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
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CSI · Cardiology · 2020
Coronary angiography with renal dysfunction
CSI · Cardiology · 2020
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ISG · Gastroenterology · 2023
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ICMR · Infectious Diseases · 2019
Preoperative cardiac evaluation for non-cardiac surgery
AHA · Cardiology · 2025
Other Corticosteroid drugs
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Sources: Goodman & Gilman 14e, Harrison 22e, Katzung, BNF·Verified: 2026-05-10 · House clinical team