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134 Cards in this Set
- Front
- Back
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sympatholytics antagonize ---- -----
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the postganglionic effects of the sympathetic nervous system
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receptors for phenoxybenzamine
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a1 blockers
a2 blockers |
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phenoxybenzamine is selectiv/nonselective
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nonselective
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prazosin receptor
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a1
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yohimbine receptor
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a2
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propanolol receptors
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b1
b2 |
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metoprolol receptor
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b1
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butoxamine receptor
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b2
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phenoxybenzamine is a noncompetitive/competitive antagonist
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noncompetitive
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since phenoxybenzamine is noncompetitive the max response increases/decreases
why |
decrases
cuz there are less receptors to work on cuz phen is attached |
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phen ---- receptors
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alkylates
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because phen alkylates receptors it binds ------ to the receptor
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reversibly
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t1/2 of pheno
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24 hrs
it has abnormal receptor kinetics |
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increase or decrease bp w/ phen
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decrease
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why have postural hypotension
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cuz vessles not constricting to pump blood back up
blocking a receptors |
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phenoxy has + --- and ---- effects
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inotrophic
chronotropic B on SA node, so there will be an increase in HR and contraction |
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t/f
phen stimulates uptake 1 and 2 |
f
it blocks it so there's less ne being taken up |
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low bp w/ phen because. . .
threre's no activation of the -------, so there's no stimulation to constrict bl vessels this is due to the blockage of a, so ---- is not release to constrict blood vessels |
baroreceptor
NE |
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t/f
sympatholytics have intrinsic activity |
f
they don't. they don't activate antagonist. they just block the activity of the agonist |
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hyper/hypo glycemia w/ phen
why |
hypo
cuz blocks alpha which inhibits release of insulin, so now there's going to be a lot of insulin |
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miosis or mydriasis in phen
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miosis
cuz blocking alpha in radial, so this will constrict |
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t/f
phen help w/ ejaculation |
f
inhibits ejaculation |
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tx effects of phen
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pheochromocytoma
PAD |
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pheochromocytoma is a tumor of the ---- ----. it causes secretion of ---- and --- .
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adrenal medulla
NE Epi |
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when is phen used in pheochromocytoma
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given to prevent the effects of the NE and epi until sx can be done to remove the tumor
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side effects of phen
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reflex tachycardia
orthostatic hypotension |
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how can you get reflex tachycardia in pheno
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because b1 is unimpeded so there's an increase in hr
tries to compensate for the hypotension |
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why have orthostatic hypotension
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blocked baroreflex
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phentolamine is a -------- alpha 1 and 2 blocker
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nonselective
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t/f
pentolamine can be given orally only |
f
injection only! |
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pentolamine is a reversible ---- inhibitor
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f
competitive |
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group on phentolamine that makes it reversible competitive
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imidazoline
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t/f
the vmax of phentolamine will be decreased |
f
it's a competitive inhibitor it will shift to the R, so enough agonist will overcome it |
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what does phentolamine do to bp
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decrease
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will there also be reflex tachycardia w/ phentolamine
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yes
because of the decrease in Bp |
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phentolamine will also have a2 antagonist effects such as. ..
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increased insulin: hypoglycemia
myosis |
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phentolamine is used to dx pheochromocytoma w/
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measure urinary catecholamines and bp
give phentolamine monitor urine and bp again |
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what's a combo that can cause acute hypertensive crisis
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tyramine/MAOI rxn
they both allow a rapid release of NE which will increase bp |
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foods that are rich in tyramine
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cheese
wine beer fish |
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why is phentoalmine given w/ acute htn crisis
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it rapidly decreases the bp
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pentolamine is used in ---- dysfunction
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erectile
used in combo w/ papaverine for direct injection |
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what are some toxicitites of phentolamine
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priaprism
hypotension reflex tachycardia |
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prazosin is a selective ------ antagonist
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alpha 1
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route for prazosin
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oral
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prazosin relaxes/constricts the vascular smooth muscle
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relaxes
so it decreases bp |
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t/f
use caution w/ prazosin because cardiac effects are substantial |
f
cardiac effects are minimal |
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prazosin inhibits smooth muscle of the --- gland
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prostate
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what causes contraction of the prostate gland.
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alpha 1
this will cause difficulty urinating |
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baroflex w/ prazosin
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no
cuz selective; unclear why |
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tx effects for prazosin
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antiHTN
BPH |
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when should the pt take their first dose of prazosin
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at night due to orthostatic hypotension
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t/f
pt's should always take prazosin at night due to orthostatic hypotension |
f
the blockage of the baroreflex decreases over time |
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there are a1a receptors on the prostate ---- and bladder ---
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capsule
neck |
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side effects of prazosin
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postural hypotension
syncope, nasal stuffiness |
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syncope due to prazosin can be due to the -- ---
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postural hypotension
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nasal stuffiness is due to . ..
