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20 Cards in this Set
- Front
- Back
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list the main ACh-R antagonists
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curare, atropine
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what are the effects of M2 Receptors?
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inhibit adenylyl cyclase, which hyperpolarizes cell (G-IRK channels), thus work in negative feedback at neuron, or reducing HR and contractility
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what type of cholinergic receptors are in CNS?
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both nicotinic and muscarinic
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describe bethanecol
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bethanecol, w/ a quaternary amine, is a Muscarinic-R agonist
-resistant to AChE -no nicotinic activity -used to stimulate GI/bladder |
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describe pilocarpine
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tertiary amine (gets to CNS! oral! topical!), Muscarinic-R agonist, w/ no nicotinic activity
-resistant to ACh |
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what type of amine is in muscarine?
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quaternary
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what type of amine is in nicotine?
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tertiary
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nicotine poisoning will lead to:
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all ganglia activated - sympa and parasympa; NMJ activated -> depolarization blockade, CNS - alerted, tremor, convulsions
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treating nicotine poisoning -
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treat w/ atropine (mostly limits Heart ganglia parasympa effects), diazepam for convulsions, mechanical breathing if paralysis
(not trimethaphan or curare??) |
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where is AChE found?
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on post synaptic membrane at neuro synapse and NMJ. also on RBC membrane
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describe edrophonium, including charge
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REV inhib of AChE. quaternary amine
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what is the main use of edrophonium? why can't it be used more broadly?
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edrophonium has a very short half life, so its use is limited to Dxing the effectiveness of other myasthenia gravis medication. if it leads to depolarization block, dose is ok/high. if it helps, dose is too low
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list the carbamates
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physostigmine(tertiary); neostigmine, pyridostigmine (both quaternary)
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what is the MOA and uses of carbamates?
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Inhibit AChE, 1/2 life 2 hours, used in MG and reversal of NMJ blockade after surgery
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what is a common ingredient in insecticides?
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malathion, an organophosphate
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how do organophosphates work
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they are lipophilic - easy uptake thru skin. IRREV inhibit AChE.
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how does pralidoxime work?
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it attacks the organophosphate as it is enzyme-bound, generating the native enzyme, AChE. however, organophosphate-enzyme complex can change to a non-reactive form, so 2-PAM must be given early or prophylactically
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prototype organophosphate?
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DFP, diisopropylfluorophophate
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what AChE-I can be used for early Alzheimer's patients?
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Donepezil
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carbamates and organophosphates have similar effects. how can carbamates be used to block organophosphates?
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carbamates have shorter half lives than organophosphates (hours vs months) so carbamates can be used to inhibit AChE, then if organophosphates are introduced (warfare) their target will be occupied, and they will be excreted from body
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