Clear Search sequence regions
Bookmark Forward

QuickView for Megestrol (compound)


PubChem
Name: Megestrol
PubChem Compound ID: 19090
Description: 17-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.
Molecular formula: C22H30O3
Molecular weight: 342.472 g/mol
Synonyms:
3562-63-8; HSDB 3233; EINECS 222-628-6; Megestrolo [DCIT]; Megestrolum [INN-Latin]; C07120; 17-Hydroxy-6-methylpregna-4,6-diene-3,20-dione; Megestrol; Pregna-4,6-diene-3,20-dione, 17-hydroxy-6-methyl-
DrugBank
Identification
Name: Megestrol
Name (isomeric): DB00351
Drug Type: small molecule
Description: 17-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.
Synonyms:
Megestryl acetate; MGA; Megestrolum [INN-Latin]; Megestrolo [DCIT]; Megestrol Acetate
Brand: Ovaban, Megace, Maygace, Megestat, Niagestin, Megestil, Nia, Volidan, Magestin, Ovarid, Megeron, Megestin
Category: Antineoplastic Agents, Hormonal, Contraceptives, Oral, Synthetic
CAS number: 3562-63-8
Pharmacology
Indication: For the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
Pharmacology:
Megestrol is a synthetic progestin and has the same physiologic effects as natural progesterone. These effects include induction of secretory changes in the endometrium, increase in basal body temperature, pituitary inhibition, and production of withdrawal bleeding in the presence of estrogen. Mestrogel has slight glucocorticoid activity and very s...
show more »
Mechanism of Action:
The precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time, but its progestin antitumour activity may involve suppression of luteinizing hormone by inhibition of pituitary function. Studies also suggest that the megestrol's weight gain effect is related to its appetite-stimulant or meta...
show more »
Absorption: Variable, but well absorbed orally.
Biotransformation: Primarily hepatic. Megestrol metabolites which were identified in urine constituted 5% to 8% of the dose administered. Respiratory excretion as labeled carbon dioxide and fat storage may have accounted for at least part of the radioactivity not found in urine and feces. No active metabolites have been identified.
Route of elimination: The major route of drug elimination in humans is urine. Respiratory excretion as labeled carbon dioxide and fat storage may have accounted for at least part of the radioactivity not found in urine and feces.
Half Life: 34 hours
Toxicity: No serious unexpected side effects have resulted from studies involving megestrol acetate oral suspension administered in dosages as high as 1200 mg/day. Treatment with megestrol acetate, an orexigenic agent, has also resulted in iatrogenic adrenal suppression. The mechanism is presumably related to the glucocorticoid properties of megestrol acetate [PMID: 12872362].
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food.
Drug interaction:
PhenobarbitalThe enzyme inducer, phenobarbital, may decrease the effect of the hormone, megestrol.
FosphenytoinThe enzyme inducer, fosphenytoin, may decrease the effect of the hormone, megestrol.
PentobarbitalThe enzyme inducer, pentobarbital, decreases the effect of the hormone agent, megestrol.
ButalbitalThe enzyme inducer, butalbital, decreases the effect of the hormone agent, megestrol.
SecobarbitalThe enzyme inducer, secobarbital, decreases the effect of the hormone agent, megestrol.
show more »

Targets


Transporters