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药品详细

Clemastine(氯马斯汀)

化学结构式图
中文名
氯马斯汀
英文名
Clemastine
分子式
C21H26ClNO
化学名
(2R)-2-{2-[(1R)-1-(4-chlorophenyl)-1-phenylethoxy]ethyl}-1-methylpyrrolidine
分子量
Average: 343.89
Monoisotopic: 343.170292166
CAS号
15686-51-8
ATC分类
R06A 未知;D04A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

An ethanolamine-derivative, first generation histamine H1 antagonist used in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness. [PubChem]

生产厂家
  • Actavis mid atlantic llc
  • Novartis pharmaceuticals corp
  • Novex pharma
  • Perrigo co
  • Sandoz inc
  • Silarx pharmaceuticals inc
  • Teva pharmaceuticals usa
  • Teva pharmaceuticals usa inc
  • Wockhardt eu operations (swiss) ag
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Hayashi H, Okajima M, Yamada K: Atrial T (Ta) loop in dogs with or without atrial injury. Am Heart J. 1976 May;91(5):607-17. Pubmed
  2. Schran HF, Petryk L, Chang CT, O’Connor R, Gelbert MB: The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations. J Clin Pharmacol. 1996 Oct;36(10):911-22. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Diphenhydramines
Substructures
  • Diphenhydramines
  • Benzyl Alcohols and Derivatives
  • Pyrrolidines
  • Ethers
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Aliphatic and Aryl Amines
  • Diphenylmethanes
  • Heterocyclic compounds
  • Aromatic compounds
适应症
药理
Indication For the relief of symptoms associated with allergic rhinitis such as sneezing, rhinorrhea, pruritus and acrimation. Also for the management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Used as self-medication for temporary relief of symptoms associated with the common cold.
Pharmacodynamics Clemastine is an antihistamine with anticholinergic (drying) and sedative side effects. Antihistamines competitively antagonize various physiological effects of histamine including increased capillary permeability and dilatation, the formation of edema, the "flare" and "itch" response, and gastrointestinal and respiratory smooth muscle constriction. Within the vascular tree, H1- receptor antagonists inhibit both the vasoconstrictor and vasodilator effects of histamine. Depending on the dose, H1- receptor antagonists can produce CNS stimulation or depression. Most antihistamines exhibit central and/or peripheral anticholinergic activity. Antihistamines act by competitively blocking H1- receptor sites. Antihistamines do not pharmacologically antagonize or chemically inactivate histamine, nor do they prevent the release of histamine.
Mechanism of action Clemastine is a selective histamine H1 antagonist and 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.
Absorption Rapidly absorbed from the gastrointestinal tract.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Antihistamines appear to be metabolized in the liver chiefly via mono- and didemethylation and glucuronide conjugation.
Route of elimination Urinary excretion is the major mode of elimination.
Half life Not Available
Clearance Not Available
Toxicity Oral LD50 in rat and mouse is 3550 mg/kg and 730 mg/kg, respectively. Antihistamine overdosage reactions may vary from central nervous system depression to stimulation. In children, stimulation predominates initially in a syndrome which may include excitement, hallucinations, ataxia, incoordination, muscle twitching, athetosis, hyperthermia, cyanosis convulsions, tremors, and hyperreflexia followed by postictal depression and cardio-respiratory arrest. Convulsions in children may be preceded by mild depression. Dry mouth, fixed dilated pupils, flushing of the face, and fever are common. In adults, CNS depression, ranging from drowsiness to coma, is more common.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 178 °C (hydrogen fumarate formulation) Not Available
water solubility Soluble (hydrogen fumarate formulation) Not Available
logP 5.2 Not Available
Predicted Properties
Property Value Source
water solubility 4.05e-04 g/l ALOGPS
logP 5.29 ALOGPS
logP 4.92 ChemAxon
logS -5.9 ALOGPS
pKa (strongest basic) 9.55 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 12.47 ChemAxon
rotatable bond count 6 ChemAxon
refractivity 101.65 ChemAxon
polarizability 39.06 ChemAxon
药物相互作用
Drug Interaction
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Rivastigmine Possible antagonism of action
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Clemastine, 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 Clemastine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Concomitant therapy with triprolidine and clemastine, 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 Clemastine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
食物相互作用
  • Avoid alcohol.
  • Take with food.

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