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

References

• Dykewicz MS, Fineman S, Skoner DP, et al. Diagnosis and management of rhinitis: complete guidelines of the Joint Task Force on Practice Parameters in Allergy, Asthma and Immun ology. Ann Allergy Asthma Immunol 1998;81:478–518
   PubMed Web of Science ®Google Scholar
• Reed SD, Lee TA, McCrory DC. The economic burden of allergic rhinitis: a critical evaluation of the literature. Pharmacoeconomics 2004;22:345–61
   Google Scholar
• Ray NF, Baraniuk JN, Thamer M, et al. Direct expenditures for the treatment of allergic rhinoconjunctivitis in 1996, including the contributions of related airway illnesses. J Allergy Clin Immunol 1999;103:401–7
   PubMed Web of Science ®Google Scholar
• Settipane RA. Demographics and epidemiology of allergic and nonallergic rhinitis. Allergy Asthma Proc 2001;22:185–9
   PubMed Web of Science ®Google Scholar
• Thompson A, Juniper E, Meltzer E. Quality of life in patients with allergic rhinitis. Ann Allergy Asthma Immunol 2000;85:338–48
   PubMed Web of Science ®Google Scholar
• Bousquet J, van Cauwenberge PB, Khaltaev N, et al. Allergic rhinitis and its impact on asthma: ARIA workshop report. J Allergy Clin Immunol 2001;108:S147–S334
   PubMed Web of Science ®Google Scholar
• Bielory L, Ambrosio P. Conjunctivitis and allergic eye diseases. In: Kaliner MA, editor. Current Reviews of Rhinitis. Philadelphia: Current Medicine, Inc., 2002, pp.115–22
   Google Scholar
• Lieberman P, Kaliner MA, Wheeler WJ. Open-label evaluation of azelastine nasal spray in patients with seasonal allergic rhinitis and nonallergic vasomotor rhinitis. Curr Med Res Opin 2005;21:611–8
   Google Scholar
• White MV. Nasal cholinergic hyperresponsiveness in atopic subjects studied out of season. J Allergy Clin Immunol 1993;92:278–87
   PubMed Web of Science ®Google Scholar
• Skoner DP. Allergic rhinitis: definition, epidemiology, pathophysiology, detection, and diagnosis. J Allergy Clin Immunol 2001;108:S2–S8
   PubMed Web of Science ®Google Scholar
• Economides A, Kaliner MA. Allergic rhinitis. In: Kaliner MA, editor. Current Reviews of Rhinitis. Philadelphia: Current Medicine, Inc., 2002, pp.35–51
   Google Scholar
• Devyani L, Corey JP. Vasomotor rhinitis update. Curr Opin Otolaryngol Head Neck Surg 2004;12:243–7
   PubMedGoogle Scholar
• Settipane RA, Settipane GA. Nonallergic rhinitis. In: Kaliner MA, editor. Current Reviews of Rhinitis. Philadelphia: Current Medicine, Inc.; 2002. p. 53–65
   Google Scholar
• Banov CH, Lieberman P. Efficacy of azelastine nasal spray in the treatment of vasomotor (perennial nonallergic) rhinitis. Ann Allergy Asthma Immunol 2001;86:28–35
   PubMed Web of Science ®Google Scholar
• Bernstein JA, Rezvani M. Mixed rhinitis: a new subclass of chronic rhinitis? In: Kaliner MA, editor. Current Reviews of Rhinitis, 2nd ed. Philadelphia: Current Medicine, Inc.; p. 2006. p. 69–78
   Google Scholar
• Brandt D, Bernstein JA. Questionnaire evaluation and risk factor identification for nonallergic vasomotor rhinitis. Ann Allergy Asthma Immunol 2006;96:526–32
   PubMed Web of Science ®Google Scholar
• Anon. Allergies in America: a landmark survey of nasal allergy sufferers. HealthSTAR Communications, Inc. Sponsored by Altana Pharma US, Inc.; March 1, 2006
   Google Scholar
• Anon. Physician survey sponsored by the American College of Allergy, Asthma and Immunology. Rochester (NY): Harris Interactive Inc.; October 19–21, 2001
   Google Scholar
• Howard J. Azelastine hydrochloride nasal spray – twenty-nine day tolerability and safety study in healthy subjects. Data on file. Study Report 25. MedPointe Pharmaceuticals
   Google Scholar
