive form is hydrolyzed in a pharmacologically active beta gidroksimetabolity. 95% of them is bound to plasma proteins. Maximum plasma concentration is reached after 4 hours after ingestion of the drug. The unabsorbed simvastatin and its metabolites are excreted mainly in the bile (60%), about 10-15% of the inactive form of metabolites excreted by the kidneys. Acceptance of the drug immediately before a meal with a low-fat diet has no effect on the pharmacokinetics of simvastatin.
- with primary hypercholesterolemia, masterone when poor diet;
- with combined hypercholesterolemia and hypertriglyceridemia.
- Hypersensitivity to Simla, or to one of the components of the drug;
- Hypersensitivity to other statin drugs series (inhibitors reductase) in history;
- liver disease in active phase;
- persistent elevation of liver transaminases in blood serum;
- Pregnancy and lactation;
- age up to 17 years.
Simla should be used with extreme caution in the following cases:
- patients who abuse alcohol and / or have a history of liver disease;
- after organ transplantation patients undergoing immunosuppressive therapy in connection with an increased risk of rhabdomyolysis and renal failure;
- in conditions that can lead to severe renal insufficiency, such as hypotension, acute infectious diseases heavy currents expressed metabolic and endocrine disorders, disorders of water and electrolyte balance, surgery (including dental), or injury;
- patients with low or high tone of the skeletal muscles of unknown etiology;
Throughout the course of therapy with the masterone following indicators should systematically monitor:
- cholesterol concentration in the plasma after 4 weeks of treatment, and then regularly at certain intervals;
- liver function tests, which determine the pre-treatment and further preparation according to the scheme in the first three months of treatment with an interval of 6 weeks, and then approximately every six months.
In cases where there is a persistent three-fold compared with baseline levels, elevated liver transaminases, drug treatment should be discontinued .
- necessary to control the level of creatine in the blood plasma in patients taking immunosuppressants, or Simla and niacin, as well as in case of occurrence of myopathy (myalgia, muscle weakness). An increase in level in more than 10 times the normal recommended cancellation of Simla.
Dosing and Administration
The drug is taken once a day, in the evening, before a meal or during a meal.
The therapeutic effect of Simla occurs in about 2 weeks.
The dosage and duration of treatment are determined individually by your doctor.
Depending on the severity of hypercholesterolemia starting dose is 5 mg per day. In severe hypercholesterolemia – 10 mg 1 time per day in the evening. When the dose is necessary to increase an interval of 4 weeks.
The maximum daily dose -. 40 mg dosage on the background of immunosuppressive therapy is recommended starting dose of 5 mg per day, the maximum daily dose is 5 mg per day. Dosage in Renal Impairment No dosage adjustment in the presence of light and moderate renal failure severity is not required, since the allocation of kidneys Simla slightly. in severe renal insufficiency treatment starts with a dose of 5 mg per day. It should be carefully monitored for this category of patients throughout the treatment period Simla.
Interaction with other drugs
When Simla combination with immunosuppressants masterone (cyclosporine), erythromycin, gemfibrozil or nicotinic acid increases risk of rhabdomyolysis and acute renal failure.
Co-administration with indirect anticoagulants may potentiate the effect of the latter.
Cholestyramine reduces the bioavailability of simvastatin. Recommended intake Simla 4 hours after taking cholestyramine.
Simla increases the concentration of digoxin in the blood plasma.