Comparative Pharmacology
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus PROMETHAZINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AZELASTINE HYDROCHLORIDE CHILDREN S ALLERGY versus PROMETHAZINE.
AZELASTINE HYDROCHLORIDE CHILDREN'S ALLERGY vs PROMETHAZINE
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.
Promethazine is a phenothiazine derivative that acts as a potent histamine H1 receptor antagonist, thereby blocking the effects of histamine. It also has central anticholinergic, antiemetic, and sedative properties, likely mediated through antagonism at muscarinic, dopamine D2, and serotonin receptors in the brain.
Azelastine hydrochloride nasal spray: 1 spray (137 mcg) per nostril twice daily; maximum 2 sprays per nostril twice daily.
12.5-25 mg IM or IV every 4-6 hours; also 25 mg PO or PR every 6-8 hours. Maximum 100 mg/day.
None Documented
None Documented
Clinical Note
moderatePromethazine + Risedronic acid
"Promethazine can cause an increase in the absorption of Risedronic acid resulting in an increased serum concentration and potentially a worsening of adverse effects."
Clinical Note
moderatePromethazine + Methylphenidate
"Promethazine can cause an increase in the absorption of Methylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects."
Clinical Note
moderatePromethazine + Artesunate
"The serum concentration of Artesunate can be increased when it is combined with Promethazine."
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 9-16 hours; may be prolonged in hepatic impairment.
Primarily renal (approximately 75%), with about 50% as unchanged drug and 25% as metabolites via CYP3A4 and CYP2D6. Fecal excretion accounts for ~20%.
Renal (70-80% as metabolites, <1% unchanged); biliary/fecal minor.
Category C
Category A/B
Antihistamine
Antihistamine / Antiemetic
Promethazine + Clotrimazole
"The metabolism of Clotrimazole can be decreased when combined with Promethazine."