metyrapone

Metyrapone is a small molecule inhibitor of adrenal steroidogenesis, primarily used as a diagnostic agent to assess hypothalamic-pituitary-adrenal (HPA) axis function and in the management of Cushing's syndrome. Its main mechanism of action is reversible inhibition of the enzyme 11β-hydroxylase (CYP11B1) in the adrenal cortex, which blocks the conversion of 11-deoxycortisol to cortisol. This leads to reduced cortisol and corticosterone production, resulting in increased secretion of adrenocorticotropic hormone (ACTH) due to loss of negative feedback. Metyrapone may also suppress aldosterone synthesis and inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). It is rapidly absorbed orally, with peak plasma levels reached about one hour after administration. Metyrapone is mainly used for diagnostic testing but can be employed short-term for preoperative control or adjunctive treatment in Cushing’s syndrome[2][4][6][7].

Brand names

Metopirone

Other names

MetiraponaMetopiron