Adrenergic Agonists (sympathomimetics)

The Autonomic Nervous System (ANS) works to maintain the body's homeostasis against internal
and external changes in the environment that alters the body's internal functions( e.g., bp regulation,
urinary excretion, water balance and digestive functions)

Adrenergic agonists are ANS drugs which stimulates the adrenergic receptors of the sympathetic
nervous system, either directly (reacting with receptor sites) or indirectly (by increasing norepinephrine
levels)

Adrenergic agonists are also known as the sympathomimetic because it stimulates or mimics the
effects of SNS

The adrenergic agonists are classified into three:

1. Alpha- and beta-adrenergic agonists

2. Alpha specific adrenergic agonists
3. Beta specific adrenergic agonists

ALPHA- AND BETA-ADRENERGIC AGONISTS

Mechanism of action:

• drugs that are generally sympathomimetic

• stimulates all of the adrenergic receptors so they affect both alpha and beta receptors

Indications

Alpha- and beta- adrenergic agonists are indicated for the following medical conditions:

• Dopamine (intropin)- for patients that are experiencing shock as it is a naturally occurring
catecholamine. Aside from stimulating the heart to increase 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 (dobutrex) – for treatment of heart failure, it increases cardiac contractility without
causing an increase in oxygen demand
• Ephedrine – stimulates release of norepinephrine from nerve endings, used to treat breathing
problems (bronchodilator), nasal congestion (decongestant), low blood pressure problems.
• Phenylephrine – used for temporary relief of stuffy nose, sinus, and ear symptoms caused by
common cold, flu, allergies or other breathing illnesses.

Therapeutic Actions

The desired and beneficial actions are as follows:

• Acting on the adrenergic receptors of the target organs (increased heart rate and myocardial
contractility of the heart, bronchodilation of the lungs, decrease intraocular pressure of the eyes)
• Treat and manage glaucoma, anaphylactic shock, hypotension, hypertension, heart failure, nasal
congestion
• Facilitating the breakdown of glucose stores so it can be used as energy

Side Effects & Adverse Effects

The use of alpha- and beta- adrenergic agonists may result to these adverse effects:

• Sympathomimetic stimulation: headache, sweating, anxiety, piloerection

• Cardiovascular system: hypertension, palpitations, angina, dyspnea
• GI: nausea, vomiting, constipation
• WARNING: due to its vasoconstrictive effects, care must be taken to avoid any extravasation of any
infused drugs. Vasoconstriction in the area of extravasation can lead to necrosis and cell death in
the area.

Contraindications

• Allergy to any components 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 cause
by drugs can exacerbate these conditions
• hypovolemia- fluid replacement is preferred treatment associated with hypotension
• Halogenated hydrocarbon general anesthetics- 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

Interactions

the following are the drug-drug interactions involved in the use of alpha-beta agonists:
• tricyclic antidepressant (TCA) and monoamine oxidase inhibitors (MAOI) - increased effect of these
drugs related to increases norepinephrine level or increased receptor stimulation that occurs with
both drugs. TCA increase sympathomimetic effects with phenylephrine but decreased
antihypertensives 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

List Of Medications and Dosages of Alpha-Beta Adrenergic Agonist Drugs Available in the Market

• Dobutamine (dobutrex)
▪ Dosages – Adults and Pedia
• Infusion Solution in D5W – 100mg/100mL, 200mg/100mL, 400mg/100mL
• Injectable Solution – 12.5mg/mL
• Dopamine (intropin)
▪ Adult dose: initial dose- 1-5 mcg/kg by continuous IV infusion
▪ Pediatric dose: Less than 1 month old – 1 to 20 mcg/kg/min by continuous IV infusion
1 month or older- 1 to 20 mcg/kg/min by continuous IV infusion, max. 50
mcg/kg/min
• Ephedrine
▪ For the treatment of asthma – 25mg tablets q4hrs PRN , maximum dose 150mg in 24 hours
▪ For adults- bolus dose recommendation – 5-10 mg and IM 25 to 50mg
• Epinephrine (adrenalin, sus-phrine)
▪ Adult dose for cardiac arrest – 0.5 to 1mg (5-10 mL) IV once; during resuscitation effort- 0.5
mg (5mL) should be given q15mins
▪ Adrenalin – 30mg/mL (1mg/mL)
▪ Sus-phrine - 1:1,000 is 0.01 cc's per kg given every 15 minutes until the anaphylaxis or urticaria
are under good control, q5-6hours
• Norepinephrine (levophed)
▪ Initial: 8-12 mcg/minute intravenous (IV) infusion; titrate to effect.
▪ Maintenance: 2-4 mcg/minute IV infusion.

