Clinical and pharmacological group: & nbsp

Antineoplastic hormonal agents and hormone antagonists

"Estrogens, gestagens, their homologues and antagonists"

Included in the formulation
  • MEGEIS®
    pills inwards 
    VALEANT, LLC     Russia
  • АТХ:

    L.02.A.B.01   Megestrol

    L.02.A.B   Progestogens

    Pharmacodynamics:Antineoplasticth effect is due to local effects on the endometrium as a gestagenic agent, inhibition of gonadotropin secretion by the pituitary gland, suppression of estradiol and adrenostione production by the adrenal glands, modification of the effect of steroid hormones, direct cytotoxic effect on hormone-sensorytumor cells, blockade of tumor growth factors. Efficacy in the metastatic process can only occur in tissues that have cytoplasmichormone receptors. With hormonal-sensationBreast Cancer megestrol reduces the number of tumor cells, prevents their activation by estrogens, or decreases the stability, availability and turnover of estrogen receptor complexes, or by switching off specific genes (at the genome level) responsible for the effect of estrogens through progestin receptor complexes. Anti-smokingThese properties are probably realized by inhibition of the formation of cachectin and interleukin-1 or modification of their participation in intercellular interaction.
    Pharmacokinetics:Quickly and completely absorbed from the digestive tract. Time to reach Cmax (an average of 750 ng / ml) - 2-3 hours. Long circulates in the body (half-life is 2-3 days). A small amount is deposited in adipose tissue. Excretion from the body by 50-70% is carried out by the kidneys, by 30% - by the intestine, partially excreted through the respiratory tract.
    Indications:Disseminatedth breast cancer, recurrent inoperable endometrial cancer, ovarian cancer, prostate cancer (palliative treatment); anorexia, cachexia and significant (without obvious reasons) weight loss in AIDS patients, cachexia in incurable oncological patients.

    II.C50.C50   Malignant neoplasm of breast

    II.C51-C58.C54   Malignant neoplasm of uterine body

    Contraindications:Hypersensitivityas a means to diagnose pregnancy, pregnancy (possibly teratogenic effect when applied during the first 4 months of pregnancy), lactation period, age to 18 years.
    Carefully:Thrombophlebitis (in the anamnesis).
    Pregnancy and lactation:

    The action category for the fetus is FDA-D (tablets).

    The action category for the fetus is FDA-X (suspension). In the Russian Federation it is registered only in the medicinal form - tablets !!!

    Application in pregnancy and lactation is contraindicated.

    Dosing and Administration:Inside, once or in 2-4 doses. Disseminatedth breast cancer - the daily dose is 160 mg, endometrial cancer - 40-320 mg, anorexia and cachexia - 400-800 mg.
    Side effects:

    Increased body weight; thromboembolism: reported cases of thromboembolism, including thrombophlebitis and pulmonary embolism; Nausea, vomiting, swelling and blood discharge from the uterine cavity, not associated with menstruation, are noted in approximately 1-2% of patients; the presence of dyspnea, pain, heart failure, arterial hypertension, hot flashes, mood changes, Cushingoid features on the face, temporary activation of tumor development (in the absence or presence of hypercalcemia), hyperglycemia, alopecia, carpal tunnel syndrome, diarrhea, lethargy, skin rashes.

    It was reported on the development of pathological conditions associated with impaired functioning of the pituitary-adrenal system: glucose intolerance, the onset of diabetes mellitus and exacerbation of existing diabetes mellitus with a decrease in glucose tolerance and Cushing's syndrome.In rare cases, patients soon after the cessation of treatment with the drug observed clinical signs of adrenal insufficiency. It should be borne in mind the possibility of suppressing the function of the adrenal glands in all patients taking the drug for a long time, as well as after discontinuing the drug. In such cases, shock doses of glucocorticosteroids may be indicated as a substitution therapy.

    Overdose:

    In clinical trials, the drug was used in doses up to 1600 mg per day for 6 months or more. There were no acute toxic effects.

    In case of an overdose, treatment should be symptomatic.

    Interaction:

    Aminoglutethimide - decrease in the concentration of megestrol.

    Busulfan - increased risk of developing veno-occlusive disease.

    Doxorubicin, pegasgas - mutual enhancement of toxicity.

    Carbamazepine, griseofulvin, phenobarbital, phenytoin, rifampicin - increase in clearance of megestrol.

    Special instructions:

    Decide on the appointment of breast cancer should be after determining the receptor binding of estrogen and / or progesterone tumor cells.Before starting treatment for cachexia, a detailed examination should be conducted to determine the cause of weight loss.

    Megestrol is not a substitute for surgical treatment, chemotherapy or radiation therapy.

    Do not use as a test for pregnancy.

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