Aminoglutethimide is an anti-steroid drug marketed under the tradename Cytadren by Novartis around the world. It blocks the production of steroids dervied from cholesterol and is clinically used in the treatment of Cushing's syndrome and metastatic breast cancer. It is also a drug of abuse by body builders.
Aminogluthethimide has a two mechanisms of action:
- It blocks aromatase in the generation of estrogens from androstenedione and testosterone.
- It blocks the conversion of cholesterol to pregnenolone by inhibiting the enzyme P450scc and consequently decreases synthesis of all hormonally active steroids.
At low doses, aminogluthethimide is only an effective inhibitor of aromatase, but at higher doses, it effectively blocks P450scc as well.
Its side effects are skin rash, hepatotoxicity
, inhibition of cortisol
in the human body, and it may also cause hypothyroidism
. Since cortisol helps break down muscle
, aminoglutethimide is used by bodybuilders
in a steroid cycle
Aminoglutethimide is indicated in conjunction with other drugs for the suppression of adrenal
function in patients with Cushing's syndrome
Is is also a 2nd or 3rd line choice for the treatment of hormone sensitive (estrogen and progesterone) metastatic breast cancer.
Aminoglutethimide is abused by body builders and other steroid users to lower circulating levels of cortisol in the body and prevent muscle loss. Cortisol is catabolic
to protein in muscle and effective blockade of P450scc by aminogluthethimide at high doses prevents muscle loss.