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Azelastine HydrochloridePronouncation: (ah-ZELL-ass-teen HIGH-dore-KLOR-ide)
Class: Ophthalmic antihistamine, Phthalazinones, peripherally selective
- Nasal spray 137 mcg/spray
- Ophthalmic solution 0.05%
Mechanism of Action
Competitively antagonizes histamine at H 1 receptor sites.
Bioavailability of nasal spray is approximately 40% and C max is 2 to 3 h. Absorption following ocular administration is relatively low, reaching a level of 0.02 to 0.25 ng/mL after 56 days of treatment.
Vd is 14.5 L/kg. Approximately 88% (azelastine) and 97% (desmethylazelastine) are protein bound.
Oxidatively metabolized to desmethylazelastine (active) by CYP-450 system.
The t ½ is 22 h for azelastine and 54 h for desmethylazelastine. Plasma Cl is 0.5 L/h/kg. Approximately 75% was excreted in the feces, with less than 10% as unchanged azelastine.
Special PopulationsRenal Function Impairment
Based on oral doses, AUC and C max increased 70% to 75% in those with Ccr less than 50 mL/min.
Indications and Usage
Treatment of symptoms of seasonal allergic rhinitis, such as rhinorrhea, sneezing, and nasal pruritus; treatment of symptoms of vasomotor rhinitis, such as rhinorrhea, nasal congestion, and postnasal drip (nasal inhalation); treatment of itching of eye associated with allergic conjunctivitis (ophthalmic).
Dosage and AdministrationSeasonal Allergic Rhinitis
Adults and children 12 yr of age and older
Nasal Inhalation 2 sprays per nostril twice daily.Children 5 to 11 yr of age
Nasal Inhalation 1 spray per nostril twice daily.Vasomotor Rhinitis
Adults and children 12 yr of age and older
Nasal Inhalation 2 sprays per nostril twice daily.Adults and children 3 yr of age and older
Ophthalmic Instill 1 drop into each affected eye twice daily.
- Nasal spray
- For intranasal administration only. Avoid spraying into the eyes.
- Prime spray pump with 4 sprays before first use and with 2 sprays if unit has not been used for 3 or more days.
Store nasal spray at 68° to 77°F. Keep in upright position. Keep tightly closed and protect from freezing.Ophthalmic solution
Store ophthalmic solution in refrigerator (36° to 46°F) or at 47° to 77°F. Keep in upright position. Keep tightly closed and protect from freezing.
Drug InteractionsAlcohol, other CNS depressants
Effects may be enhanced by azelastine.Cimetidine
May increase azelastine plasma levels, increasing the risk of side effects.
Laboratory Test Interactions
May interfere with diagnostic test results for skin tests using allergen extracts.
Flushing, hypertension, tachycardia (less than 2%).
Headache (15%); somnolence (12%); dizziness, fatigue (2%); hyperkinesias, hypesthesia, vertigo, anxiety, depersonalization, depression, nervousness, sleep disturbances, abnormal thinking (less than 2%); confusion (postmarketing).Ophthalmic
Headache (15%); fatigue (1% to 10%).
Contact dermatitis, eczema, hair and follicle infection, furunculosis (less than 2%); application site irritation, pruritus, rash (postmarketing).Ophthalmic
Pruritus (1% to 10%).
Rhinitis (6%); conjunctivitis (5%); nasal burning, pharyngitis (4%); paroxysmal sneezing, sinusitis, epistaxis (3%); glossitis, burning throat, laryngitis, eye abnormality, eye pain, watery eyes (less than 2%); nasal congestion, parosmia, abnormal vision, xerophthalmia (postmarketing).Ophthalmic
Transient eye burning/stinging (30%); conjunctivitis, eye pain, temporary blurring, rhinitis, pharyngitis (1% to 10%).
Bitter taste (20%); dry mouth, nausea (3%); constipation, gastroenteritis, ulcerative stomatitis, vomiting, aphthous stomatitis, loss of taste, abdominal pain (less than 2%); diarrhea (postmarketing).Ophthalmic
Bitter taste (10%).
Albuminuria, amenorrhea, breast pain, hematuria, increased urinary frequency (less than 2%); urinary retention (postmarketing).
Increased ALT (less than 2%).
Weight increase (2%); increased appetite (less than 2%).
Cough (11%); asthma (5%); bronchospasm (less than 2%); dyspnea (postmarketing).Ophthalmic
Asthma, dyspnea (1% to 10%).
Dysesthesia (8%); myalgia, cold symptoms, temporomandibular dislocation, allergic reaction, back pain, herpes simplex, viral infection, pain in extremities, malaise (less than 2%); anaphylactoid reaction, chest pain, facial edema, involuntary muscle contractions, paresthesia, tolerance (postmarketing).Ophthalmic
Influenza-like symptoms (1% to 10%).
MonitorNasal spray allergy symptoms
Assess for allergy symptoms (eg, rhinitis, nasal congestion, sneezing, nasal itching) before and periodically throughout therapy. Notify health care provider if symptoms are not controlled with medication.Ophthalmic symptoms
Assess ophthalmic symptoms (eg, itching) before and periodically throughout therapy. Notify health care provider if symptoms are not controlled with medication.
Category C .
Safety and efficacy not established in seasonal allergic rhinitis in children younger than 5 yr of age (nasal inhalation). Safety and efficacy not established in children younger than 3 yr of age (ophthalmic).
Select dose with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function and comorbidity.
- Nasal spray
- Advise patient to read patient information leaflet that accompanies each spray bottle of azelastine.
- Instruct patient to prime spray unit as directed in patient instruction sheet before first use and after storage for 3 or more days.
- Ensure that patient understands how to properly administer spray.
- Advise patient that if allergy symptoms are not controlled not to increase the dose of medication or frequency of use but to inform health care provider. Inform patient that larger or more frequent dosing does not increase effectiveness and may cause drowsiness or other unwanted effects.
- Advise patient that medication may cause drowsiness or dizziness and not to drive or perform other activities requiring mental alertness until tolerance is determined.
- Caution patient that alcohol and other CNS depressants (eg, sedatives) will have additional sedative effects if taken with azelastine.
- Caution patient not to take any OTC antihistamines while taking this medication unless advised by health care provider.
- Advise patient to take sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
- Advise patient that bitter taste is a frequent side effect and to notify health care provider if this occurs and is bothersome.
- Instruct patient to stop taking drug and immediately report dizziness or excessive drowsiness to health care provider.
- Ophthalmic solution
- Advise patient that usual dose is 1 drop instilled into the affected eyes twice daily.
- Teach patient proper technique for instilling eye drops: wash hands; do not allow dropper tip to touch eye. Tilt head back, look up; pull lower eyelid down; instill prescribed number of drops. Close eye for 1 to 2 min and apply gentle pressure to bridge of nose for 3 to 5 min. Do not rub eye.
- Advise patient that if more than 1 topical ophthalmic drug is being used, to administer the drugs at least 10 min apart.
- Advise patient who wears contact lenses not to wear lenses if eyes are red.
- Advise patient who wears contact lenses, and whose eyes are not red, to remove lenses before instilling this medicine and to wait at least 10 min after instilling eye drop before inserting lenses.
- Inform patient that temporary burning or stinging of the eye, headaches, and bitter taste are the most common side effects and to contact health care provider if they occur and are bothersome.