Cholinergic Drugs Flashcards
what is the main neurotransmitter of cholinergic drugs
acetylcholine
what are the precursors of acetylcholine
acetyl coenzyme A
choline
where is acetyl coenzyme A derived and synthesized from
derived: pyruvate
Synthesized: mitochondria
True or False:
choline uptake is a rate limiting step
true
what are the choline transport systems
high affinity transport system
synaptic vesicles by vesicular transporters
what is the inhibitor of the high affinity transport system of choline
hemicholinium
what is the inhibitor of the synaptic vesicles of ACh transport
vesamicol
how is acetylcholine released
exocytosis
what can inhibit the release of acetylcholine
botulinum toxins
what can bind to the receptors of cholinergic nerve terminals to interupt the SNARE complex components
clostridium toxins
which animal uses clostridium toxins to their advantage to kill
black widow spiders
what enzyme is used to hydrolyze ACh
acetylcholinesterase
what is the purpose of AChE
recycling of choline to increase ACh synthesis
where is AChE synthesized
autonomic ganglia
neuromuscular motor endplates
visceral neuroeffector junctions
what is the pseudo chE
butyrylcholinesterase
where is butyrylcholinesterase synthesized
liver
what is the purpose of butyrylcholinesterase
metabolism of certain drugs
what occurs if there is an inhibition of AChE
accumulation of ACh in nerve terminal
which receptors are involved with cholinergic receptors
nicotinic and muscarinic receptors
what type of receptor are nicotinic receptors
ligand gated ion channel
what is the main result of activating a nicotinic receptor
skeletal muscle contraction
where are nicotinic receptors found
autonomic ganglion
adrenal medulla
CNS
what type of receptors are muscarinic receptors
GPCR
what are the responses of activating muscarinic receptors
excitatory
inhibitory
where are non-innervated muscarinic receptors found
vascular endothelium
which muscarinic receptor is normally found as non-innervated in blood vessels
M3
where are M1 receptors found
ganglia
secretory glands
where are M2 receptors found
myocardium
smooth muscle
where are M3 & M4 receptors found
smooth muscle and secretory glands
where are M5 receptors found
CNS
what is the most common muscarinic receptor
M5
which muscarinic receptors activate Gq proteins
M1
M3
M5
(odd receptors)
what type of responses are expected with the activation of M1, M3 or M5 receptors
excitatory
what muscarinic receptors are responsible for “relaxation”
M2
M4
which muscarinic receptors act on Gi protein
M2
M4
what is the result of M2 receptor activation of the heart muscle
decreased HR
decrease impulse conduction / contraction
what is the effect of activating M3 receptors of smooth muscle
increase in contraction (GI system)
what is the effect of activating M3 receptors of secretory glands
increased secretion
how do M3 receptors in vascular endothelium cause vasodilation
release of NO
what are the 2 types of cholinergic agonists
direct and indirect
how do indirect cholinergic agonists work
inhibit cholinesterase to cause accumulation of ACh
what are the direct acting agonists
carbachol
bethanechol
pilocarine
what are the reversible indirect cholinergic agonists
physostigmine
neostigmine
edrophonium
pyridostigmine
what is the irreversible indirect agonist
organophosphate
how do low doses of acetylcholine impact the cardio vascular system
rapid fall in pressure –> reflex tachycardia
muscarinic receptors of vascular endothelium are activated (M3 creates vasodilation)
what are the effects of high doses of acetylcholine
vasodilation –> decreased peripheral resistance and BP
slow HR (- chronotropic effect)
- inotropic effect
slow SA and AV node conduction
decreased cardiac output