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)
- acetylcholine
- direct-acting cholinergic agonist
- bethanechol
- direct-acting cholinergic agonist
- carbachol
- direct-acting cholinergic agonist
- pilocarpine
- 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
- Echothiophate
- 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)
- neostigmine
- indirect cholinergic agonist C: postoperative and neurogenic ileus, urinary retention, MGravis, post op reversal of neuromuscular blockade
- pyridostigmine
- STRONG indirect cholinergic agonist C: myasthenia gravis
- edrophonium
- indirect cholinergic agonist C: short acting, so used to diagnose MGravis
- physostigmine
- 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?
- benztropine
- what antimuscarinic is used for motion sickness?
- scopolamine
- what antimuscarinic is used to trat asthma and COPD?
- ipratropium
- 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