Brand names: Astelin, Optivar
Drug class: Antiallergic Agents
- Histamine H1-receptor Antagonists
VA class: OP900
Molecular formula: C₂₂H₂₄ClN₃O•ClH
CAS number: 79307-93-0

Introduction

Relatively selective histamine H₁-receptor antagonist; a phthalazinone derivative.

Uses for Azelastine

Seasonal Allergic Rhinitis

Symptomatic treatment of seasonal allergic rhinitis (e.g., hay fever). Intranasal azelastine is at least as effective as oral antihistamines (e.g., cetirizine) or intranasal corticosteroids. May provide improvement of ocular manifestations, possibly secondary to systemic absorption of the drug.

Nonallergic Rhinitis

Symptomatic treatment of nonallergic (vasomotor) rhinitis.

Allergic Conjunctivitis

Symptomatic relief of ocular itching associated with allergic conjunctivitis.

Related/similar drugs

prednisone, cetirizine ophthalmic, dexamethasone ophthalmic, prednisolone ophthalmic, doxylamine, Deltasone

Azelastine Dosage and Administration

Administration

Administer nasal solution intranasally twice daily, using a spray pump.

Apply ophthalmic solution topically to the eye twice daily. Ophthalmic solution is not for injection or oral use.

Intranasal Administration

Before initial use, prime the pump until a fine mist appears, using up to 4 actuations of the pump. Administration of solution in a stream of liquid rather than as a mist may fail to provide maximum benefit and may cause discomfort.

If inhaler has not been used for ≥3 days, reprime pump with 2 actuations or until a fine mist appears. Reprime pump when the spray pump is inserted into the second bottle.

To actuate the pump, hold the bottle in one hand, with 2 fingers on the shoulders of the pump unit and the thumb on the bottom of the bottle. Press the bottom firmly and rapidly upward with the thumb to produce a fine mist.

Prior to administration, gently blow the nose to clear nasal passages. Insert nasal spray tip ¼ to ½ inch into a nostril, tilt head slightly forward while holding the bottle vertically upright, and aim spray tip toward the back of the nose. Rapidly and firmly press and actuate pump into the nostril while holding the other nostril closed, gently sniffing at the same time; do not tilt head back after dosing.

Repeat procedure for the other nostril. Provide a second spray into each nostril, beginning with the first nostril. Alternate nostrils between each actuation of nasal spray.

Use caution to avoid spraying nasal spray into the eyes.

Ophthalmic Administration

Remove soft contact lenses prior to administration of each dose (since benzalkonium chloride may be absorbed by the lenses); may reinsert lenses 10 minutes after administration if eyes are not red.

Avoid contamination of the solution container.

Dosage

Available as azelastine hydrochloride; dosage expressed in terms of the salt.

When properly primed, the nasal spray pump delivers approximately 100 metered doses per bottle.

Pediatric Patients

Seasonal Allergic Rhinitis

Intranasal

Children ≥12 years of age: 2 sprays (274 mcg) in each nostril twice daily.

Children 5–11 years of age: 1 spray (137 mcg) in each nostril twice daily.

Nonallergic Rhinitis

Intranasal

Children ≥12 years of age: 2 sprays (274 mcg) in each nostril twice daily.

Allergic Conjunctivitis

Ophthalmic

Children ≥3 years of age: 1 drop of a 0.05% solution in the affected eye(s) twice daily.

Adults

Seasonal Allergic Rhinitis

Intranasal

2 sprays (274 mcg) in each nostril twice daily.

Nonallergic Rhinitis

Intranasal

2 sprays (274 mcg) in each nostril twice daily.

Allergic Conjunctivitis

Ophthalmic

1 drop of a 0.05% solution in the affected eye(s) twice daily.

Special Populations

Geriatric Patients

Cautious dosing of nasal solution recommended.

Cautions for Azelastine

Contraindications

• Known hypersensitivity to azelastine or any ingredient in the formulation.

Warnings/Precautions

General Precautions

CNS Effects

Somnolence reported in patients receiving azelastine nasal solution. Performance of activities requiring mental alertness and physical coordination may be impaired.

Concurrent use of nasal solution with other CNS depressants may potentiate CNS depression. (See Specific Drugs under Interactions.)

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether azelastine is distributed into milk. Use with caution in nursing women.

Pediatric Use

Safety and efficacy of nasal solution for treatment of seasonal allergic rhinitis not established in children <5 years of age; safety and efficacy for treatment of nonallergic rhinitis not established in children <12 years of age.

Safety and efficacy of ophthalmic solution not established in children <3 years of age.

Geriatric Use

Response to nasal solution does not appear to differ from that in younger adults.

No substantial differences in safety and efficacy of ophthalmic solution relative to younger adults.

Common Adverse Effects

Nasal solution: Transient nasal burning or stinging, bitter taste, somnolence, headache, pharyngitis, paroxysmal sneezing.

Ophthalmic solution: Transient ocular burning/stinging, bitter taste, headache.

Drug Interactions

Metabolized by CYP isoenzymes.

Specific Drugs

Azelastine Pharmacokinetics

Absorption

Bioavailability

Following intranasal administration, systemic bioavailability is 40%. Peak plasma concentrations occur 2–3 hours after intranasal administration.

Absorption following ophthalmic administration is low.

Onset

Following intranasal administration, symptomatic relief is evident within 1 hour; substantial relief usually is apparent within 3 hours; peak effect occurs between 4–6 hours.

Following ophthalmic administration, onset of action is rapid (3 minutes).

Duration

Following intranasal administration, effect persists throughout the 12-hour dosage interval.

Ophthalmic effect persists for about 8 hours.

Distribution

Plasma Protein Binding

Azelastine: Approximately 88%.

N-desmethylazelastine: 97%.

Elimination

Metabolism

Metabolized primarily to N-desmethylazelastine (an active metabolite) by CYP isoenzymes.

Elimination Route

Approximately 75% of an oral dose is excreted in feces, with <10% as unchanged drug.

Half-life

Azelastine: 22 hours (following oral and IV administration).

N-desmethylazelastine: 54 hours.

Special Populations

In patients with hepatic impairment, pharmacokinetics not altered.

Stability

Storage

Nasal

Solution

20–25°C. Protect from freezing.

Discard both bottles 3 months after initial insertion of the spray pump into the first of the 2 bottles in the dispensing package.

Ophthalmic

Solution

20–25°C. Store upright.

Actions

• Inhibits the release of histamine and other mediators (e.g., leukotrienes, platelet activating factor [PAF]) involved in allergic reactions.

• May inhibit the accumulation of eosinophils at the site of allergic inflammation and prevent eosinophil degranulation.

Advice to Patients

• Proper techniques for assembly and priming of nasal spray pump and for administration of the nasal solution. Importance of not administering the entire dose (i.e., 4 sprays) into a single nostril. Give patients a copy of the manufacturer’s patient instructions.

• Importance of learning and adhering to proper administration techniques to avoid contamination of the ophthalmic solution container.

• Importance of removing soft contact lenses prior to administration of each ophthalmic dose. May reinsert contact lenses 10 minutes after administration if eyes are not red; do not wear contact lenses if eye(s) are red. Not indicated for contact lens-related irritation.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Potential for intranasal azelastine to impair mental alertness or physical coordination; use caution when driving or operating machinery until effects on individual are known. Avoid concomitant use of alcohol-containing beverages or products.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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