• Howard J. Two-week comparative study of the safety and efficacy of azelastine nasal spray in the management of seasonal allergic rhinitis. Data on file. Study Report 26. Medpointe Pharmaceuticals
   Google Scholar
• Koplowitz LP. Determination of the bioavailability of three intranasal formulations of azelastine hydrochloride in normal, healthy, male volunteers. Data on file. Clinical Study report MP 429. MedPointe Pharmaceuticals
   Google Scholar
• Azelastine hydrochloride nasal spray 0.1% (Astelin). MedPointe Pharmaceuticals 2006. US full prescribing information. Available at www.astelin.com/Astelin.Public/AstelinPI.pdf [accessed July 9, 2007]
   Google Scholar
• Weliky I. Evaluation of the absorption, excretion and bio-transformation of [14C] azelastine hydrochloride in healthy men. Data on file. Study Report 1. MedPointe Pharmaceuticals
   Google Scholar
• Patel P, D’Andrea C, Sacks H. Onset of action of azelastine nasal spray compared with mometasone nasal spray and placebo in subjects with seasonal allergic rhinitis evaluated in an environmental exposure chamber. Am J Rhinol 2007;21:499–503
   PubMedGoogle Scholar
• Pearlman D, Grossman J, Meltzer E. Histamine skin test reactivity following single and multiple doses of azelastine nasal spray in patients with seasonal allergic rhinitis. Ann Allergy Asthma Immunol 2003;91:258–62
   Google Scholar
• Howard J. Tolerability and pharmacokinetics after single and multiple doses of 4.4 mg azelastine hydrochloride in volunteers older than 65 years. Data on file. Study Report 18. MedPointe Pharmaceuticals
   Google Scholar
• Howard J. Disposition of azelastine hydrochloride in subjects with hepatic dysfunction and with renal impairment. Data on file. Study Report 19. MedPointe Pharmaceuticals
   Google Scholar
• Zechel HJ, Brock N, Lenke D, Achterrath-Tuckerman U. Pharmacological and toxicological properties of azelastine, a novel anti-allergic agent. Arzneim-Forsch 1981;31;1184–93
   Google Scholar
• Pharmalex SA, Paris, France. Azelastine (Allergodil®): identifica tion of the pharmacological receptors involved in non H1-dependent anti-inflammatory actions. Data on file. Protocol Scientifique N PS.1000:10:06.79. MedPointe Pharmaceuticals
   Google Scholar
• Casale TB. The interaction of azelastine with human lung histamine H1, beta, and muscarinic receptor-binding sites. J Allergy Clin Immunol 1989;83:771–6
   PubMed Web of Science ®Google Scholar
• Katayama S, Akimoto N, Shionoya H, et al. Anti-allergic effect of azelastine hydrochloride on immediate type hypersensitivity reaction in vivo and in vitro. Arzneim-Forsch 1981;31:1196–203
   PubMed Web of Science ®Google Scholar
• Takao A, Shimoda T, Matsuse H, et al. Inhibitory effects of azelastine hydrochloride in alcohol-induced asthma. Ann Allergy Asthma Immunol 1999;82:390–4
   PubMed Web of Science ®Google Scholar
• Howarth PH. Mediators of nasal blockage in allergic rhinitis. Allergy 1997;52(Suppl 40):12–8
   PubMedGoogle Scholar
• Katayama S, Tsunoda H, Sakuma Y, et al. Effect of azelastine on the release and action of leukotriene C4 and D4. Int Arch Allergy Appl Immunol 1987;83:284–9
   PubMedGoogle Scholar
• Shin MH, Baroody F, Proud D, et al. The effect of azelastine on the early allergic response. Clin Exp Allergy 1992;22:289–95
   PubMed Web of Science ®Google Scholar
• Matsumura M, Matsumoto Y, Takahashi H, et al. Inhibitory effects of azelastine on leukotriene B4, C4, and D4 release and production from asthmatic eosinophils. Respir Res 1990;9:206–12
   Google Scholar
• Hamasaki Y, Shafigeh M, Yamamoto S, et al. Inhibition of leukotriene synthesis by azelastine. Ann Allergy Asthma Immunol 1996;76:469–75
   PubMed Web of Science ®Google Scholar
• Nieber K, Baumgarten C, Rathsack R, et al. Effect of azelastine on Substance P content in bronchoalveolar and nasal lavage fluids of patients with allergic asthma. Clin Exp Allergy 1993;23:69–71
