Skip to Content
Be ready for a severe allergy emergency. Read more >>

Azelastine (Nasal)

Pronunciation

Pronunciation

(a ZEL as teen)

Index Terms

  • Azelastine HCl
  • Azelastine Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Nasal, as hydrochloride:

Astelin: 137 mcg/spray (30 mL [DSC]) [contains benzalkonium chloride, edetate disodium]

Astepro: 0.15% (30 mL) [contains benzalkonium chloride, edetate disodium]

Generic: 0.1% (30 mL); 0.15% (30 mL)

Brand Names: U.S.

  • Astelin [DSC]
  • Astepro

Pharmacologic Category

  • Histamine H1 Antagonist
  • Histamine H1 Antagonist, Second Generation

Pharmacology

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

Distribution

Vd: 14.5 L/kg

Metabolism

Hepatic via CYP; active metabolite, desmethylazelastine

Excretion

Feces (75%, <10% as unchanged drug)

Clearance: 0.5 L/hour/kg

Onset of Action

30 minutes (Wallace 2008); maximum effect: 3 hours

Time to Peak

2 to 3 hours (Azelastine [generic] 0.1% solution); 3 to 4 hours (Astepro)

Duration of Action

12 hours

Half-Life Elimination

Azelastine: 22 hours (0.1% solution), 25 hours (0.15% solution); Desmethylazelastine: 52 hours (0.1% solution), 57 hours (0.15% solution)

Protein Binding

Azelastine: ~88%; Desmethylazelastine: ~97%

Use: Labeled Indications

Perennial allergic rhinitis (Astepro 0.1% and 0.15% solution only): Relief of symptoms of perennial allergic rhinitis in adults and pediatric patients ≥6 months.

Seasonal allergic rhinitis: Relief of symptoms of seasonal allergic rhinitis in adults and pediatric patients ≥2 years (Astepro 0.1% and 0.15% solution) and ≥5 years (azelastine [generic] 0.1% solution).

Vasomotor rhinitis (azelastine [generic] 0.1% solution): Relief of symptoms of vasomotor rhinitis in adults and adolescents ≥12 years.

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosing: Adult

Perennial allergic rhinitis: Intranasal: Astepro (0.15% solution): Two sprays in each nostril twice daily.

Seasonal allergic rhinitis: Intranasal:

Astepro (0.1% or 0.15% solution): One or two sprays (0.1% solution) in each nostril twice daily or two sprays (0.15% solution) in each nostril once daily

Azelastine [generic] 0.1% solution: One or two sprays in each nostril twice daily

Vasomotor rhinitis: Intranasal: Azelastine [generic] 0.1% solution: Two sprays in each nostril twice daily.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Perennial allergic rhinitis: Intranasal: Astepro:

Infants ≥6 months and Children ≤5 years: 0.1% solution: One spray in each nostril twice daily.

Children 6 to <12 years: 0.1% or 0.15% solution: One spray in each nostril twice daily.

Children ≥12 years and Adolescents: Refer to adult dosing.

Seasonal allergic rhinitis: Intranasal:

Astepro:

Children 2 to 5 years: 0.1% solution: One spray in each nostril twice daily.

Children 6 to <12 years: 0.1% or 0.15% solution: One spray in each nostril twice daily.

Children ≥12 years and Adolescents: Refer to adult dosing.

Azelastine [generic] 0.1% solution:

Children ≥5 to 11 years: One spray in each nostril twice daily.

Children ≥12 years and Adolescents: Refer to adult dosing.

Vasomotor rhinitis: Intranasal: Azelastine [generic] 0.1% solution: Children ≥12 years and Adolescents: Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Administration

Intranasal: Before initial use of the nasal spray, the delivery system should be primed with 4 sprays (azelastine [generic] 0.1% solution) or 6 sprays (Astepro), or until a fine mist appears. If 3 or more days have elapsed since last use, the delivery system should be reprimed with 2 sprays or until a fine mist appears. Blow nose to clear nostrils. Keep head tilted downward when spraying. Insert applicator into nostril, keeping bottle upright, and close off the other nostril. Aim the spray tip toward the back of nose. Breathe in through nose. While inhaling, press pump to release spray. Alternate sprays between nostrils. After each use, wipe the spray tip with a clean tissue or cloth. Avoid spraying in eyes or mouth. Do not tilt head back after use.

