Azelastine


Generic Medicine Info
Indications and Dosage
Nasal
Seasonal allergic rhinitis
Adult: As 0.1% (140 mcg/actuation) nasal spray: 1 spray (140 mcg) into each nostril bid (total dose of 560 mcg). As 0.1% (137 mcg/actuation) nasal spray: 1 or 2 sprays (137 mcg or 274 mcg) in each nostril bid. As 0.15% (205.5 mcg/actuation) nasal spray: 1 or 2 sprays (205.5 mcg or 411 mcg) in each nostril bid, or 2 sprays (411 mcg) into each nostril once daily. Dosage recommendations and treatment guidelines may vary among individual products or between countries. Refer to specific product information.
Child: As 0.1% (140 mcg/actuation) nasal spray: ≥6 years Same as adult dose. As 0.1% (137 mcg/actuation) nasal spray: 5-11 years 1 spray (137 mcg) in each nostril bid; ≥12 years Same as adult dose. As 0.15% (205.5 mcg/actuation) nasal spray: 6-11 years 1 spray (205.5 mcg) in each nostril bid; ≥12 years Same as adult dose. Dosage recommendations and treatment guidelines may vary among individual products or between countries. Refer to specific product information.

Nasal
Perennial allergic rhinitis
Adult: As 0.1% (140 mcg/actuation) nasal spray: 1 spray (140 mcg) into each nostril bid (total dose: 560 mcg). As 0.15% (205.5 mcg/actuation) nasal spray: 2 sprays (411 mcg) in each nostril bid. Dosage recommendations and treatment guidelines may vary among individual products or between countries. Refer to specific product information.
Child: As 0.1% (140 mcg/actuation) nasal spray: ≥6 years Same as adult dose. As 0.15% (205.5 mcg/actuation) nasal spray: 6-11 years 1 spray (205.5 mcg) into each nostril bid; ≥12 years Same as adult dose. Dosage recommendations and treatment guidelines may vary among individual products or between countries. Refer to specific product information.

Nasal
Vasomotor rhinitis
Adult: As 0.1% (137 mcg/actuation) nasal spray: 2 sprays (274 mcg) into each nostril bid. Dosage recommendations may vary among individual products or between countries. Refer to specific product guidelines.
Child: As 0.1% (137 mcg/actuation) nasal spray: ≥12 years Same as adult dose. Dosage recommendations and treatment guidelines may vary among individual products or between countries. Refer to specific product information.

Ophthalmic
Seasonal allergic conjunctivitis
Adult: As 0.05% ophthalmic solution: Instil 1 drop into the affected eye(s) bid, may be increased to 4 times daily if necessary.
Child: ≥4 years Same as adult dose.

Ophthalmic
Perennial allergic conjunctivitis
Adult: As 0.05% ophthalmic solution: Instil 1 drop into affected eye(s) bid, may be increased to 4 times daily if necessary. Max treatment duration: 6 weeks.
Child: ≥12 years Same as adult dose.
Special Precautions
Not intended to treat eye infections (ophthalmic). Children. Pregnancy and lactation.
Adverse Reactions
Eye disorders: Mild transient eye irritation (e.g. burning or stinging sensation), transient blurred vision, eye pain.
Gastrointestinal disorders: Bitter taste, dry mouth, nausea, dysgeusia, vomiting.
General disorders and administration site conditions: Fatigue.
Immune system disorders: Very rarely, hypersensitivity reactions (e.g. rash, pruritus, urticaria).
Nervous system disorders: Headache, dizziness, dysaesthesia.
Psychiatric disorders: Somnolence.
Respiratory, thoracic and mediastinal disorders: Mild transient irritation of the inflamed nasal mucosa (e.g. stinging, itching, sneezing, epistaxis), nasal discomfort, cough, pharyngitis, sinusitis, asthma.
Inhalation/Respiratory/Nasal/Ophth: C
Patient Counseling Information
This drug may cause somnolence (nasal) or transient effects on vision (ophthalmic); if affected, do not drive or operate machinery. Ophthalmic: Do not wear contact lenses if the eyes are red. Remove soft contact lenses prior to instillation of eye drops and wait for at least 15 minutes before reinsertion.
Drug Interactions
Nasal: Concurrent use with CNS depressants may lead to reduced alertness and impaired CNS function.
Food Interaction
Nasal: Alertness and CNS function may be reduced or impaired with alcohol.
Action
Description:
Mechanism of Action: Azelastine is a phthalazinone derivative long-acting antihistamine that competes with histamine for H1-receptors on effector cells, thereby inhibiting the release of histamine and other chemical mediators involved in allergic responses such as leukotriene, platelet activation factor (PAF), and serotonin. Additionally, it decreases hyperactivity of the airways and increases bronchial epithelial cilia motility, thus improving mucociliary transport when given intranasally.
Onset: 3 minutes (ophthalmic); 15-30 minutes (nasal).
Duration: 8 hours (ophthalmic); 12 hours (nasal).
Pharmacokinetics:
Absorption: Ocular absorption is low. Bioavailability: Approx 40% (nasal). Time to peak plasma concentration: 2-3 hours (0.1% nasal spray); 4 hours (0.15% nasal spray).
Metabolism: Metabolised in the liver via oxidation by CYP450 enzyme system to the major active metabolite, N-desmethylazelastine.
Excretion: Mainly via faeces (approx 75%, <10% as unchanged drug). Elimination half-life: As 0.15% nasal spray: 25 hours (azelastine); 57 hours (N-desmethylazelastine).
Chemical Structure

Chemical Structure Image
Azelastine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2267, Azelastine. https://pubchem.ncbi.nlm.nih.gov/compound/Azelastine. Accessed Nov. 23, 2022.

Storage
Ophthalmic solution/drops: Store between 2-25°C. Nasal spray: Store between 20-25°C. Do not refrigerate or freeze. Storage recommendations may vary among individual products or between countries. Refer to specific product guidelines.
MIMS Class
Nasal Decongestants & Other Nasal Preparations / Ophthalmic Decongestants, Anesthetics, Anti-Inflammatories
ATC Classification
R01AC03 - azelastine ; Belongs to the class of topical antiallergic preparations, excluding corticosteroids. Used as antiallergic agents.
S01GX07 - azelastine ; Belongs to the class of other ophthalmologic antiallergics.
References
Anon. Azelastine (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/10/2022.

Anon. Azelastine (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/10/2022.

Anon. Azelastine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 11/10/2022.

Azelastine HCl Nasal Spray (Padagis Israel Pharmaceuticals Ltd). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/10/2022.

Azelastine Hydrochloride 0.5 mg/mL Eye Drops, Solution (Brown & Burk UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 11/10/2022.

Azelastine Hydrochloride Ophthalmic Solution 0.05% Solution/Drops (Alembic Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/10/2022.

Azelastine Hydrochloride Spray, Metered (Amneal Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/10/2022.

Azelastine-Comod (Konimex). MIMS Indonesia. http://www.mims.com/indonesia. Accessed 09/11/2022.

Buckingham R (ed). Azelastine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/10/2022.

Joint Formulary Committee. Azelastine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/10/2022.

Rhinolast Nasal Spray (Mylan Products Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 11/10/2022.

Disclaimer: This information is independently developed by MIMS 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 MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS 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 © 2024 MIMS. All rights reserved. Powered by MIMS.com
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