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药品详细

Azelastine(氮卓斯汀)

化学结构式图
中文名
氮卓斯汀
英文名
Azelastine
分子式
C22H24ClN3O
化学名
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one
分子量
Average: 381.898
Monoisotopic: 381.160790112
CAS号
58581-89-8
ATC分类
R01A 未知;R06A 未知;S01G 解充血药及抗过敏药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista™. Dymista™ is indicated in patient over 12 years old for symptomatic relief of seasonal allergic rhinitis.

生产厂家
  • Apotex inc
  • Apotex inc richmond hill
  • Meda Pharmaceuticals
  • Meda pharmaceuticals inc
  • Meda pharmaceuticals meda pharmaceuticals inc
  • Sun pharma global fze
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Horak F: Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis. Ther Clin Risk Manag. 2008 Oct;4(5):1009-22. Pubmed
  2. Bernstein JA: Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Curr Med Res Opin. 2007 Oct;23(10):2441-52. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phthalazines
Substructures
  • Phthalazines
  • Benzene and Derivatives
  • Aryl Halides
  • Pyridazines
  • Halobenzenes
  • Aliphatic and Aryl Amines
  • Heterocyclic compounds
  • Aromatic compounds
  • Imines
适应症
药理
Indication For the symptomatic treatment of seasonal allergic rhinitis and non-allergic rhinitis, as well as symptomatic relief of ocular itching associated with allergic conjunctivitis.
Pharmacodynamics Azelastine is a relatively selective histamine H1 antagonist, which inhibits the release of histamine and other mediators from cells (e.g. mast cells) involved in the allergic response. It has some affinity to H2 receptors. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g. leukotrienes and PAF) has been demonstrated with azelastine. Azelastine may also inhibit the accumulation and degranulation of eosinophils at the site of allergic inflammation.
Mechanism of action Azelastine competes with histamine for the H1-receptor sites on effector cells and acts as an antagonist by inhibiting the release of histamine and other mediators involved in the allergic response.
Absorption Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration.
Volume of distribution
  • 14.5 L/kg
Protein binding In-vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97%, respectively.
Metabolism
Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Azelastine
Desmethylazelastine Details
Route of elimination Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system.
Half life Elimination half-life (based on intravenous and oral administration) is 22 hours. Elimination half-life of the active metabolite, desmethylazelastine, is 54 hours (after oral administration of azelastine).
Clearance
  • 0.5 L/h/kg [symptomatic patients]
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 225 °C (hydrochloride salt) Not Available
water solubility Sparingly soluble (hydrochloride salt) Not Available
logP 4.9 Not Available
Predicted Properties
Property Value Source
water solubility 9.20e-03 g/l ALOGPS
logP 3.81 ALOGPS
logP 4.04 ChemAxon
logS -4.6 ALOGPS
pKa (strongest basic) 8.88 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 35.91 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 110.52 ChemAxon
polarizability 41.54 ChemAxon
药物相互作用
Drug Interaction
Dihydrocodeine Enhanced CNS depressant effects contraindicates concurrent use.
gabapentin enacarbil Avoid combination due to increased CNS depression.
Perampanel Avoid combination with azelastine or other CNS depressants due to the combined increase of CNS depression.
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Azelastine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Trimethobenzamide Trimethobenzamide and Azelastine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Concomitant therapy with triprolidine and azelastine, two anticholinergics and CNS depressants, may result in additive adverse/toxic effects. Monitor for enhanced anticholinergic and CNS depressant effects during concomitant therapy.
Trospium Trospium and Azelastine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
食物相互作用
Not Available

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