This MedLibrary.org supplementary page on Aminoglutethimide is provided directly from the open source Wikipedia as a service to our readers. Please see the note below on authorship of this content, as well as the Wikipedia usage guidelines. To search for other content from our encyclopedia supplement, please use the form below:
Related Sponsors
 |
|
|
Aminoglutethimide
|
|
| Systematic (IUPAC) name | |
| 3-(4-aminophenyl)-3-ethyl-piperidine-2,6-dione | |
| Identifiers | |
| CAS number | |
| ATC code | L02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C13H16N2O2 |
| Mol. mass | 232.278 g/mol |
| Pharmacokinetic data | |
| Bioavailability | >95% |
| Metabolism | Hepatic |
| Half life | 12.5 ± 1.6 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral |
Aminoglutethimide is an anti-steriod drug marketed under the tradename Cytadren by Novartis around the world. It blocks the production of steroids dervied from cholesterol and is clinically used in the treatment of Cushing's syndrome and metastatic breast cancer. It is also a drug of abuse by body builders.
Contents |
Mechanism
Aminogluthethimide has a two mechanisms of action:
- It blocks aromatase in the generation of estrogens from androstenedione and testosterone.
- 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 effects
Its side effects are skin rash, hepatotoxicity, inhibition of cortisol in the human body, and it may also cause hypothyroidismcitation needed. Since cortisol helps break down muscle, aminoglutethimide is used by bodybuilders in a steroid cycle.
Clinical uses
Aminoglutethimide is indicated in conjunction with other drugs for the suppression of adrenal function in patients with Cushing's syndrome.
Is is also a 2nd or 3rd line choice for the treatment of hormone sensitive (estrogen and progesterone) metastatic breast cancer.
Abuse
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.
External links
- Cytadren prescribing information (from the FDA website)
- Medline Plus
See also
|
|||||||||||||||||||||||||||||||||||||||||||||||||||
Wikipedia content modification information:
- This page was last modified on 4 August 2008, at 02:31.
Wikipedia Authorship and Review
Wikipedia content provided here is not reviewed directly by MedLibrary.org. Wikipedia content is authored by an open community of volunteers and is not produced by or in any way affiliated with MedLibrary.org.
Wikipedia Usage Guidelines
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article on "Aminoglutethimide".
The URL for this specific entry is:
All Wikipedia text is available under the terms of the GNU Free Documentation License. (See Copyrights for details). Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc.