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Aminoglutethimide chemical structure
|ATC code |
|Molecular weight||232.278 g/mol|
|Elimination half-life||12.5 ± 1.6 hours|
|Routes of administration||Oral|
Aminoglutethimide is an anti-steroid drug marketed under the tradename Cytadren by Novartis around the world. It blocks the production of steroids derived from cholesterol and is clinically used in the treatment of Cushing's syndrome and metastatic breast cancer. It is also used by body builders.
Aminoglutethimide has 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 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.
- Gross BA, Mindea SA, Pick AJ, Chandler JP, Batjer HH (2007). Medical management of Cushing disease. Neurosurgical focus 23 (3): E10.
- Siraki AG, Bonini MG, Jiang J, Ehrenshaft M, Mason RP (July 2007). Aminoglutethimide-induced protein free radical formation on myeloperoxidase: a potential mechanism of agranulocytosis. Chemical research in toxicology 20 (7): 1038–45.
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