Comparative Pharmacology
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus BENADRYL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus BENADRYL.
AZELASTINE HYDROCHLORIDE CHILDREN'S ALLERGY vs BENADRYL
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.
Antihistamine; inverse agonist at histamine H1 receptors, blocking histamine-induced vasodilation, increased capillary permeability, and bronchoconstriction; also anticholinergic and sedative.
Azelastine hydrochloride nasal spray: 1 spray (137 mcg) per nostril twice daily; maximum 2 sprays per nostril twice daily.
25-50 mg orally every 4-6 hours as needed; maximum 300 mg per day. Alternatively, 10-50 mg intramuscularly or intravenously once, maximum 100 mg per dose (IV route preferred).
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).
Terminal elimination half-life 4-8 hours; prolonged in hepatic impairment (up to 20 hours).
Primarily renal (approximately 75%), with about 50% as unchanged drug and 25% as metabolites via CYP3A4 and CYP2D6. Fecal excretion accounts for ~20%.
Renal (90% as metabolites, <5% unchanged); minimal biliary/fecal.
Category C
Category C
Antihistamine
Antihistamine