Cholinergic and
Anticholinergic Drugs
Dr. Osama
Adrenergic and
Antiadrenergic Drugs
Prof. Khatab
Quiz?
Major neurotransmitter
released at end organ
effectors of the thoracolumbar
division of the autonomic
nervous system:-
dopamine
adrenaline
noradrenaline
acetylcholine
Quiz?
Preganglionic fibers
terminating on adrenal
medullary chromaffin cells
release:-
a- noradrenaline
b- adrenaline
c- acetylcholine
d- dopamine
Quiz?
Activation of the sympathetic
nervous system will cause which
change in the skeletal muscle
versus cutaneous vascular beds?
vasoconstriction,vasoconstriction
vasodilatation, vasodilatation
vasodilatation, vasoconstriction
vasoconstriction, vasodilation
1-Synthesis of Acetylcholine
Drugs that impair Ach. Synthesis:-
1-Direct inhibitors of choline
acetyltransferase:- BromoacetylCoA.
2-Inhibitors of choline transport
Hemicholiniums
Quiz?
Rate-limiting step in
acetylcholine synthesis:-
choline acetyltransferase
activity.
vesicular protein synthesis.
choline uptake.
acetylcholinesterase activity
availability of acetate
2-Storage of Acetylcholine:-
Ach is stored in vesicles.
Vesicular –associated transporter.
Quiz?
Inhibits choline
transport into
cholinergic vesicles:-
bretylium
vesamicol
reserpine
atropine
3-Release
of Ach:-
“excitation –
release
coupling” .
exocytosis
Quiz?
Influx of this ion
promotes fusion
between axoplasmic
membrane and nearby
vesicles:-
sodium
potassium
calcium
chloride
Drugs affecting Ach. Release:-
Botulinum toxin from [Link].
prevention of transmission
agglutination of RBC’s.
Quiz?
Clostridium
toxins inhibit:-
Acetylcholinesterase
prevent reuptake of
choline .
inhibit vesicular
acetylcholine release.
prevent calcium influx
Botulinum
Quiz?
The following drugs all have
the ability to inhibit
acetylcholine release from
cholinergic nerve terminals,
but by different
mechanisms. Describe the
mechanism of action of:-
a. Hemicholinium
b. Vesamicol
c. Botulinus toxin
Hydrolysis of Ach. is by cholinesterases.
Types of cholinesterases:-
1-True or specific cholinesteraseSpecific
substrate is methacholine.
2-Pseudocholinesterase:- Specific
substrates are succinylcholine
They both act on acetylcholine.
Cholinesterase is inhibited by
neostigmine.
Quiz?
True"
acetylcholinesterase
is found in:-
A- intestine
B-liver
C- erythrocytes
D- plasma
Muscarinic & nicotinic receptors
Muscarinic receptors , 5 subtypes
M1: ‘neuronal’
Excitatory,
Formation of IP3,DAG & Ca++.
Antagonist is pirenzepine
M2: ‘cardiac’.
Inhibitory effect
Openning of K+ channels, of adenylate
cyclase.
Antagonist is gallamine
M3:-’glandular, smooth muscles’.
Excitatory mainly,
vascular smooth muscles NO release
antagonist is hexahydrosiladifenol [HHSD]
M5 ,cerebral blood vessels →dilatation.
All are G-
protein coupled
receptors.
M1,M3,M5
inositol
triphosphate
M2,M4
adenylate
cyclase
Quiz?
Cholinergic receptor
type that mediates the
decrease in heart rate
by activating potassium
channels:-
a - M1– muscarinic
b - M2-muscarinic
c -M3-muscarinic
d -nicotinic
Quiz?
Cholinergic receptor type
that mediates vasodilation
following low-dose i.v.
acetylcholine
administration:-
a nicotinic
muscarinic
nitric oxide receptor
substance P receptor
Nicotinic receptors:-Nm ‘muscle’
& Nn ‘neuronal’
They are both ligand –gated.
Agonist at Nm is decamethonium, at Nn is
epibatidine.
Antagonist at Nm is
- bungarotoxin,
at Nn is mecamylamine
