Azelastine


Full Generic Medicine Info
Dosage/Direction for Use

Nasal
Allergic rhinitis
Adult: As spray: 140 mcg into each nostril bid.
Child: ≥6 years Same as adult dose.

Ophthalmic
Seasonal allergic conjunctivitis
Adult: As 0.05% solution: Instill 1 drop into affected eye(s) bid. For severe cases, increase to 4 times daily. Max duration: 6 weeks.
Child: ≥4 years Same as adult dose.

Ophthalmic
Allergic conjunctivitis, perennial
Adult: As 0.05% solution: Instill 1 drop into affected eye(s) bid. For severe cases, increase to 4 times daily. Max duration: 6 weeks.
Child: ≥12 years Same as adult dose.
Special Precautions
Pregnancy and lactation. Patient Counselling Avoid contact with soft contact lenses. This drug may cause somnolence and eye irritation, if affected, do not drive or operate machinery.
Adverse Reactions
Significant:: Irritation of nasal mucosa (e.g. stinging, itching, sneezing, epistaxis) and eyes (e.g. burning, pain); conjunctivitis. Gastrointestinal disorders: Dry mouth. Rarely, nausea. General disorders and administration site conditions: Fatigue. Nervous system disorders: Headache, bitter taste. Psychiatric disorders: Somnolence.
Drug Interactions
Reduced CNS function and alertness with CNS depressants.
Food Interaction
Reduced CNS function and alertness with alcohol.
Action
Azelastine, a phthalazinone derivative, selectively blocks H1-receptors on effector cells, inhibiting the release of histamine involved in allergic response. Additionally, it inhibits the accumulation of other inflammatory mediators like leukotriene, platelet activation factor (PAF), serotonin, and eosinophil.
Onset: 15-30 minutes (nasal).
Duration: 8 hours (ophthalmic); 12 hours (nasal).
Absorption: Ocular absorption is low. Nasal: Bioavailability: Approx 40%. Time to peak plasma concentration: 4 hours.
Distribution: Plasma protein binding: Approx 88%.
Metabolism: Metabolised in the liver by CYP isoenzyme into the major metabolite, N-desmethylazelastine.
Excretion: Mainly via faeces (approx 75%, <10% as unchanged drug) and urine. Elimination half-life: 22-25 hours (nasal).
Storage
Nasal: Nasal spray: Store between 20-25<28>C. Protect from freezing. Ophthalmic: Ophthalmic solution: Store between 2-25°C. Protect from freezing.
ATC Classification
R06AX19 - azelastine ; Belongs to the class of other antihistamines for systemic use.
S01GX07 - azelastine ; Belongs to the class of other ophthalmologic antiallergics.
R01AC03 - azelastine ; Belongs to the class of topical antiallergic preparations, excluding corticosteroids. Used as antiallergic agents.
Disclaimer: This information is independently developed by CIMS based on azelastine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in