Comparative Pharmacology
Head-to-head clinical analysis: ACTIDIL versus AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ACTIDIL versus AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY.
ACTIDIL vs AZELASTINE HYDROCHLORIDE CHILDREN'S ALLERGY
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
H1-receptor antagonist; competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract, blocking histamine-induced bronchoconstriction, vasodilation, and increased capillary permeability.
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.
2.5 mg orally every 4 to 6 hours as needed; maximum 10 mg per day.
Azelastine hydrochloride nasal spray: 1 spray (137 mcg) per nostril twice daily; maximum 2 sprays per nostril twice daily.
None Documented
None Documented
Terminal elimination half-life is approximately 20-25 hours in healthy adults; may be prolonged in elderly or patients with hepatic impairment.
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).
Renal excretion of unchanged drug and metabolites accounts for approximately 60-80% of the administered dose; biliary/fecal elimination comprises the remainder (20-40%).
Primarily renal (approximately 75%), with about 50% as unchanged drug and 25% as metabolites via CYP3A4 and CYP2D6. Fecal excretion accounts for ~20%.
Category C
Category C
Antihistamine
Antihistamine