CHOLINERGIC PHARMACOLOGY

DRUG / CLASS SIMILAR DRUG/S MECHANISM OF ACTION USES SIDE EFFECTS NOTES
CHOLINOMIMETIC (CHOLINERGIC) DRUGS
A. Direct-Acting Cholinomimetics
Muscarinic (Choline Esters)
Acts on M and N receptor Ocular surgery – CNS stimulation, miosis, cyclospasm, bronchoconstriction, Very short lived DOA: 5-30sec,
Activates M1-M3 receptors in miotic excessive GI and GU smooth muscle contraction, Rapidly hydrolyzed by AChE
ACETYLCHOLINE
all peripheral tissues increased secretory activity of sweat gland, airways etc,
vasodilation
CARBACHOL Act on M receptors only BLADDER & BOWEL Cylospasm, diarrhea, urinary urgency, vasodilation, reflex Carbachol – for Glaucoma, used
BETANECHOL* – both M&N Activates M1-M3 receptors ATONY (post-surgery tachycardia, sweating as miotic
or spinal cord injury)
Muscarinic (Alkaloids)
CEVIMELINE Activates M3 receptors in GLAUCOMA Miosis, blurring of vision (due to cyclospasm) Good lipid solubility
— M3 selective ciliary muscle (↑ aqueous SJORGREN Syndrome Increased salivation
PILOCARPINE
humor outflow) and salivary SICCA Syndrome
glands (↑ salivation)
Nicotinic
VERENICLINE Activates nicotinic Ach Smoking Cessation Generalized ganglionic stimulation (hypertension, Overdose leads to convulsions,
— selective partial agonist at receptors (Nn and Nm) tachycardia, nausea, vomiting, diarrhea) paralysis and coma
nicotinic receptors Activates post-ganglionic
NICOTINE
— DOA 12-24h neurons (BOTH PANS and SANS)
Able to enter CNS and activate
Nn receptors; DOA 1-6h only
B. Indirect-Acting Cholinomimetics (Cholinesterase Inhibitors)
SHORT Acting (Alcohol)
Inhibits acetylchoninesterase MYASTHENIA GRAVIS Miosis, salivation, nausea, vomiting, diarrhea, bradycardia IV route
Amplifies endogenously (Dx: Tensilon test) Very short lived
released Ach Differentiation of DOA: 5-15min
ENDROPHONIUM cholinergic crisis
(OVER: weakens) and
myasthenic crisis
(UNDER: improves)
INTERMEDIATE Acting (Carbamates)
PYRIDOSTIGMINE Inhibits acetylchoninesterase MYASTHENIA GRAVIS Miosis, salivation, nausea, vomiting, diarrhea, bradycardia Muscarinic effects are blocked
PHYSOSTIGMINE Amplifies endogenously (treatment) by ATROPINE
— tertiary amine (cross BBB) released Ach Reversal of non- Neostigmine: POOR lipid
AMBENOMIUM depolarizing NMB solubility, oral, DOA: 30min-2h
DEMECARIUM (Carbamates) GLAUCOMA Pyridostigmine: POOR lipid
NEOSTIGMINE ECHOTHIOPHATE (physostigmine, solubility, oral, DOA: 4-8h
(Organophosphate) echotiophate, Physostigmine: GOOD lipid
demecarium) solubility: able to enter the
CNS, DOA: 4-8h
Echothiophate: MODERATE
lipid solubility, DOA: 2- 7days

1
 GALANTAMINE Inhibits acetylchoninesterase ALZHEIMER’S Miosis, salivation, nausea, vomiting, diarrhea, bradycardia Rivastigmine available as
DONEPEZIL* Amplifies endogenously DISEASE TRANSDERMAL PATCH
RIVASTIGMINE TACRINE released Ach Donepezil is combined with
Memantine (NMDA antagonist)
for ALZHEIMER’S DIMENTIA
LONG Acting (Organophosphates)
See neostigmine
Organophosphate toxicity: “DUMBBELSS” — diarrhea, urination, miosis, bronchospasm, bradycardia, excitation (NICOTINIC: skeletal muscle and CNS), lacrimation, sweating, salivation
ECHOTHIOPHATE
Treatment: ATROPINE (first choice; no effect on nicotinic signs of toxicity), PRALIDOXIME (early stage; must be administered before “aging”— 6-8h)

CHOLINOEPTOR BLOCKERS / ANTICHOLINERGIC DRUGS

A. Antimuscarinic

B. Antinicotinic
Ganglion Blockers

Neuromuscular Clockers

C. Cholinesterase regenerators: Oximes (Pralidoxime)