Anticholinesterases: endplate and central nervous system effects
THE CONTEXT
The interpretable text describes neuromuscular blockade from persistent endplate depolarization and the central effects of brain-penetrating anticholinesterases.
Neuromuscular effects
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Persistent depolarization of muscle endplates blocks neuromuscular transmission, causing weakness and paralysis.
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The direct action of neostigmine and its congeners at muscle endplates augments these effects.
Central nervous system effects
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Lipophilic anticholinesterases that penetrate the brain produce a generalised alerting response and may improve cognitive function in Alzheimer's disease.
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Higher doses produce excitement, mental confusion, disorientation, tremors and convulsions, followed by coma.
Enzyme reactivation
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The figure caption describes reactivation of phosphorylated cholinesterase by an oxime.