Cholinomimetics Flashcards
Bethenachol MoA
direct agonist
Activates bowel and bladder smooth muscle
resistant to AChE
Bethanechol clinical use
Postoperative ileus, neurogenic ileus, urinary retention
Carbachol MoA
Direct Agonist
Carbon copy of acetylcholine.
Carbachol clinical use
Constricts pupil and relieves intraocular pressure in glaucoma
Methacholine MoA
direct agonist
Stimulates muscarinic receptors in airway when inhaled.
Methacholine clinical use
Challenge test for diagnosis of asthma
Pilocarpine MoA
Direct agonist
Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma)
resistant to AChE
Pilocarpine clinical use
Potent stimulator of sweat, tears, and saliva
Open-angle and closed-angle glaucoma
Donepezil, galantamine, rivastigmine MoA and clinical use
anti-cholinesterase
Alzheimer Disease
Edrophonium MoA and clinical use
anti-cholinesterase
Historically, diagnosis of myasthenia gravis (extremely short acting). Myasthenia now diagnosed by anti-AChR Ab test.
Neostigmine MoA and clinical use
anti-cholinesterase
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative).
No CNS penetration
Physostigmine MoA and clinical use
anti-cholinesterase
Reverses Atropine overdose
Anticholinergic toxicity; crosses blood-brain barrier -> CNS.
Pyridostigmine MoA and clinical use
anti-cholinesterase
Myasthenia gravis (long acting); increases muscle strength
does not penetrate CNS.
With all cholinomimetic agents, watch for exacerbation of…? (3)
COPD, asthma, and peptic ulcers
What compounds irreversibly inhibit AChE and cause poisoning?
Organophosphates are often components of
insecticides; poisoning usually seen in farmers.
