605
Views
73
CrossRef citations to date
0
Altmetric
Review

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

Pages 2441-2452 | Accepted 23 Jul 2007, Published online: 24 Aug 2007

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (8)

Swapnil Sharadkumar Chudiwal & Mohamed Hassan G. Dehghan. (2016) Quality by design approach for development of suspension nasal spray products: a case study on budesonide nasal suspension. Drug Development and Industrial Pharmacy 42:10, pages 1643-1652.
Read now
Dariusz Sroczyński, Zbigniew Malinowski, Aleksandra K. Szcześniak & Wanda Pakulska. (2016) New 1(2H)-phthalazinone derivatives as potent nonpeptidic HIV-1 protease inhibitors: molecular docking studies, molecular dynamics simulation, oral bioavailability and ADME prediction. Molecular Simulation 42:8, pages 628-641.
Read now
Jean Bousquet, Claus Bachert, Jonathan Bernstein, G Walter Canonica, Warner Carr, Ronald Dahl, Pascal Demoly, Philippe Devillier, Peter Hellings, Wytske Fokkens, Ludger Klimek, Phil Lieberman, Eli Meltzer, David Price, Dermot Ryan & Ulrich Wahn. (2015) 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. Expert Opinion on Pharmacotherapy 16:6, pages 913-928.
Read now
Patricia B Williams, Elizabeth Crandall & John D Sheppard. (2010) Azelastine hydrochloride, a dual-acting anti-inflammatory ophthalmic solution, for treatment of allergic conjunctivitis. Clinical Ophthalmology 4, pages 993-1001.
Read now
Friedrich Horak & Ursula Petra Zieglmayer. (2009) Azelastine nasal spray for the treatment of allergic and nonallergic rhinitis. Expert Review of Clinical Immunology 5:6, pages 659-669.
Read now
Robert Anolik. (2009) Desloratadine and pseudoephedrine combination therapy as a comprehensive treatment for allergic rhinitis and nasal congestion. Expert Opinion on Drug Metabolism & Toxicology 5:6, pages 683-694.
Read now
Friedrich Horak. (2008) Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis. Therapeutics and Clinical Risk Management 4:5, pages 1009-1022.
Read now

Articles from other publishers (65)

Ewa Trybus, Wojciech Trybus & Teodora Król. (2023) Cytological Study of Topical Effect of Azelastine Hydrochloride on the Nasal Mucous Membrane Cells in Various Nasal Rhinitis Types. Cells 12:23, pages 2697.
Crossref
Jasmin Kuratli, Cory Ann Leonard, Robert Schoborg & Nicole Borel. (2023) Anti-chlamydial effects of azelastine hydrochloride and the impact of the histamine H1 receptor on chlamydial development. Journal of Medical Microbiology 72:5.
Crossref
Devulapally Yogananda Chary, Minpoor Soumya Reddy, Chidrawar Ajay, Balasubramanian Sridhar & Basi V Subba Reddy. (2023) Ir(III)-Catalyzed Dual C–H Activation of 2-Aryl Phthalazinediones and 3-Aryl-2 H -benzo[ e ][1,2,4]thiadiazine-1,1-dioxides for the Construction of Spiro-Fused Cyclic Frameworks . The Journal of Organic Chemistry 88:5, pages 2758-2772.
Crossref
Anna Gumieniczek, Karolina Lejwoda & Natalia Data. (2022) Chemical Stability Study of H1 Antihistaminic Drugs from the First and the Second Generations, Diphenhydramine, Azelastine and Bepotastine, in Pure APIs and in the Presence of Two Excipients, Citric Acid and Polyvinyl Alcohol. Molecules 27:23, pages 8322.
Crossref
Christiane Dings, Peter Meiser, Frank Holzer, Michael Flegel, Dominik Selzer, Eszter Nagy, Ralph Mösges, Jens Peter Klussmann & Thorsten Lehr. (2022) Pharmacometric Modeling of the Impact of Azelastine Nasal Spray on SARS-CoV-2 Viral Load and Related Symptoms in COVID-19 Patients. Pharmaceutics 14:10, pages 2059.
