Aminoglutethimide

[8][4] Side effects of AG include lethargy, somnolence, dizziness, headache, appetite loss, skin rash, hypertension, liver damage, and adrenal insufficiency, among others.[9][13][6] However, although used in the past, it has mostly been superseded by newer agents with better efficacy and lower toxicity such as ketoconazole, abiraterone acetate, and other aromatase inhibitors.[15][6][12][7] It is also used to treat secondary hyperaldosteronism, edema, adrenocortical carcinoma, and ectopic adrenocorticotropic hormone (ACTH) producing tumors.[6] Nonetheless, AG was found to be non-significantly different in effectiveness from surgical adrenalectomy in terms of prostate cancer tumor regression.[17] AG should only be used under close medical supervision and with laboratory tests including thyroid function, baseline hematological, serum glutamic-oxaloacetic transaminase, alkaline phosphatase, and bilirubin.[1][8] Ketoconazole can achieve similar decreases in steroid hormone levels as AG but is more effective in promoting tumor regression and is moderately less toxic in comparison.[7][8] AG is used by bodybuilders, athletes, and other men to lower circulating levels of cortisol in the body and thereby prevent muscle loss.[7][1] In any case, AG is also used by bodybuilders and other men for its actions as an aromatase inhibitor in order to decrease estrogen levels.[7] It is said to be useful for inhibiting the estrogenic side effects of certain anabolic steroids such as gynecomastia, increased water retention, and fat gain.[4][6] The side effects of AG include lethargy, fatigue, weakness, malaise, drowsiness, somnolence, depression, apathy, sleep disturbances, stomach discomfort, nausea, vomiting, ataxia, joint aches and pains, fever, skin rash, hypotension or hypertension, high cholesterol levels, virilization, hypothyroidism, thyroid abnormalities, elevated liver enzymes, jaundice, hepatotoxicity, weight gain, leg cramps, personality changes, blood dyscrasias, and adrenal insufficiency (e.g., hyponatremia, hypoglycemia, others).[6] Hematological and bone marrow toxicity, including marked depression of white blood cell count, platelets, or both, occurs rarely, with an incidence of about 0.9%.[19] Treatment of AG overdose can include gastric lavage to decrease absorption and dialysis to enhance elimination.[25] In terms of adrenal androgens, AG has been shown to significantly suppress dehydroepiandrosterone sulfate, androstenedione, testosterone, and dihydrotestosterone levels in men.[7] AG has largely been superseded by medications with better effectiveness and tolerability and reduced toxicity, such as ketoconazole, abiraterone acetate, and other aromatase inhibitors.
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