Safety and Efficacy of Azelastine Nasal Spray (Astelin NS) for Seasonal Allergic Rhinitis: a 4-Week Comparative Multicenter Trial

LaForce, Craig; Dockhorn, Robert J.; Prenner, Bruce M.; Chu, Theodore J.; Kraemer, Michael J.; Widlitz, Michael D.; D'eletto, T. A.; Freitag, Jeffrey J.

doi:10.1016/s1081-1206(10)63420-5

Cited by 69 publications

(34 citation statements)

References 17 publications

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“…46 Combination therapy with intranasal corticosteroids may provide added benefit. 339 The only intranasal antihistamines currently available in the United States, azelastine, [332][333][334][335][336][337][338] and olopatadine, 340 have a rapid onset of action. 341 Bitter taste has been reported with both preparations, and sedation may occur 342 (Table VII).…”

Section: Intranasal Antihistamines [Summary Statements 65-69]mentioning

confidence: 99%

“…917 In contrast with oral second-generation antihistamines, intranasal azelastine and olopatadine have been associated with clinically significant reduction in nasal congestion. [336][337][338]340 Because intranasal antihistamines are absorbed via the gastrointestinal tract, they can suppress skin test response for at least 48 hours in the case of azelastine. 657 Oral and topical decongestants 70.…”

Section: Intranasal Antihistaminesmentioning

confidence: 99%

See 1 more Smart Citation

The diagnosis and management of rhinitis: An updated practice parameter

Wallace¹,

Dykewicz²,

Bernstein³

et al. 2008

Journal of Allergy and Clinical Immunology

941

953

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Section: Intranasal Antihistamines [Summary Statements 65-69]mentioning

confidence: 99%

Section: Intranasal Antihistaminesmentioning

confidence: 99%

The diagnosis and management of rhinitis: An updated practice parameter

Wallace¹,

Dykewicz²,

Bernstein³

et al. 2008

Journal of Allergy and Clinical Immunology

941

953

View full text Add to dashboard Cite

“…In the 4-week study in SAR, 133 patients 12 years of age or older were randomized to receive two sprays per nostril twice daily of azelastine (n = 66) or placebo (n = 67) at five US study sites during the spring pollen season 56 . The primary outcome measure was the change from baseline in the TSC severity score.…”

Section: Pivotal Efficacy Studiesmentioning

confidence: 99%

Azelastine hydrochloride:a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability

Bernstein

2007

Current Medical Research and Opinion

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Azelastine is an effective, rapid-acting, and well-tolerated second-generation antihistamine that improves nasal symptoms associated with SAR and VMR. Clinical studies demonstrated that azelastine nasal spray can improve symptoms of SAR in patients who remained symptomatic after treatment with oral antihistamines and that azelastine nasal spray in combination with fluticasone nasal spray provided significantly (p < 0.05) greater relief than either agent alone in patients with SAR.

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“…Azelastine is pharmacologically active and is metabolized by CYP3A4 and 2D6 isozymes to its major, active metabolite, desmethylazelastine (4,5). The most common adverse events related to azelastine were alterations in taste perception, nasal burning, headaches, and dry mouth (6). In addition, this agent has been shown to modify the electrical activity in several types of tissues.…”

Section: Introductionmentioning

confidence: 99%

Effect of Azelastine on Cardiac Repolarization of Guinea-Pig Cardiomyocytes, hERG K+ Channel, and Human L-type and T-type Ca2+ Channel

et al. 2013

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Abstract. Azelastine is a second generation histamine H 1 -receptor antagonist used as an antiasthmatic and anti-allergic drug that can induce QT prolongation and torsades de pointes. We investigated the acute effects of azelastine on human ether-a-go-go-related gene (hERG) channels, action potential duration (APD), and L-type (I Ca,L ) and T-type Ca 2+ current (I Ca,T ) to determine the electrophysiological basis for its proarrhythmic potential. Azelastine increased the APD at 90% of repolarization concentration dependently, with an IC 50 of 1.08 nM in guinea-pig ventricular myocytes. We examined the effects of azelastine on the hERG channels expressed in Xenopus oocytes and HEK293 cells using two-microelectrode voltage-clamp and patch-clamp techniques. Azelastine induced a concentration-dependent decrease of the hERG current amplitude at the end of the voltage steps and tail currents. The IC 50 for the azelastine-induced block of the hERG currents expressed in HEK293 cells was 11.43 nM, while the drug inhibited I Ca,L and I Ca,T with IC 50 values of 7.60 and 26.21 mM, respectively. The S6 domain mutations, Y652A partially attenuated and F656A abolished hERG current block. These results suggest that azelastine is a potent blocker of hERG channels rather than I Ca,L or I Ca,T , providing molecular mechanisms for the arrhythmogenic side effects during the clinical administration of azelastine.

show abstract

Safety and Efficacy of Azelastine Nasal Spray (Astelin NS) for Seasonal Allergic Rhinitis: a 4-Week Comparative Multicenter Trial

Cited by 69 publications

References 17 publications

The diagnosis and management of rhinitis: An updated practice parameter

The diagnosis and management of rhinitis: An updated practice parameter

Azelastine hydrochloride:a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability

Effect of Azelastine on Cardiac Repolarization of Guinea-Pig Cardiomyocytes, hERG K+ Channel, and Human L-type and T-type Ca2+ Channel

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