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Azelastine Hydrochloride

Pronunciation

Pronunciation: a-ZEL-as-teen HYE-droe-KLOR-ide
Class: Antihistamine

Trade Names

Astelin
- Nasal spray 137 mcg/spray

Astepro
- Nasal spray 205.5 mcg/spray (0.15%)

Optivar
- Ophthalmic solution 0.5 mg/mL

Pharmacology

Competitively antagonizes histamine at H 1 receptor sites.

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Pharmacokinetics

Absorption

Bioavailability of nasal spray is approximately 40% and C max is 2 to 3 h. Absorption following ocular administration is relatively low, reaching a level of 0.02 to 0.25 ng/mL after 56 days of treatment.

Distribution

Vd is 14.5 L/kg. Approximately 88% (azelastine) and 97% (desmethylazelastine) are protein bound.

Metabolism

Oxidatively metabolized to desmethylazelastine (active) by CYP-450 system.

Elimination

The half-life is 22 h for azelastine and 54 h for desmethylazelastine. Plasma Cl is 0.5 L/h/kg. Approximately 75% was excreted in the feces, with less than 10% as unchanged azelastine.

Special Populations

Renal Function Impairment

Based on oral doses, AUC and C max increased 70% to 75% in those with CrCl less than 50 mL/min.

Hepatic Function Impairment

Pharmacokinetic parameters were not influenced based on oral doses.

Gender

Pharmacokinetic parameters were not influenced based on oral doses.

Race

Pharmacokinetic parameters were not influenced based on oral doses.

Age

Pharmacokinetic parameters were not influenced based on oral doses.

Indications and Usage

Treatment of symptoms of seasonal allergic rhinitis, such as rhinorrhea, sneezing, and nasal pruritus (nasal spray); treatment of symptoms of vasomotor rhinitis, such as rhinorrhea, nasal congestion, and postnasal drip ( Astelin only); treatment of symptoms of perennial allergic rhinitis ( Astepro only); treatment of itching of eye associated with allergic conjunctivitis (ophthalmic).

Contraindications

Standard considerations.

Dosage and Administration

Allergic Conjunctivitis
Adults and children 3 yr of age and older

Ophthalmic Instill 1 drop into each affected eye twice daily.

Perennial Allergic Rhinitis
Adults and Children 12 yr of age and older

Nasal Inhalation ( Astepro 0.15%) 2 sprays per nostril twice daily.

Seasonal Allergic Rhinitis
Adults and Children 12 yr of age and older

Nasal Inhalation ( Astepro ) 1 or 2 sprays per nostril twice daily.

Children 5 to 11 yr of age

Nasal Inhalation ( Astelin ) 1 spray per nostril twice daily.

Vasomotor Rhinitis
Adults and children 12 yr of age and older

Nasal Inhalation ( Astelin ) 2 sprays per nostril twice daily.

General Advice

  • Nasal spray
  • For intranasal administration only. Avoid spraying into the eyes.
  • Prime spray pump with 4 sprays before first use and with 2 sprays if unit has not been used for 3 or more days.

Storage/Stability

Nasal spray

Store at 68° to 77°F. Keep in upright position. Keep tightly closed and protect from freezing.

Ophthalmic solution

Store in upright position between 36° and 77°F.

Drug Interactions

Alcohol, other CNS depressants

Effects may be enhanced by azelastine.

Cimetidine

May increase azelastine plasma levels, increasing the risk of side effects.

Laboratory Test Interactions

May interfere with diagnostic test results for skin tests using allergen extracts.

Adverse Reactions

Cardiovascular

Flushing, hypertension, tachycardia (less than 2%); atrial fibrillation, hypertension, palpitations (postmarketing).

CNS

Headache (15%); somnolence (12%); dizziness, fatigue (2%); abnormal thinking, anxiety, depersonalization, depression, hyperkinesis, hypoesthesia, nervousness, sleep disturbances, vertigo (less than 2%); confusion (postmarketing).

Ophthalmic

Headache (15%); fatigue (1% to 10%).

Dermatologic

Contact dermatitis, eczema, furunculosis, hair and follicle infection (less than 2%); application-site irritation, pruritus, rash (postmarketing).

Ophthalmic

Pruritus (1% to 10%).

