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药品详细

Olopatadine(奥洛他定)

化学结构式图
中文名
奥洛他定
英文名
Olopatadine
分子式
C21H23NO3
化学名
2-[(2Z)-2-[3-(dimethylamino)propylidene]-9-oxatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-5-yl]acetic acid
分子量
Average: 337.4122
Monoisotopic: 337.167793607
CAS号
113806-05-6
ATC分类
S01G 解充血药及抗过敏药;R01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Used to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells.

生产厂家
  • Alcon inc
  • Alcon laboratories inc
  • Alcon Laboratories, Inc.
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, Mukouyama A: Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol. 2002 Apr;88(4):379-97. Pubmed
  2. Yanni JM, Stephens DJ, Miller ST, Weimer LK, Graff G, Parnell D, Lang LS, Spellman JM, Brady MT, Gamache DA: The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther. 1996 Winter;12(4):389-400. Pubmed
  3. Ohmori K, Hasegawa K, Tamura T, Miyake K, Matsubara M, Masaki S, Karasawa A, Urayama N, Horikoshi K, Kajita J, Hasegawa M, Taniguchi K, Komada T, Kawamoto Y: Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. Arzneimittelforschung. 2004;54(12):809-29. Pubmed
  4. Ohmori K, Ikemura T, Kobayashi H, Mukouyama A: [Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride’ (olopatadine), an antiallergic drug] Nippon Yakurigaku Zasshi. 2001 Jul;118(1):51-8. Pubmed
  5. Kaliner MA, Oppenheimer J, Farrar JR: Comprehensive review of olopatadine: the molecule and its clinical entities. Allergy Asthma Proc. 2010 Mar;31(2):112-9. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenylpropenes
  • Phenylacetates
Substructures
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Benzyl Alcohols and Derivatives
  • Acetates
  • Phenols and Derivatives
  • Carboxylic Acids and Derivatives
  • Phenylpropenes
  • Phenylacetates
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Isoprenes
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Phenyl Esters
适应症
药理
Indication For the treatment of ocular itching associated with allergic conjunctivitis.
Pharmacodynamics Used to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells.
Mechanism of action Olopatadine is a selective histamine H1 antagonist that binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Olopatadine is devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors.
Absorption Ophthalmic use of olopatadine usually does not produce measurable plasma concentrations.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
The mono-desmethyl and the N-oxide metabolites have been detected at low concentrations in the urine.

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

Substrate Enzymes Product
Olopatadine
    		Mono-desmethyl olopatadine Details
    Olopatadine
      		Olopatadine n-oxide Details
      Route of elimination Elimination was predominantly through renal excretion.
      Half life 3 hours
      Clearance Not Available
      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 248 °C Not Available
      water solubility Soluble Not Available
      logP 3.4 Not Available
      Predicted Properties
      Property Value Source
      water solubility 3.13e-02 g/l ALOGPS
      logP 3.99 ALOGPS
      logP 0.75 ChemAxon
      logS -4 ALOGPS
      pKa (strongest acidic) 3.78 ChemAxon
      pKa (strongest basic) 9.76 ChemAxon
      physiological charge 0 ChemAxon
      hydrogen acceptor count 4 ChemAxon
      hydrogen donor count 1 ChemAxon
      polar surface area 49.77 ChemAxon
      rotatable bond count 5 ChemAxon
      refractivity 109.55 ChemAxon
      polarizability 37.44 ChemAxon
      药物相互作用
      食物相互作用
      Not Available

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