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Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H₁-receptor antagonist) used a first line therapy of mild intermittent, moderate/severe intermittent and mild persistent rhinitis (new classification system for rhinitis).

Azelastine has been formulated both as a nasal spray and as eye drops and are available worldwide under many brand names.^[1]

Medical uses

Azelastine nasal spray is indicated for the local treatment of the symptoms of seasonal allergic rhinitis and perennial allergic rhinitis, such as rhinorrhea, sneezing and nasal pruritis in adults and children 5 years of age and older.^[2]^[3]^[4] In some countries, it is also indicated for the treatment of vasomotor rhinitis in adults and children ≥ 12 years old.^[4] Azelastine eyes drops are indicated for the local treatment of seasonal and perennial allergic conjunctivitis.^[5]^[6]

Side effects

Azelastine is safe and well tolerated in both adults and children with allergic rhinitis.^[7]^[8]^[9] Bitter taste, headache, nasal burning and somnolence are the most frequently reported adverse events. US prescribing recommendations warn against the concurrent use of alcohol and/or other central nervous system depressants, but to date there have been no studies to assess the effects of azelastine nasal spray on the CNS in humans. More recent studies^[10]^[11] have shown similar degrees of somnolence (approx. 2%) compared with placebo treatment. The problem of bitter taste may be reduced by correct application of the nasal spray (i.e. slightly tipping the head forward and not inhaling the medication too deeply), or alternatively using the azelastine/sucralose formulation.

Pharmacokinetics and metabolism

The systemic bioavailability of azelastine is approximately 40% when administered intranasally. Maximum plasma concentrations (Cmax) are observed within 2–3 hours. The elimination half life, steady-state volume of distribution and plasma clearance are 22 h, 14.5 l/kg and 0.5 l/h/kg respectively (based on intravenous and oral administration data). Azelastine is oxidatively metabolized by the cytochrome P450 family into its active metabolite, desmethylazelastine, and two inactive carboxylic acid metabolites. Approximately 75% of an oral dose is excreted in feces. Pharmacokinetics of orally administered azelastine are not affected by age, gender or hepatic impairment.^[12]

Mode of action

Azelastine has a triple mode of action:^[12]

Anti-histamine effect,
Mast-cell stabilizing effect and
Anti-inflammatory effect.

Chemical properties

The chemical nomenclature of azelastine is (±)-1-(2H)-phthalazinone, 4-[(4-chlorophenyl) methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-monohydrochloride. It is white, almost odorless with a bitter taste.^[13]

Society and culture

Availability

Azelastine is generic and available worldwide under many brand names.^[1]

References

^ ^a ^b ^c Drugs.com Drugs.com international listings for azelastine Page accessed June 28, 2015
^ AHRQ Allergic Rhinitis and its Impact on Asthma (ARIA) treatment guidelines
^ "Rhinolast Nasal Spray Summary of Product Characteristics". Oct 2009. Retrieved 2010-04-27.
^ ^a ^b "Astelin FDA Prescribing Information". Retrieved 2010-04-27.
^ "Optilast Eye Drops Summary of Product Characteristics". Jan 2010. Retrieved 2010-04-27.
^ "Optivar Eye Drops FDA Prescribing Information". Jan 2010. Retrieved 2010-04-27.
^ McNeely, W; Wiseman, LR (July 1998). "Intranasal azelastine. A review of its efficacy in the management of allergic rhinitis.". Drugs 56 (1): 91–114. doi:10.2165/00003495-199856010-00011. PMID 9664202.
^ Ratner PH, Findlay SR, Hampel F, van Bavel J, Widlitz MD, Freitag JJ (November 1994). "A double-blind, controlled trial to assess the safety and efficacy of azelastine nasal spray in seasonal allergic rhinitis". The Journal of Allergy and Clinical Immunology 94 (5): 818–25. doi:10.1016/0091-6749(94)90148-1. PMID 7963150.
^ LaForce C, Dockhorn RJ, Prenner BM; et al. (February 1996). "Safety and efficacy of azelastine nasal spray (Astelin NS) for seasonal allergic rhinitis: a 4-week comparative multicenter trial". Annals of Allergy, Asthma & Immunology 76 (2): 181–8. doi:10.1016/S1081-1206(10)63420-5. PMID 8595539.
^ Corren J, Storms W, Bernstein J, Berger W, Nayak A, Sacks H (May 2005). "Effectiveness of azelastine nasal spray compared with oral cetirizine in patients with seasonal allergic rhinitis". Clinical Therapeutics 27 (5): 543–53. doi:10.1016/j.clinthera.2005.04.012. PMID 15978303.
^ Berger W, Hampel F, Bernstein J, Shah S, Sacks H, Meltzer EO (September 2006). "Impact of azelastine nasal spray on symptoms and quality of life compared with cetirizine oral tablets in patients with seasonal allergic rhinitis". Annals of Allergy, Asthma & Immunology 97 (3): 375–81. doi:10.1016/S1081-1206(10)60804-6. PMID 17042145.
^ ^a ^b Horak, Friedrich; Zieglmayer, Ursula Petra (2009). "Azelastine nasal spray for the treatment of allergic and nonallergic rhinitis". Expert Review of Clinical Immunology 5 (6): 659–69. doi:10.1586/eci.09.38. PMID 20477689.
^ drugs.com Azelastine Page accessed June 28, 2015

