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

@article{Bernstein2007AzelastineHR,
  title={Azelastine hydrochloride:a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability},
  author={Jonathan A. Bernstein},
  journal={Current Medical Research and Opinion},
  year={2007},
  volume={23},
  pages={2441 - 2452}
}
  • J. Bernstein
  • Published 24 August 2007
  • Medicine
  • Current Medical Research and Opinion
ABSTRACT Introduction: Azelastine hydrochloride (Astelin) nasal spray 0.1% solution is a second-generation intranasal antihistamine available in the US for treatment of both seasonal allergic rhinitis (SAR) and nonallergic vasomotor rhinitis (VMR). Scope: Searches of journal articles including the title word ‘azelastine’ from 1979 through the present were conducted by the product manufacturer primarily through Medline and EMBASE but also included, at various times, Dialog, Biosis, Toxline, and… 
Azelastine HCl: A Review of the Old and New Formulations
TLDR
The new formulation (Astepro™ 0.1%) is approved for seasonal and perennial allergic rhinitis and has been demonstrated to have comparable pharmacokinetics, pharmacodynamics and therapeutic efficacy compared to Astelin.
Pharmacokinetic characteristics and safety and tolerability of a reformulated azelastine hydrochloride nasal spray in patients with chronic rhinitis
TLDR
The new formulation of azelastine nasal spray with sorbitol-based vehicle and sucralose as a taste-masking agent was safe and well tolerated with long-term use and had a comparable pharmacokinetic profile to the original formulation.
Azelastine and olopatadine in the treatment of allergic rhinitis.
  • M. Kaliner
  • Medicine
    Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
  • 2009
TLDR
The data support current recommendations for nasal antihistamines as first-line therapy for allergic rhinitis, and the combination of a nasalAntihistamine and intranasal steroid may provide additive benefits for treating patients with more severe disease.
Azelastine hydrochloride, a dual-acting anti-inflammatory ophthalmic solution, for treatment of allergic conjunctivitis
TLDR
Because it can often produce maximal effect with just twice-daily dosing, azelastine is a particularly good choice for the allergic population in whom minimizing exposure to topical products and preservatives is a key concern.
Comparative study of the efficacy and safety of intranasal azelastine hydrochloride and fluticasone furoate in the treatment of allergic rhinitis
TLDR
Fluticasone furoate produced sustained relief of symptoms, signs, and sensory attributes with a greater reduction in eosinophil count in comparison with AH in patients with allergic rhinitis.
Advances in pharmacotherapy for the treatment of allergic rhinitis; MP29-02 (a novel formulation of azelastine hydrochloride and fluticasone propionate in an advanced delivery system) fills the gaps
TLDR
MP29-02 simplifies AR management, surpassing the efficacy of gold standard treatment, intranasal corticosteroids (INS), for the first time, and is indicated for the treatment of moderate-to-severe seasonal allergic rhinitis and perennial allergic Rhinitis when monotherapy is NOT considered sufficient.
A role for the intranasal formulation of azelastine hydrochloride/fluticasone propionate in the treatment of allergic rhinitis.
TLDR
MP29-02 (Dymista(®)) is a novel intranasal formulation combining the second-generation antihistamine, azelastine hydrochloride, with fluticasone propionate in a single device that has recently been developed and the efficacy and safety profile is reviewed.
Azelastine nasal spray for the treatment of allergic and nonallergic rhinitis
TLDR
Combination therapy with intranasal FP has the potential to enhance clinical benefit, as the combination of azelastine and FP nasal sprays reduce symptoms in allergic rhinitis patients more than either agent alone.
Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis
  • F. Horak
  • Medicine
    Therapeutics and clinical risk management
  • 2008
TLDR
Unlike most oral antihistamines, azelastine nasal spray is effective in alleviating nasal congestion, a particularly bothersome symptom for rhinitis sufferers.
Antihistamine Therapy in AllergicRhinitis
TLDR
The history and classification of antihistamines as well as their role in the treatment of allergic rhinitis and the evidence supporting this use are discussed.
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References

SHOWING 1-10 OF 79 REFERENCES
Azelastine nasal spray in the management of seasonal allergic rhinitis.
TLDR
Azelastine nasal spray, administered either once or twice daily, was effective in treating the symptoms of seasonal allergic rhinitis and demonstrated a rapid onset of action with a duration of response lasting 12 to 24 hours.
The effect of azelastine on the early allergic response
TLDR
It is suggested that azelastine does not inhibit mast cell activation but affects the consequences of released histamine, namely sneezing, increased vascular permeability and the generation of kinins, and that other cells, in addition to mast cells, might be responsible for thegeneration of leukotrienes during the early allergic response.
Effectiveness of Azelastine Nasal Solution in Seasonal Allergic Rhinitis
TLDR
The results of this trial demonstrate that azelastine nasal solution provides an alternative to oral medication in the treatment of SAR and its rapid onset and prolonged duration of action in relieving rhinitis symptoms and advantages over currently marketed topical treatments make it a good choice for Treatment of SAR.
Safety and efficacy of azelastine nasal spray (Astelin NS) for seasonal allergic rhinitis: a 4-week comparative multicenter trial.
  • C. Laforce, R. Dockhorn, +5 authors J. Freitag
  • Medicine
    Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
  • 1996
TLDR
For both azelastine treatment groups, improvements in all of the individual rhinitis symptoms were superior to those for the placebo group and, in general were clinically and statistically significant.
Lack of Effect of Azelastine and Ketoconazole Coadministration on Electrocardiographic Parameters in Healthy Volunteers
TLDR
In vitro tests and the absence of electrocardiographic effects suggests azelastine can be safely administered with CYP3A4 inhibitors, and in vitro tests with human liver microsomes were used to characterize azelasta's inhibition spectrum.
Rapid anti-inflammatory action of azelastine eyedrops for ongoing allergic reactions.
TLDR
The ability of azelastine to reduce symptoms and inflammation during an ongoing allergic reaction can be considered concrete and convincing proof of a clinically relevant anti-inflammatory activity.
A dose-ranging study of the efficacy and safety of azelastine nasal spray in the treatment of seasonal allergic rhinitis with an acute model.
TLDR
This study supports a once to twice daily dosing regimen for 2 sprays of 0.1% azelastine in the acute treatment of allergic rhinitis with onset of action within 2 to 3 hours.
Seasonal rhinitis and azelastine: long- or short-term treatment?
TLDR
Continuous treatment was more effective than on-demand use as assessed by both clinical evaluation and antiinflammatory action.
Antihistamines: topical vs oral administration
The pathogenesis of allergic rhinitis is complex, involving not only histamine and mast cell‐derived tryptase, but also eosinophil‐ and neutrophil‐derived mediators, cytokines, and intercellular cell
Efficacy of azelastine nasal spray in the treatment of vasomotor (perennial nonallergic) rhinitis.
  • C. Banov, P. Lieberman
  • Medicine
    Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
  • 2001
TLDR
This is the first demonstration of the efficacy of an antihistamine in the therapy of VMR in two double-blind, placebo-controlled clinical trials.
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