Crossref
Erick J. Carlson, Rawle Francis, Yutong Liu, Ping Li, Maximilian Lyon, Celia M. Santi, Derek J. Hook, Jon E. Hawkinson & Gunda I. Georg. (2022) Discovery and Characterization of Multiple Classes of Human CatSper Blockers. ChemMedChem 17:15.
Crossref
Rungsima Hadsarung, Sanit Thongnest, Sittisak Oekchuae, Duangduan Chaiyaveij, Jutatip Boonsombat & Somsak Ruchirawat. (2022) Facile synthesis of 1-substituted 4-H phthalazine, a versatile scaffold for chemically diverse phthalazines. Tetrahedron 121, pages 132920.
Crossref
E.V. Nosulya, I.A. Kim, V.Ya. Kunelskaya & Yu.V. Luchsheva. (2022) Fixed-dose combination of azelastine hydrochloride and mometasone furoate in the treatment of allergic rhinitis. Rossiiskaya rinologiya 30:3, pages 185.
Crossref
Nevreste Didem Sonbay Yılmaz, Özer Erdem Gür & Andrey Lopatin. 2022. ENT Diseases: Diagnosis and Treatment during Pregnancy and Lactation. ENT Diseases: Diagnosis and Treatment during Pregnancy and Lactation 613 623 .
Natalie K. Boyd, Grace C. Lee, Chengwen Teng & Christopher R. Frei. (2021) In vitro activity of non-antibiotic drugs against Staphylococcus aureus clinical strains. Journal of Global Antimicrobial Resistance 27, pages 167-171.
Crossref
Phuong Linh Nguyen, Bich Phuong Bui, Men Thi Hoai Duong, Kyeong Lee, Hee-Chul Ahn & Jungsook Cho. (2021) Suppression of LPS-Induced Inflammation and Cell Migration by Azelastine through Inhibition of JNK/NF-κB Pathway in BV2 Microglial Cells. International Journal of Molecular Sciences 22:16, pages 9061.
Crossref
S. Shekhar & A. Bali. (2021) Spectrofluorimetric Method for the Determination of Azelastine Hydrochloride in Bulk and Nasal Formulations. Journal of Applied Spectroscopy 88:3, pages 674-680.
Crossref
Dagmar Stumpfe, Alexander Hoch & Jürgen Bajorath. (2021) Introducing the metacore concept for multi-target ligand design. RSC Medicinal Chemistry 12:4, pages 628-635.
Crossref
Hermann A.M. Mucke. (2021) Drug Repurposing Patent Applications October–December 2020. ASSAY and Drug Development Technologies 19:3, pages 209-214.
Crossref
Cemal Cingi, Nuray Bayar Muluk, Dimitrios I. Mitsias, Nikolaos G. Papadopoulos, Ludger Klimek, Anu Laulajainen-Hongisto, Maija Hytönen, Sanna Katriina Toppila-Salmi & Glenis Kathleen Scadding. (2021) The Nose as a Route for Therapy: Part 1. Pharmacotherapy. Frontiers in Allergy 2.
Crossref
Yong Sun Cho, Hak Do Kim, Euntaek Kim, Sang Hoon Han, Soo Bong Han, Neeraj Kumar Mishra, Young Hoon Jung, Taejoo Jeong & In Su Kim. (2020) Direct Integration of Phthalazinone and Succinimide Scaffolds via Rh(III)‐Catalyzed C−H Functionalization. Asian Journal of Organic Chemistry 10:1, pages 202-209.
Crossref
Daniel L. Krinsky. 2020. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 20th Edition. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 20th Edition.
Daniel L. KrinskyKelly L. Scolaro. 2020. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 20th Edition. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 20th Edition.
Daniel L. Krinsky. 2020. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 20th Edition. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 20th Edition.