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less constriction
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other a1 selective agents
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terazosin
doxazosin alfuzosin bph |
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of the other a1 selective agents which has the longest duration of action
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doxazosin
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t/f
a1 antagonist are good antiHTN |
true
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tamsulosin is an ------- selective antagonist
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a1a
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why's there limited effects on the vasculature
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cuz mainly a1b on vasculature
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se of tamsulosin
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hypotenstion
dizziness diarrhea |
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tx effects of the selective agents
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HTN
BPH |
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why are the other a1 selective agents better than prazosin
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longer t1/2
qd dosing decreased insulin resistance |
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ALLHAT:
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antihypertensive lipid lowering heart attack trial
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what part of the ALLHAT trial was stopped?
why |
doxazosin
due to increase incidence of CHF |
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yohimbine is a ---- selective antagonist
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a2
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yohimbine is an alkaloid r/t ------
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reserpine
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yohimbine only had central effects
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f
central and peripheral |
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yohimbine's tx effect
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erectile dysfunction
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t/f
yohimbine is more effective than alprostadil or slidenafil |
f
less effective |
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propranolol is a nonselective -- antagonist
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beta
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prolonged administration can lead to an ---- ---- of receptors
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up-regulation
so, don't stop abruptly |
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what regulates # of beta receptors
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thyroid hormone
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in a thyroid storm the pt's at risk for ---- -----
why |
increased hr, palpitations
cuz beta receptors increased |
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the b1 receptor blockers will decrease
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HR
contractility conduction CO renin release |
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what will b2 blocker decrease
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vascular relaxation
bronchodilation glucose production ocular fluid production insulin release neurotransmitter |
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tx effects of propranolol
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antiHTN
angina antiarrhythmic MI glucoma pheochromocytoma |
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t/f
propanol wil cause a decrease in norm pressure |
f
no decrease in norm pressure |
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how will propranolol decrease bp
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decrease renin
decrease CO (eventually CO will increase) late appearing decrease in TPR |
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how will propranolol decrease angina
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decrease workload
decrease CO, afterload, preload decrease O2 demand of the heart |
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how does propanolol decrease arrhythmias
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decrease cardiac stimulation, tachycardia, pvc's
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how will propanolol decrease PVC's
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decrease excitability
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how will propanolol decrease chances of an MI
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decrease cardiac excitability
decrase cardiac workload decrease demand in ischemic area |
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how will propranolol decrease glaucoma
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decrease in aq humor production
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how will propranolol treat pheochromocytoma
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decrease HR
decrease CO |
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for pheochromocytoma what should be given first
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an alpha antagonist to decrease BP then give B blocker
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how does propranolol tx acute panic attacks
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decrease hr
decrease palpitations decrease sweating |
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how does propranolol tx thyrotoxicosis
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decrease sympathetic effects
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how does propranolol tx acute panic attacks
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decrease hr
decrease palpitations decrease sweating |
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how does propranolol tx essential tremors
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suppresses b2 which are on the skeletal muscle
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how does propranolol tx thyrotoxicosis
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decrease sympathetic effects
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how does propranolol tx alcohol withdrawal syndrome
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decrease delirium tremens
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how does propranolol tx essential tremors
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suppresses b2 which are on the skeletal muscle
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how does propranolol tx migraines
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prophylactic use. . . it makes HA worse
it should be taken btwn migraines decreases frequency and severity of HA |
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how does propranolol tx alcohol withdrawal syndrome
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decrease delirium tremens
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how does propranolol tx migraines
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prophylactic use. . . it makes HA worse
it should be taken btwn migraines decreases frequency and severity of HA |
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se of propranolol
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bradycardia
fatigue sedation caution in asthmatics avoid in dm altered lipoproteins nightmares impotence potentiation of allergic response |
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why should dm pts avoid propranolol
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cuz it block the s/s
which are sympathetic responses |
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w/ propranolol insulin users should look out for -----
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hypoglycemia
b receptors increase insulin |
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other nonselective b agents
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pindolol
timolol |
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what's pindolol used for
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cardiac actions
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what's timolol used for
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cardiac action
glaucoma tremor |
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what's nadolol used for
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cardiac actions
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what's sotalol used for
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cardiac actions
antiarrhythmics |
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metoprolol is a selective ---- antagonist
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B1
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what generation is metoprolol
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2nd
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t/f
metoprolol has the most effects on the bronchial muscle and on insulin |
f
mainly cardiac less effects on bronchial muscle and insulin |
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other selective B1 antagonist
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atenolol
esmolol acebutolol bisoprolol |
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effects of atenolol
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cardiac
migraine arrhythmias |
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esmolol treats
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arrhytmias
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which other B1 selective antagonist is short acting and is given via infusion
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esmolol
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acebutolol treats
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HTN
arrhythmias |
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bisoprolol treats
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HTN
CHF ( in low doses) |
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a selective B2 antagonist
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butoxamine
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what's the tx use of butoxamine
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no therapeutic use
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butoxamine ---- broncho smooth muscle
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constricts
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3rd generation beta blocker
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labetalol
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what receptors blocked w/ labetalol
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a1
b1 b2 |
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how many isomers of labetalol
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4
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which isomer is an a1 antagonist
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S,S isomer
S,R isomer |
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which isomer is an B1 blocker and partial B2 agonist
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R,R isomer
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which isomer inactive
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R,S isomer
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t/f
labetolol has more a activity than B activity |
f
more B activity than alpha activity |
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what's beneficial about acting as both an antagonist and agonist
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eliminates SE
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labetaolol decreases ----
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bp
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t/f
labetalol decreases bp, but has reflex tachycardia and increased cardiac output |
f
decreased bp, but has no reflex bradycardia or increased CO due to the mix of antagonist or agonist |
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SE of labetalol
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similar to beta blockers
but no bl glucose effects |
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3rd generation B-blocker
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labetalol
carvedilol |
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receptors that carvedilol works on
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a1
b1 b2 |
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carvedilol is vaso-----
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dilatory
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carvedilol has ---- and ----- effects
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antioxidant
antiproliferative |
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t/f
caution w/ increase in receptor density w/ carvedilol |
f
no increase in receptor density |
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what does carvedilol tx
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CHF
angina HTN |
