Trade Names:Astelin- Nasal spray 137 mcg/spray
Trade Names:Astepro- Nasal spray 137 mcg/spray (0.1%)- Nasal spray 205.5 mcg/spray (0.15%)
Trade Names:Optivar- Ophthalmic solution 0.5 mg/mL
Competitively antagonizes histamine at H 1 receptor sites.
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.
Vd is 14.5 L/kg. Approximately 88% (azelastine) and 97% (desmethylazelastine) are protein bound.
Oxidatively metabolized to desmethylazelastine (active) by CYP-450 system.
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.
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.
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).
Ophthalmic Instill 1 drop into each affected eye twice daily.Perennial Allergic RhinitisAdults and Children 12 yr of age and older
Nasal Inhalation ( Astepro 0.15%) 2 sprays per nostril twice daily.Seasonal Allergic RhinitisAdults 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 RhinitisAdults and children 12 yr of age and older
Nasal Inhalation ( Astelin ) 2 sprays per nostril twice daily.
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.
Effects may be enhanced by azelastine.Cimetidine
May increase azelastine plasma levels, increasing the risk of side effects.
May interfere with diagnostic test results for skin tests using allergen extracts.
Flushing, hypertension, tachycardia (less than 2%); atrial fibrillation, hypertension, palpitations (postmarketing).
Headache (15%); somnolence (12%); dizziness, fatigue (2%); abnormal thinking, anxiety, depersonalization, depression, hyperkinesias, hypoesthesia, nervousness, sleep disturbances, vertigo (less than 2%); confusion (postmarketing).Ophthalmic
Headache (15%); fatigue (1% to 10%).
Contact dermatitis, eczema, furunculosis, hair and follicle infection (less than 2%); application-site irritation, pruritus, rash (postmarketing).Ophthalmic
Pruritus (1% to 10%).
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%).
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%).
Albuminuria, amenorrhea, breast pain, hematuria, increased urinary frequency (less than 2%); urinary retention (postmarketing).
Increased ALT (less than 2%).
Weight increase (2%); increased appetite (less than 2%).
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%).
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%).
MonitorNasal 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.
Category C .
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).
Select dose with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function and comorbidity.
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