FA Cholinomimetics Flashcards
Bethanechol
Direct muscarinic receptor agonist; activates bowel and bladder smooth muscle; resistant to AChE;
Carbachol
Carbon copy of ACh;
CU bethanechol
postoperative ileus, neurogenic ileus, urinary retention
CU carbechol
glaucoma, pupillary constriction, relief of IOP
CU pilocarpine
potent stimulator of sweat, tears and saliva; open and closed angle glaucoma
CU methacholine
challenge test for diagnosis of asthma
Pilocarpine
Contracts ciliary muscle of eye (open-angle glaucoma), contracts pupillary sphincter (closed-angle glaucoma);
“you cry, drool, and sweat on your pillow”
Methacholine
Stimulates muscarinic receptors in airway when inhaled
CU neostigmine
postoperative and neurogenic ileus and urinary retention, Myasthenia gravis, reversal of NMJ blockage (postoperative)
Neostigmine
anticholinesterase (neo CNS = no CNS)
CU pyridostigmine
Myasthenia gravis (long acting); does not penetrate CNS
Pyridostigmine
anticholinesterase –> inc ACh and strength; does not penetrate CNS
CU Physostigmine
anticholinergic toxicity (ie jimson weed, atropine overdose); crosses BBB –> CNS
physostigmine
anti cholinesterase that crosses BBB
Name three AChE inhibitors that work for Alzheimer’s
rivastigmine, galantamine, donepezil
Historically, dx of myasthenia gravis (extremely short acting). MG now diagnosed by anti-ChR aAB test.
Edrophonium
General toxicities of all indirect and direct cholinomimetics
exacerbation of COPD, asthma, PUD
4 direct cholinomimetics
bethanechol, carbachol, pilocarpine, methacholine
7 indirect cholinomimetics
Neo-, pyrido-, physio- stigmine
rivastigmine, galantamine, donepezil
Cholinesterase inhibitor poisoning (often due to organophosphates (parathion) that irreversibly inhibit AChE –> too much ACh)
DUMBBELS Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle and CNS Lacrimation, Sweating Salivation
Antidote to organophosphate poisoning
atropine (competitive inhibitor) + pralidoximine (regenerates AChE if given early)
Atropine, homatropine, tropic amide effect on eye
mydriasis (pupil dilation) and cycloplegia (paralysis of the ciliary muscle of the eye –> loss of accommodation)
benztropine
muscarinic antagonist for Parkinson’s disease
scopolamine
muscarinic antagonist for motion sickness
