azelastine hydrochloride

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azelastine

WordNet

1. a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/14 22:13:03」(JST)

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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 Y
ATC code	R01AC03 R06AX19, S01GX07
PubChem	CID 2267
IUPHAR/BPS	7121
DrugBank	DB00972 Y
ChemSpider	2180 Y
UNII	ZQI909440X Y
KEGG	D07483 Y
ChEBI	CHEBI:2950 Y
ChEMBL	CHEMBL639 Y
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 Y Key:MBUVEWMHONZEQD-UHFFFAOYSA-N Y
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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.

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. In some countries, it is also indicated for the treatment of vasomotor rhinitis in adults and children ≥ 12 years old. Azelastine eyes drops are indicated for the local treatment of seasonal and perennial allergic conjunctivitis.

Side effects

Azelastine is safe and well tolerated in both adults and children with allergic rhinitis. 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 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.

Mode of action

Azelastine has a triple mode of action:

1. Anti-histamine effect,
2. Mast-cell stabilizing effect and
3. 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.

Society and culture

Availability

Azelastine is generic and available worldwide under many brand names.

References

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

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 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. 春季カタル vernal keratoconjunctivitis
• 5. アトピー性角結膜炎 atopic keratoconjunctivitis

English Journal

• Unique immunomodulatory effects of azelastine on dendritic cells in vitro.

• Schumacher S1, Kietzmann M, Stark H, Bäumer W.
• Naunyn-Schmiedeberg's archives of pharmacology.Naunyn Schmiedebergs Arch Pharmacol.2014 Nov;387(11):1091-9. doi: 10.1007/s00210-014-1033-x. Epub 2014 Aug 15.
• Allergic contact dermatitis and atopic dermatitis are among the most common inflammatory skin diseases in western countries, and antigen-presenting cells like dendritic cells (DC) are key players in their pathophysiology. Histamine, an important mediator of allergic reactions, influences DC maturati
• PMID 25119779

• Design and characterization of chitosan-alginate microspheres for ocular delivery of azelastine.

• Shinde UA1, Shete JN, Nair HA, Singh KH.
• Pharmaceutical development and technology.Pharm Dev Technol.2014 Nov;19(7):813-23. doi: 10.3109/10837450.2013.836217. Epub 2013 Sep 13.
• The use of mucoadhesive biopolymers is one of the best approaches to prolong the drug residence inside the cul-de-sac, consequently increasing the bioavailability. Thus, the focus of this work was to develop mucoadhesive microspheres to overcome the limitations of ocular drug delivery. The chitosan-
• PMID 24032373

• Complication prevalence following use of tutoplast-derived human acellular dermal matrix in prosthetic breast reconstruction: a retrospective review of 203 patients.

• Rundell VL1, Beck RT1, Wang CE2, Gutowski KA3, Sisco M1, Fenner G1, Howard MA4.
• Journal of plastic, reconstructive & aesthetic surgery : JPRAS.J Plast Reconstr Aesthet Surg.2014 Oct;67(10):1345-51. doi: 10.1016/j.bjps.2014.05.032. Epub 2014 May 28.
• Use of human acellular dermal matrix (ADM) during prosthetic breast reconstruction has increased. Several ADM products are available produced by differing manufacturing techniques. It is not known if outcomes vary with different products. This study reports the complication prevalence following use
• PMID 24917371

Japanese Journal

• 新一般用医薬品の製造販売後調査結果と適正使用のための情報提供

• 和田 義男,森 義高,岩渕 令子,井上 法子,滝田 諭,大村 和也,宇田 恒信
• 医薬品情報学 12(4), 168-172, 2011
• … To investigate frequency of adverse drug reactions (ADR) on HIGURD ®, a switch OTC product of azelastine hydrochloride, in a three-year post-marketing surveillance study.Methods: We conducted two surveys in this study a solicited survey with a questionnaire and a survey of spontaneous ADR reports.Results: A total of 183 cases with 293 ADRs were reported in the solicited survey on 3,453 consumers and a total of 29 cases with 37 ADRs were reported from spontaneous sources.  No serious ADRs were reported.  Most …
• NAID 130004551347

• 難治性口腔咽頭潰瘍の５症例

• 松尾 美央子
• 口腔・咽頭科 22(2), 103-107, 2009
• 難治性口腔咽頭潰瘍は比較的最近の概念である. 本疾患は, 口腔咽頭領域にできる潰瘍病変で, 治療抵抗性であり, 再発傾向をもつ. この病気は診断に苦慮することが多く, 今回報告する5例とも診断までは最低2ヶ月を要している. 今回我々は難治性口腔咽頭潰瘍に対し, ステロイド, コルヒチン, セファランチン, 塩酸アゼラスチンを使用することで, 速やかな症状の改善を得られたためこれを報告する.
• NAID 130004553077

• 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 Links

• Azelastine - Wikipedia, the free encyclopedia

Spangler DL, Bensch G, Berdy GJ (August 2001). "Evaluation of the efficacy of olopatadine hydrochloride 0.1% ophthalmic solution and azelastine hydrochloride 0.05% ophthalmic solution in the conjunctival allergen challenge model".

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