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Anti
Histamines
A Quick Overview
 Mechanism of Action

Antihistamines are drugs that inhibit the action of histamine by

blocking the H1 histamine receptors. This action prevents the
histamine-induced responses in various tissues, such as
vasodilation, increased vascular permeability, and sensory
nerve stimulation, which lead to symptoms like itching, swelling,
and redness.
 Indications
Allergic rhinitis
Urticaria (hives)
Conjunctivitis
Atopic dermatitis
Anaphylaxis (as adjunctive therapy)
Nausea and vomiting (certain antihistamines)
Motion sickness
Insomnia (sedative properties of some antihistamines)
 Anti histamines
First-Generation antihistamines: Diphenhydramine,
Chlorpheniramine, Hydroxyzine, Promethazine.

Second-generation antihistamines (e.g., loratadine,

cetirizine)

Third-generation antihistamines (e.g., levocetirizine,

fexofenadine)
 Generations
01 02 03

These are known for their These have reduced These have reduced
sedative properties due sedative effects and a sedative effects and even
to their ability to cross lower tendency to cross lower tendency to cross
the blood-brain barrier. the blood-brain barrier. the blood-brain barrier.
 Dosing
1 2 3
Diphenhydramine: Loratadine: Fexofenadine:
Adults: 25-50 mg every Adults and children ≥12 Adults and children ≥12
4-6 hours years: 10 mg once daily. years: 180 mg PO qDay
Children: Dose based on Children 2-12 years: 5 or 60 mg PO BID.
weight (5 mg/kg/24 mg PO qDay. Children 2-12 years:
hours divided into 4-6 >6 years: 10 mg PO 30 mg PO BID
doses. qDay
 Counseling

Caution against driving Advise patients to Avoiding known

or operating heavy avoid alcohol while allergens, using air
machinery, especially taking antihistamines, filters, and maintaining
with first-generation a clean environment.
as it can increase
antihistamines, due to can reduce allergy
sedation.
potential sedation. incidents.
 Women
Studies consistently show no significant risk of
fetal malformations with first-generation
antihistamines, and these agents are considered
safe. The second & third-generation
antihistamines loratadine (Claritin), cetirizine
(Zyrtec), and fexofenadine (Allegra) do not
appear to increase overall fetal risk.

- AAFP
 Most Common Side
Effects
Sedation and drowsiness (more common with first-generation
antihistamines)
Dry mouth
Dizziness
Headache
Blurred vision
Constipation
Urinary retention
 Drug and Food Interactions

Monoamine Oxidase Inhibitors (MAOls): Concurrent use with antihistamines

can lead to increased anticholinergic effects or central nervous system
(CNS) depression.
Central Nervous System Depressants: The sedative effects of antihistamines
can be potentiated by other CNS depressants, including benzodiazepines,
opioids, and muscle relaxants.
Alcohol: Increases sedation and impairs cognitive function when taken with
antihistamines.
Grapefruit Juice: May interact with some antihistamines metabolized by the
CYP3A4 enzyme, increasing their blood levels and potential for side effects.
 Conclusion
Antihistamines play a vital role in managing allergic
conditions, but understanding their characteristics and
considerations is essential for safe and effective use in
clinical practice.
Stay informed, stay compassionate, and continue providing
excellent patient care!
Thank You
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