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Drug nameMegestrol
Description17-Hydroxy-6-methylpregna-3,6-diene-3,20-dione. A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer. [PubChem]
DrugBankPrimary Accession Number: DB00351
TypeApproved, Small Molecule
IndicationFor the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used to treat breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
Mechanism of ActionSeveral investigators have reported on the appetite enhancing property of megestrol acetate and its possible use in cachexia. The precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time. The biochemical mechanism of progestin antitumour activity is not well but may involve interaction with progesterone and glucocorticoid receptors, androgenic properties. Megestrol also has direct cytotoxic effects on breast cancer cells in tissue culture and suppresses luteinising hormone release from the pituitary.
AbsorptionVariable, but well absorbed orally.
ToxicityNo serious unexpected side effects have resulted from studies involving megestrol acetate oral suspension administered in dosages as high as 1200 mg/day.
Protein BindingNot available