   PubMed Web of Science ®Google Scholar
• Hide I, Toriu N, Nuibe T, et al. Suppression of TNF-a secretion by azelastine in a rat mast (RBL-2H3) cell line. J Immunol 1997;159:2932–40
   PubMed Web of Science ®Google Scholar
• Matsuo S, Takayama S. Influence of the anti-allergic agent, azelastine, on tumor necrosis factor-alpha (TNF-a) secretion from cultured mouse mast cells. In Vivo 1998;12:481–4
   PubMed Web of Science ®Google Scholar
• Yoneda K, Yamamoto T, Ueta E, Osaki T. Suppression by azelastine hydrochloride of NF-kB activation involved in generation of cytokines and nitric oxide. Jpn J Pharmacol 1997;73:145–53
   PubMedGoogle Scholar
• Ito H, Nakamura Y, Takagi S, Sakai K. Effects of azelastine on the level of serum interleukin-4 and soluble CD23 antigen in the treatment of nasal allergy. Arzneim-Forsch 1998;48:1143–7
   PubMed Web of Science ®Google Scholar
• Beck G, Mansur A, Afzal M, et al. Effect of azelastine nasal spray on mediators of inflammation in patients with seasonal allergic rhinitis (SAR). Presented at the American Academy of Allergy, Asthma, and Immunology 56th Annual Meeting, San Diego (CA); March 3–8, 2000
   Google Scholar
• Ciprandi G, Pronzato C, Passalacqua G, et al. Topical azelastine reduces eosinophil activation and intercellular adhesion molecule-1 expression on nasal epithelial cells: an antiallergic activity. J Allergy Clin Immunol 1996;98:1088–96
   PubMed Web of Science ®Google Scholar
• Ciprandi G, Cosentino C, Milanese M, Tosca MA. Rapid anti-inflammatory action of azelastine eye drops for ongoing allergic reactions. Ann Allergy Asthma Immunol 2003;90:434–8
   PubMed Web of Science ®Google Scholar
• Busse W, Randley B, Sedgwick J, Sofia RD. The effect of azelastine on neutrophil and eosinophil generation of superoxide. J Allergy Clin Immunol 1989;83:400–5
   PubMed Web of Science ®Google Scholar
• Umeki S. Effects of antiallergic drugs on human neutrophil superoxide-generating NADPH oxidase. Biochem Pharmacol 1992;43:1109–17
   PubMed Web of Science ®Google Scholar
• Morita M, Ohshima Y, Akutagawa H, et al. Inhibitory effects of azelastine hydrochloride on Ca2+ influx, actin polymerization and release of eosinophils cationic protein of an eosinophilic leukaemia cell line EoL-1. Curr Med Res Opin 1993;13:163–74
   PubMed Web of Science ®Google Scholar
• Nakamura T, Nishizawa Y, Sato T, Yamato C. Effect of azelastine on the intracellular Ca2+ mobilization in guinea pig peritoneal macrophages. Eur J Pharmacol 1988;148:35–41
   PubMed Web of Science ®Google Scholar
• Morganroth J, Lyness WH, Perhach JL, et al. Lack of effect of azelastine and ketaconazole coadministration on electrocardiographic parameters in healthy volunteers. J Clin Pharmacol 1997;37:1065–72
   PubMed Web of Science ®Google Scholar
• Sale M, Lyness W, Perhach J, et al. Lack of effect of coadministration of erythromycin with azelastine on pharmacokinetic or ECG parameters (abstract). Ann Allergy Asthma Immunol 1996;76:91
   Google Scholar
• Weiler JM, Meltzer EO, Benson PM, et al. A dose-ranging study of the efficacy and safety of azelastine nasal spray in the treatment of seasonal allergic rhinitis with an acute model. J Allergy Clin Immunol 1994;94:972–80
   PubMed Web of Science ®Google Scholar
• Meltzer EO, Weiler JM, Dockhorn RJ, et al. Azelastine nasal spray in the management of seasonal allergic rhinitis. Ann Allergy 1994;72:354–9
   PubMedGoogle Scholar
• Ratner PH, Findlay SR, Hampel F, et al. A double-blind, controlled trial to assess the safety and efficacy of azelastine nasal spray in seasonal allergic rhinitis. J Allergy Clin Immunol 1994;94:818–25
   PubMed Web of Science ®Google Scholar
