Megestrol

Oral
Anorexia and cachexia in patients with cancer or AIDS

Oral
Palliative treatment of breast carcinoma

Oral
Palliative treatment of endometrial carcinoma

Standard Formulation: Should be taken with food.
Megace Es: May be taken with or without food.

Pregnancy and lactation. Severe hepatic impairment.

History of thrombophlebitis, mild to moderate hepatic impairment, risk of fluid retention, history of depression, diabetes, hypertension, renal or cardiac dysfunction.

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, alopecia, hirsutism, anaphylactoid-like reaction, jaundice, hot flushes, adrenocortical suppression, carpal tunnel syndrome, hypercalcaemia, tumour flare, hypertension.

PO: X (for oral suspension), D (for  tablet)

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.

Description: Megestrol is a progestogen used as an antineoplastic 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.
Pharmacokinetics:
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.

Oral Contraceptives / Cancer Hormone Therapy / Oestrogens, Progesterones & Related Synthetic Drugs