氢羟肾上腺皮质素

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氢羟肾上腺皮质素(英语:Hydrocortisone),又称氢化皮质酮氢化可体松,是皮质醇作为药物的名称[13]。它是一种糖皮质激素,具有抗炎免疫抑制作用。可以治疗:肾上腺机能不全英语Adrenal_insufficiency肾上腺生殖器综合症高血钙甲状腺炎类风湿性关节炎皮肤炎哮喘慢性阻塞性肺病(COPD)等疾病[1]。它是治疗肾上腺机能不全的首选药物[14]。此药可以口服、局部涂抹或注射给药[1]。在长期使用而要停药时,应逐渐减少后才能完全停用[1]

氢羟肾上腺皮质素
临床资料
商品名英语Drug nomenclatureA-hydrocort, Cortef, Solu-cortef, others[1]
其他名称Cortisol; 11β,17α,21-Trihydroxypregn-4-ene-3,20-dione; 11β,17α,21-Trihydroxyprogesterone
AHFS/Drugs.comMonograph
MedlinePlusa682206
核准状况
怀孕分级
给药途径口服给药 (片剂), 静脉注射, 外涂, 肛门给药英语rectal administration
药物类别英语Drug class皮质类固醇; 糖皮质素; 矿物皮质素
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度口服: 96 ± 20%[10][11]
血浆蛋白结合率92 ± 2% (92–93%)[10][11]
药物代谢11β-HSDs, 其它[11]
代谢产物可体松, 其它[11]
药效起始时间英语Onset of action口服: 1.2 ± 0.4 hours (Tmax)[10]
生物半衰期1.2–2.0 小时[10][11]
作用时间8–12 小时[12]
识别信息
  • (8S,9S,10R,11S,13S,14S,17R)-11,17-Dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
CAS号50-23-7  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
化学信息
化学式C21H30O5
摩尔质量362.47 g·mol−1
3D模型(JSmol英语JSmol
  • O=C4\C=C2/[C@]([C@H]1[C@@H](O)C[C@@]3([C@@](O)(C(=O)CO)CC[C@H]3[C@@H]1CC2)C)(C)CC4
  • InChI=1S/C21H30O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h9,14-16,18,22,24,26H,3-8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1 checkY
  • Key:JYGXADMDTFJGBT-VWUMJDOOSA-N checkY

它的副作用包括情绪改变、增加感染风险和水肿[1]。长期使用后,常见副作用包括骨质疏松胃部不适身体虚弱、容易瘀青念珠菌感染[1]。虽然可以在怀孕期使用,但安全性仍未确认[15]

此药于 1936 年获得专利,并于 1941 年获准用于治疗[16] [17]。并列入世界卫生组织基本药物标准清单[18],市面上有多家学名药[1]。2014年发展中国家每日口服药物的每日费用约0.27美元[19]。在美国,一个月的治疗费用通常不到 25美元[20]。 2017 年,它是美国最常用处方药的第 154 名,开立的处方超过 400 万张[21] [22]

参考资料

  1. ^ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 Hydrocortisone. Drugs.com. American Society of Health-System Pharmacists. February 9, 2015 [30 August 2016]. (原始内容存档于20 September 2016). 
  2. ^ Prescribing medicines in pregnancy database. Therapeutic Goods Administration (TGA). [21 February 2021]. (原始内容存档于20 December 2016). 
  3. ^ Hydrocortisone Notice of enforcement policy (PDF). FDA. [31 December 2022]. (原始内容存档 (PDF)于12 March 2023). 
  4. ^ Ala-cort- hydrocortisone cream. DailyMed. [21 February 2021]. (原始内容存档于27 October 2020). 
  5. ^ Ala-scalp- hydrocortisone lotion. DailyMed. [21 February 2021]. (原始内容存档于21 April 2021). 
  6. ^ Alkindi Sprinkle- hydrocortisone granule. DailyMed. [21 February 2021]. (原始内容存档于10 February 2022). 
  7. ^ Anusol HC- hydrocortisone acetate suppository. DailyMed. [21 February 2021]. (原始内容存档于10 February 2022). 
  8. ^ Cortef- hydrocortisone tablet. DailyMed. [21 February 2021]. (原始内容存档于17 April 2021). 
  9. ^ Efmody EPAR. European Medicines Agency (EMA). 24 March 2021 [14 June 2021]. (原始内容存档于14 June 2021).  Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  10. ^ 10.0 10.1 10.2 10.3 Czock D, Keller F, Rasche FM, Häussler U. Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clinical Pharmacokinetics. 2005, 44 (1): 61–98. PMID 15634032. S2CID 24458998. doi:10.2165/00003088-200544010-00003. 
  11. ^ 11.0 11.1 11.2 11.3 11.4 Lennernäs H, Skrtic S, Johannsson G. Replacement therapy of oral hydrocortisone in adrenal insufficiency: the influence of gastrointestinal factors. Expert Opinion on Drug Metabolism & Toxicology. June 2008, 4 (6): 749–758. PMID 18611115. S2CID 73248541. doi:10.1517/17425255.4.6.749. 
  12. ^ Liu D, Ahmet A, Ward L, Krishnamoorthy P, Mandelcorn ED, Leigh R, Brown JP, Cohen A, Kim H. A practical guide to the monitoring and management of the complications of systemic corticosteroid therapy. Allergy Asthma Clin Immunol. August 2013, 9 (1): 30. PMC 3765115 . PMID 23947590. doi:10.1186/1710-1492-9-30 . 
  13. ^ Becker, Kenneth L. Principles and Practice of Endocrinology and Metabolism. Lippincott Williams & Wilkins. 2001: 762. ISBN 9780781717502. (原始内容存档于2016-09-14) (英语). 
  14. ^ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 202. ISBN 9781284057560. 
  15. ^ Hydrocortisone Pregnancy and Breastfeeding Warnings. Drugs.com. [1 September 2016]. (原始内容存档于20 September 2016). 
  16. ^ 美国专利第2,183,589号
  17. ^ Fischer, Jnos; Ganellin, C. Robin. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 484 [2019-03-01]. ISBN 9783527607495. (原始内容存档于2019-03-02) (英语). 
  18. ^ WHO Model List of Essential Medicines (19th List) (PDF). World Health Organization. April 2015 [8 December 2016]. (原始内容存档 (PDF)于13 December 2016). 
  19. ^ Hydrocortisone. International Drug Price Indicator Guide. [1 September 2016]. (原始内容存档于2018-08-27). 
  20. ^ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 202. ISBN 9781284057560. 
  21. ^ The Top 300 of 2020. ClinCalc. [11 April 2020]. (原始内容存档于12 February 2021). 
  22. ^ Hydrocortisone - Drug Usage Statistics. ClinCalc. [11 April 2020]. (原始内容存档于12 April 2020).