Adrenergic Antagonists Flashcards by Jenna Nicole

nonselective antagonism of ALPHA receptors is useful in treating ?

phaeochromocytoma

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alpha 1 selective antagonists treat ? and ?

Htn

BPH

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most common adrenergic antagonists used?

beta antagonists

*Htn, ischemic heart disease, arrhythmias, endocrinologic, neurologic disorders

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phentolamine

phenoxybenzamine

non selective alpha 1 antagonists

phenoxybenzamine is slightly alpha 1

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only alpha 2 selective?

yohimbine

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alpha 1 selective?

prazosin
doxazosin
terazosin
tamsulosin

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reversible nonselective alpha? irreversible?

phentolamine

phenoxybenzamine

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irreversible will shift the curve to higher concentrations (also reversible) AND it will ?

reduce the maximum effect

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blockade of alpha receptors in smooth m reduces ? and ?

peripheral resistance

blood pressure

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giving an alpha antagonist to a mixed a&b agonist i.e. epi would result in?
known as??

fall in peripheral resistance (NO EFFECT ON B)
fall in BP (antagonizes alpha)
EPINEPHRINE REVERSAL

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giving an alpha antagonist to NE?

just blocks the increase in BP

practically no B receptor activity w/ NE

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on the heart, alpha antagonists do two things:

decreased blood pressure leads to reflex tachycardia via B1 receptors
presynaptic a2 receptors that decrease NE release are blocked, increasing NE release on heart & increasing HR and force of contraction

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blockade of a1 receptors in VEINS can results in ?

orthostatic hypotension

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phentolamine used in treatment of ? and ?

|&raquo_space;causes a drop in ? thru inhibiting a1 and reflex stim of ? to the heart (tachycardia)

hypertension
pheochromocytoma
peripheral resistance
SNS nerve terminals

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presynaptic inhibition of a2 causes an increased release of ? from sympathetic nerve terminals and an ? of reflex tachycardia

exacerbation

net result is vasodilatation, increased CO&rate
little effect on BP of patients with essential hypertension

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phentolamine ALSO inhibits ? receptors and activates ? and ? receptors

dopamine
muscarinic, histaminergic
*adverse effects include severe tachycardia, arrhythmias, myocardial ischemia, nasal congestion, and headache

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phenoxybenzamine inhibits ?, histamine, Ach, and serotonin receptors
-can cause ? from the presynaptic a2 blockade

NE reuptake
reflex tachycardia
*treatments same as phentolamine- Htn, phaeochromocytoma

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A/E of phentolamine and phenoxybenzamine include tachycardia, postural ?, nasal stuffiness, sexual ?, fatigue, sedation, and nausea

hypotension, dysfunction

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Tx for raynaud’s syndrome?

*also relieve Sx in ? and useful in ?

prazosin*, terazosin, doxazosin

BPH, BPH w/ comorbid Htn

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alpha 1 selective adr ant have less ? due to its lack of ?

reflex tachycardia, a2

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alpha one selective
3 hours?
9-12 hours?
22 hours?

praZOSIN
teraZOSIN
doxaZOSIN

4th a1 selective but structurally diff?
-met in the ?
higher potency for inhibiting ? contraction but less potency at vascular smooth m compared to other three
-used for relieving ? while producing less ?

tamsuLOSIN
liver
urinary retention in BPH
BPH, hypotension (use other in hypertensive pts)

a2 selective adrenoceptor antagonist?

-? effect that produces increases in HR, BP, anxiety and agitation

yohimbine
antidiuretic
**more serious a/e have been reported including renal failure, seizures, death

partial agonists that are also beta blockers? (2)

inhibit activation of B receptors in presence of ? but moderately activate receptors in presence of ?
said to have?

pindolol, acebutolol
high catecholamine concentrations
endogenous agonists

block alpha and beta receptors?

carvedilol, labetalol

in normotensive patients, taking beta antagonists does not usually cause ?

hypotension

at rest the PNS innervation of heart dominates>> therefore blockade of B receptors would ?

have little effect

Propanolol - decreased CO results in a transient reduction in ? activating a baroreflex increase in SNS outflow - ? will increase due to ? (normally vasodilatory) - the reflex increase in SNS outflow and less B2 receptor mediated vasodilation combine to increase the ? on vascular resistance causing an increase in ?

blood pressure peripheral resistance, blockade of B2 receptors SNS, arterial pressure

B1 selective agents will not block B2 vasodilation so there will be less of a decrease in ?

diastolic pressure

CHRONIC USE of B blockers: - in presence of ? total peripheral resistance returns to ? or is ? - delayed fall in ? and persistent reduction of ? accounts for its ? actions - beta blockers also reduce the release of ? from the kidney

hypertension, initial value, decreased peripheral resistance, CO, antihypertensive renin

drugs used to treat supraventricular arrhythmias and ventricular arrhythmias?

beta blockers | **also useful in angina, MI, and HF (the HF is counterintuitive because the heart is failing/decreased CO)

due NOT give an asthma patient a B2 blocker ie?

propanolol | *EVEN B1 selective agents at a high enough concentration can antagonize B2 receptors

mixed acting agents like ? hold promise in patients w/ asthma

celiprolol

nonselective B ant and B2 ant are CI in ? due to its blockage of glycogenolysis and gluconeogenesis -B blockers also mask the ? associated with ?, which is a warning sign in diabetics

insulin independent diabetes tachycardia hypoglycemia

chronic use of B blockers is associated with an increase in ? and decreased ? which is undesirable in CVD; also increases risk of CAD

VDL, HDL

b blocker used to decrease IOP in GLC? used in conjunction with muscarinic agonist?

timolol | pilocarpine

labetolol penbutolol pindolol acebutolol

partial agonists

longest acting beta blocker?

nadolol

alpha 1, beta 1 and partial agonist B2; can cause orthostatic hypotension

labetalol

ultra short B-1 selective?

esmolol

b1 selective widely used, htn, angina, MI

metoprolol

most b1 selectivity, NO mediated vasodilation, hypertension

nebivolol

to reduce effects like fatigue, sedation, sleep disturbances, depression, etc. use agents with lower ? like ? or ?

lower lipid solubility | nadolol, atenolol

B1 selective agents should only be used when completely necessary because they still ?

acting on the b2 receptor (asthma- bronchoconstriction)

life threatening a/e from b-blockers - being used in CHF or MI- reverse with ? or ?

isoproterenol | glucagon

b-blockers can interact with the ca2+ channel antagonist ? and cause bradycardia, HF, severe hypotension

verapamil

insulin dependent diabetes- give a ?

b1 selective blocker (as little activity on b2 as possible bc that deals with liver glycogenolysis&gluconeogenesis)

men complain of ? from b-blockers

impaired sexual activity

guanethidine metyrosine reserpine

indirect adrenergic; nonselective! | blocks the synthesis or release of catecholamines

blocks release of NE & can displace NE from storage vesicles?

guanethidine

inhibits tyrosine hydroxylase and prevents catecholamine synthesis?

metyrosine; rarely used to reduce pheochromocytoma

blocks uptake of catecholamines from cytoplasm to vesicles? results in accumulation of NE in cytoplasm degraded by MAO, decreasing BP and HR

reserpine | *long-acting and effects persist for days