Pharmacology II

Antihistamines, Sympathomimetics, β-Adrenergic Agonists

Adapted from Pharmacology for Nurses: A Pathophysiologic Approach (Adams, et al., 2013)

JONATHAN PLASKETT – WCSN

 :
Classification

Sympathomimetic

Exemplar: oxymetazoline (Afrin)

 Indications

• Nasal Congestion (Exemplar - oxymetazoline [Afrin])

• Asthma

• HTN

• Shock

• Cardiac Arrest (Epinephrine)

Mechanism of Action

Similar to Anticholinergics
§

Can be divided into TWO main categories

Mechanism of Action
Catecholamines Non-Catecholamines
• Biochemical structure • Longer duration of action
similar to NE
• Can administer orally
• Short half-life

• Must Administer
Parenterally
Mechanism of action*
Directly Indirectly
• Binds to/Activates 1. Release of NE from
Adrenergic Receptors presynaptic neurons

2. Inhibits NE reuptake

• Endogenous examples
• Epinephrine
• Examples
• Nor-Epinephrine
• Amphetamine
• Dopamine
• Cocaine
Predictable
Mechanism of action
Based on Autonomic Reaction of the Receptors (4 types)
α1- Tx of Nasal congestion*, HTN, dilates pupils during
ophthalmic exams
α2- Tx of HTN
β1- Tx of Cardiac Arrest, HF, Shock
β2- Tx of Asthma, premature labor contractions

*Exemplar – oxymetazoline (Afrin)

 Side effects
DON’T SWEAT IT

Just think about what they do to the

Nervous System
CARDIAC

Side effects
• Tachycardia, HTN, Dysrhythmias

CNS excitement

• Anxiety, Insomnia, Seizures

Others

• Dry Mouth, N/V, Anorexia(!?)… yup at least

some of them.
Nursing implications

• Assessment:
• Assess ECG for dysrhythmias
• BP for HTN
• Pulse for Tachycardia
Nursing implications

• Safety:
• Watch dosages (don’t overdose)
• Most in Pregnancy Category C.
• Contact Health Care provider before using especially in
in patients with
• Thyroid disorders
• HTN
• Diabetes
• Heart disease.
Nursing Implications

• Teaching: Avoid using St John’s Wort. Body may

develop tolerance if used over long periods of time and
may experience rebound symptoms, for this reason
many are not generally prescribed for longer than a few
days.

• Labs: Unknown interactions with lab tests.

• Overdose: No specific treatment for overdose

 Evaluation

• BP is Within “Normal” Limits

• Airway Sounds are Clear

• Decreased Signs/Symptoms of Shock

β-Adrenergic Agonists
(or justβ-Agonists)
Really just a subcategory of Sympathomimetics

Exemplar: albuterol (Proventil, Ventolin, VoSpire)

 Indications

• Asthma

• Pulmonary diseases

• Acute Bronchoconstriction (First Line of Therapy)

Mechanism of action

Activates:

β1 – Heart

β2 – Lungs*, Uterus and others

*Exemplar: albuterol
Mechanism of Action
Selective* Non-Selective
• Act on ONLY β2 receptors • Work on BOTH β1 and β2
receptors.

*Exemplar: albuterol
Mechanism of Action

• Classify by duration of action

• Short (most frequently prescribed, also referred to as
RESCUE DRUGS)
• Rapid onset of usually several minutes
• Therapeutic effect lasts about 2-6 hours
• Intermediate
• Therapeutic effect lasts about 8 hours
• Long
• Therapeutic effect lasts about 12 hours.
• BLACK BOX Warning – Long onset time can lead to death
 Side effects
Common

• Headaches, dizziness, tremors, nervousness,

throat irritation, tolerance

More Severe (mostly due to overdose)

• Tachycardia, dysrhythmias, hypokalemia,

hyperglycemia, hypotension, seizures,
pharyngitis, paradoxical bronchoconstriction,
circulatory failure, respiratory arrest.
Nursing Implications

• Assessment:
• Assess lung sounds
• Respirations
• Pulse
• BP
• ECG
Nursing implications

• Safety: Long acting aerosol drugs may appear similar

to short acting, use caution when administering drugs
for acute asthma attacks, administering long acting
drugs will delay the onset of therapeutic effects and
may result in death.
Nursing implications

• Teaching: Short, intermediate and long acting drugs

available. Drugs available PO, inhaled, and parentally.
PO drugs may cause systemic adverse reactions and
should be used judiciously. Tolerance may occur if
used chronically or over long periods, consult with
health care provider before stopping medication as
rebound effects may also occur.

• Labs: May cause hypokalemia at high doses. Monitor

K levels.
 evaluation

• Patient airway sounds are clear

• Patient exhibits no difficulty breathing

Antihistamines
(H1 Receptor Antagonists)

Exemplar: diphenhydramine (Benadryl)

 Indication

• Nasal Congestion*

• Vertigo/ Motion Sickness

• Parkinson’s Disease

• Insomnia

• Hives (Urticaria) and other skin rashes.

*Exemplar: diphenhydramine (Benadryl)

 Histamine?

The Mediator of Inflammation

Released from basophils and mast cells. Once at receptors

it can cause:

• Itching, Increased Mucous Secretion, Nasal Congestion

May cause Bronchoconstriction, Edema and

Hypotension (Just think Anaphylaxis)
 histamine
H1 Receptors H2 Receptors
• Responsible for • In Gastric Mucosa
Allergic Reactions
• Responsible for
Peptic Ulcers
Mechanism of Action

ANTI-Histamines selectively block H1 Receptors

(they only block these)

• May also cause Anticholinergic effects

(drying mucous membranes)
Mechanism of action

Motion Sickness/Vertigo

• Suppresses the vomiting center in medulla and

depresses neurons of the vestibular status of the inner
ear.

Parkinson’s Disease

• May treat mild forms – see chapter 20

 Side effects
• Significant drowsiness (Typically only older
generations of drugs)
• Often develop tolerance to this reaction

• CNS Stimulation
• Insomnia
• Nervousness
• Tremors
Nursing Implications

• Assessment:
• Assess for SS of allergic reactions
• Respirations
• Lung sounds
Nursing implications

• Teaching:
• Avoid taking henbane as it may cause increased
anticholinergic effects
• If taking for insomnia the effects may decrease after a few
days, not recommended to take for more than 2 weeks.
• Best when taken prophylactically.
• Also may cause typical Anticholinergic effects (e.g.
drying mucous membranes)
Nursing implications

• Labs: Drug should be discontinued at least 4 days

prior to skin allergy tests, otherwise may produce false-
negative results.

• Safety: Fall risk, don’t operate heavy machinery if

drowsy

• Overdose: may cause CNS depressions or excitation.

No specific treatment.
 Evaluation

• Pt has clear lung sounds

• Pt skin is clean and intact

• Pt can sleep through the night

• Pt movements are steady

• Pt has increased appetite

• Pt is able to ambulate safely

 References

Adams, M. P., Holland, N., & Carol Urban PhD, R. N. (2013). Pharmacology for
nurses: A pathophysiologic approach. Pearson Higher Ed.