NCM 106 Adrenergic Agonists PDF

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Adrenergic Agonists

(Sympathomimetics)

The autonomic nervous system (ANS) works to keep the


body’s homeostasis against internal and external changes in the
environment which alter the body’s internal functions
(e.g., blood pressure regulation, urinary excretion, water
balance, and digestive functions).

Adrenergic agonists are autonomic nervous system drugs that


stimulate the adrenergic receptors of the sympathetic nervous
system (SNS), either directly (by reacting with receptor sites)
or indirectly (by increasing norepinephrine levels). An
adrenergic agonist is also called a sympathomimetic because it
stimulates the effects of SNS.

Adrenergic agonists are further classified into three: alpha-


and beta-adrenergic agonists, alpha-specific adrenergic
agonists, and beta-specific adrenergic agonists.

• Adreneric Agonists: Generic and Brand Names


• Disease Spotlight: Glaucoma, Shock, and Asthma
• Alpha- and Beta-Adrenergic Agonists
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
o Interactions
o Nursing Considerations
▪ Nursing Assessment
▪ Nursing Diagnosis and Care Planning
▪ Implementation with Rationale
▪ Evaluation
• Alpha-Specific Adrenergic Agonists
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
o Interactions
o Nursing Considerations
▪ Nursing Assessment
▪ Nursing Diagnosis and Care Planning
▪ Implementation with Rationale
▪ Evaluation
• Beta-Specific Adrenergic Agonists
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
o Interactions
o Nursing Considerations
▪ Nursing Assessment
▪ Nursing Diagnosis and Care Planning
▪ Implementation with Rationale
▪ Evaluation
• References and Sources
• See Also
• Further Reading and External Links

Adreneric Agonists: Generic and Brand Names

Here is a table of commonly encountered adrenergic agonists,


their generic names, and brand names:

Classification Generic Name Brand Name

dobutamine Dobutrex

dopamine Intropin

Alpha- and Beta- ephedrine (generic)


Adrenergic Drugs
Adrenalin, Sus-
epinephrine
Phrine

norepinephrine Levophed
clonidine Catapress
Alpha-Specific Adrenergic
Agonists
phenylephrine Neo-Synephrine

Proventil,
albuterol
Ventolin

arformoterol Brovana

isoproterenol Isuprel

Beta-Specific Adrenergic levalbuterol Xopenex


Agonists
metaproterenol Alupent

pirbuterol Maxair Autohaler

salmetrol Serevent Diskus

terbutaline Brethine

Disease Spotlight: Glaucoma, Shock, and Asthma

• These agents are commonly used for treatment of


glaucoma, asthma, and shock or shock-like conditions.
• Glaucoma is an eye condition characterized by increased
in intraocular pressure. Alpha adrenergic agonists help
dilate the pupils, decrease the secretion of
aqueous humor, and increase the uveoscleral outflow. This
mechanisms relieve the eyes of too much pressure.
• Shock is a complication most commonly caused by acute
blood loss that can significantly alter the functions of
the organs and tissues. The effects of these agents
to cardiovascular system include pressure increase,
vasoconstriction, and increase blood flow to the muscles.
• Asthma is a hypersensitivity reaction to specific
triggers characterized by inflammatory reactions and
bronchospasm. Beta agonists are usually used for
treatment of bronchospasm and other obstructive
respiratory conditions.

Alpha- and Beta-Adrenergic Agonists

• Alpha- and beta- agonists are drugs that are generally


sympathomimetic. These agonists stimulate all of the
adrenergic receptors so they affect both alpha- and beta-
receptors.
• Popular examples of drugs under this class include
dopamine, dobutamine, and epinephrine.

Therapeutic Action

The desired and beneficial actions of alpha- and beta-agonists


are as follows:

• Acting on the adrenergic receptors of the target organs,


(i.e., increased heart rate and myocardial contractility
with the heart, bronchodilation with lungs, decrease
intraocular pressure with eyes).
• Other effects include: sweating, pupil dilation, increase
in rate and depth of respirations
• Facilitating the breakdown of glucose stores
(glycogenolysis) so it can be used as energy.

