Pharmacodynamics<unk>  is a potent and non-selective steroidogenesis inhibitor, acting as a reversible and competitive inhibitor of multiple steroidogenic enzymes, including: * Aromatase (CYP19A1) (600 nM). Inhibits the formation of the estrogens estradiol and estrone from testosterone and androstenedione, respectively. * Cholesterol side-chain cleavage enzyme (P450scc; CYP11A1) (~20,000 nM). Inhibits the conversion of cholesterol into pregnenolone and consequently decreases the synthesis of all steroid hormones including the progestogens, androgens, estrogens, glucocorticoids, and mineralocorticoids, as well as neurosteroids. * 21-Hydroxylase (CYP21A2). Prevents the conversion of progesterone and 17α-hydroxyprogesterone into 11-deoxycorticosterone and 11-deoxycortisol, respectively. * 11β-Hydroxylase (CYP11B1). Prevents the conversion of 11-deoxycorticosterone and 11-deoxycortisol into corticosterone and cortisol, respectively. * Aldosterone synthase (18-hydroxylase; CYP11B2). Prevents the conversion of corticosterone into aldosterone. As such,<unk>  is an estrogen synthesis inhibitor and adrenal steroidogenesis inhibitor, including both an androgen synthesis inhibitor and a corticosteroid synthesis inhibitor. For these reasons,<unk>  has functional antiestrogenic, antiandrogenic, antiglucocorticoid, and antimineralocorticoid actions. In terms of its actions as an adrenal steroidogenesis inhibitor, it is described as a form of reversible "medical adrenalectomy" or "chemical adrenalectomy". While<unk>  inhibits all of the enzymes listed above, inhibition of P450scc is primarily responsible for its inhibition of adrenal steroidogenesis. In terms of adrenal androgens,<unk>  has been shown to significantly suppress dehydroepiandrosterone sulfate, androstenedione, testosterone, and dihydrotestosterone levels in men. Although it is most potent in inhibiting aromatase among the enzymes it targets,<unk>  is described nonetheless as a relatively weak aromatase inhibitor. In addition, it is described as a much more potent aromatase inhibitor than adrenal steroidogenesis inhibitor.<unk>  can inhibit aromatase by 74 to 92% and decrease circulating estradiol levels by 58 to 76% in men and postmenopausal women.<unk>  is not an effective ovarian steroidogenesis inhibitor in premenopausal women. However, interference with ovarian steroidogenesis by<unk>  may in any case result in hyperandrogenism and virilization in premenopausal women. Pharmacokinetics With oral administration, the absorption of<unk>  is rapid and complete. It is well-distributed throughout the body. In terms of metabolism, a portion of<unk>  is acetylated in the liver. The biological half-life of<unk>  is 12.5 hours. It is excreted in urine 34 to 54% unchanged.
Aminoglutethimide
Vinyltestosterone
Ethinylestradiol sulfonate
Haloprogesterone
Ethinylestradiol
Ethinylestradiol sulfate
Retroprogesterone
Hydroxyprogesterone acetate