Comparative Pharmacology
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus DIPHENHYDRAMINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus DIPHENHYDRAMINE.
AZELASTINE HYDROCHLORIDE CHILDREN'S ALLERGY vs Diphenhydramine
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.
Inverse agonist at histamine H1 receptors, blocking histamine-mediated effects in blood vessels, respiratory smooth muscle, and GI tract; also anticholinergic by blocking muscarinic receptors and sedative via central H1 receptor antagonism.
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; maximum 300 mg/day. Intravenous administration: 10-50 mg slow IV push (max 25 mg/min).
None Documented
None Documented
Clinical Note
moderateDiphenhydramine + Deferasirox
"The serum concentration of Deferasirox can be increased when it is combined with Diphenhydramine."
Clinical Note
moderateDiphenhydramine + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Diphenhydramine is combined with Fluticasone propionate."
Clinical Note
moderateDiphenhydramine + Tenofovir disoproxil
"The metabolism of Tenofovir disoproxil can be decreased when combined with Diphenhydramine."
Clinical Note
moderateTerminal 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 in adults; prolonged in hepatic impairment (up to 20 hours) and elderly.
Primarily renal (approximately 75%), with about 50% as unchanged drug and 25% as metabolites via CYP3A4 and CYP2D6. Fecal excretion accounts for ~20%.
Primarily renal (90-95% as metabolites, <5% unchanged). Minor biliary/fecal elimination (<5%).
Category C
Category C
Antihistamine
Antihistamine
Diphenhydramine + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Diphenhydramine."