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

Indirect-acting:
demecarium (reversible)
physostigmine (reversible)
isofluorophate (irreversible)
echothiaphate (irreversible)
4 cholinergic drugs used in the diagnosis and/or treatment of myasthenia gravis
edrophonium (diagnosis only)
ambenomium
pyridostigmine
neostigmine
2 cholinergic drugs used in the treatment of GI/GU atony
neostigmine
bethanecol
2 drugs completely resistant to acetylcholinesterase (AchE)
Carbachol
Bethanechol
1 cholinergic drug moderately resistant to AchE
methacholine
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)