Astepro (azelastine hydrochloride nasal spray)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.

Approval Status:

Approved October 2008

Specific Treatments:

seasonal and perennial allergic rhinitis

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General Information

Astepro is an H1-receptor antagonist indicated for the relief of the symptoms of seasonal and perennial allergic rhinitis. It is administered via a metered dose nasal spray.

Astepro Nasal Spray 0.1% and 0.15% is specifically indicated for the relief of the symptoms of seasonal and perennial allergic rhinitis in patients 12 years of age and older.

Astepro Nasal Spray is supplied as a solution for intranasal administration. The recommended initial dose of Astepro Nasal Spray 0.1% and 0.15% is as follows:
Seasonal Allergic Rhinitis:
1 or 2 sprays per nostril twice daily. The 0.15% formulation may also be administered as 2 sprays per nostril once daily.
Perennial Allergic Rhinitis:
0.15% formulation- 2 sprays per nostril twice daily.

Clinical Results

FDA Approval
The FDA approval of Astepro Nasal Spray 0.1% for seasonal allergic rhinitis was based on the following studies:
A 2-week, randomized, multicenter, double-blind, placebo-controlled clinical trial enrolled 834 adults and adolescents 12 years of age and older with symptoms of seasonal allergic rhinitis. The subjects were randomized to one of six treatment groups: 1 spray per nostril of either Astepro Nasal Spray 0.1%, Astelin (azelastine hydrochloride) Nasal Spray or vehicle placebo twice daily; or 2 sprays per nostril of Astepro Nasal Spray 0.1%, Astelin (azelastine hydrochloride) Nasal Spray or vehicle placebo twice daily. Efficacy was based on the 12-hour reflective total nasal symptom score (rTNSS) assessed daily in the morning and evening, in addition to the instantaneous total nasal symptom score (iTNSS). Astepro Nasal Spray 0.1% two sprays twice a day demonstrated a greater decrease in rTNSS and iTNSS than placebo; the difference was statistically significant. Astepro Nasal Spray 0.1% one spray per nostril twice daily for seasonal allergic rhinitis was also assessed in two, 2-week, placebo-controlled clinical trials with Astelin (azelastine hydrochloride) Nasal Spray in 413 subjects. In these trials, efficacy was assessed using the TNSS. Astelin Nasal Spray demonstrated a greater decrease from baseline in the summed AM and PM rTNSS compared with placebo; the difference was statistically significant.

The FDA approval of Astepro Nasal Spray 0.15% was based on the following studies:
Seasonal Allergic Rhinitis
Five randomized, multicenter, double-blind, placebo-controlled clinical trials were conducted in 2,499 adults and adolescents 12 years and older with symptoms of seasonal allergic rhinitis (Trials 2, 3, 4, 5, and 6). The primary efficacy endpoint was the mean change from baseline in rTNSS over 2 weeks.
Trials 2 and 3
These 2-week trials evaluated the efficacy of Astepro Nasal Spray 0.15% dosed at 2 sprays twice daily. Trial 2 compared the efficacy of Astepro Nasal Spray 0.15% and Astelin (azelastine hydrochloride) Nasal Spray to vehicle placebo. Trial 3 compared the efficacy of Astepro Nasal Spray 0.15% and Astepro Nasal Spray 0.1% to vehicle placebo. In these two trials, Astepro Nasal Spray 0.15% demonstrated greater decreases in rTNSS than placebo and the differences were statistically significant.
Trials 4, 5 and 6
These trials evaluated the efficacy of Astepro Nasal Spray 0.15% dosed at 2 sprays once daily compared to the vehicle placebo. Trial 4 demonstrated a greater decrease in rTNSS than placebo and the difference was statistically significant. Trial 5 and Trial 6 were conducted in patients with Texas mountain cedar allergy. In Trial 5 and Trial 6, Astepro Nasal Spray 0.15% demonstrated a greater decrease in rTNSS than placebo and the differences were statistically significant. In Trials 5 and 6, Astepro Nasal Spray 0.15% demonstrated a greater decrease in iTNSS than placebo and the differences were statistically significant.
Perennial Allergic Rhinitis
One randomized, multicenter, double-blind, placebo-controlled clinical trial enrolled 578 adults and adolescents 12 years and older with symptoms of perennial allergic rhinitis. The trial evaluated the efficacy of Astepro Nasal Spray 0.15%, Astepro Nasal Spray 0.1%, and vehicle placebo dosed at 2 sprays per nostril twice daily. The primary efficacy endpoint was the mean change from baseline rTNSS over 4 weeks. In this trial, Astepro Nasal Spray 0.15% demonstrated a greater decrease in rTNSS than placebo and the difference was statistically significant.

In a 12-month, long-term safety trial, 466 subjects (12 years of age and older) with perennial allergic rhinitis were treated with Astepro Nasal Spray 0.15% two sprays per nostril twice daily and 237 subjects were treated with mometasone nasal spray two sprays per nostril once daily. The most frequently reported adverse reactions with Astepro Nasal Spray 0.15% were bitter taste, headache, sinusitis, and epistaxis. Focused nasal examinations were performed and no nasal ulcerations or septal perforations were observed. There were no reports of severe epistaxis.

Side Effects

Adverse events associated with the use of Astepro Nasal Spray may include, but are not limited to, the following:

  • Bitter Taste
  • Epistaxis
  • Headache
  • Nasal Discomfort
  • Fatigue
  • Sneezing
  • Somnolence

Mechanism of Action

Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1 -receptor antagonist activity in isolated tissues, animal models, and humans. It is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H1 -receptor antagonist activity.

Literature References

van Bavel J, Howland WC, Amar NJ, Wheeler W, Sacks H Efficacy and safety of azelastine 0.15% nasal spray administered once daily in subjects with seasonal allergic rhinitis. Allergy and Asthma Proceedings : the Official Journal of Regional and State Allergy Societies 2009 Sep 10

Horak F Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis. Therapeutics and Clinical Risk Management 2008 Oct;4(5):1009-22

Lumry W, Prenner B, Corren J, Wheeler W Efficacy and safety of azelastine nasal spray at a dose of 1 spray per nostril twice daily. Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology 2007 Sep;99(3):267-72

Banov CH, Lieberman P; Vasomotor Rhinitis Study Groups Efficacy of azelastine nasal spray in the treatment of vasomotor (perennial nonallergic) rhinitis. Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology 2001 Jan;86(1):28-35

Herman D, Garay R, Le Gal M A randomized double-blind placebo controlled study of azelastine nasal spray in children with perennial rhinitis. International Journal of Pediatric Otorhinolaryngology 1997 Feb 14;39(1):1-8

Additional Information

For additional information regarding Astepro Nasal Spray or seasonal and perennial allergic rhinitis, please visit the Astepro web page.