Aminoglutethimide: Review of Pharmacology and Clinical Use

作者: Richard J. Santen , Robert I. Misbin

DOI: 10.1002/J.1875-9114.1981.TB03557.X

关键词: AminoglutethimideEndocrinologyTamoxifenMedicineHypophysectomyInternal medicinePharmacologyAntiestrogenMetyraponeHydrocortisoneBreast cancerAdrenalectomy

摘要: Aminoglutethimide blocks several cytochrome P-450 mediated steroid hydroxylation steps, including those required for conversion of cholesterol to pregnenolone and the aromatization androgens estrogens. Through these actions it adrenal steroidogenesis production estrogens in extraglandular tissues. is indicated treatment certain patients with Cushing's syndrome breast cancer. Other potential uses (prostate carcinoma, low renin hypertension, etc.) remain investigational. For syndrome, aminoglutethimide usually given alone or combination metyrapone. In women replacement hydrocortisone must be administered prevent reflex ACTH hypersecretion from overcoming inhibition. Administration results improvement clinical status 56% cases. Results are most favorable tumors ectopic production. glucocorticoid produce objective disease regression 32% unselected postmenopausal metastatic carcinoma 52% whose estrogen receptor positive. Responses similar duration frequency produced by surgical adrenalectomy hypophysectomy antiestrogen, tamoxifen.

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