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Aminoglutethimide

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Aminoglutethimide chemical structure
Aminoglutethimide

(RS)-3-(4-aminophenyl)-3-ethyl-piperidine-2,6-dione
IUPAC name
CAS number
125-84-8
ATC code

L02BG01

PubChem
2145
DrugBank
DB00357
Chemical formula {{{chemical_formula}}}
Molecular weight 232.278 g/mol
Bioavailability >95%
Metabolism Hepatic
Elimination half-life 12.5 ± 1.6 hours
Excretion Renal
Pregnancy category {{{pregnancy_category}}}
Legal status {{{legal_status}}}
Routes of administration Oral


Aminoglutethimide is an anti-steroid drug marketed under the tradename Cytadren by Novartis around the world. It blocks the production of steroids derived from cholesterol and is clinically used in the treatment of Cushing's syndrome[1] and metastatic breast cancer. It is also used by body builders.

MechanismEdit

Aminoglutethimide has two mechanisms of action:

  1. It blocks aromatase[2] in the generation of estrogens from androstenedione and testosterone.
  2. It blocks the conversion of cholesterol to pregnenolone by inhibiting the enzyme P450scc and consequently decreases synthesis of all hormonally active steroids.

At low doses, aminogluthethimide is only an effective inhibitor of aromatase, but at higher doses, it effectively blocks P450scc as well.

Side effectsEdit

Its side effects are skin rash, hepatotoxicity, inhibition of cortisol in the human body, and it may also cause hypothyroidism[citation needed]. Since cortisol helps break down muscle, aminoglutethimide is used by bodybuilders in a steroid cycle.

Clinical usesEdit

Aminoglutethimide is indicated in conjunction with other drugs for the suppression of adrenal function in patients with Cushing's syndrome.

It is also a 2nd or 3rd line choice for the treatment of hormone sensitive (estrogen and progesterone) metastatic breast cancer.

AbuseEdit

Aminoglutethimide is abused by body builders and other steroid users to lower circulating levels of cortisol in the body and prevent muscle loss. Cortisol is catabolic to protein in muscle and effective blockade of P450scc by aminogluthethimide at high doses prevents muscle loss.[citation needed]

ReferencesEdit

  1. Gross BA, Mindea SA, Pick AJ, Chandler JP, Batjer HH (2007). Medical management of Cushing disease. Neurosurgical focus 23 (3): E10.
  2. Siraki AG, Bonini MG, Jiang J, Ehrenshaft M, Mason RP (July 2007). Aminoglutethimide-induced protein free radical formation on myeloperoxidase: a potential mechanism of agranulocytosis. Chemical research in toxicology 20 (7): 1038–45.

External linksEdit

See alsoEdit


Template:Estrogenics Template:Glucocorticoids Template:Mineralocorticoids Template:Progestogenics

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