Autonomic drugs Flashcards
What are symptoms of “cholinergic syndrome”, or cholinesterase inhibitor poisoning? Tx?
MS: weakness, confusion, drowsiness –> coma, seizures
Pupils: miosis (small, fixed or sl reactive)
Bradycardia, paralysis, muscle fasciculations
SLUDGE: salivation/sweating, lacrimation, urination, defecation, GI hyperactivity, emesis.
Tx: atropine (muscarinic antagonist), pralidoxime (regenerates AChE)
What are cholinomimetics? What are the two types?
Drugs that increase acetylcholine signaling
1) Direct cholinergic agonists
2) Anti-cholinesterases
Name 4 cholinergic direct agonists
Bethanechol, carbachol, pilocarpine, methacholine
Name 7 acetylcholinesterase inhibitors
Neostigmine, pyridostigmine, physostigmine, Donepezil, rivastigmine, galantamine, edrophonium
Bethanechol
Cholinergic direct agonist
Activates badder and bowel smooth muscle
Resistant to AChE
Used for post-op ileus, neurogenic ileus, urinary retention
Carbachol
Direct cholinergic, ACh mimic
Used for relief of intraocular pressure, glaucoma pupillary constriction
Pilocarpine
Direct cholinergic agonist
Contracts ciliary muscle of eye and pupillary sphincter, resistant to AChE
Used for glaucoma, stimulator of sweat and tears
Methacholine
Direct cholinergic agonist
Works in airway to constrict airways, used as asthma challenge
Neostigmine
Anticholinesterase
Used for post-op and neurogenic ileus, urinary retention, myasthenia gravis, reversal of NMJ blockade
Pyridostigmine
Anticholinesterase
Used as long-acting to improve strength in myasthenia gravis
Does not penetrate CNS
Physostigmine
Anticholinesterase
Used for anticholinergic toxicity (eg atropine OD)
Penetrates CNS
Donepezil, rivastigmine, galantamine
Anticholinesterase
Used for Alzheimer’s disease
Edrophonium
Anticholinesterase
Historically used for diagnosis of myasthenia gravis
Treatment for cholinesterase inhibitor poisoning
Atropine (competitive inhibitor) and pralidoxime (regenerates AChE)
Muscarinic Antagonist Effects
Oppose cholinergics. Dilate eyes, decrease secretions (airways, GI), decrease GI motility, decrease bladder urgency.
Muscarinic antagonist toxicity
Hot as a hare (no sweating), dry as a bone (no secretions), red as a beet (flushing), blind as a bat (cycloplegia), mad as a hatter (disorientation), bloated as a toad (constipation and urinary retention
Atropine
Muscarinic antagonist
Mydriasis and cycloplegia in eye
Homatropine
Muscarinic antagonist
Mydriasis and cycloplegia in eye