External links

Rhinolast Nasal Spray Summary of Product Characteristics
Optilast Eye Drops Summary of Product Characteristics
Allergic Rhinitis and its Impact on Asthma (ARIA) Guidelines

UpToDate Contents

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1. 慢性非アレルギー性鼻炎 chronic nonallergic rhinitis
2. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis
3. アレルギー性結膜炎：マネージメント allergic conjunctivitis management
4. アトピー性角結膜炎 atopic keratoconjunctivitis
5. 職業性鼻炎 occupational rhinitis

English Journal

Safety evaluation of MP29-02 (a novel intranasal formulation of azelastine hydrochloride and fluticasone propionate) for allergic rhinitis.

Klimek L1,2,3, Jean B1,2,3, David P1,2,3.
Expert opinion on drug safety.Expert Opin Drug Saf.2015 Nov 19. [Epub ahead of print]
INTRODUCTION: As a chronic disease, allergic rhinitis (AR) requires regular use of allergy medications for the effective management of symptoms. It is therefore imperative that AR treatments not only provide adequate symptom control, but are also well-tolerated. Area covered: MP29-02 (Dymista, Meda,
PMID 26581312

Interactions between histamine H1 receptor and its antagonists by using cell membrane chromatography method.

Ma W1, Zhang D1, Li J1, Che D1, Liu R1, Zhang J1, Zhang Y1.
The Journal of pharmacy and pharmacology.J Pharm Pharmacol.2015 Nov;67(11):1567-74. doi: 10.1111/jphp.12453. Epub 2015 Jul 6.
OBJECTIVES: A high histamine H1 receptor (H1 R) expression cell membrane chromatography (CMC) method was developed to investigate the affinity of ligands for H1 R.METHODS: The affinity of ligands for H1 R was evaluated by frontal analysis. Competition studies and molecular docking study were utilize
PMID 26147217

Effects of azelastine nasal spray on nasal and nasopharyngeal microflora.

Aksoy F1, Senturk E1, Doğan R1, Veyseller B1, Ozturan O1, Gönüllü N2, Yilmaz F2.
The Journal of laryngology and otology.J Laryngol Otol.2015 Oct 30:1-5. [Epub ahead of print]
OBJECTIVE: Azelastine nasal spray is a topical antihistaminic drug for the symptomatic treatment of allergic rhinitis. This study aimed to investigate the effects of azelastine on nasal and nasopharyngeal microflora.METHODS: Swab samples from 25 patients prescribed azelastine nasal spray monotherapy
PMID 26515526

Japanese Journal

Inhibitory Effects of the Methanol Extract of Ganoderma lucidum on Mosquito Allergy-Induced Itch-Associated Responses in Mice

Andoh Tsugunobu,Zhang Qun,Yamamoto Takumi [他],Tayama Manabu,Hattori Masao,Tanaka Ken,Kuraishi Yasushi
Journal of Pharmacological Sciences 114(3), 292-297, 2010
… histamine–receptor antagonist azelastine, but not by the peripherally acting H1-antagonist terfenadine, at the oral dose of 30 mg/kg. …
NAID 130000439885

Intact Cell Binding for In Vitro Prediction of Sedative and Non-sedative Histamine H_1-Receptor Antagonists Based on Receptor Internalization

Hishinuma Shigeru,Sato Yuko,Kobayashi Yusuke [他],KOMAZAKI Hiroshi,SAITO Masaki
Journal of pharmacological sciences 107(1), 66-79, 2008-05-20
… Displacement curves for sedative H1-receptor antagonists (diphenhydramine, chlorpheniramine, promethazine, ketotifen, azelastine and oxatomide) against [3H]mepyramine binding were not changed by histamine pretreatment. …
NAID 10024320504

Azelastine hydrochloride on behavioral and psychological symptoms and activities of daily living in dementia patients

HATAKEYAMA Aiko,FUJII Masahiko,HATAKEYAMA Reiko,FUKUOKA Yumiko,SATOH NAKAGAWA Takuma,SASAKI Hidetada
Geriatrics & gerontology international 8(1), 59-61, 2008-03-01
NAID 10021252500

Related Pictures

Azelastine : Uses, Dosage, Side Effects, Interactions, & Contraindications - DoctorAlerts Azelastine Images and Labels - GoodRx Azelastine Nasal : Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD AZELASTINE HCL 0.05% DROPS - A - ALL Astelin | Bad Drug Astelin Images and Labels - GoodRx