Indications

Alpha- and beta-agonists are indicated for the following medical


conditions:

• Sympathomimetic of choice for shock is dopamine, a


naturally occurring catecholamine. Aside from stimulating
the heart to increase the rate and force of its
contractions, it also causes dilation of the renal and
splanchnic arterioles increasing blood flow to the
kidneys. This way, renal shutdown is prevented.
• Dobutamine and ephedrine are synthetic catecholamines
indicated for treatment of heart failure. They increase
cardiac contractility without causing increase in oxygen
demand.
• Ephedrine stimulates release of norepinephrine from nerve
endings. Its use is declining because of availability of
drugs with more predictable onset and action. Many OTC
cold products contain this.
Here are some important aspects to remember for indication of
adrenergic agonists in different age groups:

Children

• They are at greater risk for GI and CV


complications. Dosage should be exact and should be
validated.
• NOTE Phenylephrine is often found in OTC allergy and
cold preparations so primary caregivers should be
instructed to check labels for ingredients and not
combine drugs with similar ingredients.
Adults

• Constant dosage adjustments based on response in patients


with shock or shock-like states is needed, especially
those on increased risk for cardiac complications.
• Most of these are emergency drugs and can be used in
patients who are pregnant and/or lactating. While there
are no adequate studies entailing their effects, use of
these drugs is justified when benefits clearly outweigh
the risks.
Older adults

• Dose adjustment is needed as this age group is also more


susceptible to drug side effects.
• They are more likely to have toxic levels of the drug
because of renal or hepatic impairments.
• Both adults and older adults must be cautioned against
using OTC drugs and complementary therapies.

Pharmacokinetics

Here are the characteristic interactions of alpha- and beta-


adrenergic agonists and the body in terms of absorption,
distribution, metabolism, and excretion:
Route Onset Peak Duration

Length of
IV 1-2 min 10 min
infusion

T1/2: 2 min
Metabolism: liver
Excretion: urine

Contraindications and Cautions

The following are contraindications and cautions for the use of


alpha- and beta-agonists:

• Allergy to any component of the drug. To prevent


hypersensitivity reactions.
• Pheochromocytoma. Systemic overload of catecholamines
could be fatal.
• Pulmonary hypertension. Exacerbated by the effect of the
drug.
• Tachyarrhythmias and ventricular fibrillation. Increased
heart rate and oxygen consumption caused by drugs can
exacerbate these conditions.
• Hypovolemia. Fluid replacement is the preferred treatment
associated with hypotension.
• Halogenated hydrocarbon general anesthetics. This
sensitizes the myocardium to catecholamines and could
cause serious cardiac effects.
• Peripheral cardiovascular disease. Caution should be used
as this can be exacerbated by systemic vasoconstriction
effect of the drug.

Adverse Effects

Use of alpha- and beta-agonists may result to these adverse


effects:
• Related to sympathetic stimulation: headache, sweating,
feelings of tension or anxiety, piloerection
• CV: arrhythmias, hypertension, palpitations, angina,
dyspnea
• GI: nausea, vomiting, constipation
• WARNING Because of vasoconstrictive effects, care must
be taken to avoid extravasation of any infused drugs. The
vasoconstriction in the area of extravasation can lead to
necrosis and cell death in that area.

Interactions

The following are drug-drug interactions involved in the use of


alpha- and beta-agonists:

• Tricyclic antidepressant (TCA) and monoamine oxidase


inhibitors (MAOI). Increased effects of these drugs
related to increased norepinephrine levels or increased
receptor stimulation that occurs with both drugs. TCAs
increase sympathomimetic effects with phenylephrine but
decreased antihypertensive effects with clonidine.
• Ma huang, guarana, caffeine. Increased risk of
hypertension especially with alpha agonists.
• Propranolol. Paradoxical hypertension with clonidine
• Any other adrenergic antagonist. Loss of effectiveness of
drugs.

