Aminoglutethimide
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Aminoglutethimide
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| 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 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. It blocked the conversion of cholesterol to pregnenolone and inhibits synthesis of all hormonally active steroid. It can be used in conjunction with other drugs for treatment of steroid-producing adrenocortical cancer.
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.
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