Cytadren is used in the treatment of Cushing's syndrome, a disease caused due to an increased production of cortisol and other hormones. The generic name of Cytadren is aminoglutethimide, which is the active ingredient of this drug. The inactive ingredients of Cytadren include: Cellulose compounds. Colloidal silicon dioxide. Starch. Stearic acid. Talc. It functions by inhibiting the adrenocortical steroid synthesis, thereby reducing the production of adrenal glucocorticoids, androgens, estrogens, and mineralocorticoids. This inturn helps in suppressing the adrenal function in selected patients with Cushing’s syndrome. It is recommended that this medication be administered only in people who respond to this treatment.

Aminoglutethimide is a first generation aromatase inhibitor used in the treatment of breast cancer and Cushing's syndrome. It blocks the synthesis of estrogen through inhibition of the aromatase enzyme. Aminoglutethimide also inhibits many of the enzymes involved in the generation of corticosteroids. It blocks the conversion of cholesterol to pregnenolone and inhibits synthesis of all hormonally active steroids. It can be used in conjunction with other drugs for treatment of steroid-producing adrenocortical cancer.

Its major side effects are liver toxicity, 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 no longer used medicinally as an aromatase inhibitor since many newer and more specific inhibitors have been discovered. It is still used to suppress corticosteroid production in Cushing's Syndrome.