Nursing Considerations

Here are important nursing considerations when administering


alpha- and beta-agonists:

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, pheochromocytoma, fatal arrhythmias, etc.) to
avoid adverse effects.
• Establish baseline physical assessment to monitor for any
potential adverse 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 urine output to evaluate perfusion of the kidneys
and therapeutic effects.
• Monitor laboratory test results (e.g. liver and renal
function tests) to determine need for possible dose
adjustment, and serum electrolyte levels to evaluate
fluid loss and appropriateness of therapy.

Nursing Diagnosis and Care Planning

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 tissue perfusion related to CV effects

Implementation with Rationale

These are vital nursing interventions done in patients who are


taking alpha- and beta-agonists:

• Use extreme caution in calculating and preparing doses of


these drugs because even small errors could have serious
effects.
• Use proper, aseptic technique when administering
ophthalmic or nasal agents (alpha- and beta- adrenergic
agonists) to prevent injection and assure the therapeutic
effectiveness of the drug.
• Monitor patient response closely (vital signs, ECG, urine
output) to ensure the most benefit with the least amount
of toxicity.
• Maintain phentolamine on standby in case extravasation
occurs. Save the area by infiltrating 10 mL of saline
containing 5-10 mg of phentolamine.
• Provide comfort measures (e.g. light control,
encouragement to void, monitoring bowel functions,
support and relaxation measures) to help patient cope
with the sympathomimetic effects of the drug.
• Provide patient education about drug effects and warning
signs to report.

Evaluation

Here are aspects of care that should be evaluated to determine


effectiveness of drug therapy:

• Monitor patient response to therapy (improvement in blood


pressure, ocular pressure, bronchial airflow).
• Monitor for adverse effects (e.g. CV changes, decreased
urine output, headache, GI upset).
• 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.

Alpha-Specific Adrenergic Agonists

• Alpha-specific adrenergic agonists or alpha-agonists are


drugs that bind primarily to alpha-receptors rather than
to beta-receptors.
• Popular examples of drugs under this class include
clonidine, midodrine, and phenylephrine.

Therapeutic Action

The desired and beneficial action of alpha-agonists is:

• Acting as a powerful postsynaptic alpha-adrenergic


receptor stimulant causing vasoconstriction and raising
systolic and diastolic blood pressure with little effect
on the beta-receptors of the heart.

Indications

Alpha-agonists are indicated for the following medical


conditions:

• Phenylephrine is a potent vasoconstrictor and alpha1-


agonist with little or no effect on the heart or bronchi
and is used in many combination cold and allergy
products. Parenterally, it is used in the following
medical conditions: shock or shock-like states
and paroxysmal supraventricular tachycardia. It is also
used to prolong local anesthesia and to maintain blood
pressure during spinal anesthesia. Topically, it used for
treatment of allergic rhinitis and symptoms of otitis
media.
• Midodrine is an oral drugs used to treat
orthostatic hypotension in patients who do not respond to
traditional therapy. It activates alpha1-adrenergic
receptors, leading to peripheral vasoconstriction and an
increase in vascular tone and blood pressure.
• Clonidine specifically stimulates alpha2-receptors of the
CNS leading to decreased CNS outflow of norepinephrine.
Orally and transdermally, it is used to control
hypertension and as an injection, it is for epidural
infusion for controlling cancer pain.

