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Pharm: Principles of Cholinergics


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name the 2 major cholinergic receptor families.
nicotinic and muscarinic
what are the 2 nicotinic receptor types?
neuronal nicotinic muscular nicotinic
what are the 2 major groups of cholinergic agonists? how do they work?
a. direct acting (receptor agonists) b. indirect acting (inhibit acetycholinesterase)
direct-acting cholinergic agonist
direct-acting cholinergic agonist
direct-acting cholinergic agonist
direct-acting cholinergic agonist
name 4 direct-acting cholinergic agonists
Acetylcholine Bethanechol Carbachol Pilocarpine
what receptor types does ACh stimulate?
both muscarinic and nicotinic
what is the clinical use of ACh?
achieve miosis during opthalmic surgery; otherwise it's rarely used due to widespread effects and its rapid hydrolysis in the synapse by ACh-ase
what are the side effects from excessive cholinergic stimulation?
DUMBBELSS Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle and CNS Lacrimation Sweating Salivation
what is the antidote to ACh-ase inhibitor poisoning?
atropine (muscarinic antagonist) plus pralidoxime (chemical antagonist used to regenerate active cholinesterase)
on what receptors does bethanechol work? what are the clinical uses?
works primarily on muscarinic and a little on nicotinic receptors BBB: Bethanecol stimulates Bladder and Bowel used to increase intestinal motility and to treat urinary retention
when is carbachol used?
rarely, but can be used for glaucoma and to stimulate miosis in opthalmic surgery
what is Xtraordinary about pilocarpine?
is not cleaved by ACh-ase; affects mainly muscarinic receptors
name 5 key indirect acting cholinergic agonists.
Echothiophate Edrophonium Physostigmine Pyridostigmine Neostigmine
organophosphate indirect acting cholinergic agonist; binds ACh-ase irreversibly
how do you treat organophosphate poisoning?
atropine gastric lavage and charcoal
how can you mitigate the effects of organophosphates?
pralidoxime (a cholinesterase reactivator)
indirect cholinergic agonist C: postoperative and neurogenic ileus, urinary retention, MGravis, post op reversal of neuromuscular blockade
STRONG indirect cholinergic agonist C: myasthenia gravis
indirect cholinergic agonist C: short acting, so used to diagnose MGravis
indirect cholinergic agonist (crosses BBB!) C: glaucoma and atropine O/D
what is pralidoxime?
a cholinesterase reactivator
what are the effects of organophosphate poisoning?
respiratory muscle paralysis and convulsions
what 3 antimuscarinics are used to produce mydriasis and cycloplegia in the eye?
HAT Homatropine Atropine Tropicamide
what antimuscarinic is used to treat Parkinson's?
what antimuscarinic is used for motion sickness?
what antimuscarinic is used to trat asthma and COPD?
hexamethonium. mxn and clinical use?
nicotinic ACh receptor antagonist; ganglionic blocker (prevent reflex bradycardia caused by NE)
what is atropine and what are its typical effects?
muscarinic blocker blocks SLUD Salivation Lacrimation Urination Defecation
atropine side effects (typical antimuscarinic side effects)?
hot as a hare dry as a bone red as a beet blind as a bat mad as a hatter
what is cycloplegia?
loss of function of the ciliary muscle -> loss of accomodation
effects of atropine on the... eye airway stomach gut bladder

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