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Adrenergic antagonists are also referred to as sympatholytics because they lyse, or block, the
effects of the sympathetic nervous system. They react with specific adrenergic receptor sites
without activating them, thus preventing the typical manifestations of SNS activation.
These drugs occupy the adrenergic receptor site so released norepinephrine can be prevented
from activating the receptor.
Adrenergic antagonists have varying degrees of specificity and are therefore classified into five:
nonselective adrenergic antagonists, nonselective alpha- and beta- adrenergic antagonists, and
selective alpha1– and beta-adrenergic antagonists.
Andrenergic Antagonists: Generic and Brand Names
Andrenergic Antagonists: Generic and Brand Names
Here is a table of commonly encountered adrenergic antagonists, their generic names, and brand
names:
amiodarone Cordarone
Nonselective Adrenergic
carvedilol Coreg
Blocking Agents
labetalol Normodyne, Trandate
Nonselective Alpha-
Adrenergic Blocking phentolamine Regitine
Agent
alfuzosin Uroxatral
doxazosin Cardura
Alpha1-Selective
Adrenergic Blocking prazosin Minipress
Agents
tamsulosin Flomax
terazosin Hytrin
propranolol Inderal
timolol Blocarden, Timoptic
bisoprolol Zebeta
Beta1-Selective
Adrenergic Blocking esmolol Brevibloc
Agents
metoprolol Lopressor, Toprol XL
T1/2: 6-8 h
Metabolism: liver
Excretion: urine
Interactions
The following are drug-drug interactions involved in the use of nonselective adrenergic
antagonists:
Volatile liquid anesthetics (e.g. halothane, isoflurane). Increased risk of excessive hypotension.
Antidiabetics. Increased effects of antidiabetics so hypoglycemia should be watched out for.
Verapamil and diltiazem. Potentially dangerous conduction system disturbances if combined
with carvedilol.
Nursing Considerations
Here are important nursing considerations when administering nonselective adrenergic
antagonists:
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking,
and examination:
Assess for contraindications or cautions (e.g. history of allergy to drug, heart blocks, asthma,
pregnancy or lactation status, etc.) to avoid adverse effects.
Establish baseline physical assessment to monitor for any potential adverse effects.
Assess the level of orientation and for any complaints of dizziness, paresthesias, or vertigo to
monitor CNS drug effects.
Assess vital signs, especially pulse and blood pressure to monitor for possible excess stimulation
of the cardiac system.
Note respiratory rate and auscultate lungs for adventitious sounds to evaluate effects on bronchi
and respirations.
Monitor laboratory test results (e.g. liver and renal function tests) to determine need for possible
dose adjustment, serum electrolyte levels to evaluate fluid loss and appropriateness of therapy,
and blood glucose to evaluate for hyper- or hypoglycemia.
Nursing Diagnoses
Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
Decreased cardiac output related to CV effects
Ineffective airway clearance related to lack of bronchodilating effects
Risk for injury related to CNS effects
Diarrhea related to increased parasympathetic activity
T1/2: Unknown
Metabolism: Unknown
Excretion: Unknown
Adverse Effects
Use of nonselective alpha-adrenergic antagonists may result to these adverse effects:
CNS: headache, weakness, dizziness
CV: hypotension, orthostatic hypotension, angina, MI, cerebrovascular accident, flushing,
tachycardia, arrhythmia
GI: nausea, vomiting, diarrhea
Interactions
The following are drug-drug interactions involved in the use of nonselective alpha-adrenergic
antagonists:
Ephedrine and epinephrine. Decreased hypertensive and vasoconstrictive effects
Alcohol. Increased hypotension
Nursing Considerations
Here are important nursing considerations when administering nonselective alpha-adrenergic
antagonists:
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking,
and examination:
Assess for contraindications or cautions (e.g. history of allergy to drug, CV diseases, pregnancy
or lactation status, etc.) to avoid adverse effects.
Establish baseline physical assessment to monitor for any potential adverse effects.
Assess orientation, affect, and reflexes to monitor for CNS changes related to drug therapy.
Monitor CV status (blood pressure, pulse rate, peripheral perfusion) to determine changes in
function.
Monitor urine output which will reflect perfusion of the kidney as another assessment of cardiac
function.
