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非索非那定 .
非索非那定 臨床資料 商品名 originally Allegra, others[1] AHFS /Drugs.com Monograph MedlinePlus a697035 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 Y PubChem CID IUPHAR/BPS DrugBank ChemSpider UNII KEGG ChEBI ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.228.648 化学信息 化学式 C 32 H 39 N O 4 摩尔质量 501.68 g/mol 3D模型(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
Y
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 等副作用 。
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。含有鋁 或鎂 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
^ Fexofenadine - international brand names . Drugs.com. [18 January 2017] . (原始内容 存档于2021-04-21) (英语) .
^ 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 .
^ 3.0 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 .
外部連結
氨基烷基醚
溴苯海拉明
Carbinoxamine
氯马斯汀
Chlorphenoxamine
Diphenylpyraline
苯海拉明
多西拉敏
Orphenadrine
Phenyltoloxamine
脂肪胺 替代物
溴苯那敏
氯苯那敏
Dexbrompheniramine (Dexbrompheniramine/pseudoephedrine )
Dexchlorpheniramine (Betamethasone/dexchlorpheniramine )
二甲茚定
非尼拉敏
Talastine
乙二胺 替代物
Chloropyramine
Histapyrrodine
Mepyramine
Methapyrilene
Tripelennamine (pyribenzamine)
吩噻嗪 衍生物
Alimemazine
Hydroxyethylpromethazine
Isothipendyl
Mequitazine
Methdilazine
奥索马嗪
鹽酸異丙嗪
哌嗪 衍生物其它三环化合物 其他全身使用
Antazoline
Bamipine
依巴斯汀
依美斯汀
Mizolastine
Pyrrobutamine
Quifenadine
Triprolidine
選擇使用 (Acrivastine
Astemizole
氮䓬斯汀
Bilastine
非索非那定
Terfenadine )
外用
Bamipine
Chloropyramine
Chlorphenoxamine
氯马斯汀
二甲茚定
苯海拉明
Isothipendyl
Mepyramine
鹽酸異丙嗪
Thenalidine
組胺受體 調節劑
組胺受體
H2
激動劑 : Amthamine
Betazole
Dimaprit
組織胺
HTMT
Impromidine
UR-AK49 拮抗劑 : Bisfentidine
Burimamide
西咪替丁
Dalcotidine
Donetidine
Ebrotidine
Etintidine
法莫替丁
Lafutidine
Lamtidine
Lavoltidine/Loxtidine
Lupitidine
Metiamide
Mifentidine
Niperotidine
Nizatidine
Osutidine
Oxmetidine
Pibutidine
Quisultazine/Quisultidine
Ramixotidine
雷尼替丁
Roxatidine
Sufotidine
Tiotidine
Tuvatidine
Venritidine
Xaltidine
H3
激動劑 : α-Methylhistamine
Cipralisant
組織胺
Imetit
4-(1H-咪唑-5-基甲基)哌啶
Immethridine
Methimepip
Proxyfan 拮抗劑 : A-349,821
A-423,579
ABT-239
Betahistine
Burimamide
Ciproxifan
Clobenpropit
Conessine
GSK-189,254
Impentamine
Iodophenpropit
JNJ-5,207,852
MK-0249
NNC-38-1,049
PF-03654746
替洛利生
SCH-79,687
Thioperamide
VUF-5,681
H4
激動劑 : 4-甲基组胺
組織胺
VUF-8,430 拮抗劑 : JNJ-7,777,120
Thioperamide
VUF-6,002
轉運
VMAT
抑製劑: Ibogaine
利血平
Tetrabenazine
酶
抑製劑: 儿茶素
Meciadanol
Naringenin
Tritoqualine
抑製劑: Amodiaquine
苯海拉明
Harmaline
Metoprine
Quinacrine
SKF-91,488
Tacrine
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