Azelastine HydrochlorideClass: Ophthalmic antihistamine, Phthalazinones, peripherally selective Trade Names:
Astelin
- Nasal spray 137 mcg/spray Trade Names:
Optivar
- Ophthalmic solution 0.05% Mechanism of ActionPharmacologyCompetitively antagonizes histamine at H 1 receptor sites. PharmacokineticsAbsorptionBioavailability 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. DistributionVd is 14.5 L/kg. Approximately 88% (azelastine) and 97% (desmethylazelastine) are protein bound. MetabolismOxidatively metabolized to desmethylazelastine (active) by CYP-450 system. EliminationThe t ½ 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 PopulationsRenal Function Impairment
Based on oral doses, AUC and C max increased 70% to 75% in those with Ccr less than 50 mL/min. Indications and UsageTreatment of symptoms of seasonal allergic rhinitis, such as rhinorrhea, sneezing, and nasal pruritus; treatment of symptoms of vasomotor rhinitis, such as rhinorrhea, nasal congestion, and postnasal drip (nasal inhalation); treatment of itching of eye associated with allergic conjunctivitis (ophthalmic). ContraindicationsStandard considerations. Dosage and AdministrationSeasonal Allergic Rhinitis
Adults and children 12 yr of age and older Nasal Inhalation 2 sprays per nostril twice daily. Children 5 to 11 yr of age Nasal Inhalation 1 spray per nostril twice daily. Vasomotor Rhinitis
Adults and children 12 yr of age and older Nasal Inhalation 2 sprays per nostril twice daily. Adults and children 3 yr of age and older Ophthalmic Instill 1 drop into each affected eye 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/StabilityNasal spray Store nasal spray at 68° to 77°F. Keep in upright position. Keep tightly closed and protect from freezing. Ophthalmic solution Store ophthalmic solution in refrigerator (36° to 46°F) or at 47° to 77°F. Keep in upright position. Keep tightly closed and protect from freezing.
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