Simvastatin

When ATH:
C10AA01

Characteristic.

White or off-white crystalline powder. Practically insoluble in water, very soluble in chloroform, methanol and ethanol.

Pharmacological action.
Hypocholesteremic.

Application.

Hypercholesterolemia in the absence of effect of diet, Combined hypercholesterolemia and triglyceridemia, CHD, prevention of myocardial infarction and stroke, atherosclerosis.

Contraindications.

Hypersensitivity, acute liver dysfunction, severe renal insufficiency, pregnancy, lactation, childhood.

Pregnancy and breast-feeding.

Category actions result in FDA - X. (Animal tests or clinical trials revealed a violation of the fetus and / or there is evidence of the risk of adverse effects on the human fetus, obtained in research or practice; risk, associated with the use of drugs in pregnancy, greater than the potential benefits.)

Side effects.

Dyspepsia, diarrhea, flatulence, nausea, exacerbation of pancreatitis and hepatitis, transaminase elevation, CNS disorders (headache, paresthesia, convulsions), myalgia, asthenia, myopathy, raʙdomioliz, photosensitivity, allergic reactions (vasculitis, hives, artralgii, thrombocytopenia, eozinofilija, angioedema, symptoms, similar to lupus erythematosus).

Cooperation.

Immunodepressivnaya therapy, high doses of nicotinic acid, antifungals - azole derivatives (ketoconazole, itraconazole) increase the risk of myopathy and rhabdomyolysis. Proximity effect anticoagulants, hepatotoxicity of alcohol and drugs, adverse effects on the liver.

Dosing and Administration.

Inside: in the early course of a single dose of 5-10 mg / day, optionally up 40 mg per day depending on the content of cholesterol and lipoproteins in the blood. In CHD initial dose 20 mg / day one.

Precautions.

Before and during treatment is recommended to monitor liver function and caution is prescribed for her violations.

Cooperation

Active substanceDescription of interaction
WarfarinFMR: synergism. Against the background of enhanced effect of simvastatin.
VerapamilFMR. It may increase the risk of myopathy.
DigoxinFKV. Against the backdrop of increased simvastatin (insignificantly) level in plasma.
Indinavir sulfateFKV. FMR. Slows biotransformation (It competes for CYP450), may increase the plasma levels and increases the risk of myopathy and rhabdomyolysis.
KetoconazoleFMR: synergism. Slows biotransformation, increases plasma levels and may increase the risk of myopathy and rhabdomyolysis.
ClarithromycinFKV. FMR. Reduces the activity of CYP450, slows the biotransformation, It increases the concentration in the blood and may increase the risk of myopathy and rhabdomyolysis (reported several cases).
MikonazolFKV. FMR. Slows biotransformation (It competes for CYP450), increases plasma levels and increases the risk of myopathy and rhabdomyolysis.
NelfinavirFKV. FMR. Slows biotransformation (It competes for CYP450), may increase the plasma levels and increases the risk of myopathy and rhabdomyolysis.
A nicotinic acidFMR: synergism. In high doses increases the risk of myopathy and rhabdomyolysis.
RitonavirFKV. FMR. Slows biotransformation (It competes for CYP450), may increase the plasma levels and increases the risk of myopathy and rhabdomyolysis.
SaquinavirFKV. FMR. Slows biotransformation (It competes for CYP450), may increase the plasma levels and increases the risk of myopathy and rhabdomyolysis.
FenofibrateFMR: synergism. Increases (mutually) the likelihood of rhabdomyolysis and acute renal failure; assigning the combined simvastatin dose should not exceed 10 mg / day.
CyclosporineFKV. FMR.

Slows biotransformation (competes for cytochrome P450-dependent monoksigenazy), may increase the plasma levels and increase the risk of myopathy and rhabdomyolysis; in combination therapy of simvastatin dose should not exceed 10 mg / day.

EthanolFMR. Against the background of simvastatin amplified negative effect on the liver; at the time of treatment should abandon the use of alcoholic beverages.

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