Nursing Considerations and Intervention

• 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.
ALPHA-SPECIFIC ADRENERGIC AGONISTS

Mechanism of Action:

• Drugs that bind primarily to alpha-receptors

Indications

• Phenylephrine – used in many combinations of 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 – oral drugs that is used to treat orthostatic hypotension in patients who does not
respond to traditional therapy.
• Clonidine – decrease CNS outflow of norepinephrine. PO and TD, used to control hypertension as
injection and for epidural infusion for controlling cancer pain.

Therapeutic Action

• Acts as powerful postsynaptic alpha-adrenergic receptor stimulant causing vasoconstriction and

raising systolic and diastolic blood pressure with little effect of the beta-receptors of the heart.
• Management of vasodilatory shock, hypotension, hypoperfusion, septic shock, cardiopulmonary
arrest, heart failure decompensation.

Side Effects & Adverse Effects

• CNS: anxiety, restlessness, depression, fatigue, strange dreams, personality changes

• Sympathetic stimulation: blurred vision, photosensitivity
• CV: arrythmias, 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, arrythmias, flushing and
even death. Taper drugs over 2-4 days.

Contraindications

• 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.

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

List Of Medications and Dosages of Alpha Specific Adrenergic Agonist Drugs Available in the Market

• Phenylephrine
▪ Nasal Congestion – 0.25 -1% solution, instill 2-3 drops or sprays in each nostril q4hrs PRN for
3 days
▪ IV- initially 500mcg via FD (within 20-30 secs) increase in increments of 100-200 mg up to 1
mg PRN
 • Midodrine
▪ Orthostatic Hypotension – 2.5 mg 3 times a day with not more than 30mg per day.
▪ Children – must be determined by doctor
• Clonidine (catapres)
▪ PO 3 dosage strength: 0.1 mg, 0.2mg and 0.3 mg

Nursing Considerations/Interventions

• 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 phenylephrine 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.
•

BETA SPECIFIC ADRENERGIC AGONISTS

Mechanism of Action

• Drugs that bind primarily to beta-receptors

Indications

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

Therapeutic Actions

• Acting on beta-adrenergic receptors to produce increased heart rate, positive inotropic effect,
bronchodilation and vasodilation

Side Effects & 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

Contraindications

• 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

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

List Of Medications and Dosages of Beta Specific Adrenergic Agonist Drugs Available in the Market

• Albuterol
▪ Nebulizer Inhalation Solution- 2.5mg 3-4 times a day over approximately 5-15 minutes
 • Salmeterol
▪ 50mcg (1 inhalation) PO BID, 12hr interval
• Terbutaline
▪ Adults – 5mL(mg) three times a day, not more than 15mg/day
▪ Children – 2.5mg three times a day, not more than 7.5 mg/day

Nursing Considerations/Interventions

• 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.

References:

Tabangcora, I. RN (2023, July 2). Adrenergic Agonists (Sympathomimetics.

https://nurseslabs.com/adrenergic-agonists-sympathomimetics/?fbclid=IwAR0D_FUvdArsrxKJ-
OETgdTabq_CTHULodd-2QsxA2Iz97pvAmcie8fdFBs#google_vignette

Sinja, S. (2023, April 4). Dopamine Injection.

https://www.drugs.com/dopamine.html

Dean, J. (2023, June 5). Alpha-1 Receptor Agonists

https://www.ncbi.nlm.nih.gov/books/NBK551698/#:~:text=Alpha%2D1%20agonists%20are%20a
,as%20other%20lower%20acuity%20conditions.