Jasmin Kuratli, Cory Ann Leonard, Lisbeth Nufer, Hanna Marti, Robert Schoborg & Nicole Borel. (2020) Maraviroc, celastrol and azelastine alter Chlamydia trachomatis development in HeLa cells. Journal of Medical Microbiology 69:12, pages 1351-1366.
Crossref
Mark S. Dykewicz, Dana V. Wallace, David J. Amrol, Fuad M. Baroody, Jonathan A. Bernstein, Timothy J. Craig, Chitra Dinakar, Anne K. Ellis, Ira Finegold, David B.K. Golden, Matthew J. Greenhawt, John B. Hagan, Caroline C. Horner, David A. Khan, David M. Lang, Desiree E.S. Larenas-Linnemann, Jay A. Lieberman, Eli O. Meltzer, John J. Oppenheimer, Matthew A. Rank, Marcus S. Shaker, Jeffrey L. Shaw, Gary C. Steven, David R. Stukus, Julie Wang, Mark S. Dykewicz, Dana V. Wallace, Chitra Dinakar, Anne K. Ellis, David B.K. Golden, Matthew J. Greenhawt, Caroline C. Horner, David A. Khan, David M. Lang, Jay A. Lieberman, John J. Oppenheimer, Matthew A. Rank, Marcus S. Shaker, David R. Stukus, Julie Wang, Mark S. Dykewicz, Dana V. Wallace, David J. Amrol, Fuad M. Baroody, Jonathan A. Bernstein, Timothy J. Craig, Ira Finegold, John B. Hagan, Desiree E.S. Larenas-Linnemann, Eli O. Meltzer, Jeffrey L. Shaw & Gary C. Steven. (2020) Rhinitis 2020: A practice parameter update. Journal of Allergy and Clinical Immunology 146:4, pages 721-767.
Crossref
Ludger Klimek, Ingrid Casper, Karl-Christian Bergmann, Tilo Biedermann, Jean Bousquet, Peter Hellings, Kirsten Jung, Hans Merk, Heidi Olze, Ralph Mösges, Wolfgang Schlenter, Moritz Gröger, Johannes Ring, Adam Chaker, Oliver Pfaar, Wolfgang Wehrmann, Torsten Zuberbier & Sven Becker. (2020) Therapy of allergic rhinitis in routine care: evidence-based benefit assessment of freely combined use of various active ingredients. Allergo Journal International 29:5, pages 129-138.
Crossref
Ludger Klimek, Ingrid Casper, Karl-Christian Bergmann, Tilo Biedermann, Jean Bousquet, Peter Hellings, Kirsten Jung, Hans Merk, Heidi Olze, Ralph Mösges, Wolfgang Schlenter, Moritz Gröger, Johannes Ring, Adam Chaker, Oliver Pfaar, Wolfgang Wehrmann, Torsten Zuberbier & Sven Becker. (2020) Die Therapie der allergischen Rhinitis in der Routineversorgung: evidenzbasierte Nutzenbewertung der kombinierten Anwendung mehrerer Wirkstoffe. Allergo Journal 29:5, pages 14-24.
Crossref
Daeun Jeoung, Kunyoung Kim, Sang Hoon Han, Prithwish Ghosh, Suk Hun Lee, Saegun Kim, Won An, Hyung Sik Kim, Neeraj Kumar Mishra & In Su Kim. (2020) Phthalazinone-Assisted C–H Amidation Using Dioxazolones Under Rh(III) Catalysis. The Journal of Organic Chemistry 85:11, pages 7014-7023.
Crossref
Nandish Chennakeshavaraju, Sarala Narayana & AzeemS M. Mohiyuddin. (2020) Comparative study of the efficacy and safety of intranasal azelastine hydrochloride and fluticasone furoate in the treatment of allergic rhinitis. Journal of Family and Community Medicine 27:3, pages 186.
Crossref
Anna V Maximova & Y S Smolkin. (2019) Postnasal drip syndrome as a cause of cough in allergic rhinitis. Russian Journal of Allergy 16:4, pages 57-65.
