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Acetylcholinesterase inhibitor

Synonyms: AChEI, anti-cholinesterase
German: Acetylcholinesterase-Blocker

1 Definition

Substances that inhibit the action of the acetylcholinesterase (AChe) enzyme in the synaptic cleft are referred to as Acetylcholinesterase inhibitors or anti-cholinesterases.

2 Physiology

Cholinergic neurons transmit their excitation via the release of acetylcholine into the synaptic cleft. There the acetylcholine binds to the receptors on the secondary side. Acetylcholinesterase inactivates the acetylcholine molecules through hydrolysis.

3 Clinical Relevance

When the neuronal excitability is supposed to be increased, for example in the case of Alzheimer’s disease, it can be achieved through the inhibition of the degrading enzymes, which in this case would be the acetylcholinesterase. This mechanism of action is used by many drugs. For example the therapy of Alzheimer’s disease with rivastigmine (Exelon®), donepezil (Aricept®) or tacrine (Cognex®) and galanthamine (Reminyl®) is based on this principle. Also the mechanism of action of physostigmine is based on the same idea. However the clinical effectiveness of these substances is critically debated by some authors.

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