drugsTreatmentEstablished

Metyrapone

aka Metyrapone capsules

Metyrapone is an older tablet that blocks cortisol production in the adrenal glands. It is used to bring cortisol down quickly in Cushing's disease before or after pituitary surgery, and in the United States mainly as a diagnostic test.

Metyrapone has been used since the 1960s. In Europe it is licensed for the management of Cushing's syndrome, including Cushing's disease caused by a pituitary corticotroph adenoma, and is a mainstay for rapid pre-operative control of hypercortisolism or when surgery has failed. In the United States it is approved as a diagnostic agent for testing hypothalamic-pituitary ACTH function, and its therapeutic use is off-label.

It is taken several times a day and titrated against cortisol levels; adverse effects include nausea, dizziness, hirsutism and acne from androgen precursors, and hypertension and hypokalaemia from mineralocorticoid precursors. Osilodrostat is the newer, more potent inhibitor of the same enzyme. The pituitary tumours page names both.

See it in action

Inhibits adrenal 11-beta-hydroxylase, reducing cortisol synthesis; ACTH rises in response, so 11-deoxycortisol accumulates, which is the basis of its use as a test of pituitary reserve as well as a treatment.

1. What happens next: the small molecule schematic

How targeted therapy works, step by step · animated schematic, not to scale; chosen from the modality "Oral 11-beta-hydroxylase inhibitor"

Targeted Therapy →

2. Step by step

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1.Metyrapone slips into a pocket on its target.

Modality

Oral 11-beta-hydroxylase inhibitor

Mechanism

Brand / code

Metopirone

Trials

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Metyrapone

intervention: Metyrapone

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