Comparative Pharmacology
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus HISTAFED.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus HISTAFED.
AZELASTINE HYDROCHLORIDE CHILDREN'S ALLERGY vs HISTAFED
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Azelastine hydrochloride is a phthalazinone derivative that acts as a selective histamine H1-receptor antagonist. It inhibits the release of histamine and other mediators from mast cells, reduces chemotaxis, and decreases eosinophil activation. It also suppresses leukotriene and cytokine production.
HISTAFED is a combination of pseudoephedrine, a sympathomimetic amine that acts as a decongestant by stimulating alpha-adrenergic receptors in the nasal mucosa causing vasoconstriction, and triprolidine, a first-generation antihistamine that competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract, thereby preventing histamine-mediated effects.
Azelastine hydrochloride nasal spray: 1 spray (137 mcg) per nostril twice daily; maximum 2 sprays per nostril twice daily.
60 mg orally every 4 to 6 hours as needed; maximum 360 mg per day.
None Documented
None Documented
Terminal elimination half-life is 22–25 hours in adults; steady state achieved in 3–5 days. In children (6–11 years), half-life is similar (mean 22 hours).
3-4 hours for pseudoephedrine component; shorter in children (2-3 h), prolonged in renal impairment
Primarily renal (approximately 75%), with about 50% as unchanged drug and 25% as metabolites via CYP3A4 and CYP2D6. Fecal excretion accounts for ~20%.
Renal (approximately 65% as unchanged drug and metabolites), biliary/fecal (35%)
Category C
Category C
Antihistamine
Antihistamine/Decongestant Combination