氨鲁米特：一种化“副作用”为治疗优势的药物。
Aminoglutethimide: a "side-effect" turned to therapeutic advantage.
作者信息
Hughss S W, Burley D M
出版信息
Postgrad Med J. 1970 Jul;46(537):409-16. doi: 10.1136/pgmj.46.537.409.
Abstract
Aminoglutethimide was introduced as an anti-convulsant drug in the U.S.A. in 1960. The occurrence of a number of side-effects, including several endocrine effects such as goitrogenesis, sexual precocity and virilization, led to its withdrawal. Further investigation indicated that the drug inhibited adrenal biosynthesis, particularly of aldosterone, cortisol and androgens, probably by interfering with the conversion of cholesterol to delta-5-pregnenolone. Aminoglutethimide has also been shown to modify the extra-adrenal metabolism of cortisol. The possible clinical applications of these ‘side-effects’ are discussed.
摘要
1960年，氨鲁米特作为一种抗惊厥药物在美国被引入。由于出现了许多副作用，包括一些内分泌方面的影响，如甲状腺肿形成、性早熟和男性化，该药物被停用。进一步研究表明，该药物抑制肾上腺生物合成，特别是醛固酮、皮质醇和雄激素的合成，可能是通过干扰胆固醇向δ-5-孕烯醇酮的转化。氨鲁米特还被证明可以改变皮质醇的肾上腺外代谢。本文讨论了这些“副作用”可能的临床应用。
相似文献
1
Aminoglutethimide: a "side-effect" turned to therapeutic advantage.氨鲁米特：一种化“副作用”为治疗优势的药物。
Postgrad Med J. 1970 Jul;46(537):409-16. doi: 10.1136/pgmj.46.537.409.
2
[Clinical and biological study of an inhibitor of adrenocortical hormone synthesis: aminoglutethinide].肾上腺皮质激素合成抑制剂氨鲁米特的临床与生物学研究
Ann Endocrinol (Paris). 1968 Mar-Apr;29(2):189-210.
3
The treatment of congenital adrenal hyperplasia with aminoglutethimide.用氨鲁米特治疗先天性肾上腺皮质增生症。
Q J Med. 1971 Oct;40(160):568-9.
4
[Corticosteroidogenesis inhibitors. II. A new cortico-adrenal inhibitor: amino-glutethimide (16,038Ba)].[皮质类固醇生成抑制剂。II. 一种新的肾上腺皮质抑制剂：氨基谷氨酰胺（16,038Ba）]
Presse Med (1893). 1968 May 11;76(23):1107-10.
5
[Clinical experiences with aminoglutethimide (Elipten), a new inhibitor of steroid biosynthesis in the adrenal gland].[氨鲁米特（依立替坦）——一种新型肾上腺类固醇生物合成抑制剂的临床经验]
Schweiz Med Wochenschr. 1968 Nov 23;98(47):1843-51.
6
Fatty acid composition of the sterol ester fraction of human adrenal cortex in Cushingś syndrome and after treatment with aminoglutethimide.
Lipids. 1972 Jul;7(7):474-82. doi: 10.1007/BF02533164.
7
Effects of aminoglutethimide in a case of ectopic ACTH syndrome. Influence on steroid metabolism.氨鲁米特对异位促肾上腺皮质激素（ACTH）综合征一例的影响。对类固醇代谢的作用。
Acta Endocrinol (Copenh). 1970 Aug;64(4):676-86. doi: 10.1530/acta.0.0640676.
8
Amino-glutethimide (elipten) in adenocortical carcinoma.氨基谷氨酰胺（氨鲁米特）治疗肾上腺皮质癌。
Bol Asoc Med P R. 1968 Dec;60(12):611-8.
9
Qualitative alterations in urinary 17-ketosteroid excretion during aminoglutethimide administration.氨鲁米特给药期间尿17-酮类固醇排泄的定性改变。
J Clin Endocrinol Metab. 1969 Feb;29(2):297-9. doi: 10.1210/jcem-29-2-297.
10
Effect of aminoglutethimide and reserpine on the human pituitary-adrenal axis: remission of a case of Cushing's disease.氨鲁米特和利血平对人垂体-肾上腺轴的作用：库欣病一例的缓解
Metabolism. 1970 Oct;19(10):818-30. doi: 10.1016/0026-0495(70)90079-x.
引用本文的文献
1
Thiourea-functionalized aminoglutethimide derivatives as anti-leishmanial agents.硫脲功能化氨苯蝶啶衍生物作为抗利什曼原虫药物。
Future Med Chem. 2024 Aug 2;16(15):1485-1497. doi: 10.1080/17568919.2024.2359362. Epub 2024 Jul 2.
2
Towards understanding aromatase inhibitory activity via QSAR modeling.通过定量构效关系建模理解芳香酶抑制活性。
EXCLI J. 2018 Jul 20;17:688-708. doi: 10.17179/excli2018-1417. eCollection 2018.
