No

Antihistamine

Nasal spray: Treatment of the symptoms of seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus in adults and children >12 years of age

Ophthalmic: Treatment of itching of the eye associated with seasonal allergic conjunctivitis

C

Hypersensitivity to azelastine or any component

Use with caution in asthmatics; patients with hepatic or renal dysfunction may require lower doses

>10%:

Central nervous system: Headache (14.8%), somnolence (11.5%)

Gastrointestinal: Bitter taste (19.7%)

2% to 10%:

Central nervous system: Dizziness (2%), fatigue (2.3%)

Gastrointestinal: Nausea (2.8%), weight increase (2%), dry mouth (2.8%)

Respiratory: Nasal burning (4.1%), pharyngitis (3.8%), paroxysmal sneezing (3.1%), rhinitis (2.3%), epistaxis (2%)

<2%:

Body as a whole: Allergic reactions, back pain, viral infections, malaise, extremity pain, abdominal pain

Cardiovascular: Flushing, hypertension, tachycardia

Central nervous system: Drowsiness, fatigue, vertigo, depression, nervousness, hypoesthesia

Dermatologic: Contact dermatitis, eczema, hair and follicle infection, furunculosis

Gastrointestinal: Constipation, gastroenteritis, glossitis, increased appetite, ulcerative stomatitis, vomiting, increased ALT, aphthous stomatitis

Genitourinary: Urinary frequency, hematuria, albuminuria, amenorrhea

Neuromuscular & skeletal: Myalgia, vertigo, temporomandibular dislocation, hypoesthesia, hyperkinesia

Ocular: Conjunctivitis, watery eyes, eye pain

Respiratory: Bronchospasm, coughing, throat burning, laryngitis

Psychological: Anxiety, depersonalization, sleep disorder, abnormal thinking

There have been no reported overdoses with azelastine; increased somnolence is likely to occur; supportive measures should be employed

May cause additive sedation when concomitantly administered with other CNS depressant medications; cimetidine can increase the AUC and C_max of azelastine by as much as 65%

Stable 3 months after opening

Competes with histamine for H₁-receptor sites on effector cells in the blood vessels and respiratory tract; reduces hyper-reactivity of the airways; increases the motility of bronchial epithelial cilia, improving mucociliary transport

Peak effect: 3 hours

Duration of action: 12 hours

Metabolism: Metabolized by cytochrome P-450 enzyme system; active metabolite desmethylazelastine

Bioavailability: After intranasal administration: 40%

Protein binding: 88%

Half-life, elimination: 22 hours

Time to peak serum concentration: 2-3 hours

Nasal spray: Children greater than or equal to 12 years and Adults: 2 sprays (137 mcg/spray) each nostril twice daily. Before initial use, the delivery system should be primed with 4 sprays or until a fine mist appears. If 3 or more days have elapsed since last use, the delivery system should be reprimed.

Ophthalmic: Instill 1 drop into affected eye(s) twice daily

Drowsiness is common; rare reports of anxiety and nervousness

Concurrent use with psychotropics may produce additive sedation

No information available to require special precautions

2% to 10% of patients experience dry mouth; chronic use of antihistamines will inhibit salivary flows particularly in elderly patients; this may contribute to periodontal disease and oral discomfort

Causes drowsiness and may impair ability to perform hazardous activities requiring mental alertness or physical coordination; avoid spraying in eyes

Solution, nasal: 1 mg/mL (137 mcg/spray) (17 mL)

Solution, ophthalmic: 0.05% (10 mL)

McNeely W and Wiseman LR, "Intranasal Azelastine. A Review of Its Efficacy in the Management of Allergic Rhinitis," Drugs, 1988, 56(1):91-114.