CHOLINERGICS

DIRECT
NON-SELECTIVE MOA USES SE NOTES
ACETYLCHOLINE Act on Miotic during DUMBELLS Short lived
- Primary NT in both M&N ocular surgery DOA – 5-30
all autonomic receptors. s
ganglia at the
synapses Activates Rapidly
between M1-M3 hydrolyzes
parasympathetic receptors by AChE
post ganglion in all
and at the peripheral  secretion,
Somatic tissues smooth
(voluntary) muscle
skeletal muscle contraction
(except
vascular
SM) &
changes in
HR
MUSCARINIC MOA USES SE NOTES
BETHANECOL Activates Bladder & Atony Cyclospasm,  secretion,
CARBACHOL M1-M3 (post-surgery or Diarrhea, Urinary smooth
receptors spinal cord urgency, muscle
injury) vadodilation, contraction
Reflex (except
CARBACHOL – tachycardia, vascular
for glaucoma & Sweating SM)
used as mitotic
Resistant to
AChE

Orally
active

Acts on M
receptor
only
PILOCARPINE Activates Glaucoma DUMBELLS Good lipid
CIVEMELINE M3 solubility
receptors Sicca syndrome compared to
on Ciliary choline
Muscles esters
(aq.
Humor
outflow) &
 Salivary Sjogren syndrome
glands (
salivation)

NICOTINIC MOA USES SE NOTES

NICOTINE Activates Smoking Generalized OVERDOSE:
VARENICLINE – nicotinic cessation ganglionic Coma
(selective partial Ach stimulation Convulsions
agonist at nicotinic receptors (hypertension, Paralysis
receptors) – DOA: 12- (Nn&Nm) tachycardia,
24hr. nausea, vomiting, Activates
diarrhea) autonomic
post-
ganglionic
neurons
(para&sympa)
& skeletal
muscle
neuromuscular
end plates

DOA: 1-6 hr
only

INDIRECT
MOA USES SE NOTES
NEOSTIGMINE Inhibits Myasthenia DUMBELLS Muscarinic effects
PYRIDOSTIGMINE AChE Gravis (tx) are blocked by
PHYSOSTIGMINE ATROPINE
AMBENONIUM Reversal non
DAMECARIUM depolarizing NEOSTIGMINE:
(Carbamates) NM blockade Poor lipid solubility,
ECHOTHIOPATE oral DOA=30min-
(Organophosphate) Glaucoma 2hr.
(Physostigmine,
echothiopate, PYRIDOSTIGMINE:
demecarium) Poor lipid solubility,
oral, DOA=4-8hr

PHYSOSTIGMINE:
 Good lipid solubility,
able to enter CNS,
DOA=4-8hr.

Other
organophosphates:
MALATHION
(Scabicide)
PARATHION
(Insecticide)
:High Lipid
Solubility DOA=7-30
days

SARIN, TABUN,
SOMAN = Nerve
Gases
EDROPHONIUM Inhibits Myasthenia DUMBELLS IV
AChE Gravis
(Diagnosis- Short lived DOA = 5-
tensilon test) 15 min.

Differentiation
of cholinergic
crisis and
myasthenic
crisis
RIVASTIGMINE Inhibits Alzheimer’s DUMBELLS RIVASTIGMINE:
GALANTAMINE AChE Disease available at
DONEPEZIL Transdermal Patch
TACRINE
DONEPEXIL:
combined w/
Memantine (NMDA
antagonist) for AD
ANTI-CHOLINERGCIS
ANTI MUSCARINIC
SELECTIVE MOA USES SE NOTES
IPRATROPIUM Blocks M3 Acute Asthma Alice in
TIOTROPIUM (bronchial SM) wonderlan
UMECLIDINIUM COPD d
GLYCORRONIUM Prevents vagal
stimulated
bronchoconstricti
on
DICYCLOMINE Completely IBS Alice in Available in PO &
HYOSCYAMINE blocks M3 wonderlan IV forms
GLYCOPYRROLAT receptors Minor Diarrhea d
E Relatively short
acid secretion half-life (6hr.)
in GIT
Name:
DOCYCLOVERI
NE
OXYBUTYNIN Slightly blocks Urge Alice in Available as Patch
DARIFENACIN M3 receptor impotence wonderlan (may cause
SOLIFENACIN d pruritus)
TOLTERADINE Reduces detrusor Post-op spasms
TROSPIUM muscle tone
IMIDAFENACIN
NON-SELECTIVE MOA USES SE NOTES
 ATROPINE Completely Mydriatic, Alice in
HOMATROPINE blocks ALL cyclopedic, wonderlan
CYCLOPENTOLAT muscarinic bradycardia, d
E receptors hypersalivation
TROPICAMIDE
(Prototype, DOC =
Nonselective organophospha
Muscular Blocker) te poisoning

BENZTROPINE Completely Parkinson’s Alice in Reduces tremors

BIPERIDEN blocks ALL Disease wonderlan more than
TRIHEXYPHENID muscarinic d bradykinesia or
YL receptors rigidity

Restore NT
balance in Basal
ganglia
SCOPOLAMINE Completely Motion Alice in Applied as
blocks ALL Sickness wonderlan transdermal patch
muscarinic d
receptors acid secretion
in GIT
Antagonize
histamine & N/V
serotonin

ANTI NICOTINIC
NEUROMUSCULAR MOA USES SE NOTES
BLOCKER
DEPOLARIZING __ __ __ __
SUCCINYLCHOLIN
E
NON- __ __ __ __
DEPOLARIZING
TUBOCURARINE
PANCURONIUM
ATRACURONIUM
VEROCURONIUM
ROCURONIUM
GANGLION MOA USES SE NOTES
BLOCKER
HEXAMETHONIUM Completely HTN (obsolete) Postural __
blocks Nn Hypertensive hypotension
nicotinic Emergencies
receptors Sexual
Dysfunction
 Constipation,
dry mouth, &
blurred vision

CHOLINESTERASE MOA USES SE NOTES

REGENERATOR
PRALIDOXIME Binds ANTIDOTE for Muscle Must be
phosphorus of early weakness administered
organophosphate cholinesterase before 6-8hr of
. inhibitor organophosphate
poisoning bond w/
Breaks (Organophosphate cholinesterase
organophosphate & Nerve gas occurs
bond w/ poisoning)
cholinesterase Has oxime
Relive skeletal group w/c has
Regenerate muscle and high affinity for
active AChE endplate block phosphate