• Storms WW, Pearlman DS, Chervinsky P, et al. Effectiveness of azelastine nasal solution in seasonal allergic rhinitis. ENT J 1994;73:382–94
   Google Scholar
• LaForce C, Dockhorn RJ, Prenner BM, et al. Safety and efficacy of azelastine nasal spray (Astelin NS) for seasonal allergic rhinitis. Ann Allergy Asthma Immunol 1996;76:181–8
   PubMed Web of Science ®Google Scholar
• Lumry W, Prenner B, Corren J, Wheeler W. Efficacy and safety of azelastine nasal spray at a dosage of one spray per nostril twice daily. Ann Allergy Asthma Immunol. 2007 [in press]
   Google Scholar
• Berger WE, White MV, the Rhinitis Study Group. Efficacy of azelastine nasal spray in patients with an unsatisfactory response to loratadine. Ann Allergy Asthma Immunol 2003;91:205–11
   PubMed Web of Science ®Google Scholar
• LaForce CF, Corren J, Wheeler WJ, et al. Efficacy of azelastine nasal spray in seasonal allergic rhinitis patients who remain symptomatic after treatment with fexofenadine. Ann Allergy Asthma Immunol 2004;93:154–9
   PubMed Web of Science ®Google Scholar
• Corren J, Storms WW, Bernstein J, et al. Effectiveness of azelastine nasal spray compared to oral cetirizine in patients with seasonal allergic rhinitis. Clin Ther 2005;27:543–3
   PubMed Web of Science ®Google Scholar
• Berger W, Hampel F, Bernstein J, et al. Impact of azelastine nasal spray on symptoms and quality of life compared with cetirizine oral tablets in patients with seasonal allergic rhinitis. Ann Allergy Asthma Immunol 2006;97:375–81
   PubMed Web of Science ®Google Scholar
• Georgitis JW. Nasal hyperthermia and simple irrigation for perennial rhinitis: changes in inflammatory mediators. Chest 1994;106:1487–92
   PubMed Web of Science ®Google Scholar
• Tomooka LT, Murphy C, Davidson TM. Clinical study and literature review of nasal irrigation. Laryngoscope 2000;110: 1189–93
   Google Scholar
• Juniper EF, Guyatt GH, Thompson AK, et al. Validation of the standardized version of the Rhinoconjunctivitis Quality of Life Questionnaire. J Allergy Clin Immunol 1999;104:364–9
   PubMed Web of Science ®Google Scholar
• Sacks H, Wheeler W, Dai Y. Double-blind trial of Astelin® (azelastine hydrochloride) Nasal Spray compared to Zyrtec® (cetirizine) tablets in the treatment of patients with seasonal allergic rhinitis. Data on file. Clinical Study Reports MP 425 and MP 426. MedPointe Pharmaceuticals
   Google Scholar
• Juniper EF, Thompson AK, Roberts JN. Can the standard gamble and rating scale be used to measure quality of life in rhinoconjunctivitis? Comparison with the RQLQ and SF-36. Allergy 2002;57: 201–6
   Google Scholar
• Meltzer EO, Tyrell RJ, Rich D, Wood CC. A pharmacologic continuum in the treatment of rhinorrhea: the clinician as economist. J Allergy Clin Immunol 1995;95:1147–52
   PubMed Web of Science ®Google Scholar
• Weiner JM, Abramson MJ, Puy RM. Intranasal corticosteroids versus oral H1 receptor antagonists in allergic rhinitis: systematic review of randomized controlled trials. Br Med J 1998;317: 1624–9
   Google Scholar
• Nielsen LP, Dahl R. Comparison of intranasal corticosteroids and antihistamines in allergic rhinitis. Am J Respir Med 2003;2:55–65
   PubMedGoogle Scholar
• Ratner P, Sacks H. Randomized, double-blind trial of azelastine nasal spray plus fluticasone nasal spray compared to either agent alone in patients with allergy to Texas Mountain Cedar [abstract 28] Ann Allergy Asthma Immunol 2007;98(Suppl 1):A20
   Google Scholar
• Ciprandi G, Ricca V, Passalaqua G, et al. Seasonal rhinitis and azelastine: long- or short-term treatment? J Allergy Clin Immunol 1997;99:301–7
   PubMed Web of Science ®Google Scholar
• Davies RJ, Bagnall AC, McCabe RN, et al. Antihistamines: topical vs oral administration. Clin Exp Allergy 1996:26(Suppl 3):11–7
   PubMed Web of Science ®Google Scholar