Instruction for use: Megestrol (Megestrolum)

Pharmacological group

Estrogens, gestagens; Their homologues and antagonists

Antineoplastic hormonal agents and hormone antagonists

Nosological classification (ICD-10)

C50 Malignant neoplasm of breast

Cancer of the nipple and areola of the breast, Breast carcinoma, The hormone-dependent form of recurrent breast cancer in women in menopause, Hormone-dependent breast cancer, Disseminated breast carcinoma, Disseminated Breast Cancer, Malignant breast cancer, Malignant neoplasm of breast, Contralateral breast cancer, Locally advanced or metastatic breast cancer,Locally-distributed breast cancer, Locally-recurring breast cancer, Metastatic breast carcinoma, Metastasis of breast tumors, Metastatic breast carcinoma, Inoperable breast carcinoma, Incompatible breast cancer, Breast cancer in women with metastases, Breast cancer in men with metastases, Breast Cancer, Breast cancer in men, Mammary cancer, Breast cancer with distant metastases, Breast cancer in postmenopausal women, Breast cancer hormone-dependent, Breast cancer with local metastases, Breast cancer with metastases, Breast cancer with regional metastases,Breast cancer with metastases, Common hormone-dependent forms of breast cancer, Common Breast Cancer, Recurrent Breast Cancer, Recurrence of breast tumors, Breast cancer, Estrogen-dependent breast cancer, Estrogen-Dependent Breast Cancer, Disseminated breast cancer with overexpression of HER2, Tumors of the mammary glands

C54.1 Malignant neoplasm of endometrium

Recurrent inoperable endometrial cancer, Endometrial cancer, Metastatic endometrial carcinoma, Metastatic Endometrial Cancer, Endometrial carcinoma, Recurrent carcinomas of the endometrium, Recurrent endometrial cancer

C56 Malignant neoplasm of ovary

Adenocarcinoma of the ovary psevdomutsinoznaya, Germinogenic swelling of the ovaries, Malignant ovarian tumor, Carcinoma of the ovary mucinous, Ovarian carcinoma, Metastatic malignant tumor of the ovaries, Metastatic ovarian carcinoma, Metastatic ovarian cancer, Metastatic ovarian cancer, Tumor of the ovaries, Cancer from the pseudomucinous cyst, Cancer of the ovary, Ovarian Cancer, Common metastatic ovarian cancer, Common Ovarian Cancer, Trophoblastic tumors, Chorionic carcinoma, Ovarian cystadenocarcinoma mucinous, Cystocarcinoma of the ovary pseudomucinou, Epithelial tumor of the ovaries

C61 Malignant neoplasm of prostate

Adenocarcinoma of the prostate, Hormone-dependent prostate cancer, Hormone-Resistant Prostate Cancer, Malignant tumor of prostate, Malignant neoplasm of prostate, Carcinoma of the prostate, Locally-distributed non-metastatic prostate cancer, Locally advanced prostate cancer, Locally spread prostate cancer, Metastatic prostatic carcinoma, Metastatic prostate cancer, Metastatic hormone-resistant prostate cancer, Non-metastatic prostate cancer, Incompatible prostate cancer, Prostate Cancer, Prostate cancer, Common prostate cancer, Testosterone-Depot Prostate Cancer

R63.0 Anorexia

Impairment of appetite, Anorexia in liver disease, Lack of appetite, Easing appetite, Appetite Disorders, Reduced appetite, Decreased appetite

R64 Cachexia

Cachexia for oncological diseases, Cachexia in incurable oncological patients

Code CAS 3562-63-8

Characteristics

Megestrol acetate is a white crystalline substance, solubility in water at 37 ° C 2 mg / ml, in plasma - 24 mg / ml. Molecular weight 384.52.

Pharmacology

The pharmacological action is gestagenic, antitumoral, antiecemetic.

The antitumor effect is due to local influence on the endometrium as progestational agents, the inhibition of pituitary gonadotropin secretion, suppression of the production of oestradiol and androstenedione adrenal steroid hormones modification effect, direct cytotoxic effect on hormone-sensitive tumor cells, releasing tumor blockade of growth factors. Efficacy in the metastatic process can occur only in tissues that have cytoplasmic hormonal receptors. In hormone-sensitive breast cancer, megestrol reduces the number of tumor cells, inhibits their activation by estrogens, or reducing the stability, availability and turnover estrogen receptor complexes or disabling through progestin receptor complexes specific genes (genomic level) responsible for estrogen effect. Anti-cancer properties may be realized by inhibition of cachectin and interleukin-1 factor formation or modification of their participation in intercellular interaction.

Quickly and completely absorbed from the digestive tract (gastrointestinal tract). The time to reach Cmax (averaging 750 ng / ml) is 2-3 hours. It circulates for a long time in the body (T1 / 2 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. When assigning kaheksichnym AIDS patients, 70% for 3 weeks showed an increase in body weight, and almost 90% - increased appetite (the effect was more pronounced at higher doses).

Application of Megestrol

Disseminated 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.

Contraindications

Hypersensitivity, as a means for the diagnosis of pregnancy, pregnancy (possible teratogenic effects when used during the first 4 months of pregnancy), lactation, age under 18 years old.

Restrictions for use

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).

Side effects

Bleeding from the vagina, fluid retention, thrombophilic state, weight gain, Itsenko - Cushing syndrome, abdominal pain in the chest, nausea, vomiting, constipation, dry mouth, hepatomegaly, cardiomyopathy, depression, paresthesias, cramps, dyspnea, cough, thromboembolism of small branches of the pulmonary arteries, increased blood pressure (blood pressure), carpal tunnel syndrome, alopecia, hyperglycaemia, pituitary-adrenal disorders, rash, metrorrhagia.

Routes of administration

Inside.

Precautions

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