Storage

Store upright at 20°C to 25°C (68°F to 77°F); protect from freezing.

Drug Interactions

Alcohol (Ethyl): May enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

CNS Depressants: May enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

Adverse Reactions

Adverse reactions may be dose-, indication-, or product-dependent:

>10%:

Central nervous system: Bitter taste (4% to 20%), headache (1% to 15%), drowsiness (≤12%)

Infection: Cold symptoms (children ≤17%)

Respiratory: Rhinitis (exacerbation; ≤17%), cough (children: 11%; infants and children: ≥2%)

2% to 10%:

Central nervous system: Dysesthesia (8%), dizziness (2%), fatigue (2%)

Dermatologic: Contact dermatitis

Endocrine & metabolic: Weight gain (2%)

Gastrointestinal: Dysgeusia (children: 2% to 4%), nausea (3%), xerostomia (3%), vomiting

Infection: Upper respiratory tract infection (children: ≥2% to 3%)

Neuromuscular & skeletal: Myalgia (≤2%)

Ophthalmic: Conjunctivitis (<2% to 5%)

Otic: Otitis media (infants & children: ≥2%)

Respiratory: Epistaxis (2% to 7%), asthma (5%), sinusitis (3% to >5%), burning sensation of the nose (4%), pharyngitis (4%), nasal discomfort (≤4%), sneezing (1% to 3%), sore nose (infants and children: ≥2%), nasal mucosa ulcer (≤2%), pharyngolaryngeal pain

Miscellaneous: Fever

<2%:

Cardiovascular: Flushing, hypertension, tachycardia

Central nervous system: Abnormality in thinking, anxiety, depersonalization, depression, hypoesthesia, malaise, nervousness, sleep disorder, vertigo

Dermatologic: Eczema, folliculitis, furunculosis

Endocrine & metabolic: Albuminuria, amenorrhea

Gastrointestinal: Abdominal pain, ageusia, aphthous stomatitis, constipation, diarrhea, gastroenteritis, glossitis, increased appetite, toothache

Genitourinary: Hematuria, mastalgia

Hepatic: Increased serum ALT

Hypersensitivity: Hypersensitivity reaction

Infection: Herpes simplex infection, viral infection

Neuromuscular & skeletal: Back pain, dislocation of temporomandibular joint, hyperkinesia, limb pain, rheumatoid arthritis

Ophthalmic: Eye pain, watery eyes

Renal: Polyuria

Respiratory: Bronchitis, bronchospasm, laryngitis, nasal congestion, paranasal sinus hypersecretion, paroxysmal nocturnal dyspnea, postnasal drip, sore throat

Miscellaneous: Laceration

<1% (Limited to important or life-threatening): Altered sense of smell, anaphylactoid reaction, anosmia, atrial fibrillation, chest pain, confusion, drug tolerance, increased serum transaminases, insomnia, muscle spasm, urinary retention, xerophthalmia

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in some animal reproduction studies. Azelastine is systemically absorbed following nasal inhalation and may have side effects similar to other antihistamines. However, data related to the use of azelastine in pregnancy is limited; if treatment for rhinitis in a pregnant woman is needed, other agents are preferred (Wallace 2008).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience fatigue, headache, cough, rhinitis, rhinorrhea, pharyngitis, nose pain, burning, loss of strength and energy, nausea, vomiting, dry mouth, dizziness, weight gain, sneezing, or change in taste. Have patient report immediately to prescriber shortness of breath, severe nose irritation, ear pain, or nose bleeds (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Hide