達那唑

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[5][1][10][11][12],主要經口服给药[1]

達那唑
系统(IUPAC)命名名称
(1S,2R,13R,14S,17R,18S)-17-ethynyl-2,18-dimethyl-7-oxa-6-azapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-ol
临床数据
商品名Danatrol, Danocrine, Danol, Danoval, others
Drugs.comMonograph
MedlinePlusa682599
妊娠分级
  • AU: D
  • US: X (禁忌)
给药途径口服给药
合法狀態
合法状态
  • AU: 限医生处方 (S4)
  • CA: 处方药(-only)
  • UK: 处方药(-only) (POM)
  • US: 处方药(-only)
药代动力学数据
生物利用度Saturable with dosage, higher with food intake[1]
蛋白结合度會與白蛋白SHBG, CBG結合[2][3][4]
代谢肝臟CYP3A4[5][6][7][1][8]
代謝產物2-OHM-Ethisterone[6]
Ethisterone[8][9]
生物半衰期Acute: 3–10 hours[5][1]
Chronic: 24–26 hours[5]
排泄尿糞便[5][1]
识别
CAS注册号17230-88-5  
ATC代码G03XA01
PubChemCID 28417
IUPHAR/BPS6942
DrugBankDB01406 
ChemSpider26436 
UNIIN29QWW3BUO 
KEGGD00289 
ChEBICHEBI:4315 
ChEMBLCHEMBL1479 
其他名称WIN-17757; 2,3-Isoxazolethisterone; 2,3-Isoxazol-17α-ethynyltestosterone; 17α-Ethynyl-17β-hydroxyandrost-4-en-[2,3-d]isoxazole
化学
化学式C22H27NO2
摩尔质量337.463 g/mol

達那唑具有雄性化副作用,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[1][13]。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[4][7][14][7][14][15]

達那唑發現於1963年,並於1971年應用於醫學[7][16][17][18]。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[3]

參考文獻

  1. https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/017557s033s039s040s041s042lbl.pdf
  2. J.P. Griffin; P.F. D'Arcy. . Elsevier. 17 November 1997: 194–. ISBN 978-0-08-052583-9.
  3. Eberhard Nieschlag; Hermann M. Behre; Susan Nieschlag. . Springer Science & Business Media. 13 January 2010: 426–428. ISBN 978-3-540-78355-8.
  4. Eric J. Thomas; John Rock. . Springer Science & Business Media. 6 December 2012: 239–256. ISBN 978-94-011-3864-2.
  5. Brayfield, A (编). . Martindale: The Complete Drug Reference. Pharmaceutical Press. 30 October 2013 [1 April 2014].
  6. Thomas L. Lemke; David A. Williams. . Lippincott Williams & Wilkins. 24 January 2012: 1361–. ISBN 978-1-60913-345-0.
  7. Howard W. Jones; John A. Rock. . Wolters Kluwer Health. 10 July 2015: 1327–1330. ISBN 978-1-4963-1521-2.
  8. Florencio Zaragoza Dörwald. . John Wiley & Sons. 4 February 2013: 485–. ISBN 978-3-527-64565-7.
  9. Robert J. Kurman. . Springer Science & Business Media. 17 April 2013: 390–. ISBN 978-1-4757-3889-6.
  10. J. Elks. . Springer. 14 November 2014: 345–. ISBN 978-1-4757-2085-3.
  11. . Taylor & Francis. January 2000: 293–. ISBN 978-3-88763-075-1.
  12. I.K. Morton; Judith M. Hall. . Springer Science & Business Media. 6 December 2012: 91–. ISBN 978-94-011-4439-1.
  13. Selak V, Farquhar C, Prentice A, Singla A. Farquhar C , 编. . Cochrane Database of Systematic Reviews. 2007, (4): CD000068. PMID 17943735. doi:10.1002/14651858.CD000068.pub2.
  14. Aurel Lupulescu. . CRC Press. 24 October 1990: 103–. ISBN 978-0-8493-5973-6.
  15. Albert Altchek; Liane Deligdisch; Nathan Kase. . Academic Press. 4 September 2003: 376–. ISBN 978-0-08-049451-7.
  16. G.P. Ellis and G.B. Ellis, doi:10.1016/S0079-6468(08)70187-5 (1979),  pp. 126, note 158, 130, notes 1513, 2369, citing doi:10.1021/jm00299a034
  17. Alan N. Elias; Grant Gwinup. . Praeger. 1 January 1983: 70.
  18. Dmowski WP, Scholer HF, Mahesh VB, Greenblatt RB. . Fertil. Steril. 1971, 22 (1): 9–18. PMID 5538758. doi:10.1016/S0015-0282(16)37981-X.

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