Metyrapone

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Metyrapone
Clinical data
Trade namesMetopirone
AHFS/Drugs.comConsumer Drug Information
Pregnancy
category
  • C
    US
Routes of
administration
By mouth
ATC code
Pharmacokinetic data
Elimination half-life1.9 ± 0.7 hours
Identifiers
  • 2-methyl-1,2-di(pyridin-3-yl)propan-1-one
JSmol)
  • O=C(c1cccnc1)C(c2cccnc2)(C)C
  • InChI=1S/C14H14N2O/c1-14(2,12-6-4-8-16-10-12)13(17)11-5-3-7-15-9-11/h3-10H,1-2H3 checkY
  • Key:FJLBFSROUSIWMA-UHFFFAOYSA-N checkY
  (verify)

Metyrapone, sold under the brand name Metopirone, is a medication which is used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism). It is part of the steroidogenesis inhibitor class of drugs.

Medical uses

Metyrapone can be used in the diagnosis of

pituitary or hypothalamus
.

The 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.

Metyrapone is used for the medical control of hypercortisolism in Cushing's syndrome (ACTH dependent or independent). The aim for medical treatment is to achieve pre-operative control of hypercortisolism, or for control of residual disease persisting post-operatively (TSS, adrenalectomy). It is not for long term definitive treatment/cure, only as an adjunct (surgery is the aim for cure in most causes of Cushing's syndrome). Metyrapone hence acts by inhibiting adrenal steroidogenesis. One side effect is hirsutism (in women) because of the excess androgen precursors created. The other commonly used agent for medical treatment of Cushing's is ketoconazole (an anti-fungal agent). This does not exhibit the side effect of hirsutism.

Pharmacology

Pharmacodynamics

Metyrapone blocks

11-deoxycortisol
levels.

Chemistry

Analogues of metyrapone include aminoglutethimide, amphenone B, and mitotane.

Research

Metyrapone has been found in early human trials to reduce recollection of emotional memories in normal volunteers. The volunteers showed significant impairment in ability to retrieve memories with negative emotional content while not impairing memories with neutral content. This has significant implication in the study of the process of emotional healing in

post traumatic stress disorder.[2][3]

Due to the permissive action of cortisol on glucagon, partial blockade of cortisol may reduce the effects of circulating glucagon in chronically increasing blood glucose in metabolic syndrome (syndrome X) and type 2 diabetes.

See also

References

  1. PMID 17462829
    .
  2. ^ University of Montreal (27 May 2011). "Drug may help overwrite bad memories". Science Daily. online: ScienceDaily. Retrieved 27 May 2011.
  3. PMID 21593118
    .