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非索非那定

非索非那定
Skeletal formula of fexofenadine
Ball-and-stick model of fexofenadine
臨床資料
商品名英语Drug nomenclatureoriginally Allegra, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa697035
核准狀況
懷孕分級
给药途径口服
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度30-41%[2]
血漿蛋白結合率60-70%[3]
药物代谢Hepatic (≤5% of dose)[3]
生物半衰期14.4小時
排泄途徑Feces (~80%) and urine (~10%) as unchanged drug[3]
识别信息
  • (±)-4-[1-Hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]-α, α-dimethyl benzeneacetic acid
CAS号83799-24-0  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.228.648 編輯維基數據鏈接
化学信息
化学式C32H39NO4
摩尔质量501.68 g/mol
3D模型(JSmol英语JSmol
手性Racemic mixture
  • O=C(O)C(c1ccc(cc1)C(O)CCCN2CCC(CC2)C(O)(c3ccccc3)c4ccccc4)(C)C
  • InChI=1S/C32H39NO4/c1-31(2,30(35)36)25-17-15-24(16-18-25) 29(34)14-9-21-33-22-19-28(20-23-33)32(37, 26-10-5-3-6-11-26)27-12-7-4-8-13-27/h3-8, 10-13,15-18,28-29,34,37H,9,14,19-23H2,1-2H3,(H,35,36) ☒N
  • Key:RWTNPBWLLIMQHL-UHFFFAOYSA-N checkY

非索非那定(fexofenadine),販賣藥名為艾來錠(Allegra),劑型為60mg,120mg或180mg錠劑。是特芬那定(Terfenadine)衍生而來的活性代謝物,它是一種具有選擇性末稍H1受體拮抗活性的抗組織胺藥。非索非那定的兩種鏡像異構物均可顯現效力相當的抗組織胺作用,被稱為第二代抗組織胺的它不會通過大腦血管障壁(blood brain barrier,BBB),不會有前代製品例如嗜睡副作用

適應症

緩解季節性過敏性鼻炎引起的相關症狀,緩解慢性原發性蕁麻疹相關症狀。

注意事項

果汁類飲料會影響藥物的吸收及降低藥效,葡萄柚可以顯著降低非索非那定的血藥濃度,應該盡量避免一起服用。含有的抗胃酸劑同樣會降低藥物的吸收。另外酮康唑(抗黴菌藥物)或者红霉素(抗生素)會增強此藥的吸收,使此藥的劑量增強,如果與上述藥物合用時,至少應該與此藥相隔約兩小時。

註釋

  1. ^ Fexofenadine - international brand names. Drugs.com. [18 January 2017]. (原始内容存档于2021-04-21) (英语). 
  2. ^ Lappin G, Shishikura Y, Jochemsen R, Weaver RJ, Gesson C, Houston B, Oosterhuis B, Bjerrum OJ, Rowland M, Garner C. Pharmacokinetics of fexofenadine: evaluation of a microdose and assessment of absolute oral bioavailability. Eur J Pharm Sci. May 2010, 40 (2): 125–31. PMID 20307657. doi:10.1016/j.ejps.2010.03.009. 
  3. ^ 3.0 3.1 3.2 Smith, SM; Gums, JG. Fexofenadine: biochemical, pharmacokinetic and pharmacodynamic properties and its unique role in allergic disorders.. Expert Opinion on Drug Metabolism & Toxicology. July 2009, 5 (7): 813–22. PMID 19545214. doi:10.1517/17425250903044967. 

參考文獻

外部連結

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非索非那定
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