Comparative Pharmacology
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE versus HYDROXYZINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE versus HYDROXYZINE.
AZELASTINE HYDROCHLORIDE vs HYDROXYZINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Azelastine hydrochloride is a phthalazinone derivative that exerts its effect by competitively inhibiting histamine at the H1 receptor site. It also stabilizes mast cells, reducing the release of inflammatory mediators such as histamine, leukotrienes, and cytokines. This dual action provides both antihistaminic and anti-inflammatory effects.
Hydroxyzine is a first-generation antihistamine that acts as a competitive antagonist at histamine H1 receptors in the gastrointestinal tract, blood vessels, and respiratory tract. It also exhibits sedative, anxiolytic, and antiemetic properties, possibly through central nervous system depression and anticholinergic effects.
1 spray (137 mcg) per nostril twice daily; ophthalmic: 1 drop in affected eye(s) twice daily.
25-100 mg orally 3-4 times daily; 50-100 mg IM every 4-6 hours as needed. Maximum oral dose: 600 mg/day in divided doses.
None Documented
None Documented
Clinical Note
moderateHydroxyzine + Venlafaxine
"The risk or severity of adverse effects can be increased when Hydroxyzine is combined with Venlafaxine."
Clinical Note
moderateHydroxyzine + Nefazodone
"The risk or severity of adverse effects can be increased when Hydroxyzine is combined with Nefazodone."
Clinical Note
moderateHydroxyzine + Mifepristone
"Hydroxyzine may increase the QTc-prolonging activities of Mifepristone."
Clinical Note
moderateHydroxyzine + Fesoterodine
Terminal elimination half-life is approximately 22 hours (range 20–25 hours) following oral administration, supporting twice-daily dosing. For ophthalmic and intranasal routes, systemic half-life is similar due to absorption.
Terminal elimination half-life: 14-25 hours (mean ~20 h). In elderly or hepatic impairment, may be prolonged; antihistamine effect persists beyond half-life due to active metabolite.
Approximately 75% of the dose is excreted in feces as unchanged drug and metabolites; about 25% is excreted renally, with less than 10% as unchanged drug.
Renal: approximately 70% as metabolites, less than 1% unchanged. Fecal/biliary: minor. Cetirizine (active metabolite) also renally eliminated.
Category C
Category A/B
Antihistamine
Antihistamine
"The serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Hydroxyzine."