NM

NMJ Pharmacology
Acetylcholine Synthesis Blockers

Hemicholinium Not used Competitive No Ach synthesis

inhibitor of choline
uptake (acts on
choline active
transport
mechanism) (not
taken up itself)
Vesamicol Not used Prevents packaging No Ach synthesis
of Ach into vesicles
Triethylcholine Not used Inhibits choline No Ach synthesis
uptake, taken up
and acetylated to
acetyltriethylcholine.
Stored as a false
neurotransmitter

Ach release blocker

Botulinum Toxin Muscle spasms, Degradation of Prevents release

(Botox) migraine, eyelid SNAP-23 (SNARE of vesicles
spasm/twitch, protein)
paralyse facial
muscles to
alleviate wrinkles

Muscarinic Agonists (Cholinomimetics)

Pilocarpine and Used in eye drops Acts on Cause miosis, Poor absorption
Carbachol for glaucoma and muscarinic increases from the GI tract
after cataract receptors aqueous humour and has
surgery outflow, and considerable side
carbachol effects
stimulates
bladder emptying
(effects resemble
parasympa
stimulation)
 Muscarinic antagonists

Atropine In eye drops, as a Competitively In eye: mydriasis,

drying agent, blocks Ach cycloplegia, and
counteract receptor sites increase in
muscarinic effects intraocular
of neostigmine pressure
GIT effects:
Reduce hyper-
motility states,
relaxes the GIT
and bladder, and
causes enuresis
among children.
Cardiovascular:
Low doses
decrease cardiac
rate, high doses
increase cardiac
rate, and toxic
levels dilate the
cutaneous
vasculature.
Secretions:
causes
xerostomia,
blocks sweat
glands,
xeropthalmia, and
blocks secretions
in the upper and
lower respiratory
tracts

AchE inhibitors/Indirect cholinomimetics

Tacrine, Alzheimer’s Tacrine:

Donepezil, disease Prototypical AchE
Rivastigmine, inhibitor
Galantamine Donepezil:
Centrally acting
reversible AchE
inhibitor
Rivastigmine:
Used for
Parkinson’s
Disease
Galantamine:
Competitive
reversible AchE
inhibitor
 NMJ Blockers

D-Tubocurare Relaxant during Binds to nicotinic Decrease in EPP,

surgery to stop receptors at NMJ relaxation of
muscle spasms as a competitive Skeletal muscle,
antagonist motor paralysis
(eyes first
respiratory last),
lowers BP, and
produces
bronchoconstriction
Succinylcholine Muscle relaxant Block is caused Muscle relaxant Pain, raises intra-
in anaesthesia by membrane gastric pressure,
depolarization dangerous if
and maintains it serum K+ is
above threshold, raised,
which may lead dangerous if
to muscle second dose
twitching and given quickly,
muscles revert to may cause
flaccid state malignant
rather than hyperthermia
tetany.