Crossref
Serena Perrone, Luigino Troisi & Antonio Salomone. (2019) Heterocycle Synthesis through Pd-Catalyzed Carbonylative Coupling. European Journal of Organic Chemistry 2019:29, pages 4626-4643.
Crossref
Annabelle M. Watts, Allan W. Cripps, Nicholas P. West & Amanda J. Cox. (2019) Modulation of Allergic Inflammation in the Nasal Mucosa of Allergic Rhinitis Sufferers With Topical Pharmaceutical Agents. Frontiers in Pharmacology 10.
Crossref
Remzi Doğan, Fadlullah Aksoy, Seda Sezen Goktas, Ilker Kocak, Yavuz Selim Yıldırım, Said Incir & Orhan Özturan. (2017) Effect of nasal antihistamine on secretory IgA in nasal lavage of rats. European Archives of Oto-Rhino-Laryngology 275:1, pages 111-115.
Crossref
Justin C. Greiwe. 2018. Rhinitis and Related Upper Respiratory Conditions. Rhinitis and Related Upper Respiratory Conditions 17 27 .
A V Sobolev, Ya I Kozlova, A V Pyatakova, O V Aak & N N Klimko. (2017) Allergic rhinitis: the choice of rational treatment. Russian Journal of Allergy 14:2, pages 71-75.
Crossref
Panayiotis A. Procopiou, Alison J. Ford, Paul M. Gore, Brian E. Looker, Simon T. Hodgson, Duncan S. Holmes, Sadie Vile, Kenneth L. Clark, Ken A. Saunders, Robert J. Slack, James E. Rowedder & Clarissa J. Watts. (2017) Design of Phthalazinone Amide Histamine H 1 Receptor Antagonists for Use in Rhinitis . ACS Medicinal Chemistry Letters 8:5, pages 577-581.
Crossref
E. V. Nosulya & I. A. Kim. (2017) The use of modern topical medications for the stepwise treatment of allergic rhinitis: the effectiveness and prospects for the further extension of their application. Vestnik otorinolaringologii 82:2, pages 65.
Crossref
N M Nenasheva, N I Ilina & T G Fedoskova. (2016) The effectiveness of intranasal corticosteroids and antihistamines combination - mometasone furoate and azelastine hydrochloride nasal spray in adults with seasonal allergic rhinitis (The results of clinical trial). Russian Journal of Allergy 13:2, pages 54-64.
Crossref
T G Fedoskova, V M Svistushkin & E A Shevchik. (2016) Allergic rhinitis is a seasonal trouble and off-seasonal problem. Russian Journal of Allergy 13:2, pages 36-43.
Crossref
Bin Liu, Chunlei Zhang & Xigeng Zhou. (2016) Access to phthalazinones via palladium-catalyzed three-component cycloamino-carbonylation of 2-formylaryl tosylates, hydrazines and CO. Tetrahedron 72:50, pages 8282-8286.
Crossref
S. S Chudiwal & M. H. G. Dehghan. (2016) DEVELOPMENT AND VALIDATION OF SPECTROPHOTOMETRIC METHOD FOR BUDESONIDE ESTIMATION IN NASAL SPRAY FORMULATIONS. INDIAN DRUGS 53:07, pages 42-45.
Crossref
David I. Bernstein, Gene Schwartz & Jonathan A. Bernstein. (2016) Allergic Rhinitis. Immunology and Allergy Clinics of North America 36:2, pages 261-278.
Crossref
Manu De Rycker, John Thomas, Jennifer Riley, Stephen J. Brough, Tim J. Miles & David W. Gray. (2016) Identification of Trypanocidal Activity for Known Clinical Compounds Using a New Trypanosoma cruzi Hit-Discovery Screening Cascade. PLOS Neglected Tropical Diseases 10:4, pages e0004584.
Crossref
E. V. Nosulya & I. A. Kim. (2016) The modern strategies for the treatment of allergic rhinitis. Vestnik otorinolaringologii 81:2, pages 74.
