5.16
抗コリンエステラーゼ剤：中毒と治療
Anticholinesterase agents prevent acetylcholine hydrolysis to enhance cholinergic actions.
Organophosphates—a type of anticholinesterase—interact covalently with AChE, yielding an irreversible phosphorylated enzyme.
It further undergoes aging with the loss of an alkyl group, and the complex formed is resistant to hydrolytic regeneration.
Aging inhibits AChE functioning and promotes acetylcholine accumulation, potentiating cholinergic responses leading to acute toxicity.
The handling of anticholinesterases, such as insecticides, can lead to accidental poisoning, and the symptoms manifest as a result of muscarinic and nicotinic activation.
In organophosphate poisoning, cholinesterase reactivators, such as pralidoxime, are effective before the enzyme undergoes aging. Pralidoxime binds to the anionic site of the enzyme through its charged quaternary nitrogen, while the oxime end reacts with the phosphorus atom. The resulting complex diffuses away, reactivating the enzyme.
The muscarinic symptoms are managed by IV administration of atropine.
Other treatment measures include gastric lavage, maintaining blood pressure, and ensuring airway patency.
抗コリンエステラーゼ剤、別名コリンエステラーゼ阻害剤とも呼ばれていますが、アセチルコリンの分解を阻害し、その蓄積をシナプス間隙で引き起こします。この蓄積は間接的にムスカリン作用とニコチン作用の両方を強化します。これらの薬物は、作用機序に基づいて可逆性または不可逆性に分類されます。
不可逆性の薬物は、…
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