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Ach對Muscarinic receptor跟Nicotinic 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:
- Diarrhea (Diaphoresis) 腹瀉(發汗)
- Urination排尿
- Miosis瞳孔縮小
- Bronchospasm(secretion)支氣管痙攣(分泌)
- Bradycardia心動過緩
- Excite skeletal muscle and CNS (Emesis)刺激骨骼肌和中樞神經系統(嘔吐)
- Lacrimation流淚
- Lethargy昏睡
- 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)如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
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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