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盐酸异丙嗪

异丙嗪
临床资料
AHFS/Drugs.comMonograph
MedlinePlusa682284
怀孕分级
  • 澳: C
给药途径Oral, rectal, IV, IM, topical
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度88% absorbed but after first-pass metabolism reduced to 25% absolute bioavailability[1]
血浆蛋白结合率93%
药物代谢Hepatic glucuronidation and sulfoxidation
生物半衰期10-19 hours[1][2]
排泄途径Renal and biliary
识别信息
  • (RS)-N,N-dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine
CAS号60-87-7  checkY
58-33-3（盐酸盐）  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.000.445 编辑维基数据链接
化学信息
化学式C17H20N2S
摩尔质量284.42 g/mol
3D模型（JSmol（英语：JSmol））
  • S2c1ccccc1N(c3c2cccc3)CC(N(C)C)C
  • InChI=1S/C17H20N2S/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19/h4-11,13H,12H2,1-3H3 checkY
  • Key:PWWVAXIEGOYWEE-UHFFFAOYSA-N checkY

盐酸异丙嗪（英语：Promethazine，又名盐酸普鲁米近（Promethazine Hydrochloride）或非那根（Phenergan））是一种常见的止咳药物，为第一代抗组胺药，能竞争性阻断组胺H1受体，对抗组胺所致之毛细血管扩张，并降低其通透性。因此，能够平复因为气管受刺激而引起的咳嗽。

有糖浆溶液及片状两种，以糖浆溶液较常见，呈铬黄色，药性与可待因相似，忌光，可令服用者口干及产生睡意。这种药水在其他国家一般都很容易可以在药房无需处方购买。不过，由于在美国─特别是德萨斯州的休斯顿─经常被当地的年青人滥用，所以在美国需要医生处方才可以购买。

2006年4月25日，美国食品药物管理局发布有关盐酸异丙嗪药品安全警示，警告医生和家长含有盐酸异丙嗪药物不宜给不满两岁孩子，给超过两岁较年长的小孩，给予这些药物应该小心。美国食品药物管理局在这个安全警示说，已被证实关联到盐酸异丙嗪，而发生严重呼吸困难的22份报告中有7例死亡，所有儿童年龄均小于两岁。这种药物，最初于1951年批准，通常规定为抗组胺药或过敏药物。[3]3岁以下小孩不应注射盐酸异丙嗪药品。

参考书目

  • Katzung, Bertram G. "Basic and Clinical Pharmacology", 9th ed (2004). pp. 264–265.

参考文献

  1. ^ 1.0 1.1 Strenkoski-Nix LC, Ermer J, DeCleene S, Cevallos W, Mayer PR. Pharmacokinetics of promethazine hydrochloride after administration of rectal suppositories and oral syrup to healthy subjects. American Journal of Health-system Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists. August 2000, 57 (16): 1499–505 [2012-01-18]. PMID 10965395. （原始内容存档于2020-03-06）. 
  2. ^ Paton DM, Webster DR. Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clinical Pharmacokinetics. 1985, 10 (6): 477–97. PMID 2866055. [永久失效链接]
  3. ^ Phenergan And Similar Drugs Associated With Infant Deaths. [2015-06-02]. （原始内容存档于2015-09-20）. 

外部链接

抗组胺药(ATC code R06（英语：ATC code R06）)
氨基烷基醚
脂肪胺替代物
乙二胺替代物
吩噻嗪衍生物
哌嗪衍生物
其它三环化合物
其他全身使用
外用
组胺受体（英语：Histamine receptor）调节剂
组胺受体（英语：Histamine receptor）
  • 未分组: Belarizine
  • Efletirizine
  • Elbanizine
  • Flotrenizine
  • Medrylamine（英语：Medrylamine）
  • Napactadine
  • Pibaxizine
  • Tagorizine
  • Trelnarizine
  • Trenizine
  • Vapitadine
H2（英语：Histamine H2 receptor）
H3（英语：Histamine H3 receptor）
H4（英语：Histamine H4 receptor）
转运（英语：Neurotransmitter transporter）
酶
其它相关
内源性
迷幻药物
5-HT2AR激动剂
麦角酰胺类（英语：Lysergamides）
25-NB（英语：25-NB）
其它
其它药物
解离性药物
NMDAR拮抗剂
  • 3-MeO-PCP
  • 4-MeO-PCP
  • Dieticyclidine
  • Diphenidine
  • Esketamine
  • Ethketamine
  • Eticyclidine
  • Gacyclidine
  • 氯胺酮
  • Methoxetamine
  • Methoxyketamine
  • Neramexane
  • PCPr
  • Phencyclidine
  • Rolicyclidine
  • Tenocyclidine
  • Tiletamine
其它药物
致谵妄药
mAChR拮抗剂
其它相关药物
D2R 激动剂（英语：Dopamine receptor agonists）
吸入剂（英语：Inhalant）
混合MOA
  • 二氢骆驼蓬碱
  • 骆驼蓬碱
  • 四氢骆驼蓬碱
  • 育亨宾
其它药物
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盐酸异丙嗪
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