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Azelastine (Nasal)

Medically reviewed by Drugs.com. Last updated on Jul 8, 2020.

Pronunciation

(a ZEL as teen)

Index Terms

  • Astelin
  • Azelastine HCl
  • Azelastine Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Nasal, as hydrochloride:

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

Generic: 137 mcg/spray (30 mL); 0.1% (30 mL); 0.15% (30 mL)

Brand Names: U.S.

  • 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.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Perennial allergic rhinitis: Intranasal:

Infants ≥6 months and Children <6 years: 0.1% solution: 1 spray per nostril twice daily.

Children 6 to <12 years: 0.1% or 0.15% solution: 1 spray per nostril twice daily

Children ≥12 years and Adolescents: 0.15% solution: 2 sprays per nostril twice daily

Seasonal allergic rhinitis: Intranasal:

Children 2 to <6 years: 0.1% solution: 1 spray per nostril twice daily

Children 6 to <12 years: 0.1% or 0.15% solution: 1 spray per nostril twice daily

Children ≥12 years and Adolescents:

0.1% solution: 1 or 2 sprays per nostril twice daily

0.15% solution: 1 or 2 sprays per nostril twice daily or 2 sprays per nostril once daily

Vasomotor rhinitis: Intranasal: Children ≥12 years and Adolescents: 0.1% solution: 2 sprays per nostril twice daily

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

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. Astepro 30 mL bottles contain 200 sprays; discard bottle after 200 sprays, even if not completely empty.

Storage

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

Drug Interactions

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

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

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%, postmarketing, and/or case reports: Altered sense of smell, anaphylactoid reaction, anosmia, application site irritation, atrial fibrillation, blurred vision, chest pain, confusion, drug tolerance, dyspnea, facial edema, increased serum transaminases, insomnia, muscle spasm, nasal sores, palpitations, paresthesia, pruritus, skin rash, urinary retention, visual disturbance, 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).

Pregnancy Considerations

An increased risk of adverse pregnancy outcomes has not been observed; however, information related to the use of nasal azelastine in pregnancy is limited. Use of other agents for the treatment of allergic rhinitis in pregnant women may be preferred (BSACI [Scadding 2017]).

Patient Education

What is this drug used for?

• It is used to ease allergy signs.

• It is used to treat a runny nose.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Nosebleed

• Fatigue

• Headache

• Cough

• Stuffy nose

• Sore throat

• Loss of strength and energy

• Nausea

• Dry mouth

• Dizziness

• Weight gain

• Sneezing

• Change in taste

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Eye irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.