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药品详细

Cetirizine(西替利嗪)

化学结构式图
中文名
西替利嗪
英文名
Cetirizine
分子式
C21H25ClN2O3
化学名
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
分子量
Average: 388.888
Monoisotopic: 388.155370383
CAS号
83881-51-0
ATC分类
R06A 未知;R06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects. [PubChem]

生产厂家
  • Actavis elizabeth llc
  • Actavis mid atlantic llc
  • Amneal pharmaceuticals
  • Amneal pharmaceuticals ny llc
  • Apotex inc
  • Aurobindo pharma ltd
  • Banner pharmacaps inc
  • Cadista pharmaceuticals inc
  • Caraco pharmaceutical laboratories ltd
  • Contract pharmacal corp
  • Cypress pharmaceutical inc
  • Dr reddys laboratories ltd
  • Mcneil consumer healthcare div mcneil ppc inc
  • Mylan pharmaceuticals inc
  • Orchid healthcare
  • Perrigo israel pharmaceuticals ltd
  • Perrigo r and d co
  • Pfizer inc
  • Ranbaxy laboratories ltd
  • Sandoz inc
  • Sun pharmaceutical industries inc
  • Taro pharmaceutical industries ltd
  • Teva pharmaceuticals usa
  • Torrent pharmaceuticals llc
  • Unichem laboratories ltd
  • Unique pharmaceutical laboratories
  • Vintage pharmaceuticals llc
  • Wockhardt ltd
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Diphenylmethanes
Substructures
  • Hydroxy Compounds
  • Acetates
  • Short-chain Hydroxy Acids
  • Piperazines
  • Ethers
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Carboxylic Acids and Derivatives
  • Aliphatic and Aryl Amines
  • Diphenylmethanes
  • Heterocyclic compounds
  • Aromatic compounds
适应症
药理
Indication For the relief of symptoms associated with seasonal allergic rhinitis, perennial allergic rhinitis and the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria
Pharmacodynamics Cetirizine, the active metabolite of the piperazine H1-receptor antagonist hydroxyzine, is used to treat chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis.
Mechanism of action Cetirizine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The low incidence of sedation can be attributed to reduced penetration of cetirizine into the CNS as a result of the less lipophilic carboxyl group on the ethylamine side chain.
Absorption mean peak plasma concentration (Cmax) of 114 ng/mL at a time (Tmax) of 2.2 hours postdose was observed for cetirizine
Volume of distribution Not Available
Protein binding Very high (93%) plasma protein binding
Metabolism
Not Available
Route of elimination Not Available
Half life 8.3 hours
Clearance
  • 53 mL/min [healthy]
Toxicity Somnolence (sleepiness or unusual drowsiness), restlessness, irritability
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 112.5 °C PhysProp
water solubility 101 mg/L Not Available
logP 2.8 Not Available
Predicted Properties
Property Value Source
water solubility 6.58e-02 g/l ALOGPS
logP 2.98 ALOGPS
logP 0.86 ChemAxon
logS -3.8 ALOGPS
pKa (strongest acidic) 3.6 ChemAxon
pKa (strongest basic) 7.79 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 53.01 ChemAxon
rotatable bond count 8 ChemAxon
refractivity 106.87 ChemAxon
polarizability 41.88 ChemAxon
药物相互作用
食物相互作用
  • Avoid alcohol.
  • Take without regard to meals.

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