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35 Cards in this Set

  • Front
  • Back
rate limiting step of cholinergic neurotransmission is ___
Ch uptake
ACh is synthesized by ___ from ___ and ___
choline acetyltransferase (ChAT)
choline
Ac CoA
hemicholinium inhibits ___
Ch uptake
botulinum Tx inhibits ___
ACh exocytosis
muscarinic receptor structure
7TM GPLR
nicotinic receptor structure
5 subunit pentamer
M1, M3 and M5 signal via ___. M2 and M4 signal via ___
Gq
Gi
M1 is present in ___ (2).
nerves
brain
M2 is present in ___ (3)
cardiac muscle
nerves
GIT smooth muscle
M3 is present in ___ (3)
glands
smooth muscle
endothelium
N1 is also called ___ and is present in ___
NN
dendrites & somata of post-ganglionic cells
effects of cholinergic agonists on eye (2)
contraction of iris sphincter -> miosis
contraction of ciliary muscle -> accomodation
effects of cholinergic agonists on SA node
negative chronotropy
effects of cholinergic agonists on atria
decreased contractility
effects of cholinergic agonists on AV node (2)
decreased refractory period
decreased conduction velocity
effects of cholinergic agonists on ventricles (2)
increased refractory period
small decrease in contractility
effects of cholinergic agonists on blood vessels at low & high dose
low dose: vasodilation via endothelial M3 mediated NO release
high dose: vasoconstriction via direct action on smooth muscle M3
methacholine acts most strongly on ___. Is it susceptible to ChE? Does it have nicotinic action?
heart
yes
yes, weak
carbachol acts most strongly on ___ (2). Is it susceptible to ChE? Does it have nicotinic action?
GIs smooth muscle
bladder
no
yes, strong
bethanechol acts most strongly on ___ (2). Is it susceptible to ChE? Does it have nicotinic action?
GIs smooth muscle
bladder
no
no
___ can cause excitation block, leading to ___
carbachol
flaccid paralysis
cisapride action (2 steps)
agonizes 5-HT4R in myenteric plexus
postganglionic cell releases ACh
metoclopramide action (3 steps)
agonizes 5-HT4R and antagonizes DA
reduces GI inhibition from DA
causes ACh release
AChE anionic site function (2)
binds quaternary amine
positions ACh
AChE esteratic site function
attacks the acyl carbon
because of ___, pyridostigmine and neostigmine are used to treat MG
no CNS action
edrophonium is a short acting AChE inhibitor because ___. it is used for ___ (2).
it doesn't bind covalently to the esteratic site
diagnosing MG
managing MG drug doses
criteria for MG diagnosis (2)
alleviation of symptoms with edrophonium
no tongue fasciculation
___ can undo phosphorylation of AChE, but not after ___.
oxime aka PAM
aging
of the 4 short/medium duration AChE inhibitors, only ___ affects CNS, because ___
physostigmine
it's a tertiary amine so it can cross BBB
3 long duration AChE inhibitors are ___. they are used for ___.
tacrine
donepezil
rivastigmine
Alzheimer's
treatment for glaucoma is either ___ or ___
muscarinic agonist
AChE inhibitor
rocuronium is metabolized by
liver
2 short-acting non-depolarizing ACh blockers
rocuronium
mivacurium
mivacurium is metabolized by
plasma ChE