Activates M receptors on effector cells to alter organ function and  on nerve terminals to inhibit the release of their neurotransmitter

No clinical use because it is hydrolyzed by cholinesterase in seconds

Nonselective M and N agonist; more resistant to cholinesterase

Bronchospasm

Glaucoma - used topically to reduce intraocular pressure

Selective muscarinic agonist, negligible effect on nicotinic; not hydrolyzed by cholinesterase

Bronchospasm in asthmatics

Urinary retention or ileus - stimulates bladder contraction and GI motility

Muscarinic agonist (like Bethanechol)

Bronchospasm, bradychardia, excessive sweating/salivation

Glaucoma; Sjogren’s syndrome (autoimmune disease that destroys glands producing tears and saliva)

Synthetic M₃-selective (similar to Pilocarpine)

Sjogren’s syndrome

N_N and N_M receptor agonist

Increased GI activity and BP, high doses cause seizures

Smoking cessation

Partial agonist at α4β2 nicotinic receptors

Nausea, insomnia, exacerbation of psychiatric illnesses

Smoking cessation

Reversibly bind to the active site preventing access of Ach; ↑ PNS activity and somatic neuromuscular transmission

Parasympathomimetic excess

Myasthenia gravis (diagnosis)

Forms covalent bond with AChE, but hydrolyzed and released; like edrophonium but longer-acting

Parasympathetic excess

Myasthenia gravis, postoperative and neurogenic ileus and urinary retention

Like neostigmine, but is a tertiary amine (more hydrophobic) and can cross the blood-brain barrier and enter CNS

Parasympathetic excess

Myasthenia gravis, glaucoma, Alzheimer’s disease

Like neostigmine, but released more slowly

Brow ache, uveitis (inflammation of interior of eye), blurred vision

Obsolete – was used in glaucoma

Irreversible cholinesterase

Low toxicity

Insecticide; used in low doses to treat lice (pediculosis), scabies

Irreversible cholinesterase

Extremely toxic

Nerve gas

Anticholinesterase and other cholinomimetic actions

Hepatic toxicity

Alzheimer’s disease

More selective acetylcholinesterase inhibitor

Alzheimer’s disease

Blocks fusion of vesicles with the surface membrane of nerve terminal preventing expulsion of ACh into synaptic cleft

Botulism - paralytic illness

Cosmetic procedures