Figure 125

Action of AChE at a cholinergic neuroeffector function and effects of AChE inhibition. A. Key features of cholinergic neurotransmission in the absence of drugs. After release from a cholinergic nerve terminal or varicosity, ACh can (1) bind reversibly to cholinergic receptors in the postsynaptic membrane and elicit a response or (2) bind to AChE and undergo hydrolysis to choline and acetic acid (inactive metabolites). The survival time of released ACh is quite brief because of the abundance and effectiveness of AChE. B. The consequences of inhibiting AChE. Since ACh no longer has access to the active site of AChE, the concentration of ACh in the synaptic cleft increases. This can result in enhanced transmission due to (3) repeated activation of receptors and (4) activation of additional cholinergic receptors.

sion, including that in the adrenal medulla, can produce complicated effects on the cardiovascular system, including vasoconstrictor responses. The activation of reflexes can also complicate the total cardiovascular response to cholinesterase inhibitors.

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