Crossref
Wei Zhu, Bao Wang, Shengbin Zhou & Hong Liu. (2015) The facile construction of the phthalazin-1(2 H )-one scaffold via copper-mediated C–H(sp 2 )/C–H(sp) coupling under mild conditions . Beilstein Journal of Organic Chemistry 11, pages 1624-1631.
Crossref
Erminia Ridolo, Marcello Montagni, Valerie Melli, Laura Bonzano, Cristoforo Incorvaia & Giorgio Walter Canonica. (2015) A role for the intranasal formulation of azelastine hydrochloride/fluticasone propionate in the treatment of allergic rhinitis. Therapeutic Delivery 6:6, pages 653-659.
Crossref
Mahendra Kumar M, Muneeruddin Ahmed S, Md. Naveed Ahmed & Durga Prasad. (2014) COMPARATIVE EFFICACY OF NASAL STEROID IN COMBINATION WITH AN ANTIHISTAMINE VERSUS STEROID ALONE AS NASAL SPRAY IN NASAL POLYPOSIS. Journal of Evolution of Medical and Dental Sciences 3:27, pages 7595-7604.
Crossref
Umesh Singh, Jonathan A. Bernstein, Lauren Haar, Kristin Luther & Walter K. Jones. (2014) Azelastine Desensitization of Transient Receptor Potential Vanilloid 1: A Potential Mechanism Explaining its Therapeutic Effect in Nonallergic Rhinitis. American Journal of Rhinology & Allergy 28:3, pages 215-224.
Crossref
Paul A. JohnstonMalabika SenYun HuaDaniel CamarcoTong Ying ShunJohn S. LazoJennifer R. Grandis. (2014) High-Content pSTAT3/1 Imaging Assays to Screen for Selective Inhibitors of STAT3 Pathway Activation in Head and Neck Cancer Cell Lines. ASSAY and Drug Development Technologies 12:1, pages 55-79.
Crossref
Umesh Singh & Jonathan A. Bernstein. 2014. Capsaicin as a Therapeutic Molecule. Capsaicin as a Therapeutic Molecule 147 170 .
Anne K Ellis, Yifei Zhu, Lisa M Steacy, Terry Walker & James H Day. (2013) A four-way, double-blind, randomized, placebo controlled study to determine the efficacy and speed of azelastine nasal spray, versus loratadine, and cetirizine in adult subjects with allergen-induced seasonal allergic rhinitis. Allergy, Asthma & Clinical Immunology 9:1.
Crossref
Sudipta Pathak, Kamalesh Debnath, Sk Tofajjen Hossain, Samir Kumar Mukherjee & Animesh Pramanik. (2013) Synthesis of biologically important phthalazinones, 2,3-benzoxazin-1-ones and isoindolinones from ninhydrin and their antimicrobial activity. Tetrahedron Letters 54:24, pages 3137-3143.
Crossref
Mi-Hyeong Park, Seung Ho Lee, Dae Hyun Chu, Kwang Hee Won, Bok Hee Choi, Han Choe & Su-Hyun Jo. (2013) Effect of Azelastine on Cardiac Repolarization of Guinea-Pig Cardiomyocytes, hERG K+ Channel, and Human L-type and T-type Ca2+ Channel. Journal of Pharmacological Sciences 123:1, pages 67-77.
Crossref
Panayiotis A. Procopiou, Christopher Browning, Paul M. Gore, Sean M. Lynn, Stephen A. Richards, Robert J. Slack & Steven L. Sollis. (2012) Synthesis and pharmacological investigation of azaphthalazinone human histamine H1 receptor antagonists. Bioorganic & Medicinal Chemistry 20:20, pages 6097-6108.
Crossref
Sajjad Ahmad & Andrew Sutherland. (2012) Stereoselective synthesis of hydroxylated 3-aminoazepanes using a multi-bond forming, three-step tandem process. Organic & Biomolecular Chemistry 10:41, pages 8251.
