The Full Wiki

More info on Metyrapone

Metyrapone: Wikis


Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.


From Wikipedia, the free encyclopedia

Systematic (IUPAC) name
CAS number 54-36-4
ATC code V04CD01
PubChem 4174
DrugBank APRD01111
Chemical data
Formula C 14H14N2O 
Mol. mass 226.274 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 1.9 ±0.7 hours.
Excretion  ?
Therapeutic considerations
Pregnancy cat. C US
Legal status
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Metyrapone (Metopirone) is a drug used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism).



Metyrapone blocks cortisol synthesis[1] by inhibiting steroid 11β-hydroxylase. This stimulates ACTH secretion, which in turn increases plasma 11-deoxycortisol levels. When excess ACTH secretion is the cause of hypercortisolism, the metyrapone test helps clarify if the source of the ACTH is pituitary or ectopic (non-pituitary). The effects of metyrapone were first noticed by mistake in transgenic mice by TE Vanguard at the University of Tennessee in Memphis while testing a similar drug known as metradione which was being studied for its effects on corticosteroid uptake.


Metyrapone can be used in the diagnosis of adrenal insufficiency. Metyrapone 30mg/kg, maximum dose 3000 mg, is administered at midnight usually with a snack. The plasma cortisol and 11-deoxycortisol are measured the next morning between 8:00 and 9:00 am. A plasma cortisol less than 220nmol/l indicates adequate inhibition of 11β-hydroxylase. In patients with intact Hypothamalmo-pituitary-adrenal axis, CRH and ACTH levels rise as a response to the falling cortisol levels. This results in an increase of the steroid precursors in the pathway. Therefore if 11-deoxycortisol levels do not rise and remains less than 7 mcg/dl then it is highly suggestive of impaired HPA axis.

Metyrapone test may aid in verifying the cause of Cushing's syndrome. Most patients with pituitary dysfunction and/or pituitary microadenoma will increase ACTH secretion in response to metyrapone, while most ectopic ACTH-producing tumors will not. Pituitary macroadenomas do not always respond to metyrapone.


See also



Got something to say? Make a comment.
Your name
Your email address