Cholinergic Agonist/ antagonist

Bethanechol

• direct muscarinic agonist

• M3 (bladder, GI)

• Post-op urinary retention neurogenic bladder

Pilocarpine

• direct muscarinic agonist

• M3 (eyes, glands)

• Glaucoma, dry mouth (xerostomia)

M3 (

Carbachol

• direct muscarinic and nicotinic agonist

• Dirty drug

• M3, Nn

• Glaucoma (rare), miosis during surgery

Dir

Methacholine

• direct muscarinic agonist

• M3 (airways)

• Bronchial hyperactivity testing

Cevimeline

• direct muscarinic agonist

• M3 (glands)

• Most specific

• Dry mouth in Sjögren’s syndrome

Neostigmine

• Indirect agonist (AChE inhibitor)

• High levels of ACh at Nm junction, M3

• Myasthenia gravis, post-op ileus, urinary retention

• Injection

• Does not cross BBB

Pyridostigmine

• indirect agonist ( AChE inhibitor)

• High levels of ACh at Nm junction, M3

• Myasthenia gravis (longer acting)

• Pill

Physostigmine

• indirect agonist (AChE inhibitor)

• High levels ACh in CNS and PNS

• Anticholinergic toxicity (crosses BBB)

Edrophonium

• indirect agonist (AChE inhibitor)

• High levels of ACh (short acting)

• Diagnosis of myasthenia gravis (historical)

Donepezil, Rivastigmine, Galantamine

• indirect agonist (AChE inhibitor)

• High levels of ACh in CNS

• Alzheimer’s disease

Atropine

• muscarinic antagonist

• M1-M5 (non selective)

• Dirty drug

• Bradycardia (blocks M2), organophosphate poisoning

Scopolamine

• muscarinic antagonist

• M1 CNS

• Motion sickness, postoperative nausea

Ipratropium

• muscarinic antagonist

• M3 (lungs)

• COPD, asthma (short-acting bronchodilator)

Tiotropium

• Muscarinic antagonist

• M3 (lungs)

• COPD, asthma (long acting bronchodilator)

Oxybutynin

• Muscarinic antagonist

• M3 (bladder)

• Overactive bladder, urinary incontinence

• Cheapest, least selective

Tolterodine

• muscarinic antagonist

• M3 (bladder)

• Overactive bladder

Solifenacin

• muscarinic antagonist

• M3 (bladder)

• Overactive bladder

• Highly selective, most expensive

Benztropine

• muscarinic antagonist

• M1 (CNS)

• Parkinson’s disease, drug induced EPS

Trihexyphenidyl

• muscarinic antagonist

• M1 (CNS)

• Parkinson’s disease, drug induced EPS

Glycopyrrolate

• muscarinic antagonist

• M3 (PNS)

• Pre-op secretion reduction, peptic ulcers