Aminoglutethimide

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Aminoglutethimide chemical structure
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. weight 232.278 g/mol
Pharmacokinetic data
Bioavailability >95%
Metabolism Hepatic
Half life 12.5 ± 1.6 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

D: (USA)
D:(AUS)

Legal status
Routes Oral

Aminoglutethimide is a first generation aromatase inhibitor used in the treatment of breast cancer and Cushing's syndrome. It blocks the synthesis of estrogen through inhibition of the aromatase enzyme. Aminoglutethimide also inhibits many of the enzymes involved in the generation of corticosteroids. Its major side effects are liver toxicity, inhibition of Cortisol in the human body, and it may also cause hypothyroidism. Since cortisol helps break down muscle, Aminoglutethimide is used by bodybuilders in a steroid cycle.

Aminoglutethimide is no longer used medicinally as an aromatase inhibitor since many newer and more specific inhibitors have been discovered. It is still used to suppress corticosteroid production in Cushing's Syndrome.

[edit] See also

[edit] Reference Links

Aminoglutethimide (Cytadren) Profile


Sex hormones and related medications (primarily G03, also L02, H01C) edit
Progestogens:
(receptor)

Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone
Antiprogestogen: Mifepristone

Androgens:
(receptor)

Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, Testosterone, (see also anabolic steroids)
Antiandrogens: Bicalutamide, Cyproterone, Flutamide, Nilutamide, Spironolactone

Estrogens:
(receptor)

Chlorotrianisene, Dienestrol, Diethylstilbestrol, Estradiol, Estriol, Estrone, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate
Selective estrogen receptor modulator: Bazedoxifene, Clomifene, Fulvestrant, Raloxifene, Tamoxifen, Toremifene
Aromatase inhibitor: Aminogluthetimide, Anastrozole, Exemestane, Formestane, Letrozole, Vorozole

Gonadotropins:
(FSHR/LHCGR)

ovulation stim.: Clomifene, Urofollitropin
Antigonadotropins: Danazol, Gestrinone

GnRH:
(receptor)

Gonadotropin-releasing hormone agonist: Buserelin, Goserelin, Leuprorelin, Nafarelin, Triptorelin
Gonadotropin-releasing hormone antagonist: Histrelin, Abarelix