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達那唑
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臨床資料 | |
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商品名 | Danatrol, Danocrine, Danol, Danoval, others |
其他名稱 | WIN-17757; 2,3-Isoxazolethisterone; 2,3-Isoxazol-17α-ethynyltestosterone; 17α-Ethynyl-17β-hydroxyandrost-4-en-[2,3-d]isoxazole |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682599 |
懷孕分級 |
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给药途径 | 口服给药 |
藥物類別 | 雄激素、同化類固醇、黄体制剂、孕激素、抗促性腺激素、固醇類合成抑制劑、抗動情素藥物 |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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藥物動力學數據 | |
生物利用度 | Saturable with dosage, higher with food intake |
血漿蛋白結合率 | 會與白蛋白、SHBG, CBG結合 |
药物代谢 | 肝臟(CYP3A4) |
代謝產物 | • 2-OHM-Ethisterone • Ethisterone |
生物半衰期 | Acute: 3–10 hours Chronic: 24–26 hours |
排泄途徑 | 尿、糞便 |
识别信息 | |
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CAS号 | 17230-88-5 |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.037.503 |
化学信息 | |
化学式 | C22H27NO2 |
摩尔质量 | 337.463 g/mol |
3D模型(JSmol) | |
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達那唑(Danazol)為一種用於治療子宮內膜異位症、乳腺小叶增生、遺傳性血管性水腫及其他疾病的藥物,主要經口服给药。
達那唑具有雄性化的副作用,使其用途大受限制。常見不良反應包含痤疮、多毛症,以及聲音變低沉。達那唑的作用機轉複雜,同時具有弱雄激素、弱同化類固醇、弱孕激素,弱抗促性腺激素、弱固醇類合成抑制劑,以及功能性抗動情素藥物。
達那唑發現於1963年,並於1971年應用於醫學。隨著副作用更少的性腺激素釋放素類似物應用逐漸廣泛,達那唑在治療子宮內膜異位症的角色已被前者所取代。
參考文獻
延伸閱讀
- Dmowski WP. Endocrine properties and clinical application of danazol. Fertil. Steril. March 1979, 31 (3): 237–51. PMID 374128. doi:10.1016/S0015-0282(16)43869-0.
- Fraser IS. Danazol--a steroid with a unique combination of actions. Scott Med J. April 1979, 24 (2): 147–50. PMID 386503. doi:10.1177/003693307902400209.
- Potts GO, Schane HP, Edelson J. Pharmacology and pharmacokinetics of danazol. Drugs. May 1980, 19 (5): 321–30. PMID 6993179. doi:10.2165/00003495-198019050-00001.
- Jenkin G. Review: The mechanism of action of danazol, a novel steroid derivative. Aust N Z J Obstet Gynaecol. May 1980, 20 (2): 113–8. PMID 6998453. doi:10.1111/j.1479-828X.1980.tb00107.x.
- Barbieri RL, Ryan KJ. Danazol: endocrine pharmacology and therapeutic applications. Am. J. Obstet. Gynecol. October 1981, 141 (4): 453–63. PMID 7025640. doi:10.1016/0002-9378(81)90611-6.
- Dmowski WP. Danazol. A synthetic steroid with diverse biologic effects. J Reprod Med. January 1990, 35 (1 Suppl): 69–74; discussion 74–5. PMID 2404115.
- Barbieri RL. Danazol: molecular, endocrine, and clinical pharmacology. Prog. Clin. Biol. Res. 1990, 323: 241–52. PMID 2406750.
- Hughes E, Brown J, Tiffin G, Vandekerckhove P. Danazol for unexplained subfertility. Cochrane Database Syst Rev. January 2007, (1): CD000069. PMID 17253444. doi:10.1002/14651858.CD000069.pub2.
- Beaumont H, Augood C, Duckitt K, Lethaby A. Danazol for heavy menstrual bleeding. Cochrane Database Syst Rev. July 2007, (3): CD001017. PMID 17636649. doi:10.1002/14651858.CD001017.pub2.
- Selak V, Farquhar C, Prentice A, Singla A. Danazol for pelvic pain associated with endometriosis. Cochrane Database Syst Rev. October 2007, (4): CD000068. PMID 17943735. doi:10.1002/14651858.CD000068.pub2.
- Craig TJ. Appraisal of danazol prophylaxis for hereditary angioedema. Allergy Asthma Proc. 2008, 29 (3): 225–31. PMID 18387221. doi:10.2500/aap.2008.29.3107.
- Ke LQ, Yang K, Li J, Li CM. Danazol for uterine fibroids. Cochrane Database Syst Rev. July 2009, (3): CD007692. PMID 19588442. doi:10.1002/14651858.CD007692.pub2.
- Letchumanan P, Thumboo J. Danazol in the treatment of systemic lupus erythematosus: a qualitative systematic review. Semin. Arthritis Rheum. February 2011, 40 (4): 298–306. PMID 20541792. doi:10.1016/j.semarthrit.2010.03.005.
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