出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/09/14 20:28:23」(JST)
An acetylcholinesterase inhibitor (often abbreviated AChEI) or anti-cholinesterase is a chemical or a drug that inhibits the acetylcholinesterase enzyme from breaking down acetylcholine, thereby increasing both the level and duration of action of the neurotransmitter acetylcholine. Acetylcholinesterase inhibitors are classified as reversible, irreversible, or quasi-irreversible (also called pseudo-irreversible).[1]
Acetylcholinesterase inhibitors:[2]
Potential side effects of acetylcholinesterase inhibitors[10][11] | |||
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mild – usually goes away | potentially serious | ||
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Some major effects of cholinesterase inhibitors:
Administration of reversible cholinoesterase inhibitors is contraindicated with those that have urinary retention due to obstruction.
When used in the central nervous system to alleviate neurological symptoms, such as rivastigmine in Alzheimer's disease, all cholinesterase inhibitors require doses to be increased gradually over several weeks, and this is usually referred to as the titration phase. Many other types drug treatments may require a titration or stepping up phase. This strategy is used to build tolerance to adverse events or to reach a desired clinical effect.[12] This also prevents accidental overdose and is therefore recommended when initiating treatment with drugs that are extremely potent and/or toxic (drugs with a low therapeutic index).
Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:
Inhibitor | Duration | Main site of action | Clinical use | Adverse effects |
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Edrophonium | short (10 min.)[21] | neuromuscular junction[21] | diagnosis of myasthenia gravis[21] | |
Neostigmine | medium (1–2 hrs.)[21] | neuromuscular junction[21] |
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visceral[21] |
Physostigmine | medium (0.5-5 hrs.)[21] | postganglionic parasympathetic[21] | treat glaucoma (eye drops)[21] | |
Pyridostigmine | medium (2–3 hrs.)[21] | neuromuscular junction[21] |
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Dyflos | long[21] | postganglionic parasympathetic[21] | historically to treat glaucoma (eye drops)[21] | toxic[21] |
Echothiophate (irreversible) | long[21] | postganglionic parasympathetic[21] | treat glaucoma (eye drops)[21] | systemic effects[21] |
Parathion (irreversible) | long[21] | none[21] | toxic[21] |
Compounds which function as quasi-irreversible inhibitors of cholinesterase are those most likely to have use as chemical weapons or pesticides. These include:
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Pharmacology: enzyme inhibition
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Psychoanaleptics: Antidementia agents (N06D)
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AChE inhibitors |
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Others |
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Nootropics
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Ampakines |
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Cholinergics |
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Racetams |
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Nutrients |
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Others |
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Cholinergics
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リンク元 | 「コリンエステラーゼ阻害薬」 |
拡張検索 | 「acetylcholinesterase inhibitors」 |
関連記事 | 「inhibitor」「cholinesterase」「cholinesterases」 |
種類 | 疾患への適応 |
ムスカリン作動薬 | 緑内障、手術後の腸管麻痺、尿閉 |
コリンエステラーゼ阻害薬 | 緑内障、手術後の腸管麻痺、尿閉、重症筋無力症の診断・治療、アルツハイマー病 |
ムスカリン受容体遮断薬 | 鎮痙薬(消化管、胆管、尿路など)、胃・十二指腸潰瘍、散瞳薬、パーキンソン病、麻酔前投与 |
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