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Pronunciation:

(a ZEL as teen)

U.S. Brand Names:

Astelin®; Optivar®

Synonyms:

Azelastine Hydrochloride

Generic Available:

Canadian Brand Names:

Astelin®

Use:

Nasal spray: Treatment of the symptoms of seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus in children 5 years of age and adults; treatment of the symptoms of vasomotor rhinitis in children 12 years of age and adults

Ophthalmic: Treatment of itching of the eye associated with seasonal allergic conjunctivitis in children 3 years of age and adults

Pregnancy Risk Factor:

Pregnancy Implications:

There are no adequate and well-controlled studies in pregnant women. Animal reproduction studies have shown toxic effects to the fetus. Use during pregnancy only if the potential benefit to the mother outweighs the possible risk to the fetus.

Lactation:

Excretion in breast milk unknown/use caution

Contraindications:

Hypersensitivity to azelastine or any component of the formulation

Warnings/Precautions:

Nasal spray: May cause drowsiness in some patients; instruct patient to use caution when driving or operating machinery. Effects may be additive with CNS depressants and/or ethanol.

Ophthalmic: Solution contains benzalkonium chloride; wait at least 10 minutes after instilling solution before inserting soft contact lenses. Do not use contact lenses if eyes are red.

Adverse Reactions:

Nasal spray:

>10%:

Central nervous system: Headache (15%), somnolence (12%)

Gastrointestinal: Bitter taste (20%)

2% to 10%:

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

Gastrointestinal: Nausea (3%), weight gain (2%), dry mouth (3%)

Respiratory: Nasal burning (4%), pharyngitis (4%), paroxysmal sneezing (3%), rhinitis (2%), epistaxis (2%)

<2%:

Cardiovascular: Flushing, hypertension, tachycardia

Central nervous system: Drowsiness, fatigue, vertigo, depression, nervousness, hypoesthesia, anxiety, depersonalization, sleep disorder, abnormal thinking, malaise

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

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

Genitourinary: Urinary frequency, hematuria, albuminuria, amenorrhea

Neuromuscular & skeletal: Myalgia, vertigo, temporomandibular dislocation, hypoesthesia, hyperkinesia, back pain, extremity pain

Ocular: Conjunctivitis, watery eyes, eye pain

Respiratory: Bronchospasm, cough, throat burning, laryngitis

Miscellaneous: Allergic reactions, viral infection

<1%, postmarketing, and/or reports: Anaphylactoid reaction, chest pain, nasal congestion, confusion, diarrhea, dyspnea, facial edema, involuntary muscle contractions, paresthesia, parosmia, pruritus, rash, tolerance, urinary retention, visual abnormalities, xerophthalmia

Ophthalmic:

>10%:

Central nervous system: Headache (15%)

Ocular: Transient burning/stinging (30%)

1% to 10%:

Central nervous system: Fatigue

Genitourinary: Bitter taste (10%)

Ocular: Conjunctivitis, eye pain, blurred vision (temporary)

Respiratory: Asthma, dyspnea, pharyngitis

Miscellaneous: Flu-like syndrome

Overdosage/Toxicology:

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

Drug Interactions:

Substrate (minor) of CYP1A2, 2C19, 2D6, 3A4; Inhibits CYP2B6 (weak), 2C8/9 (weak), 2C19 (weak), 2D6 (weak), 3A4 (weak)

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

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol (may cause increased somnolence or fatigue).

Stability:

Nasal spray: Store upright at controlled room temperature of 20°C to 25°C (68°F to 77°F); stable for 3 months after opening

Ophthalmic solution: Store upright between 2°C to 25°C (36°F to 77°F)

Mechanism of Action:

Competes with histamine for H1-receptor sites on effector cells and inhibits the release of histamine and other mediators involved in the allergic response. When used intranasally, reduces hyper-reactivity of the airways; increases the motility of bronchial epithelial cilia, improving mucociliary transport

Pharmacodynamics/Kinetics:

Onset of action: Peak effect: Nasal spray: 3 hours; Ophthalmic solution: 3 minutes

Duration: Nasal spray: 12 hours; Ophthalmic solution: 8 hours

Protein binding: 88%

Metabolism: Hepatic via CYP; active metabolite, desmethylazelastine

Bioavailability: Intranasal: 40%

Half-life elimination: 22 hours

Time to peak, serum: 2-3 hours

Dosage:

Children 5-11 years: Seasonal allergic rhinitis: Intranasal: 1 spray each nostril twice daily

Children 12 years and Adults: Seasonal allergic rhinitis or vasomotor rhinitis: Intranasal: 2 sprays (137 mcg/spray) each nostril twice daily

Children 3 years and Adults: Itching eyes due to seasonal allergic conjunctivitis: Ophthalmic: Instill 1 drop into affected eye(s) twice daily

Administration:

Intranasal: Before initial use of the nasal spray, 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.

Patient Education:

Avoid alcohol. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Nasal spray: Causes drowsiness and may impair ability to perform hazardous activities requiring mental alertness or physical coordination; avoid spraying in eyes. Do not use with other antihistamines unless instructed by prescriber. The delivery system must be primed prior to first use, and again if not used for more than 3 days.

Ophthalmic: Do not touch eyelids or surrounding area with tip of dropper; wait at least 10 minutes before inserting soft contact lenses. Do not use contacts if eyes are red.

Dental Health: Effects on Dental Treatment:

Key adverse event(s) related to dental treatment: Bitter taste, xerostomia (normal salivary flow resumes upon discontinuation), aphthous stomatitis, glossitis, and burning sensation in throat. Chronic use of antihistamines will inhibit salivary flow, particularly in elderly patients; may contribute to periodontal disease and oral discomfort.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

Drowsiness is common; rare reports of anxiety and nervousness

Mental Health: Effects on Psychiatric Treatment:

Concurrent use with psychotropics may produce additive sedation

Dosage Forms:

Solution, intranasal spray, as hydrochloride (Astelin®): 1 mg/mL [137 mcg/spray] (17 mL, 30 mL) [contains benzalkonium chloride]

Solution, ophthalmic, as hydrochloride (Optivar®): 0.05% (6 mL) [contains benzalkonium chloride]

International Brand Names:

Afluon® (ES); Alerdual® (FR); Allergodil® (AR, AT, BE, CH, CL, CY, CZ, DE, DK, EG, FR, HU, IT, JO, KW, LB, LU, NL, PL, RO, RU, SI, SY, TR); Amelor® (CO); Astelin® (CA, MX); Azelast® (BR); Azelvin® (SE); Azep® (ID, SG, TH); Azeptin® (JP); Az® (MX); Cloridrato de Azelastina® (BR); Corifina® (ES); Faraler® (CO); Lasticom® (IT); Lastin® (FI, NO, SE); Loxin® (DE); Nolen® (AR); Oculastin® (CH); Optilast® (GB, IL); Otrivine Anti-Allergie® (BE); Otrivin Heuschnupfen® (CH); Rhinolast® (GB, IE, IL, NZ); Rino-Lastin® (BR); Vividrin akut Azelastin® (DE)

References

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

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