Crossref
Daniel Baumann, Claus Bachert & Petra Högger. (2012) Development of a novel model for comparative evaluation of intranasal pharmacokinetics and effects of anti-allergic nasal sprays. European Journal of Pharmaceutics and Biopharmaceutics 80:1, pages 156-163.
Crossref
Flavia C.L. Hoyte & Rohit K. Katial. (2011) Antihistamine Therapy in Allergic Rhinitis. Immunology and Allergy Clinics of North America 31:3, pages 509-543.
Crossref
Thuy-Anh N. Melvin & Alpen A. Patel. (2011) Pharmacotherapy for Allergic Rhinitis. Otolaryngologic Clinics of North America 44:3, pages 727-739.
Crossref
Jonathan A. Bernstein, Lloyd Hastings, Erin L. Boespflug, Jane B. Allendorfer, Martine Lamy & James C. Eliassen. (2011) Alteration of brain activation patterns in nonallergic rhinitis patients using functional magnetic resonance imaging before and after treatment with intranasal azelastine. Annals of Allergy, Asthma & Immunology 106:6, pages 527-532.
Crossref
Panayiotis A. Procopiou, Christopher Browning, Jennifer M. Buckley, Kenneth L. Clark, Lise Fechner, Paul M. Gore, Ashley P. Hancock, Simon T. Hodgson, Duncan S. Holmes, Michael Kranz, Brian E. Looker, Karen M. L. Morriss, Daniel L. Parton, Linda J. Russell, Robert J. Slack, Steven L. Sollis, Sadie Vile & Clarissa J. Watts. (2011) The Discovery of Phthalazinone-Based Human H 1 and H 3 Single-Ligand Antagonists Suitable for Intranasal Administration for the Treatment of Allergic Rhinitis . Journal of Medicinal Chemistry 54:7, pages 2183-2195.
Crossref
Demin Han, Lei Chen, Lei Cheng, Shixi Liu, Zheng Fu, Wei Zhang, Chengshuo Wang, Lin Xi & Luo Zhang. (2011) A Multicenter Randomized Double-Blind 2-Week Comparison Study of Azelastine Nasal Spray 0.1% versus Levocabastine Nasal Spray 0.05% in Patients with Moderate-to-Severe Allergic Rhinitis. ORL 73:5, pages 260-265.
Crossref
Jayant M Pinto & Seema Jeswani. (2010) Rhinitis in the geriatric population. Allergy, Asthma & Clinical Immunology 6:1.
Crossref
Jeffrey Suh & James Palmer. 2010. Practical Rhinology. Practical Rhinology 28 37 .
Jonathan M. HorbalJonathan A. Bernstein. (2010) Azelastine HCl: A Review of the Old and New Formulations. Clinical Medicine Insights: Therapeutics 2, pages CMT.S3865.
Crossref
Ayse Fusun Kalpaklioglu & Ayse Baccioglu Kavut. (2010) Comparison of Azelastine versus Triamcinolone Nasal Spray in Allergic and Nonallergic Rhinitis. American Journal of Rhinology & Allergy 24:1, pages 29-33.
Crossref
Michael A. Kaliner. (2009) Azelastine and olopatadine in the treatment of allergic rhinitis. Annals of Allergy, Asthma & Immunology 103:5, pages 373-380.
Crossref
Jonathan A. Bernstein, Bruce Prenner, Berrylin J. Ferguson, Jay Portnoy, William J. Wheeler & Harry J. Sacks. (2009) Double-Blind, Placebo-Controlled Trial of Reformulated Azelastine Nasal Spray in Patients with Seasonal Allergic Rhinitis. American Journal of Rhinology & Allergy 23:5, pages 512-517.
Crossref
. (2009) Current World Literature. Current Opinion in Allergy & Clinical Immunology 9:2, pages 177-184.
Crossref
Leonard Bielory. (2008) Ocular Allergy Treatment. Immunology and Allergy Clinics of North America 28:1, pages 189-224.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.