Drug lookup
Drug reference

Metyrapone

Corticosteroid · Adrenal corticosteroid inhibitor

CorticosteroidAdrenal corticosteroid inhibitor
CDSCO approved
EXCRETION
not curated
INTERACTIONS
none in our sources
PREGNANCY
not curated

Mechanism

Metyrapone inhibits 11-beta hydroxylase in the adrenal cortex, preventing the synthesis of hydrocortisone. This leads to a fall in blood cortisol levels and increased ACTH release. The increased ACTH then leads to increased synthesis, release, and excretion of 11-desoxycortisol in the urine. Metyrapone has also been observed to bind to human cytochrome P450 3A4.

Indications

Controlling symptoms of Cushing’s syndromePreparation of patient for surgery in other forms of Cushing’s syndromeTesting the responsiveness of pituitary and its ACTH producing capacitydiagnostic assessment of HPA axis functionhypercortisolism (off-label, often adjunctive therapy after pituitary irradiation)Hypercortisolism associated with Cushing’s Syndrome Caused by Ectopic ACTH Production

Dosing

Adult
Dosages are either low, tailored to cortisol production, or high, requiring concomitant corticosteroid replacement therapy.

Pharmacokinetics

Metabolism
Undergoes carbonyl reductions. Binds to human cytochrome P450 3A4.

Side effects

Common
nauseaheadachesedationrash
Serious
  • hypertension
  • hypokalemia
  • hirsutism

Related guidelines

Other Corticosteroid drugs

Ask House about Metyrapone

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, Harrison 22e, Katzung, BNF·Verified: 2026-05-10 · House clinical team