NASALAST

Azelastine, a phthalazine derivative, is an antihistamine available as an intranasal spray for the treatment of allergic and vasomotor rhinitis and as an ophthalmic solution for the treatment of allergic conjunctivitis. 10, 11 It is a racemic mixture, though there is no noted difference in pharmacologic activity between enantiomers, and was first granted FDA approval in 1996. 10, 11 Azelastine is also available in combination with fluticasone propionate as a nasal spray marketed under the trade name Dymista™, which is indicated for the symptomatic treatment of seasonal allergic rhinitis in patients 6 years of age and older.

Intranasal azelastine is indicated for the symptomatic treatment of seasonal allergic rhinitis in patients 5 years and older and for the symptomatic treatment of vasomotor rhinitis in patients 12 years and older.

Ophthalmic azelastine solution is indicated for the treatment of itchy eyes associated with allergic conjunctivitis.

As a 0.15% nasal spray, azelastine hydrochloride is also indicated for over-the-counter treatment of allergies in patients aged six years and older.

Azelastine antagonizes the actions of histamine, resulting in the relief of histamine-mediated allergy symptoms. 2, 10, 11 Onset of action occurs within 15 minutes with intranasal formulations and as quickly as 3 minutes with ophthalmic solutions.

Intranasal formulations have a relatively long-duration of action, with peak effects observed 4-6 hours after the initial dose and efficacy maintained over the entirety of the standard 12 hour dosing interval.

Systemic bioavailability of azelastine hydrochloride following intranasal administration is approximately 40%, reaching Cmax within 2-3 hours.

When administered at doses greater than the recommended maximum, greater than proportional increases in both Cmax and AUC were observed.

After intravenous and oral administration, the steady-state volume of distribution is 14.5 L/kg. 2, 10, 11.

Azelastine hydrochloride is oxidatively metabolized to its main, and biologically active, metabolite desmethylazelastine by the cytochrome P450 enzyme system. 10, 11 Though labels for azelastine state that specific CYP enzyme involvement has not been elucidated, it has been suggested that the N-demethylation of azelastine is primarily catalyzed by CYP3A4, CYP2D6, and CYP1A2.

Hover over products below to view reaction partners Azelastine Desmethylazelastine.

After an oral dose of radio-labeled azelastine hydrochloride, approximately 75% was excreted in the feces, with less than 10% as unchanged azelastine hydrochloride. 2, 10, 11.

Based on intravenous and oral administration, azelastine demonstrated an elimination half-life of 22 hours. 10, 11 Its primary active metabolite, desmethylazelastine, has an elimination half-life of 54 hours.

Based on intravenous and oral administration, azelastine demonstrated a plasma clearance of 0.5 L/h/kg. 10, 11, 6.

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Overdosage of intranasal or ophthalmic azelastine is unlikely to result in clinically significant adverse effects aside from increased drowsiness. 10, 11 If overdose does occur, employ general supportive measures.

Oral ingestion of antihistamines, including non-oral formulations of azelastine, can cause serious adverse effects in children.

• for this reason, these products should be kept out of the reach of children.

The oral

LD in rats is 580 mg/kg.

For intranasal use only Seasonal allergic rhinitis: Pediatric patients to 11 years of age: 1 spray per nostril twice daily Adults and adolescents 12 years of age and older: 1 or 2 sprays per nostril twice daily Vasomotor rhinitis: 2 sprays per nostril twice daily in adults and adolescents 12 years of age and older Prime azelastine hydrochloride nasal spray before initial use and when it has not been used for 3 or more days 2.1 Seasonal Allergic Rhinitis The recommended dosage of azelastine hydrochloride nasal spray in adults and adolescent patients 12 years and older with seasonal allergic rhinitis is one or two sprays per nostril twice daily.

The recommended dosage of azelastine hydrochloride nasal spray in pediatric patients 5 years to 11 years of age is one spray per nostril twice daily. 2.2 Vasomotor Rhinitis The recommended dosage of azelastine hydrochloride nasal spray in adults and adolescent patients 12 years and older with vasomotor rhinitis is two sprays per nostril twice daily. 2.3 Important Administration Instructions Administer azelastine hydrochloride nasal spray by the intranasal route only.

Prime azelastine hydrochloride nasal spray before initial use by releasing 4 sprays or until a fine mist appears.

When azelastine hydrochloride nasal spray has not been used for 3 or more days, reprime with 2 sprays or until a fine mist appears.

Avoid spraying azelastine hydrochloride nasal spray into the eyes.

50090-2330 NDC: 50090-2330-0 200 SPRAY, METERED in a BOTTLE, SPRAY / 1 in a CARTON.