Treatment of anorexia or loss of weight due to cancer or acquired immune deficiency syndrome (AIDS).
Composition:
1 ml of suspension contains 40 mg of micestrol acetate in micronized form (and 300 ml of liquid maltitol).
Action:
Megestrol acetate is a synthetic steroid with strong progestational, antiestrogenic and anti-gonadotropic properties. The mechanism of antineoplastic activity of megestrol acetate in breast cancer and the mechanism of action in anorexia and cachexia is not fully understood and may consist in suppression of gonadotropin production by the pituitary gland. Weight gain after treatment with megestrol acetate is associated with improved appetite, increased fat and muscle mass. The concentration of the active substance depends on the intestinal process and hepatic inactivation of the drug, which may be influenced by: intestinal motility, intestinal bacterial flora, simultaneous administration of antibiotics, body weight, diet and liver function. Metabolites account for about 5-8% of the administered dose of megestrol acetate. The drug is mainly excreted by the kidneys (about 66%) and with faeces (about 20% of the administered dose). The remaining part of the administered dose, which is not eliminated in urine or faeces, can be excreted through the respiratory system and accumulated in adipose tissue. There are no changes in the pharmacokinetic parameters of megestrol acetate (oral suspension) when zidovudine and rifabutin are co-administered.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Pregnancy and breastfeeding.
Precautions:
The preparation should be used with caution in patients with a history of thrombophlebitis and in patients with diabetes (possibility of an increased need for insulin). During therapy or after discontinuation of megestrol acetate, clinical and laboratory symptoms of mild adrenal suppression have been reported. In the event of a sudden discontinuation of the drug should be carefully observed patient, especially in the direction of such symptoms as: hypotension, nausea, vomiting, dizziness, weakness. The safety and efficacy of the preparation in children and adolescents has not yet been established. The product contains maltitol - should not be used in patients with rare hereditary problems of fructose intolerance. A study in dogs showed that the use of the drug was associated with an increased risk of benign and malignant breast tumors (studies in rats and monkeys showed no increased risk). It is not known to what extent the results of tests carried out on dogs can be referred to humans. However, when assessing the benefit / side effects, they should be taken into account when recommending megasterol acetate and a breast examination should be performed to control patients during treatment.
Pregnancy and lactation:
The drug should not be given to pregnant women. Before starting treatment, the attending physician should be informed about the patient's existing or planned pregnancy. Numerous reports suggest the possibility of a potentially damaging effect of this group's drugs on the fetus when used in the first 4 months of pregnancy. During the use of the drug, patients should be advised to use effective methods to prevent pregnancy. Due to the lack of controlled examinations for breast-feeding women, the patient should not breast-feed during the use of the drug. Animal reproduction studies have shown a transient, feminizing effect on some fetuses of male rats. The use of progestagens in women with a damaged fetus may delay spontaneous abortion, which is associated with the diastolic effects of these drugs on the uterus. There have been reports suggesting a relationship between intrauterine exposure to progestogens in the first trimester of pregnancy and ureteral organs abnormalities in male and female fetuses. The risk of hypospadias, in the general population of 5 to 8 per 1000 boys, can be doubled after exposure to these drugs.There is insufficient data to assess the risk associated with exposure to progestogens of female fetuses, but some of these drugs may cause mild virilization of the external genital organs. If the drug is used in the first 4 months of pregnancy or if a woman becomes pregnant while taking the medicine, it should be informed of the potential risk to the fetus.
Side effects:
Common: nausea, vomiting, diarrhea, bloating, rash, uterine bleeding, impotence, weakness, pain, edema. Frequency unknown: rapid tumor mass growth, adrenal insufficiency, Cushing-like symptoms, Cushing's syndrome, mood changes, lethargy, circulatory failure, thrombophlebitis, pulmonary embolism (sometimes fatal), hypertension, hot flushes, dyspnea, constipation , baldness, carpal tunnel syndrome, pollakiuria, weight gain. Constipation and frequent urination were reported in patients who received megestrol acetate in high doses. There have been reports of pituitary-adrenal axis disturbances associated with the use of megestrol acetate manifested by Glucose intolerance, freshly detected diabetes, exacerbation of previously diagnosed diabetes with a reduction in glucose tolerance and Cushing's syndrome. Occasional clinical adrenal insufficiency has been reported sporadically shortly after discontinuation of megestrol acetate therapy. The possibility of adrenal insufficiency should be considered in all patients treated with or interrupting chronic megestrol acetate therapy. It may be advisable to administer appropriate doses of glucocorticoids.
Dosage:
Orally. Adults: 400-800 mg in a single daily dose. It is recommended to continue treatment for at least 2 months.Special groups of patients. There is not enough data on clinical trials of megestrol acetate in patients aged 65 years and older to determine if it works differently than in younger patients. Based on clinical experience, there were no differences in its effect between elderly patients and younger patients. Careful dose selection in the elderly is recommended. Due to the more frequent abnormalities of liver, kidney or heart function, as well as co-morbidities and the use of other medications, treatment is usually initiated at doses from the lower end of the dosage range. The risk of toxic effects of the drug may be higher in patients with impaired renal function. Because elderly patients are more likely to experience deterioration of their renal function, caution should be used when setting the dose and monitoring of renal function may be useful. There are no data from clinical trials on the use of the preparation in children.Way of giving. Before serving, the suspension should be mixed thoroughly.
(C)
