Autonomic Drugs Flashcards
Class of edrophonium
Ache i - short acting (reversible)
Class of pilocarpine
Muscarinic agonist
Class of bethanechol
Muscarinic agonist
Class of neostigmine
Ache i - intermediate acting (reversible)
Class of pyridostigmine, physostigmine, donepezil
Ache i (reversible)
Used for Alzheimers
Intermediate acting
class of echothiophate
Irreversible Ache i
What are organophosphate insecticides
Ache i - non therapeutic
Acetylcholinesterase inhibitors
MOA and uses
Increase ach, amplifies effects at cholinergic synapses, effects at nicotinic and muscarinic
Used to reverse NDMR blockade, MG, glaucoma, ileus, urinary retention, Alzheimer’s disease
What toxicity is expected with AChE i’s?
Increased ach, so increase PSNS, so bradycardia, increased salivation, increase muscle tone/hyperexcitability, Bronchoconstriction
CNS - excitation (possible convulsion) followed by depression (unconsciousness)
Ache i is not used to Reverse depolarizing blockade of succs, why?
Because sux is an agonist
Ache i drug effects
Increased secretions, increased GI motility, Bronchoconstriction, bradycardia, hypotension, miosis, large dose = depolarizing block, MG - improves transmission, NDMR reversal
what do we use edrophonium for?
Diagnosis of MG (to increase Ach, and increase transmission) - too short acting for therapeutic use
What do we use physostigmine for?
Treatment of glaucoma to decrease intraocular pressure by increasing PSNS and decreasing pressure
Works postganglionic PSNS
Cross BBB
What do we use pyridostigmine for?
Myasthenia Gravis to increase transmission at NMJ
Cholinergic crisis S&S
D - diarrhea, diaphoresis
U - urination
M - miosis
B - bradycardia
B - bronchoconstriction E - excitation of skeletal muscle and CNS L - lacrimation S - salivation S - sweating
What do you give as an antidote for cholinergic toxicity
Atropine = muscarinic blocker
What are the muscarinic agonist drugs?
Acetylcholine, carbachol, methacholine, bethanechol Muscarine, pilocarpine, oxotremorine, cevimeline
Muscarinic agonist drug effects
“Parasympathetomimetic”
CV = decrease HR, CO, and arterial blood pressure, vasodilation
GI = increased motility
Bladder = contracts
Lungs = bronchoconstriction
Increased secretions
Eye = miosis, accommodation for near vision, decreased intraocular pressure
How do muscarinic agonists cause vasodilation in vsmc
They bind to M3 receptors on endothelial cells which secrete NO and cause vasodilation
Where are the nicotinic acetylcholine receptors
NMJ, ganglia, CNS
NicotinicN receptors do what?
Stimulation of post-ganglionic neuronal activity and CNS stimulation
= increased autonomic outflow
NicotinicM receptors do what
Activation of skeletal muscle endplates leading to contraction
What is the class of atropine
Muscarinic antagonist
What is the class of glycopyrrolate
Muscarinic antagonist
What is the class of scopolomine
Muscarinic antagonist
What is the class of hexamethonium
NicotinicN ganglionic blocker
What is the class of atracurium, cisatricurium, vecuronium, roc, and panc
NicotinicM blocker
Atropine uses
Crosses BBB, useful for bradycardia and as an adjunct to blockade reversal
Scopolamine uses
Cross BBB +++
Used for motion sickness
Glycopyrrolate uses
Does not cross BBB
Blockade reversal adjunct to help wiht muscarinic activities of neostigmine (aka prevents bradycardia)
Short acting
Concerns with antimuscarinics
Hyperthermia, glaucoma, GU obstruction, prostatic hypertrophy, CV, GI ileus - further decreases motility
Medication classes with anticholinergic activities
Antihistamines, antispasmodics, antiparkinsonian, skeletal muscle relaxants, antipsychotics, antidepressants, antimuscarinics for urinary incontinence
NicotinicM antagonist effect
NDMRs
NicotinicN antagonist effects
Blocks ganglionic outflow
What is the class of norepinephrine?
Direct acting
Nonselective
Mixed alpha/beta agonist
Alpha 1 and Beta 1 (little beta2)
What is the class of phenylephrine
Direct acting selective alpha1 agonist