★リンクテーブル★

リンク元	「アゼラスチン」
拡張検索	「azelastine hydrochloride」

「アゼラスチン」

Azelastine
Systematic (IUPAC) name
	(RS)-4-[(4-chlorophenyl)methyl]-2- (1-methylazepan-4-yl)-phthalazin-1-one
Clinical data
Trade names	Generic, many names.
AHFS/Drugs.com	monograph
MedlinePlus	a603009
Pregnancy; category	US: C (Risk not ruled out); ;
Legal status	UK: Pharmacy medicines; Rx Only (US);
Routes of; administration	intranasal, ocular
Pharmacokinetic data
Bioavailability	40% (intranasal)
Biological half-life	22 hours
Identifiers
CAS Number	58581-89-8
ATC code	R01AC03 R06AX19, S01GX07
PubChem	CID: 2267
IUPHAR/BPS	7121
DrugBank	DB00972
ChemSpider	2180
UNII	ZQI909440X
KEGG	D07483
ChEBI	CHEBI:2950
ChEMBL	CHEMBL639
Chemical data
Formula	C22H24ClN3O
Molecular mass	381.898 g/mol
	SMILES Clc1ccc(cc1)CC\3=N\N(C(=O)c2ccccc2/3)C4CCCN(C)CC4 ;
	InChI InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3 ; Key:MBUVEWMHONZEQD-UHFFFAOYSA-N ;
(verify)

　　[★]

英: azelastine
化: 塩酸アゼラスチン、アゼラスチン塩酸塩
商: アストプチン, アゼプチン, アドメッセン, ビフェルチン, ラスプジン、Astelin
関: 抗ヒスタミン薬、抗アレルギー薬。その他のアレルギー用薬

抗アレルギー薬

アレルギー性抗ヒスタミン薬

薬理作用

ヒスタミンH₁受容体拮抗作用。ヒスタミン遊離抑制。
ロイコトリエンに対する産生抑制。遊離抑制作用。拮抗作用。

「azelastine hydrochloride」

　　[★]

塩酸アゼラスチン

関: azelastine

[Names-1] Drugs.com Drugs.com international listings for azelastine Page accessed June 28, 2015

[AHRQ-2] AHRQ Allergic Rhinitis and its Impact on Asthma (ARIA) treatment guidelines

[Rhinolast_Nasal_Spray-3] "Rhinolast Nasal Spray Summary of Product Characteristics". Oct 2009. Retrieved 2010-04-27.

[Astelin_FDA_Prescribing_Information-4] "Astelin FDA Prescribing Information". Retrieved 2010-04-27.

[Optilast_Eye_Drops_Summary_of_Product_Characteristics-5] "Optilast Eye Drops Summary of Product Characteristics". Jan 2010. Retrieved 2010-04-27.

[Optivar_Eye_Drops_FDA_Prescribing_Information-6] "Optivar Eye Drops FDA Prescribing Information". Jan 2010. Retrieved 2010-04-27.

[7] McNeely, W; Wiseman, LR (July 1998). "Intranasal azelastine. A review of its efficacy in the management of allergic rhinitis.". Drugs 56 (1): 91–114. doi:10.2165/00003495-199856010-00011. PMID 9664202.

[Ratner_et_al.2C_1994-8] Ratner PH, Findlay SR, Hampel F, van Bavel J, Widlitz MD, Freitag JJ (November 1994). "A double-blind, controlled trial to assess the safety and efficacy of azelastine nasal spray in seasonal allergic rhinitis". The Journal of Allergy and Clinical Immunology 94 (5): 818–25. doi:10.1016/0091-6749(94)90148-1. PMID 7963150.

[LaForce_et_al.2C_1996-9] LaForce C, Dockhorn RJ, Prenner BM; et al. (February 1996). "Safety and efficacy of azelastine nasal spray (Astelin NS) for seasonal allergic rhinitis: a 4-week comparative multicenter trial". Annals of Allergy, Asthma & Immunology 76 (2): 181–8. doi:10.1016/S1081-1206(10)63420-5. PMID 8595539.

[Corren_et_al.2C_2005-10] Corren J, Storms W, Bernstein J, Berger W, Nayak A, Sacks H (May 2005). "Effectiveness of azelastine nasal spray compared with oral cetirizine in patients with seasonal allergic rhinitis". Clinical Therapeutics 27 (5): 543–53. doi:10.1016/j.clinthera.2005.04.012. PMID 15978303.

[Berger_et_al.2C_2006-11] Berger W, Hampel F, Bernstein J, Shah S, Sacks H, Meltzer EO (September 2006). "Impact of azelastine nasal spray on symptoms and quality of life compared with cetirizine oral tablets in patients with seasonal allergic rhinitis". Annals of Allergy, Asthma & Immunology 97 (3): 375–81. doi:10.1016/S1081-1206(10)60804-6. PMID 17042145.

[Horak_.26_Zieglmayer.2C_2009-12] Horak, Friedrich; Zieglmayer, Ursula Petra (2009). "Azelastine nasal spray for the treatment of allergic and nonallergic rhinitis". Expert Review of Clinical Immunology 5 (6): 659–69. doi:10.1586/eci.09.38. PMID 20477689.

[13] rugs.com Azelastine Page accessed June 28, 2015

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azelastine