Apegestrol tablet is indicated for the palliative treatment of advanced carcinoma of the breast or endometrium (i.e., recurrent, inoperable or metastatic disease). It should not be used instead of currently accepted procedures such as surgery, radiation or chemotherapy. Apegestrol oral suspension is indicated for the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of Acquired Immunodeficiency Syndrome (AIDS) & cancer.
Megestrol Acetate is a synthetic, antineoplastic and progestational drug. While the precise mechanism by which Megestrol Acetate produces its antineoplastic effects against endometrial carcinoma is unknown at the present time, inhibition of pituitary gonadotrophin production and resultant decrease in estrogen secretion may be factors. The antineoplastic action of megestrol acetate on carcinoma of the breast is effected by modifying the action of other steroid hormones and by exerting a direct cytotoxic effect on tumor cells. In metastatic cancer, hormone receptors may be present in some tissues but not others. The receptor mechanism is a cyclic process whereby estrogen produced by the ovaries enters the target cell, forms a complex with cytoplasmic receptor and is transported into the cell nucleus. There it induces gene transcription and leads to the alteration of normal cell functions. Pharmacologic doses of megestrol acetate not only decrease the number of hormone-dependent human breast cancer cells but also are capable of modifying and abolishing the stimulatory effects of estrogen on these cells. Estimates of plasma levels of Megestrol Acetate are dependent on the measurement method used. Peak plasma concentrations occur 2 to 3 hours after a single oral dose 160 mg tablets. The plasma half-life of Megestrol Acetate is 33 to 38 hours. Approximately 66% of an administered dose is excreted in the urine and approximately 20% in the faeces.
Always consult a registered doctor before taking any medicine. This information is for general knowledge only.
Tablet : Breast cancer: 160 mg/day Endometrial carcinoma: 40-320 mg/day in divided doses. At least 2 months of continuous treatment is considered an adequate period for determining the efficacy of Megestrol. Oral Suspension : The recommended adult initial dosage of Megestrol Oral Suspension is 800 mg/day (20 ml/day).
Weight gain is a frequent side effect of Apegestrol when it is used in patients with cancer of the breast or endometrium. This gain is associated with increased appetite. It is this effect which forms the basis for use of Apegestrol in patients with anorexia, cachexia or weight loss. Weight gain is associated with an increase in fat and body cell mass. Untoward reactions that have been reported to occur in patients receiving Apegestrol include nausea, vomiting, edema and breakthrough uterine bleeding and occur in approximately 1% to 2% of patients. Gynecomastia and loss of hearing have also been reported. Dyspnea, heart failure, hypertension, hot flashes, mood changes, Cushingoid facies, tumor flare (with or without hypercalcemia), hyperglycemia, alopecia, carpal tunnel syndrome and rash have also occurred. Thromboembolic phenomenon including thrombophlebitis and pulmonary embolism (in some cases fatal) have also been reported.
History of hypersensitivity to Megestrol Acetate or any component of the formulation. Known or suspected pregnancy.
With medicine : Possible interactions of Apegestrol with concomitant medications have not been investigated. With food and others : Estrogens and Progestogens may cause fluid retention, particularly when given in high dosages or for prolonged periods. Therapy with these agents should be administered cautiously in patients who have preexisting problems with excess fluid.
Apegestrol should be used with caution in patients with a history of thrombophlebitis and in patients with severe impaired liver function. Apegestrol should be used under the supervision of a specialist and the patients kept under regular surveillance. Apegestrol can exert adrenocortical effects. This should be borne in mind in patient surveillance. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. Insufficient data from clinical studies of megesterol acetate are available for patients 65 years of age and older to determine whether they respond differently than younger patients. Other reported clinical experience has not identified differences in responses between elderly and younger patients. In general, use in elderly patients should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Apegestrol is known to be substantially excreted by the kidney, and the risk of toxic reactions to Apegestrol may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken during treatment with Apegestrol, and it may be useful to monitor renal function.