Adrenergics Flashcards
SA node - B1 - __________
increased rate
AV node - B1 - __________
increased conduction
Ventricles - B1 - __________
increased contractility
Increased automaticity
Blood vessels in skin/mucosa - a1 - _________
constriction
Blood vessels in skeletal muscle - B2 - ________
dilation
Blood vessels in skeletal muscle - a1 - __________
constriction
Blood vessels in abdominal viscera - a1 - _________
constriction
Blood vessels in abdominal viscera - B2 - __________
dilation
Blood vessels in lungs - a1 - __________
constriction
juxtaglomerular apparatus - B1 - __________
renin release
GI - B2 - ___________
decreased motility
GI - a1 - ___________
sphincter contraction
Bladder - B3 - ________
detrusor relaxation (prevent urination)
Bladder - a1 - _________
sphincter contraction (urine retention)
Sex organs - a1 - ___________
ejaculation/orgasm
uterus - a1 - ____________
contraction in pregnancy
uterus - B2 - ___________
relaxation (pregnant or non pregnant)
prazosin
selective, reversible alpha 1 blocker
hypertension
PTSD
BPH
phentolamine
nonselective alpha blockers, reversible
pheochromocytoma
phenoxybenzamine
alpha blocker, somewhat alpha1 selective, IRREVERSIBLE
BPH
postural hypotension
reflex tachycardia (esp non-selective)
nasal conjestion
anorgasmia
ARE ADVERSE EFFECTS OF
ALPHA BLOCKERS
EPI reversal
giving epi + alpha blocker reduces blood pressure
lungs - B2 - ___________
bronchodilation
propranolol
nonselective beta blocker.
(but beta-2 blockade is overcome by beta-1 block)
antihypertensive
migraine ppx
performance anxiety
early in MI
heart block hypoglycemia in DM dyslipidemia bronchoconstriction CNS depression, lethargy SIDE EFFECTS OF
beta-blockers
timolol
non-selective beta blocker
eye drops, for glaucoma
atenolol
selective beta-1 blocker
esmolol
selective beta-1 blocker
8 minute half life for emegency procedures
benefit of selective beta-1 blockers for treating hypertension
less risk of respiratory effects
enters via NET
concentrates in vesicle
slowly kicks out NE which is metabolized by MAO
guanethidine
historically used for HTN
enters terminal and blocks vesicle, which prevents entry of NE into vesicle
depletes NE over time
reserpine
historically used for HTN
clonidine
direct alpha-2 agonists
inhibit NE presynaptic release
decrease sympathetic outflow
a-methyldopa
metabolized to a-methyl-NE
which acts as a2-agonist
pregnant patient with essential hypertension can take:
a-methyldopa
patient with opioid withdrawal symptoms might benefit from:
clonidine
how does a-2 agonist treat glaucoma?
decreases production of aqueous humor
treats ADHD
clonidine
guanfacine
(sympatholytic in brain)
dry mouth
sedation
hypertensive crisis after abrupt withdrawal
clonidine
dry mouth
sedation
autoimmune response (+ Coombs test)
a-methyldopa
dexemedetomide (Precedex)
a2 agonist
rhinitis
phenylephrine
bronchial asthma
terbutaline
cardiogenic shock
dopamine
heart failure
dobutamine
precursor to dopamine
tyrosine
dopamine –> ________ –> epinephrine
norepinephrine
most CIRCULATING epinephrine is metabolized by _____________.
monoamine oxidase (MOA) and catechol-o-methyl-transferase (COMPT)
NE levels WITHIN the terminal are regulated by ___________
monoamine oxidase
About 90% of released NE is recycled via _________
re-uptake by the presynaptic neuron at NET (NE transporter)
taken up by NET and vesicle in presynaptic neuron,
this rapidly kicks NE out of the vesicle which then diffuses into the terminal
amphetamine
increases BP and HR
reversing action of the NET and increasing NE in the terminal is generally called:
FACILITATED EXCHANGE DIFFUSION
normally metabolized by MOA in the gut
goes through NET and kicks NE out of presynaptic neuron –> hypertension
tyramine
blocks NET (reuptake of NE) leading to rapid increase of NE in the synapse
cocaine
imipramine
atomoxetine
phenylephrine
a1 agonist
in nasal spray, constricts blood vessels in nose
chronic use of an adrenergic agonist causes ______ of receptors
desensitization and down regulation
except nicotine at nicotinic receptors
chronic use of adrenergic antagonist causes _______ of receptors
super sensitization and up-regulation
NE is released by______
postganglionic sympathetic neurons
NE likes to bind to ________ receptors
a1 and B1
Isoproterenol selectively binds to _______ receptors
Beta (1 and 2)
Epinephrine binds to _______ at low concentrations, but binds to ______ at high doses.
beta receptors (1 and 2) alpha
Dopamine binds to _______ most, but also binds ______ at low doses and ______ at high doses.
dopamine receptors beta receptors all receptors (promiscuous!)
Dobutamine preferentially binds to _______ receptors.
beta-1
at high doses will bind to anything
Which drug stimulates contractility without affecting HR?
dobutamine
B1 receptors prefer __________ over _______ and ______.
isoproterenol
epi = NE
B2 receptors prefer ________ over ________ over ______.
isoproterenol > epi»_space; NE
NE likes the 1s
a1 receptors prefer _________ over _______ over _________.
epi > NE»_space; isoproterenol
iso likes beta
Drugs without hydroxyl groups get into the brain easily. These include:
phenylephrine
ephedrine
amphetamine
Which adrenergic agonist cannot be metabolized by MOA?
amphetamine
no reflex tachycardia
alpha-2 agonists
