Megestrol Acetate

Indications
 Oral
Palliative treatment of breast carcinoma
Adult: 40 mg 4 times daily or 160 mg once daily.
Oral
Palliative treatment of endometrial carcinoma
Adult: 40-320 mg daily in divided doses.
Oral
Anorexia and cachexia in patients with cancer or AIDS
Adult: Initial: 800 mg daily. Usual range: 400-800 mg daily. As suspension containing 625 mg megestrol acetate in 5 ml: 625 mg daily.
Contraindications
 Pregnancy and lactation. Severe hepatic impairment.
Warnings / Precautions
 History of thrombophlebitis, mild to moderate hepatic impairment, risk of fluid retention, history of depression, diabetes, hypertension, renal or cardiac dysfunction.
Adverse Reactions
 Acne, urticaria, fluid retention, wt gain, heart failure, nausea, vomiting, GI disturbances, changes in libido, breast discomfort, premenstrual symptoms, irregular menstrual cycles, depression, insomnia, somnolence, alopoecia, hirsutism, anaphylactoid-like reaction, jaundice, hot flushes, adrenocortical suppression, nausea, carpal tunnel syndrome, hypercalcaemia, tumour flare, hypertension.
Drug Interactions
 Concentrations of indinavir may be reduced. Possible reduced efficacy of cisplatin. Warfarin half life may be increased. Megestrol concentration may be decreased by aminoglutethimide and enzyme-inducing drugs.
See Below for More megestrol Drug Interactions
Mechanism of Actions
 Megestrol is a progestogen used as an antineplastic and appetite stimulant. The mechanism of it's antineoplastic effects is not known but may be due to inhibition of oestrogen synthesis, modulation of other steroid hormones and/or a direct cytotoxic effect on tumour cells.
Absorption: Variable absorption from the GIT (oral); peak plasma concentrations after 1-3 hrs.
Distribution: Protein-binding: High.
Metabolism: Hepatic.
Excretion: Urine (as steroid metabolites and inactive compound), faeces.
Administration
 Standard formulation: Should be taken with food.
Megace ES: May be taken with or without food.
ATC Classification
 G03AC05 - megestrol ; Belongs to the class of progestogens. Used as systemic contraceptives.
G03DB02 - megestrol ; Belongs to the class of pregnadien derivative progestogens used in progestogenic hormone preparations.
L02AB01 - megestrol ; Belongs to the class of progestogens.
Available As
  • Megestrol Acetate 160 mg
  • Megestrol Acetate 40 mg

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