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56 Cards in this Set
- Front
- Back
Acetylcholine (Ach)
|
direct acting cholinergic agonist
very short duration of action degraded primarily by AchE |
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Methacholine
|
direct acting cholinergic agonist
more selective for M receptors longer acting than Ach |
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Carbachol
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direct acting cholinergic agonist
not very selective used locally (e.g., glaucoma) |
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Bethanechol
|
direct acting cholinergic agonist
long acting selective for M receptors |
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Muscarine
|
direct acting cholinergic agonist
selective for M receptors |
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Pilocarpine
|
direct acting cholinergic agonist
selective for M receptors |
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Nicotine
|
direct acting cholinergic agonist
selective for N receptors |
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Lobeline
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direct acting cholinergic agonist
selective for N receptors |
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Cevilemine
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direct acting cholinergic agonist
selective for M receptors |
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Ach use(s)
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produces complete miosis in eye surgery
|
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Carbachol use(s)
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produces complete miosis in eye surgery
|
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Methacholine use(s)
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diagnosis of bronchial airway hyperreactivity
|
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Bethanechol use(s)
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bladder and GI hypotonia
|
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Muscarine use(s)
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none
|
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Pilocarpine use(s)
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Glaucoma
Sjogren's syndrome |
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Oxotremorine use(s)
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used as experimental model of Parkinson's disease tremor
|
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chem structure of neostigmine
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quaternary amine
|
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chem structure of physostigmine
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tertiary amine
|
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chem structure of carbaryl
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tertiary amine
|
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chem structure of edrophonium
|
quaternary amine
|
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tubocurarine
|
competitive antagonist of Ach
selective for Nm non-depolarizing neuromuscular blocker |
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Doxacurium
|
competitive antagonist of Ach
selective for Nm non-depolarizing neuromuscular blocker |
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Pancuronium
|
competitive antagonist of Ach
selective for Nm non-depolarizing neuromuscular blocker |
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Atracurium
|
competitive antagonist of Ach
selective for Nm non-depolarizing neuromuscular blocker |
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Succinylcholine
|
non-competitive ("irreversible") cholinergic agonist
selective for Nm depolarizing neuromuscular blocker occupies receptor and blocks end plate channel causes persistent depolarization |
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nicotine
|
direct acting cholinergic agonist
selective for N receptor |
|
McN-A-343
(from virtual dog lab) |
cholinergic agonist
selective for M1 |
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Oxotremorine receptor selectivity
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M1 M2 M3
|
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Methacholine receptor selectivity
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M1 M2 M3
|
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Carbamylcholine receptor selectivity
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M1 M2 M3 Nn
|
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Ach receptor selectivity
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M1 M2 M3 Nn Nm
|
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N-methylatropine
|
cholinergic antagonist
nonselective |
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Atropine
|
cholinergic antagonist
selective for M receptor |
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Pirenzepine
|
cholinergic antagonist
selective for M1 |
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Tiotropium
|
cholinergic antagonist
selective for M3 |
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Hexamethonium
|
cholinergic antagonist
selective for Nn |
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Trimethaphan
|
cholinergic antagonist
selective for Nn |
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Mecamylamine
|
cholinergic antagonist
selective for Nn |
|
Tubocurarine selectivity
|
cholinergic antagonist
selective for N |
|
direct-acting cholinergic agonist selective for N receptor
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nicotine
|
|
2 direct-acting cholinergic agonists that produce complete miosis in eye surgery
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Ach
Carbachol |
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2 direct-acting cholinergic agonists used for smoking cessation
|
nicotine
lobeline |
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name 6 irreversible indirect-acting cholinergic agonists. these 6 also classified as?
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echothiaphate
isofluorophate parathion malathion Soman Sarin (all 6 are organophosphates) |
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Name 3 drugs used as insecticides
|
parathion
malathion carbaryl |
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Name 2 drugs used as nerve gases. Class?
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soman and sarin
organophosphates (irreversible indirect-acting cholinergic agonists) |
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drug used in the diagnosis of myasthenia gravis. class? duration of action?
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edrophonium
reversible indirect-acting cholinergic agonist 5-15 min DOA |
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name 9 direct-acting cholinergic agonists
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Ach
Muscarine Nicotine Bethanechol Carbachol Pilocarpine Methacholine Cevimeline Lobeline |
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name 11 reversible indirect-acting cholinergic agonists
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carbaryl
ambenomium edrophonium neostigmine physostigmine pyridostigmine rivastigmine oxotremorine galantamine tacrine donepezil |
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2 reversal agents for organophosphates
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pralidoxime (PAM, Tupam) -- must be given before aging process; doesn't cross BBB
atropine ("heroic" doses) -- crosses BBB to reverse CNS effects |
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8 cholinergic drugs used in the treatment of glaucoma
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direct-acting:
pilocarpine (most commonly used) carbechol methacholine neostigmine Indirect-acting: demecarium (reversible) physostigmine (reversible) isofluorophate (irreversible) echothiaphate (irreversible) |
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4 cholinergic drugs used in the diagnosis and/or treatment of myasthenia gravis
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edrophonium (diagnosis only)
ambenomium pyridostigmine neostigmine |
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2 cholinergic drugs used in the treatment of GI/GU atony
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neostigmine
bethanecol |
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2 drugs completely resistant to acetylcholinesterase (AchE)
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Carbachol
Bethanechol |
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1 cholinergic drug moderately resistant to AchE
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methacholine
|
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talsaclidine: class? receptor selectivity?
|
cholinergic agonist
selective for M1 used in Alzheimer's dz |
|
Gallamine: class? receptor selectivity? clinical use? undesired effect?
|
competitive cholinergic antagonist
nondepolarizing NM blocker also has M2 blocking activity (incr HR) |