Comparative Pharmacology
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus DIPHENHYDRAMINE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus DIPHENHYDRAMINE HYDROCHLORIDE.
AZELASTINE HYDROCHLORIDE CHILDREN'S ALLERGY vs DIPHENHYDRAMINE HYDROCHLORIDE
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.
Competitive antagonist of histamine H1 receptors, reducing allergic symptoms; also exerts anticholinergic, sedative, and antiemetic effects via central and peripheral receptor blockade.
Azelastine hydrochloride nasal spray: 1 spray (137 mcg) per nostril twice daily; maximum 2 sprays per nostril twice daily.
25-50 mg orally or intramuscularly every 4-6 hours as needed; maximum 300 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).
Terminal elimination half-life 4–10 hours (mean ~7 hours); prolonged in elderly, hepatic impairment, and with CYP2D6 poor metabolizers.
Primarily renal (approximately 75%), with about 50% as unchanged drug and 25% as metabolites via CYP3A4 and CYP2D6. Fecal excretion accounts for ~20%.
Renal elimination of metabolites accounts for ~60% of the dose; <5% excreted unchanged. Fecal excretion ~40% via bile.
Category C
Category A/B
Antihistamine
Antihistamine