Mezestrol Acetate oral suspension is a progestin indicated for the treatment of anorexia,cachexia,or an unexplained significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS) .
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.
The recommended adult initial dosage of its oral suspension is 625 mg/day (5 mL/day or one teaspoon daily). Shake container well before using.
With medicine: Possible interactions of Megestrol Acetate 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. Precautions & Warnings
Megestrol Acetate should be used with caution in patients with a history of thrombophlebitis and in patients with severe impaired liver function.
This product should be used under the supervision of a specialist and the patients kept under regular surveillance. This product 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. Megestrol acetate is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug 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 megestrol acetate, and it may be useful to monitor renal function.
nausea,diarrhea,impotence,rash,flatulence, hypertension,and asthenia
Because of the potential for adverse effects on the newborn,nursing should be discontinued if its oral suspension is required.
No acute toxicological effects have resulted from studies involving megestrol acetate administered in dosages as high as 1600 mg/day for six months or more. Reports of overdose have also been received in the postmarketing setting. Signs and symptoms reported in the context of overdose included diarrhoea, nausea, abdominal pain, shortness of breath, cough, unsteady gait, listiessness, and chest pain. There is no specific antidote for overdose with Megestrol Acetate. In case of overdose, appropriate supportive measures should be taken.
Store in a cool (below 30°C) and dry place, away from light & moisture. Keep all medicines out of reach of children.
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