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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/30 00:33:38」(JST)

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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

Computational and experimental investigation of DNA repair protein photolyase interactions with low molecular weight drugs.

Azizoğlu S, Kizilel R, Marušič M, Kavakli IH, Erman B, Kizilel S.SourceKoç University, College of Engineering, Chemical and Biological Engineering, Istanbul, 34450, Turkey.
Journal of molecular recognition : JMR.J Mol Recognit.2013 Jul;26(7):297-307. doi: 10.1002/jmr.2258.
This paper reports the previously unknown interactions between eight low molecular weight commercially available drugs (130-800 Da) and DNA repair protein photolyase using computational docking simulations and surface plasmon resonance (SPR) experiments. Theoretical dissociation constants, Kd , ob
PMID 23657985

A clinical pharmacokinetic study comparing two azelastine hydrochloride nasal formulations in a single-dose design.

Du D, Targett D, Stolberg E, Canali A.SourceMedical Affairs, GSK Consumer Healthcare, 1500 Littleton Rd, Parsippany, NJ, 07054, USA, daniel.y.du@gsk.com.
European journal of drug metabolism and pharmacokinetics.Eur J Drug Metab Pharmacokinet.2013 May 17. [Epub ahead of print]
Azelastine hydrochloride is a potent second-generation antihistamine, available in Europe and the USA as a nasal spray formulation for the treatment of allergic rhinitis symptoms. GlaxoSmithKline (GSK) Consumer Healthcare has developed a new nasal formulation of azelastine hydrochloride. The present
PMID 23681835

Clinically Relevant Effect of a New Intranasal Therapy (MP29-02) in Allergic Rhinitis Assessed by Responder Analysis.

Meltzer E, Ratner P, Bachert C, Carr W, Berger W, Canonica GW, Hadley J, Lieberman P, Hampel FC, Mullol J, Munzel U, Price D, Scadding G, Virchow JC, Wahn U, Murray R, Bousquet J.SourceAllergy and Asthma Medical Group and Research Center, San Diego, Calif., USA.
International archives of allergy and immunology.Int Arch Allergy Immunol.2013 May 4;161(4):369-377. [Epub ahead of print]
Background: It is unclear what constitutes a clinically meaningful response for allergic rhinitis (AR) outcomes. The objectives of these post hoc analyses were (1) to define a clinically meaningful response using novel efficacy analyses (including a responder analysis), and (2) to compare the effica
PMID 23652808

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★リンクテーブル★

リンク元

「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
Molar 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 ;
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　　[★]

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。

[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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Astelin