Nursing Diagnoses
Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
Decreased cardiac output related to blood pressure changes, arrhythmias, and vasodilation
Risk for injury related to CNS and CV effects
Implementation with Rationale
These are vital nursing interventions done in patients who are taking nonselective alpha-
adrenergic antagonists:
Monitor heart rate and blood pressure closely and frequently for changes to anticipate the need to
discontinue the drug if adverse reactions are severe.
Inject phentolamine directly into area of extravasation of epinephrine or dopamine to prevent
local cell death.
Institute safety measures to prevent injury if the patient experiences weakness, dizziness, or
orthostatic hypotension.
Provide comfort measures to help patient cope with drug effects.
Provide patient education about drug effects and warning signs to report to enhance knowledge
about drug therapy and promote compliance.
Evaluation
Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
Monitor patient response to therapy (improvement in signs and symptoms of
pheochromocytoma, improvement in tissue condition after extravasation).
Monitor for adverse effects (e.g. orthostatic hypotension, arrhythmias, CNS effects).
Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
Monitor patient compliance to drug therapy.
Alpha1-Selective Adrenergic Blocking Agents
Alpha1-selective adrenergic blocking agents are drugs that have a specific affinity for alpha1-
receptors.
Common drug examples include prazosin, tamsulosin, and doxazosin.
Therapeutic Action
The desired and beneficial actions of alpha1-selective adrenergic blocking agents are as follows:
Blocking the postsynaptic alpha1-receptor sites. This causes a decrease in vascular tone and
vasodilation, which leads to a fall in blood pressure. A reflex tachycardia that accompanies a fall
in blood pressure does not occur because they do not block presynaptic alpha2-receptor sites.
Reducing total peripheral resistance through alpha blockade; it does not affect heart rate or
cardiac output.
Increasing high-density lipoproteins while lowering total cholesterol level.
Blocking smooth muscle receptors in prostate, prostatic capsule, prostatic urethra, and urinary
bladder neck leading to relaxation of bladder and prostate and improved flow of urine in male
patients.
Indications
Alpha1-selective adrenergic blocking agents are indicated for the following medical conditions:
For treatment of benign prostatic hypertrophy (BPH)
For treatment of mild to moderate hypertension as monotherapy or in combination with other
antihypertensives.
Pharmacokinetics
Here are the characteristic interactions of alpha1-selective adrenergic blocking agents and the
body in terms of absorption, distribution, metabolism, and excretion:
Route Onset Peak Duration
T1/2: 22 hours
Metabolism: liver
Excretion: bile, feces, urine
Evaluation
Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
Monitor patient response to therapy (lowering of blood pressure, improved urine flow with
BPH).
Monitor for adverse effects (e.g. GI upset, CNS, or CV changes).
Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
Monitor patient compliance to drug therapy.
Nonselective Beta-Adrenergic Blocking Agents
Nonselective beta-adrenergic blocking agents are drugs that block the beta-receptors within the
SNS. Nonselective blockade of all beta-receptors results in a loss of the reflex bronchodilation
that occurs with sympathetic stimulation.
Use of these drugs is limited in patients who smoke or have allergic or seasonal rhinitis, asthma,
or COPD.
Common drug examples include propranolol, nebivolol, and timolol.
Therapeutic Action
The desired and beneficial actions of nonselective beta-adrenergic blocking agents are as
follows:
Competitively blocks beta-adrenergic receptors in the heart and juxtaglomerular apparatus
Reduction of vascular tone in the CNS
Indications
Nonselective beta-adrenergic blocking agents are indicated for the following medical conditions:
These drugs are used for a wide range of conditions, including hypertension, stage fright
(situational anxiety), migraines, angina, and essential tremors.
Timolol and carteolol in ophthalmic form are used for reduction of intraocular pressure in
patients with open-angle glaucoma.
Pharmacokinetics
Here are the characteristic interactions of nonselective beta-adrenergic blocking agents and the
body in terms of absorption, distribution, metabolism, and excretion:
Interactions
The following are drug-drug interactions involved in the use of nonselective beta-adrenergic
blocking agents:
Clonidine. Paradoxical hypertension can occur; increased rebound hypertension with clonidine
withdrawal.