Pharmacokinetics

Here are the characteristic interactions of alpha-agonists and


the body in terms of absorption, distribution, metabolism, and
excretion:

Route Onset Peak Duration

IV Immediate – 15-20 min

IM, subcutaneous 10-15 min – 30-120 min


Very little
Topically systemic – –
absorption occurs

T1/2: 47-100 hours


Metabolism: tissues
Excretion: urine and bile

Contraindications and Cautions

The following are contraindications and cautions for the use of


alpha-agonists:

• Allergy to any component of the drug. To prevent


hypersensitivity reactions.
• Severe hypertension or tachycardia. Possible additive
effects.
• Narrow-angle glaucoma. Can be exacerbated by arterial
constriction.
• Pregnancy and lactation. No adequate studies on the
effects so use is reserved for situations in which the
benefit to the mother outweighs any potential risk to the
fetus or neonate.
• CV disease and vasospasm. Caution is used because these
conditions could be aggravate by the vascular effects of
the drug
• Thyrotoxicosis and diabetes. Sympathetic stimulation has
thyroid-stimulating and glucose-elevating effects
• Renal or hepatic impairment. Can interfere with
metabolism and excretion of the drug.

Adverse Effects

Use of alpha-agonists may result to these adverse effects:

• CNS: anxiety, restlessness, depression, fatigue, strange


dreams, personality changes
• Sympathetic stimulation: blurred vision, photosensitivity
• CV: arrhythmias, ECG changes, blood pressure changes,
peripheral vascular problem
• GI: nausea, vomiting, anorexia
• GU: decreased urinary output, difficulty
urinating, dysuria, changes in sexual function
• WARNING Sudden withdrawal can lead to: tachycardia,
hypertension, arrhythmias, flushing, and even death.
Taper drugs over 2-4 days.

Interactions

The following are drug-drug interactions involved in the use of


alpha-agonists:

• MAOIs: severe hypertension, headache, and hyperpyrexia


with phenylephrine
• TCA: increased sympathomimetic effects with
phenylephrine; decreased antihypertensive effects with
clonidine
• Digoxin, beta-blockers, antipsychotics: increased drug
effects with midodrine
• Adrenergic antagonists: loss of effectiveness of
adrenergic agonists

Nursing Considerations

Here are important nursing considerations when administering


alpha-agonists:

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, CV diseases, thyrotoxicosis or diabetes,
etc.) to avoid adverse effects.
• Establish baseline physical assessment to monitor for any
potential adverse effects.
• Assess level of orientation, affect, reflexes, and vision
to monitor for CNS changes related to drug therapy.
• Monitor blood pressure and pulse, assess peripheral
perfusion, and obtain electrocardiogram, if indicated, to
determine drug effectiveness and evaluate for adverse CV
effects.
• Monitor urine output to evaluate perfusion of the kidneys
and therapeutic effects.
• Evaluate patient for nausea and constipation to assess
adverse effects of the drug and establish appropriate
interventions.
• Monitor laboratory test results (e.g., liver and renal
function tests) to determine need for possible dose
adjustment.

Nursing Diagnosis and Care Planning

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, or vasoconstriction
• Disturbed sensory perception related to CNS effects
• Risk for injury related to CNS or CV effects

Implementation with Rationale


These are vital nursing interventions done in patients who are
taking alpha-agonists:

• Do not discontinue abruptly to prevent rebound


hypertension.
• Monitor blood pressure, orthostatic blood pressure,
pulse, rhythm, and cardiac output regularly to adjust
dose or discontinue the drug of CV effects are severe.
• Maintain phentolamine on standby when administering
phenylephrne in case extravasation occurs. Save the area
by infiltrating 10 mL of saline containing 5-10 mg of
phentolamine within 12 hours after extravasation to
preserve tissue.
• Provide comfort measures (e.g., rest and environmental
control) to help patient cope with the drug effects.
• Provide patient education about drug effects and warning
signs to report to promote understanding and compliance.

Evaluation

Here are aspects of care that should be evaluated to determine


effectiveness of drug therapy:

• Monitor patient response to therapy (improvement in


condition being treated).
• Monitor for adverse effects (e.g., GI upset, CNS, and 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.