EENT

Rhinitis (6%); conjunctivitis (5%); nasal burning, pharyngitis (4%); epistaxis, paroxysmal sneezing, sinusitis (3%); burning throat, eye abnormality, eye pain, laryngitis, watery eyes (less than 2%); abnormal vision, nasal congestion, parosmia, xerophthalmia (postmarketing).

Ophthalmic

Transient eye burning/stinging (30%); conjunctivitis, eye pain, pharyngitis, rhinitis, temporary blurring (1% to 10%).

GI

Bitter taste (20%); dry mouth, nausea (3%); abdominal pain, aphthous stomatitis, constipation, gastroenteritis, glossitis, loss of taste, ulcerative stomatitis, vomiting (less than 2%); diarrhea (postmarketing).

Ophthalmic

Bitter taste (10%).

Genitourinary

Albuminuria, amenorrhea, breast pain, hematuria, increased urinary frequency (less than 2%); urinary retention (postmarketing).

Hepatic

Increased ALT (less than 2%).

Metabolic

Weight increase (2%); increased appetite (less than 2%).

Respiratory

Rhinitis/cold symptoms (17%); cough (11%); asthma (5%); paroxysmal sneezing (3%); rhinitis (2%); bronchospasm (less than 2%); dyspnea (postmarketing).

Ophthalmic

Asthma, dyspnea (1% to 10%).

Miscellaneous

Dysesthesia (8%); allergic reaction, back pain, herpes simplex, malaise, myalgia, pain in extremities, temporomandibular dislocation, viral infection (less than 2%); anaphylactoid reaction, chest pain, facial edema, involuntary muscle contractions, paresthesia, tolerance (postmarketing).

Ophthalmic

Influenza-like symptoms (1% to 10%).

Precautions

Monitor

Nasal spray allergy symptoms

Assess for allergy symptoms (eg, nasal congestion, nasal itching, rhinitis, sneezing) before and periodically throughout therapy.

Ophthalmic symptoms

Assess ophthalmic symptoms (eg, itching) before and periodically throughout therapy.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in seasonal allergic rhinitis in children younger than 5 yr of age ( Astelin ) and in children younger than 12 yr of age ( Astepro ). Safety and efficacy not established in children younger than 3 yr of age (ophthalmic).

Elderly

Select dose with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function and comorbidity.

Overdosage

Symptoms

Somnolence.

Patient Information

  • Nasal spray
  • Advise patient to read patient information leaflet that accompanies each spray bottle of azelastine.
  • Instruct patient to prime spray unit as directed in patient instruction sheet before first use and after storage for 3 or more days.
  • Ensure that patient understands how to properly administer spray.
  • Advise patient that if allergy symptoms are not controlled, not to increase the dose of medication or frequency of use, but to inform health care provider. Inform patient that larger or more frequent dosing does not increase effectiveness and may cause drowsiness or other unwanted effects.
  • Advise patient that medication may cause drowsiness or dizziness and not to drive or perform other activities requiring mental alertness until tolerance is determined.
  • Caution patient that alcohol and other CNS depressants (eg, sedatives) will have additional sedative effects if taken with azelastine.
  • Caution patient not to take any OTC antihistamines while taking this medication unless advised by health care provider.
  • Advise patient to take sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
  • Advise patient that bitter taste is a frequent side effect and to notify health care provider if this occurs and is bothersome.
  • Instruct patient to stop taking drug and immediately report dizziness or excessive drowsiness to health care provider.
  • Ophthalmic solution
  • Advise patient that usual dose is 1 drop instilled into the affected eyes twice daily.
  • Teach patient proper technique for instilling eye drops: wash hands; do not allow dropper tip to touch eye. Tilt head back and look up, pull lower eyelid down, and instill prescribed number of drops. Close eye for 1 to 2 min and apply gentle pressure to bridge of nose for 3 to 5 min. Do not rub eye.
  • Advise patient that if more than 1 topical ophthalmic drug is being used, to administer the drugs at least 10 min apart.
  • Advise patient who wears contact lenses not to wear lenses if eyes are red.
  • Advise patient who wears contact lenses, and whose eyes are not red, to remove lenses before instilling this medicine and to wait at least 10 min after instilling eye drop before inserting lenses.
  • Inform patient that temporary burning or stinging of the eye, headaches, and bitter taste are the most common side effects and to contact health care provider if they occur and are bothersome.
  • Advise patient to notify health care provider if symptoms are not controlled with medication.

Copyright © 2009 Wolters Kluwer Health.

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