NSAIDs. Decreased antihypertensive effect
Epinephrine. Initial hypertensive episode followed by bradycardia
Ergot alkaloids. Peripheral ischemia may occur
Insulin and other antidiabetic agents. Potential change in blood glucose levels
Nursing Considerations
Here are important nursing considerations when administering nonselective beta-adrenergic
blocking agents:
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking,
and examination:
Assess for contraindications or cautions (e.g. history of allergy to drug, heart failure, pregnancy
or lactation status, etc.) to avoid adverse effects.
Establish baseline physical assessment to monitor for any potential adverse effects.
Assess orientation, affect, and reflexes to monitor for CNS changes related to drug therapy.
Monitor CV status (blood pressure, pulse rate, peripheral perfusion) to determine changes in
function.
Assess abdomen, including auscultating bowel sounds to monitor GI effects.
Monitor renal and hepatic function tests to evaluate potential need for dose adjustment, as well as
electrolyte levels to monitor for risks for arrhythmias.
Nursing Diagnoses
Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
Acute pain related to CNS, GI, and systemic
Decreased cardiac output related to CV effects
Ineffective tissue perfusion related to CNS effects
Implementation with Rationale
These are vital nursing interventions done in patients who are taking nonselective beta-
adrenergic blocking agents:
Do not stop these drugs abruptly after chronic therapy, but taper gradually over 2 weeks because
long-term use of these drugs can sensitize the myocardium to catecholamines, and severe
reactions could occur.
Continuously monitor any patient receiving an intravenous form of these drugs to avert serious
complications caused by rapid sympathetic blockade.
Provide comfort measures to help patient cope with drug effects.
Provide patient education about drug effects and warning signs to report to enhance knowledge
about drug therapy and promote compliance.
Evaluation
Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
Monitor patient response to therapy (lowering of blood pressure, decrease in angina episodes,
and improvement of condition being treated).
Monitor for adverse effects (e.g. GI upset, CNS, or CV changes).
Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
Monitor patient compliance to drug therapy.
Beta1-Selective Adrenergic Blocking Agents
Beta1-selective adrenergic blocking agents are drugs that do not block the beta1-receptors
responsible for bronchodilation. This gives them an advantage over nonselective beta-blockers.
These drugs are preferred for patients who smoke or who have asthma, any other obstructive
pulmonary disease, or seasonal or allergic rhinitis.
Popular examples under this class include atenolol, metoprolol, and esmolol.
Therapeutic Action
The desired and beneficial actions of beta1-selective adrenergic blocking agents are as follows:
Blocking the beta1-adrenergic receptors decreasing the excitability of the heart, cardiac output,
and oxygen consumption.
Decreasing renin release which lowers blood pressure.
Indications
Nonselective beta-adrenergic blocking agents are indicated for the following medical conditions:
Treatment for cardiac arrhythmias, hypertension, and chronic angina
Prevention of reinfarction after an MI by decreasing cardiac workload and oxygen consumption
In oral form, used to decrease intraocular pressure and to treat open-angle glaucoma
Pharmacokinetics
Here are the characteristic interactions of beta1-selective adrenergic blocking agents and the
body in terms of absorption, distribution, metabolism, and excretion:
IV Immediate 5 min 24 h
T1/2: 6-7 h
Metabolism: –
Excretion: bile, urine, feces
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking,
and examination:
Assess for contraindications or cautions (e.g. history of allergy to drug, bradycardia, pregnancy
or lactation status, etc.) to avoid adverse effects.
Establish baseline physical assessment to monitor for any potential adverse effects.
Assess orientation, affect, and reflexes to monitor for CNS changes related to drug therapy.
Monitor CV status (blood pressure, pulse rate, peripheral perfusion) to determine changes in
function.
Assess abdomen, including auscultating bowel sounds to monitor GI effects.
Monitor renal and hepatic function tests to evaluate potential need for dose adjustment, as well as
electrolyte levels to monitor for risks for arrhythmias.
Nursing Diagnoses
Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
Acute pain related to CNS, GI, and systemic
Decreased cardiac output related to CV effects
Ineffective tissue perfusion related to CNS effects
Evaluation
Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
Monitor patient response to therapy (lowered blood pressure, fewer angina episodes, lowered
intraocular pressure).
Monitor for adverse effects (e.g. GI upset, CNS, or CV changes).
Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication,
and adverse effects to watch for.
Monitor patient compliance to drug therapy.