Mezest
Generic Name:Megestrol Acetate
Indications
Mezest 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.
Mezest 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.
Pharmacology
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.
Dosage & Administration
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).
Interaction
With medicine: Possible interactions of Mezest 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.
Contraindications
History of hypersensitivity to Megestrol Acetate or any component of the formulation. Known or suspected pregnancy.
Side Effects
Weight Gain: Weight gain is a frequent side effect of Mezest. 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 Mezest 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 Mezest. In addition, clinical cases of adrenal insufficiency have been observed in patients receiving or being withdrawn from chronic Mezest 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 & Lactation
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 Megestrol Acetate.
