Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):ONLS
Pharmacodynamics:Suppresses the synthesis of mineralocorticoids and glucocorticoids, inhibiting the conversion of cholesterol to predninolone in the adrenal cortex. Causes the compensatory release of ACTH by the pituitary gland. Reduced synthesis of T4, and hypersecretion of thyroid-stimulating hormone begins. Due to the blockade of aromatase, peripheral tissues inhibit the conversion of androgens to estrogens.
Pharmacokinetics:Fast and complete absorption. Low connection with blood proteins: up to 25%. The concentration in the blood cells is 1.5 times greater than in the plasma. Metabolism in the liver: by induction and oxidation, inactive metabolites are formed. The half-life is 13 hours.
The maximum concentration after oral administration in an amount of 500 mg occurs in 1-2 hours. Elimination with feces (5%) and kidneys (95%). Completely removed by hemodialysis.
Indications:It is used for breast cancer (including metastases) during the menopause, as well as for prostate cancer.
Contraindications:Porphyria, liver dysfunction.
Individual intolerance.
Carefully:They are used with caution for the elderly, due to the increased danger of a toxic effect on the central nervous system.
Care should be taken when prescribing to persons with acute viral diseases (chicken pox, herpes, influenza), patients with hypothyroidism.
In the first days of treatment, patients should refuse to drive vehicles and work with moving mechanisms.
Pregnancy and lactation:Pregnancy and lactation: recommendations for FDA - category D. Absolute contraindications.
Dosing and Administration:The dosage regimen is selected individually, depending on the stage of the process, according to the standard therapy regimen taking into account the indications.
The drug is taken orally during a meal.
The highest daily dose is 2 g.
The highest single dose is 500 mg.
Side effects:The severity of side effects decreases after 2-6 weeks, due to the acceleration of the metabolism of the drug.
Central nervous system: impaired coordination, inhibition, drowsiness.
Blood system: agranulocytosis, leukopenia, thrombocytopenia.
Cardiovascular system: orthostatic or permanent hypotension due to suppression of aldosterone synthesis.
Respiratory system: the formation of infiltrates in the lung tissue, alveolitis, dyspnea.
Gastrointestinal tract: diarrhea, nausea, cholestasis.
Skin: koprepodobnye rashes on the palms and on the face.
Allergic reactions.
Overdose:Hypotension, inhibition, respiratory depression, hypovolemic shock, coma.
Treatment: gastric lavage, hemodialysis.
Interaction:It is taken with meals.
When treating aminogutetimide, women should stop taking hormonal contraceptives.
Reduces the effectiveness of coumarin anticoagulants, hypoglycemic drugs, prednisolone, theophylline. For the purpose of correcting the level of glucocorticoids, hydrocortisone.
Taking diuretics increases the risk of hyponatremia.
Increases the inhibition of the central nervous system when taking antidepressants, neuroleptics, MAO inhibitors, antihistamines, local and general anesthetics, as well as with alcohol.
Special instructions:When taking the drug should be a constant monitoring of peripheral blood (4-8-12 weeks), monitor the blood levels of ions of potassium, sodium, chlorine.
When treating prostate cancer, determine the activity of alkaline phosphatase - with a positive effect of treatment, the concentration decreases.
The treatment scheme is developed by specialists in endocrine therapy of malignant tumors.
During an acute stressful condition (shock, trauma), the use of aminoglutethimide is canceled.
In treatment, hormone replacement therapy with hydrocortisone is prescribed. At the end of taking aminoglutethimide, hydrocortisone is withdrawn without a gradual dose reduction, as the adrenal glands begin to function.