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Aminoglutethimide
drug data and news
Aminoglutethimide drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Aminoglutethimide | ||
| Brand Names/Synonyms | Aminoglutethimide; Cytadren; Dl-Aminoglutethimide; Doriden; Elipten; Glutethimide; Orimeten; P-Aminoglutethimide | ||
| Indication | For the suppression of adrenal function in selected patients with Cushing s syndrome, Malignant neoplasm of female breast, Carcinoma in situ of breast | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Aminoglutethimide inhibits the enzymatic conversion of cholesterol to D5-pregnenolone, resulting in a decrease in the production of adrenal glucocorticoids, mineralocorticoids, estrogens, and androgens. | ||
| Mechanism Of Action | Aminoglutethimide reduces the production of D5-pregnenolone and blocks several other steps in steroid synthesis, including the C-11, C-18, and C-21 hydroxylations and the hydroxylations required for the aromatization of androgens to estrogens, mediated through the binding of Aminoglutethimide to cytochrome P-450 complexes. A decrease in adrenal secretion of cortisol is followed by an increased secretion of pituitary adrenocorticotropic hormone (ACTH), which will overcome the blockade of adrenocortical steroid synthesis by aminoglutethimide. The compensatory increase in ACTH secretion can be suppressed by the simultaneous administration of hydrocortisone. Since aminoglutethimide increases the rate of metabolism of dexamethasone but not that of hydrocortisone, the latter is preferred as the adrenal glucocorticoid replacement. Although aminoglutethimide inhibits the synthesis of thyroxine by the thyroid gland, the compensatory increase in thyroid-stimulating hormone (TSH) is frequently of sufficient magnitude to overcome the inhibition of thyroid synthesis due to aminoglutethimide. In spite of an increase in TSH, aminoglutethimide has not been associated with increased prolactin secretion. | ||
| Aminoglutethimide News (When available) |
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| Dosage Forms | Tablet | ||
| Drug_Category | Antineoplastic Agents; Adrenergic Agents; ATC:L02BG01 | ||
| Absorption | Rapidly and completely absorbed grom GI tract | ||
| Interactions |
-->Interactions for Aminoglutethimide: Cytadren accelerates the metabolism of dexamethasone; therefore, if glucocorticoid replacement is needed, hydrocortisone should be prescribed. Aminoglutethimide diminishes the effect of coumarin and warfarin. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 3-(4-aminophenyl)-3-ethyl-piperidine-2,6-dione | ||
| Chemical Formula | C13H16N2O2 | ||
| Molecular Weight | 232.278 g/mol | ||
| Smiles String | CCC1(CCC(=O)NC1=O)C2=CC=C(C=C2)N | ||
| Melting Point | 149-150 °C | ||
| Water Solubility | Practically insoluble in water | ||
| State | Solid | ||
| LogP/Hphobicity | 2.029 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 12.5 +/- 1.6 hours | ||
| Protein Binding [%] | 21-25% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Aminoglutethimide.html http://www.rxlist.com/cgi/generic3/cytadren.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00592 | ||
| CAS Registry Number | 125-84-8 | ||
| KEGG Compound ID | C07617 | ||
| PubChem ID | SID:9819 | ||
| PharmGKB ID | PA448375 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 587729 |
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