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氟康唑

氟康唑
INN fluconazole
临床资料
怀孕分级
给药途径口服、静注、局部
ATC码
法律规范状态
法律规范
  • S3/S4 (Au), POM (UK), ℞-only (U.S.),处方药(CN)
药物动力学数据
生物利用度>90%
血浆蛋白结合率11–12%
药物代谢肝脏 11%
生物半衰期30小时 (可在20-50小时之间)
排泄途径肾脏 61–88%
识别信息
  • 2-(2,4-difluorophenyl)-
    1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol
CAS号86386-73-4  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.156.133 编辑维基数据链接
化学信息
化学式C13H12F2N6O
摩尔质量306.271 g/mol

氟康唑[1]INN:fluconazole)又称氟康那唑[2],属于氟代三唑抗真菌药,对白念珠菌犬小孢子菌新型隐球菌表皮癣菌荚膜组织胞浆菌等有强力抗菌活性,一般认为氟康唑透过干扰真菌的细胞膜合成达成抑制真菌生长的效果[3]

氟康唑可用于治疗多种真菌病[3],例如念珠菌症芽生菌病山谷热隐球菌病组织胞浆菌病皮癣菌病花斑癣[3]。对于罹病风险较高的患者,如:曾接受器官移植、低体重的新生儿、及嗜中性白血球低下等,氟康唑也可以用预防念珠菌病[3]。氟康唑可经口服静脉注射给药[3]

氟康唑于1981年获得专利,于1988年开始商业贩售[4]。本品名列于世界卫生组织基本药物标准清单[5],已有学名药[3]于市面上流通;2019年,于美国最常使用的药物中排行第133名,共开立逾五百万剂[6][7]

氟康唑常见的副作用为呕吐、腹泻、红疹及肝指数上升英语elevated transaminases[3]。严重的副作用有肝脏疾病长QT综合症、及癫痫发作[3]。使用于怀孕的患者,可能会增加流产风险;高剂量使用可能会导致新生儿先天性障碍[8][3]

药理

氟康唑是抗真菌药剂﹙口服或静脉注射﹚。大扶康是口服药胶囊。服食后有效成分存在于血液﹑尿﹑皮﹑汗﹑泪﹑体液等,属全身性药物。

它能抑制真菌霉菌﹙例如: 念珠菌﹚繁殖,但不能真的把霉菌杀死。

用途

常用于医治妇女阴道念珠菌症。

注意事项

有人对唑类药物出现药物敏感反应,出现不同副作用。包括呕吐头痛头晕肚痛﹑对肝脏造成损害等等。因为如果对此药敏感药物过敏反应严重可致死亡。

“氟康唑”在大部分国家属于“须医生处方药物”,所以不宜随便自行购买服用。

有研究指唑类药物可能影响女性怀孕内分泌而影响怀孕[9]。高剂量会降低 estrogen 雌激素(女性荷尔蒙)。

氟康唑与若干心脏病用药有化学反应,严重可致死亡。此药与14种有不同程度互相影响干扰,但药厂方面没有研究药物与药物之间的相互作用干扰。

参考文献

  1. ^ 存档副本. [2023-12-26]. (原始内容存档于2023-12-26). 
  2. ^ https://terms.naer.edu.tw/search/?csrfmiddlewaretoken=FXPwE2HVn7icqejw4WUfnykT7YVh2bf8ppKvAGXwQCslXZs2lNvZKZxsOMVJR6iA&match_type=phrase&query_op=&query_field=title&query_term=fluconazole
  3. ^ 3.0 3.1 3.2 3.3 3.4 3.5 3.6 3.7 3.8 Fluconazole. The American Society of Health-System Pharmacists. [8 December 2016]. (原始内容存档于20 December 2016). 
  4. ^ Fischer, Janos; Ganellin, C. Robin. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 503. ISBN 9783527607495. (原始内容存档于2017-09-10) (英语). 
  5. ^ World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. hdl:10665/325771可免费查阅. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO. 
  6. ^ The Top 300 of 2019. ClinCalc. [16 October 2021]. (原始内容存档于2020-03-18). 
  7. ^ Fluconazole - Drug Usage Statistics. ClinCalc. [16 October 2021]. (原始内容存档于2020-07-08). 
  8. ^ Fluconazole (Diflucan): Drug Safety Communication - FDA Evaluating Study Examining Use of Oral Fluconazole (Diflucan) in Pregnancy. FDA. 2016-04-26 [29 April 2016]. (原始内容存档于2016-04-29). 
  9. ^ ASSESSING PREGNANCY RISKS OF AZOLE ANTIFUNGALS USING A HIGH THROUGHPUT AROMATASE INHIBITION ASSAY: Endocrine Research: Vol 28, No 3. [2016-08-31]. (原始内容存档于2021-06-14). 

外部链接

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氟康唑
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