Glossary of cholinomimectics and cholin-antagonists

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neostigmine and physostigmine are ____. THey provide a ____ duration of effect.
anticholinesterases, long
Describe the mechanism of Ach binding to Achesterase.
Ach binds to the active/anionic ester site of Achesterase. First is the breaking of the ester bond to release choline. Next you have the intermediate sitting in the active site. last you have hydrolysis and the release of acetate.
Neostigmine is a _____ ammonium compound. Will it cross into the BBB?
quaternary, NO!!
Physostigmine is a ____ amine. Will it cross the BBB?
tertiary, YES!!
After Neostigmine binds to the active site of Achesterase, if forms an ____ intermediate.
How long is the effect of neostigmine?
2-3 hours
Name an example of an irreversible choline esterase inhibitor. How long does it stay boung to the active site of AchEsterase? This is know as ____.
DFP (nerve gas), weeks, to months, aging
What therapy can you provide if somehas has an irreversible Achesterase inhibitor.
2-PAM and atropine
What is a "side effect"
2-PAM prevents aging and thus reactivates Achesterase. It is possible to get OVER activation of the muscarinic receptors b/c now there are TONS of Ach available. Give atropine(antimuscarinic) to control this problem.
____ is the dominant influence on the GI tract.
T or F: Physostigmine can cause tremor, anxiety, restlessness, disruptive concentration and memory.
True, it can cross the BBB
echothiophate is _____.
_____ is an irreversible anticholinesterase.
How long does edrophonium last and what special use does it have?
very short--like 5 minutes, it is used to diagnose MG.
Name 3 carbamates.
1- neostigmine
2- pyridostigmine
3- physostigmine
Intermediate acting anticholinesterases are used to _______.
treat MG
Atropine is a ______.
You can use atropine to manage ______.
_______ is a quaternary derivative of atropine, thus it is an ______.
Ipratropium, antimuscarinic
Give _______ to antagonize the symptoms of asthma.
What drug is used for motion sickness?
Does Scopolamine cross the BBB?
Is Benztropine useful in management of Parkinsons?
Tropicamide in conjuction with ______ is useful to asses the retina.
how long does mydriasis last when using atropine?
7-10 days
How long does mydriasis last when using scopolamine?
3-7 days
How long does mydriasis last when using homatropine?
1-3 days
How long does mydriasis last when using cyclopentolate?
1 day--great for kids
How lond does mydriasis last when using tropicamide?
1/4 day

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