Metyrapone: Difference between revisions
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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 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. |
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===Experimental use=== |
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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]].<ref>{{Cite news | last = University of Montreal| title = Drug may help overwrite bad memories| newspaper = Science Daily| location = online| publisher = ScienceDaily| date = 27 May 2011 | url = http://www.sciencedaily.com/releases/2011/05/110526064802.htm | accessdate = 27 May 2011}}</ref><ref>{{Cite journal| last = Marin| first = Marie-Frances| authorlink = | coauthors = A. Hupbach, F. S. Maheu, K. Nader, S. J. Lupien| title = Metyrapone Administration Reduces the Strength of an Emotional Memory Trace in a Long-Lasting Manner| journal = Journal of Clinical Endocrinology & Metabolism| volume = early release abstract| issue = 8| pages = E1221| publisher = | location = | date = | language = | url = | jstor = | doi = 10.1210/jc.2011-0226| id = | mr = | zbl = | jfm = }} |
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==References== |
==References== |
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Revision as of 17:30, 30 September 2012
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| Clinical data | |
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| Trade names | Metopirone |
| AHFS/Drugs.com | Consumer Drug Information |
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| Routes of administration | Oral |
| ATC code | |
| Pharmacokinetic data | |
| Elimination half-life | 1.9 ±0.7 hours. |
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| DrugBank | |
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| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.000.188 |
| Chemical and physical data | |
| Formula | C14H14N2O |
| Molar mass | 226.274 g/mol g·mol−1 |
| 3D model (JSmol) | |
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Metyrapone (trade name Metopirone) is a drug used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism).
Mechanism
Metyrapone blocks cortisol synthesis[1] by inhibiting steroid 11β-hydroxylase. This stimulates ACTH secretion, which in turn increases plasma 11-deoxycortisol levels.
Uses
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 Hypothalamo-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 and ACTH rises, then it is highly suggestive of impaired adrenal insufficiency, if neither 11-deoxycortisol nor ACTH rise it is highly suggestive of an impaired HPA axis at either the pituitary or hypothalamus.
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.
References
- ^ Young EA, Ribeiro SC, Ye W (2007). "Sex Differences in ACTH Pulsatility following Metyrapone Blockade in Patients with Major Depression". Psychoneuroendocrinology. 32 (5): 503–7. doi:10.1016/j.psyneuen.2007.03.003. PMC 1975691. PMID 17462829.
{{cite journal}}: Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link)
See also
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