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米替福新

维基百科,自由的百科全书
米替福新
臨床資料
商品名英语Drug nomenclatureImpavido, Miltex, others
AHFS/Drugs.comMonograph
核准狀況
给药途径口服给药
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度
血漿蛋白結合率~98%
药物代谢慢 肝 (非依賴-CYP)
生物半衰期6 至 8 天 和 31 天[1]
排泄途徑Primarily fecal
识别信息
  • 2-(hexadecoxy-oxido-phosphoryl)oxyethyl-trimethyl-azanium
CAS号58066-85-6  ☒N
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
NIAID ChemDB
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.151.328 編輯維基數據鏈接
化学信息
化学式C21H46NO4P
摩尔质量407.58 g·mol−1
3D模型(JSmol英语JSmol
熔点232至234 °C(450至453 °F)
  • [O-]P(=O)(OCCCCCCCCCCCCCCCC)OCC[N+](C)(C)C
  • InChI=1S/C21H46NO4P/c1-5-6-7-8-9-10-11-12-13-14-15-16-17-18-20-25-27(23,24)26-21-19-22(2,3)4/h5-21H2,1-4H3 checkY
  • Key:PQLXHQMOHUQAKB-UHFFFAOYSA-N checkY

米替福新(Miltefosine)是主要用於治疗利什曼病和自由生活的阿米巴病(如:福氏耐格里變形蟲巴氏阿米巴變形蟲英语Balamuthia mandrillaris的口服药物[3] [4]。利什曼病則包括三种類型:皮膚型英语Visceral leishmaniasis內臟型英语Cutaneous leishmaniasis和黏膜型[4]。它可与脂質體两性霉素B巴龙霉素併用[5]

常见副作用包括呕吐、腹痛、发热頭痛和肾功能下降[3]。更严重的副作用包括可能史蒂芬斯-強森症候群血小板減少症[3]怀孕期使用可能对婴儿有害,因此也不建议在母乳哺育期使用[3]。作用機轉仍不完全清楚[3]

米替福新于 20 世纪 80 年代初首次合成,并被當成對抗癌症的治療[6]。几年后,人们发现它可用於治疗利什曼病,并于 2002 年在印度取得治疗利什曼病的醫療使用許可[7]。名列世界卫生组织基本药物标准清单[8]

参考文獻

  1. ^ Dorlo TP, Balasegaram M, Beijnen JH, de Vries PJ. Miltefosine: a review of its pharmacology and therapeutic efficacy in the treatment of leishmaniasis. The Journal of Antimicrobial Chemotherapy. November 2012, 67 (11): 2576–2597. PMID 22833634. doi:10.1093/jac/dks275可免费查阅. 
  2. ^ Anvisa. RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control]. Diário Oficial da União英语Diário Oficial da União. 2023-03-31 (2023-04-04) [2023-08-16]. (原始内容存档于2023-08-03) (巴西葡萄牙语). 
  3. ^ 3.0 3.1 3.2 3.3 3.4 American Society of Health-System Pharmacists. Miltefosine Monograph for Professionals. www.drugs.com. 26 February 2016 [16 November 2016]. (原始内容存档于17 November 2016). 
  4. ^ 4.0 4.1 FDA approves Impavido to treat tropical disease leishmaniasis. U.S. Food and Drug Administration (FDA) (新闻稿). 19 March 2014 [30 August 2014]. (原始内容存档于3 September 2014). 
  5. ^ World Health Organization. Control of the leishmaniasis: report of a meeting of the WHO Expert Committee on the Control of Leishmaniases. World Health Organization. March 2010: 59, 88, 186. ISBN 9789241209496. 
  6. ^ Greenwood, David. Antimicrobial Drugs: Chronicle of a Twentieth Century Medical Triumph. OUP Oxford. 2008: 310. ISBN 9780199534845. (原始内容存档于2017-09-10). 
  7. ^ Kumar, Awanish. Leishmania and Leishmaniasis. Springer Science & Business Media. 2013: 39. ISBN 9781461488699. (原始内容存档于2017-09-10). 
  8. ^ World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO. 

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