Beta-Specific Adrenergic Agonists

• Beta-specific adrenergic agonists or beta-agonists are


drugs that bind primarily to beta-receptors rather than
to alpha-receptors.
• Popular examples of drugs under this class include
albuterol, salmeterol, and terbutaline.

Therapeutic Action

The desired and beneficial action of beta-agonists is:

• Acting on beta-adrenergic receptors to produce increased


heart rate, positive inotropic effect, bronchodilation,
and vasodilation.

Indications

Beta-agonists are indicated for the following medical


conditions:
• Treatment of bronchial spasm, asthma, and other
obstructive pulmonary conditions.

Pharmacokinetics

Here are the characteristic interactions of beta-agonists and


the body in terms of absorption, distribution, metabolism, and
excretion:

Route Onset Peak Duration

IV Immediate – 1-2 min

T1/2: Unknown
Metabolism: tissues
Excretion: –

Contraindications and Cautions

The following are contraindications and cautions for the use of


beta-agonists:

• Allergy to any component of the drug. To prevent


hypersensitivity reactions.
• Pulmonary hypertension. Can be exacerbated by drug
effects
• Anesthesia with halogenated hydrocarbons. Can sensitize
the myocardium to catecholamines and could cause a severe
reaction
• Eclampsia, uterine hemorrhage, and intrauterine
death. Can be complicated by uterine relaxation or
increased blood pressure
• Thyrotoxicosis and diabetes. Sympathetic stimulation has
thyroid-stimulating and glucose-elevating effects
• Severe renal impairment. Can alter drug excretion
Adverse Effects

Use of beta-agonists may result to these adverse effects:

• CNS: anxiety, restlessness, fatigue, fear, tremor,


headache
• CV: tachycardia, angina, myocardial infarction,
palpitations
• Respiratory: difficulty of breathing, bronchospasm,
severe pulmonary edema
• GI: nausea, vomiting, anorexia, GI upset
• Others: sweating, pupil dilation, rash, muscle cramps

Interactions

The following are drug-drug interactions involved in the use of


beta-agonists:

• Other sympathomimetic drugs: increased sympathomimetic


effects
• Beta-blockers: decreased therapeutic effects

Nursing Considerations

Here are important nursing considerations when administering


beta-agonists:

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, uterine hemorrhage, thyrotoxicosis or
diabetes, etc.) to avoid adverse effects.
• Establish baseline physical assessment to monitor for any
potential adverse effects.
• Assess CV status (pulse rate and blood pressure) to
evaluate for any CV effects associated with SNS
stimulation.
• Assess respiratory status to monitor drug effects and
assess for respiratory adverse effects.
• Monitor urine output to evaluate perfusion of the kidneys
and therapeutic effects.
• Monitor laboratory test results (e.g., liver and renal
function tests) to determine need for possible dose
adjustment.

Nursing Diagnosis and Care Planning

Here are some of the nursing diagnoses that can be formulated in


the use of this drug for therapy:

• Acute pain related to CV and systemic effects


• Decreased cardiac output related to CV effects
• Ineffective tissue perfusion related to CV effects

Implementation with Rationale

These are vital nursing interventions done in patients who are


taking beta-agonists:

• Monitor pulse and blood pressure carefully during


administration to arrange to discontinue the drug at any
sign of toxicity.
• Ensure that a beta-blocker is readily available when
giving parenteral isoproterenol in case severe reaction
occurs.
• Use minimal doses of isoproterenol needed to achieve
desired effects to prevent adverse effects and maintain
patient safety.
• Provide comfort measures to help patient cope with the
drug effects.
• Provide patient education about drug effects and warning
signs to report to promote understanding and compliance.
Evaluation

Here are aspects of care that should be evaluated to determine


effectiveness of drug therapy:

• Monitor patient response to therapy (improvement in


condition being treated, stabilization of blood pressure,
prevention of preterm labor).
• Monitor for adverse effects (e.g., GI upset, respiratory,
and 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.

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