抗膽鹼酯酶(Acetylcholinesterase, AChE inhibitor)

膽鹼酯酶(AChE)位於節後神節(post-synaptic membrane)分解Ach,停止AchMuscarinic receptorNicotinic receptor的刺激。如果我們使用藥物使AChE無法作用,將導致Ach在神經間隙大量累積、持續刺激。因此AChE inhibitor又被稱作「間接型致效劑」(Indirect agonists)。其中又可分為可逆型跟不可逆型:
  • 可逆型:Edrophonium, Neostigmine, Pryidostigmine
  • 不可逆型:有機磷(Organophosphates) 
      殺蟲劑
    (insecticides)Parathion, Malathion 
      神經毒氣
    (nerve agents)Soman, Sarin

常見的副作用似副交感神經興奮過度,以口訣DUMBBELLS背誦:
  1. Diarrhea (Diaphoresis) 腹瀉(發汗)
  2. Urination排尿
  3. Miosis瞳孔縮小
  4. Bronchospasm(secretion)支氣管痙攣(分泌)
  5. Bradycardia心動過緩
  6. Excite skeletal muscle and CNS (Emesis)刺激骨骼肌和中樞神經系統(嘔吐)
  7. Lacrimation流淚
  8. Lethargy昏睡
  9. Salivate流涎

用藥過度或中毒時的治療:
  • Atropine: 拮抗Muscarinic receptor的作用(anti-muscarinic agent)
  • Pralidoxime (2-PAM): 用於有機磷中毒

*補充:直接型致效劑(direct agonists)Methacholine, Carbachol, Bethanechol, Pilocarpine直接作用在Ach receptor上,模仿其作用。

Reference:
Harvard-MIT Division of Health Sciences and Technology
HST.151: Principles of Pharmocology

Instructor: Dr. Carl Rosow, Dr. David Standaert and Prof. Gary Strichartz

留言

  1. Acetylcholinesterase, also known as AChE or acetylhydrolase, is a hydrolase that hydrolyzes the neurotransmitter acetylcholine. AChE is found at mainly neuromuscular junctions and cholinergic brain synapses, acetylcholinesterase>

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