What is Astepro (Azelastine)?

From the Guidelines

Astepro (azelastine hydrochloride) is an effective treatment for seasonal and perennial allergic rhinitis, and the recommended dose is typically two sprays in each nostril twice daily for adults and children 12 years and older, and one spray in each nostril twice daily for children 6-11 years old.

Key Points

• Astepro works by blocking histamine receptors, which reduces allergic symptoms such as sneezing, itchy nose, runny nose, and nasal congestion 1.
• It's available in both prescription and over-the-counter formulations (Astepro Allergy) and has been shown to be effective in treating nasal symptoms, with benefits even in patients who fail oral antihistamine treatment 1.
• Side effects may include bitter taste, headache, drowsiness, and nasal irritation, but recent studies have found somnolence rates to be low, ranging from 0.4% to 3%, which are equal or only slightly greater than in placebo groups 1.
• For best results, clear your nasal passages before use, shake the bottle gently, and keep your head upright during administration, and avoid alcohol while using Astepro as it may increase drowsiness.
• Improvement typically begins within 3 hours, but regular use provides better symptom control, and if symptoms persist beyond 2 weeks of regular use, consult your healthcare provider.

Considerations

• Intranasal antihistamines, such as Astepro, have been shown to be effective in treating nasal symptoms and may be preferred over oral antihistamines due to targeted delivery and increased dosage to nasal tissues while limiting systemic effects 1.
• Astepro may be used as first- or second-line therapy for allergic rhinitis, and its rapid onset of action makes it especially useful in patients with episodic nasal symptoms or as a pretreatment prior to nasal allergen exposure 1.

From the FDA Drug Label

Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1 -receptor antagonist activity in isolated tissues, animal models, and humans. Astelin® Nasal Spray 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.

The drug Astepro is another name for Azelastine. Azelastine is an antihistamine that exhibits histamine H1-receptor antagonist activity.

• Key points about Azelastine include:
  • It is administered as a racemic mixture.
  • The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity.
  • Azelastine is used to treat allergic rhinitis.
  • It is available as a nasal spray.
  • The pharmacokinetics of azelastine include a systemic bioavailability of approximately 40% and an elimination half-life of 22 hours 2.

From the Research

Astepro Overview

• Astepro, also known as azelastine nasal spray, is a second-generation antihistamine used to treat allergic and nonallergic rhinitis in adults and children 3.
• It has a rapid onset of action, typically within 15 minutes, and offers flexibility in dosing, with options for one or two sprays per nostril twice daily 3.

Efficacy and Safety

• Studies have shown that azelastine nasal spray is effective in reducing symptoms of allergic rhinitis, including nasal congestion, runny nose, itchy nose, and sneezing 4, 5, 6, 7.
• Azelastine has been compared to other treatments, such as oral antihistamines (e.g., cetirizine) and intranasal corticosteroids (e.g., fluticasone propionate), and has been found to have comparable or superior efficacy in some cases 3, 6, 7.
• The safety profile of azelastine nasal spray is excellent, with common side effects including bitter taste, headache, and drowsiness 4, 5.

Dosage and Administration

• Azelastine nasal spray is commercially available as a 0.1% w/v solution and is typically administered twice daily 5.
• A higher concentration of 0.15% has been studied and found to be effective with once-daily dosing, although this formulation is not commercially available 5.

Comparison to Other Treatments

• Azelastine nasal spray has been compared to fluticasone nasal spray and found to have comparable efficacy in symptom control, with the advantage of fewer side effects 6.
• Azelastine has also been compared to oral cetirizine and found to have greater improvements in total nasal symptom score and quality of life questionnaire scores 7.