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Anticholinesterases

QuestionAnswer
What enzyme is responsible for the breakdown of ACh? Acetylcholineesterase
How do antidotes to acetylcholinesterase inhibtors work? e.g. 2-PAM chemically displace phosphoryl group to reactivate enzyme (prevents aging by irreversibly bound inhibitors)
Why are many anticholinesterase drugs poor BBB crossers? They are normally charged (mimic charged moeity of ACh)
Why is it ok to use organophosphate drugs on the eye (for glaucoma)? Do not appreciably enter the circulation
What drug could you use to diagnose myasthenia gravis? How could you treat it? short acting anticholinesterase (edrophonium); it allows acetylcholine to persist in synaptic cleft longer; longer acting anticholinesterases with atropine (for muscarinic ADR)
Why are anticholinesterases used for in surgery? Used to displace NMJ blocking agents (after surgery); CANNOT be used with succinylcholine (depolarizing drug)
How can anticholinesterases be used in the eye? Used to reduce presure in WIDE ANGLE GLAUCOMA and to reverse ATROPINE POISNONING
How do you treat anticholinesterase toxicity? Atropine (for muscarinic receptors and CNS effects) and 2-PAM for the PNS
What drug is believed to have caused gulf war syndrome? pyridostigmine
What is the long term pathological effect of organophosphates? Demyelination and axon loss due to inhibition of another esterase: neuropathy target esterase
What is pseudocholinesterase? plasma enzyme made in liver; not required for survival, but may account for differences among individuas in sensitivity / time course of cholinergics
Created by: karkis77
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