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
What is the class of dexmeditominide
Direct acting alpha 2 agonist
What is the class of epinephrine
Direct acting mixed alpha/beta agonist, nonselective
What is the class of isoproterenol
Direct acting non-selective beta agonist
What is the class of dobutamine
Direct acting beta 1 agonist
What ist he class of albuterol
Direct acting beta 2 agonist
What is the class of ephedrine?
Indirect acting adrenergic agonist via NT release - can also act on receptors
“Mixed” acting
How does cocaine work
NE Reuptake inhibition
What is the class of tranylcypromine and selegiline
MAOi which stops breakdown of NE and dopamine
Tranylcypromine = nonselective Selegiline = selective for MAO-b (dopamine)
What is the class of prazosin
Selective alpha 1 antagonist
What is the class of metoprolol and atenolol
Selective beta 1 antagonist
What is the class of clonidine
Selective alpha 2 agonist
What do amphetamines do
Displaces/releases stored catecholamine NT (NT releaser)
Inhibits catecholamine Reuptake
How does tyramine work
NT releaser of catecholamines
Found in food, not a drug - this is the food-drug interactions of MAOis
Dopamine receptor affinity
Low dose = dopa
Med dose = beta
High dose = alpha
What does alpha 1 do?
Vasoconstriction (skin and splanchnic)
Mydriasis
Smooth muscle contracts (except GI)
GI/GU sphincter contract
What does alpha 2 do
Decrease NE release presynaptically
CNS inhibit SNS outflow
Platelet aggregation
Pancreas = decrease insulin
What does beta 1 do?
Increase heart rate and contractility
Renin release
Trophic effect = hypertrophy
What does beta 2 do
Bronchodilator Vasodilation (skeletal muscle beds) Relaxes smooth muscle mostly Skeletal muscle contracts = tremor Relax GI/GU Relax uterine smooth muscle Glycogenolysis
What class is phenoxybenxamine
Nonselective alpha blocker
What class is phentolamine
Non selective alpha blocker
what class is prazosin
Alpha 1 blocker
What class is yohimbine
Alpha 2 blocker
What class is propanolol
Nonselective beta blocker
What class for metoprolol and esmolol
Beta 1 specific blocker
Why wouldn’t you use selective beta 2 blockers
Risk for bronchoconstriction
What type of innervation to the adrenal medulla, sweat glands, and blood vessels
SNS innervation only
What is the dominant tone in cardiac, bronchial smooth muscle, GI tract, salivary glands?
PSNS
What is the basal tone for sweat glands, arterioles, veins
SNS
What does botulinum toxin do
Blocks release of Ach from presynaptic terminal
What is acetylcholine synthesized from
Choline and acetyl-coA
Name the M receptors and where they are
M1,4,5 = CNS m2 = heart M3 = smooth muscle, glands, endothelium, eye (circular)
Norepinephrine synthesis
Tyrosine - dopa - dopamine - norepinephrine
What does methylphenidate do
Stops Reuptake of norepinephrine (like cocaine)
Alpha one and camp
Increases camp = smooth muscle contraction
Alpha 2 and camp
Decreases camp - decreased NE release
Betas and camp
Adenyl Cyclase = increased camp = increased kinase = activation to do the things it needs to do
Sympathetic action on the heart
B1 - increase chronotropy and inotropy
Parasympathetic action on the heart
M2 - decrease heart rate and inotropy
SNS and PSNS actions on the lungs
Beta 2 - bronchodilation
M3,2 - bronchoconstriction
SNS action on kidney
B1 - increase RASS
SNS action on liver
b2 - increase gluconeogenesis
SNS action on VSMC
Apha1 - constriction (skin and splanchnic)
Beta2 - dilation (sk muscle)
SNS and PSNS action on GI walls
B2 - relax
M3 - contract
What are the SNS and PSNS actions on GI sphincters
Alpha 1 - contract
M3 - relax
What are the PSNS actions on GI secretions
M3 - increased secretions
What are the SNS and PSNS effects on urinary bladder wall
Beta2 - relax
M3 - contracts
SNS and PSNS effects on urinary bladder sphincter
Alpha1 - contract
M3 - relax
SNS and PSNS effects on uterine smooth muscle
B2 = relax M = contract
SNS and PSNS on reproductive
Alpha 1 - ejaculate
M3 - erection
SNS effect on adrenal medulla
NicotinicN - epi/norepinephrine release
SNS and PSNS effect on eye
Alpha 1 - contract radial (SNS) - mydriasis
M3,2 - contract circular (PSNS) - miosis
SNS effect on pilomotor smooth muscle
Contract alpha 1
SNS effect on sweat glands - thermoregulatory
M - increased sweat
SNS effect on sweat glands - aprocrine (stress)
Alpha 1 - sweat
SNS effect on fat cells
B3 - lipolysis
