Aminoglutethimide is mainly identified as an inhibitor of adrenocortical steroid synthesis. Its primary function is to block the conversion of cholesterol to pregnenolone, which is required for the biosynthesis of adrenal glucocorticoids, mineral corticoids, estrogens, and androgens. Aminoglutethimide is a nonspecific inhibitor, and also blocks several other steps in steroid synthesis including hydroxylation at C-11, C-18, and C-21, and the aromatization of androgen to estrogens, The drug may be used clinically to treat estrogen dependent breast cancer, and to treat Cushing’s syndrome, which is a condition where the body overproduces the hormone cortical. The effect that Aminoglutethimide can have on cortical and estrogen production is what makes this a drug of interest to athletes and bodybuilders. The drug also works by inhibiting cortical production. While cortical is an essential hormone for life, its levels may also vary greatly within “normal” ranges depending on the individual, their training and dietary status. Aminoglutethimide was FDA approved as an anticonvulsant drug in 1960 under the main trade name of Cytadren. Side effects were common with treatment, however, including drowsiness, dizziness, and partial loss of motor control. In 1966 reports of adrenal insufficiency subsequent to Aminoglutethimide use were reported. The drug was withdrawn from the U.S market as an anticonvulsant that same year due to its recently understood effects on the adrenal gland. The drug is most commonly supplied in tablets of 250mg.