3
Suppression of estrogens with aminoglutethimide and hydrocortisone (medical adrenalectomy) as treatment of advanced breast carcinoma: a review.用氨鲁米特和氢化可的松抑制雌激素（药物性肾上腺切除）治疗晚期乳腺癌：综述
Breast Cancer Res Treat. 1981;1(3):183-202. doi: 10.1007/BF01806259.
4
Effect of hormonal therapy on plasma testosterone levels in prostatic carcinoma.激素疗法对前列腺癌患者血浆睾酮水平的影响。
Br Med J. 1971 Nov 13;4(5784):391-4. doi: 10.1136/bmj.4.5784.391.
5
Treatment of Cushing's disease with adrenal blocking drugs and megavoltage therapy to the pituitary.用肾上腺阻断药物及垂体的兆伏级放疗治疗库欣病。
Proc R Soc Med. 1974 Dec;67(12 Pt 1):1225. doi: 10.1177/003591577406712P113.
6
Effects of aminoglutethimide (Elipten Ciba), a steroid biosynthesis blocking agent, on adrenal glands in Cushing's syndrome.
Virchows Arch A Pathol Pathol Anat. 1973;360(1):11-26. doi: 10.1007/BF00548654.
7
Could aminoglutethimide replace adrenalectomy?氨鲁米特能否替代肾上腺切除术？
Breast Cancer Res Treat. 1985;6(3):201-11. doi: 10.1007/BF01806770.
8
Mechanisms of action of aminoglutethimide as endocrine therapy of breast cancer.氨鲁米特作为乳腺癌内分泌治疗的作用机制
Drugs. 1988 Jun;35(6):685-710. doi: 10.2165/00003495-198835060-00005.
9
Proceedings: Preliminary pharmacological study of N,2-dimethyl,2-(p-aminophenyl) succinimide.论文：N,2-二甲基,2-(对氨基苯基)琥珀酰亚胺的初步药理学研究
Br J Pharmacol. 1975 Jun;54(2):242P.
10
Drug-induced endocrine disorders.药物性内分泌紊乱。
Drugs. 1977 May;13(5):353-65. doi: 10.2165/00003495-197713050-00002.
本文引用的文献
1
The metabolism of gluethimide (Doriden).格鲁米特（多睡丹）的代谢
Experientia. 1962 Mar 15;18:105-11. doi: 10.1007/BF02153841.
2
Elipten: A clinical evaluation of a new anticonvulsant. Preliminary report.依立普坦：一种新型抗惊厥药的临床评估。初步报告。
Can Med Assoc J. 1960 May 7;82(19):953-9.
3
Elipten in the treatment of organic epilepsy.埃利普坦治疗器质性癫痫。
Dis Nerv Syst. 1960 Apr;21:230-3.
4
EFFECT OF DIPHENYLHYDANTOIN ON CORTISOL METABOLISM IN MAN.二苯乙内酰脲对人体皮质醇代谢的影响。
J Clin Invest. 1964 Sep;43(9):1824-35. doi: 10.1172/JCI105056.
5
DIAGNOSTICALLY CONFUSING COMPLICATIONS OF DIPHENYLHYDANTOIN THERAPY. A REVIEW.苯妥英治疗的诊断混淆并发症。综述。
Ann Intern Med. 1963 Dec;59:914-30. doi: 10.7326/0003-4819-59-6-914.
6
Treatment of advanced malignancy and Cushing's syndrome with DDD.用双氯苯二氯乙烷（DDD）治疗晚期恶性肿瘤和库欣综合征。
Cancer Chemother Rep. 1962 Feb;16:335-9.
7
[A new anticonvulsant: the preparation Ciba 16-0-38 or elipten. Its importance in refractory epilepsy].一种新型抗惊厥药：西巴16-0-38制剂或依立替坦。其在难治性癫痫中的重要性
Ann Med Psychol (Paris). 1961 Mar;119(1):501-18.
8
Aminoglutethimide in the treatment of epilepsy.氨鲁米特治疗癫痫
Can Med Assoc J. 1961 Feb 18;84(7):374-6.
9
A clinical trial with a new anticonvulsant drug, alpha-(p-aminophenyl)-alpha-ethyl glutarimide preparation 16038 (Ciba).一项使用新型抗惊厥药物α-（对氨基苯基）-α-乙基戊二酰亚胺制剂16038（汽巴公司）的临床试验。
J Ment Sci. 1959 Apr;105(439):448-56. doi: 10.1192/bjp.105.439.448.
10
Diphenylhydantoin (dilantin) after 20 years; a review with re-emphasis by treatment of 84 patients.20年后的苯妥英（大仑丁）；对84例患者治疗情况的回顾及重点再强调
Pediatrics. 1959 Jan;23(1 Pt 1):151-61.
Zotero 插件