Apegestrol160 mg

Megestrol 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.Megestrol oral suspension ... Read moreMegestrol 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.Megestrol 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.

Hormonal Chemotherapy

Apegestrol 160 mg is a synthetic, antineoplastic and progestational drug. While the precise mechanism by which Apegestrol 160 mg 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 Apegestrol 160 mg 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 Apegestrol 160 mg 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 Apegestrol 160 mg 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 Apegestrol 160 mg is 33 to 38 hours. Approximately 66% of an administered dose is excreted in the urine and approximately 20% in the faeces.

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.

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).

With medicine: Possible interactions of Apegestrol 160 mg 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.

History of hypersensitivity to Apegestrol 160 mg or any component of the formulation. Known or suspected pregnancy.

Weight Gain: Weight gain is a frequent side effect of Apegestrol 160 mg. This gain has been associated with increased appetite and is not necessarily associated with fluid retention.Thromboembolic Phenomena: Thromboembolic phenomena including thrombophlebitis and pulmonary embolism (in some cases fatal) have been reported.Glucocorticoid Effects: The glucocorticoid activity of Apegestrol 160 mg has not been fully evaluated. Clinical cases of new onset diabetes mellitus, exacerbation of preexisting diabetes mellitus, and overt Cushing’s syndrome have been reported in association with the chronic use of Apegestrol 160 mg. In addition, clinical cases of adrenal insufficiency have been observed in patients receiving or being withdrawn from chronic Apegestrol 160 mg therapy in the stressed and non-stressed state.Other: Nausea, dyspnea, tumor flare, hyperglycemia, glucose intolerance, alopecia, hypertension, carpal tunnel syndrome, mood changes, hot flashes, malaise, asthenia, lethargy, sweating and rash.

Pregnancy Category D. The use of progestational agents during the first four months of pregnancy is not recommended. Very small amounts (approximately 0.1%) are excreted in mother's milk. It is however, not known whether these amounts exert any harmful effect on the newborn. Because of the potential for adverse effects on the new born, nursing should be discontinued during treatment with Apegestrol 160 mg.

General: Close surveillance is indicated for any patient treated for recurrent or metastatic cancer. Use with caution in patients with a history of thromboembolic disease.Use in Diabetics: Exacerbation of preexisting diabetes with increased insulin requirements has been reported in association with the use of Apegestrol 160 mg.

No serious unexpected side effects have resulted from studies involving Apegestrol 160 mg administered in dosages as high as 1600 mg/day.

Store in a cool (below 30°C) and dry place, away from light & moisture. Keep all medicines out of reach of children.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.Geriatric Use: In the dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

Apegestrol 160 mg is a synthetic, antineoplastic and progestational drug. While the precise mechanism by which Apegestrol 160 mg 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 Apegestrol 160 mg 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 Apegestrol 160 mg 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 Apegestrol 160 mg 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 Apegestrol 160 mg is 33 to 38 hours. Approximately 66% of an administered dose is excreted in the urine and approximately 20% in the faeces.

Pregnancy Category D. The use of progestational agents during the first four months of pregnancy is not recommended. Very small amounts (approximately 0.1%) are excreted in mother's milk. It is however, not known whether these amounts exert any harmful effect on the newborn. Because of the potential for adverse effects on the new born, nursing should be discontinued during treatment with Apegestrol 160 mg.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.Geriatric Use: Insufficient data from clinical studies of Apegestrol 160 mg tablets are available for patients 65 years of age and older to determine whether they respond differently than younger patients.