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14-September-2008 11:27:24 - Aminoglutethimide Aminoglutethimide Systematic IUPAC name 3-4-aminophenyl-3-ethyl-piperidine-2,6-dione Identifiers CAS number 125-84-8 ATC code L02BG01 PubChem 2145 DrugBank APRD00592 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. DAU DUS Legal status Routes Oral Aminoglutethimide is an anti-steroid 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 1 Mechanism 2 Side effects 3 Clinical uses 4 Abuse 5 External links 6 See also 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 Glutethimide v d e Sex hormones and related agents primarily G03, also L02, H01C - human endogenous in CAPS Progestogens: receptor Agonist PROGESTERONE, Dienogest, Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone SPRM Asoprisnil, CDB-4124 Antiprogestogen Mifepristone Androgens: receptor Agonist TESTOSTERONE, Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, see also anabolic steroids Antiandrogen Bicalutamide, Cyproterone, Dienogest, Flutamide, Nilutamide, Spironolactone Estrogens: receptor Agonist ESTRADIOL, ESTRIOL, ESTRONE, Chlorotrianisene, Dienestrol, Diethylstilbestrol, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate SERM Afimoxifene, Arzoxifene, Bazedoxifene, Clomifene, Fulvestrant, Lasofoxifene, Raloxifene, Tamoxifen, Toremifene AI Aminoglutethimide, Anastrozole, Atamestane, Exemestane, Fadrozole, Formestane, Letrozole, Vorozole Antiestrogen Mepitiostane Gonadotropins: FSHR/LHCGR ovulation stim. Clomifene, Urofollitropin Antigonadotropin Danazol, Gestrinone GnRH: receptor Agonist Buserelin, Goserelin, Histrelin, Leuprorelin, Nafarelin, Triptorelin Antagonist Abarelix, Cetrorelix, Ganirelix Retrieved from http://en..org/wiki/Aminoglutethimide Categories: Aromatase inhibitorsHidden categories: All articles with statements | Articles with statements since June 2008 Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Português This page was last modified on 10 September 2008, at 04:13
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