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药品详细

Carbinoxamine(卡比沙明)

化学结构式图
中文名
卡比沙明
英文名
Carbinoxamine
分子式
C16H19ClN2O
化学名
{2-[(4-chlorophenyl)(pyridin-2-yl)methoxy]ethyl}dimethylamine
分子量
Average: 290.788
Monoisotopic: 290.118590947
CAS号
486-16-8
ATC分类
R06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Carbinoxamine is a first generation antihistamine that competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. The product label for carbinoxamine as an over the counter cough and cold medicine is being modified to state “do not use” in children under 4 years of age in order to prevent and reduce misuse, as many unapproved carbinoxamine-containing preparations contained inappropriate labeling, which promoted unapproved uses (including management of congestion, cough, the common cold, and the use in children under 2 years of age), which can potentially cause serious health risks.

生产厂家
  • Boca pharmacal inc
  • Cypress pharmaceutical inc
  • Invagen pharmaceuticals inc
  • Mcneil pharmaceutical co div mcneilab inc
  • Mikart inc
  • Ortho mcneil pharmaceutical inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. BEALE HD, RAWLING FF, FIGLEY KD: Clistin maleate; a clinical appraisal of a new antihistaminic. J Allergy. 1954 Nov;25(6):521-4. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Diphenhydramines
Substructures
  • Diphenhydramines
  • Benzyl Alcohols and Derivatives
  • Pyridines and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Aliphatic and Aryl Amines
  • Heterocyclic compounds
  • Aromatic compounds
  • Imines
适应症
药理
Indication For symptomatic relief of seasonal and perennial allergic rhinitis and vasomotor rhinitis, as well as allergic conjunctivitis caused by foods and inhaled allergens. Also for the relief of allergic reactions to blood or plasma, and the symptomatic management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.
Pharmacodynamics Carbinoxamine is a first generation antihistamine of the ethanolamine class. Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease. Rather than preventing the release of histamine, as do cromolyn and nedocromil, carbinoxamine competes with free histamine for binding at HA-receptor sites. Carbinoxamine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Ethanolamine derivatives have greater anticholinergic activity than do other antihistamines, which probably accounts for the antidyskinetic action of carbinoxamine.
Mechanism of action Carbinoxamine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Carbinoxamine's anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life 10 to 20 hours
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Experimental Properties
Property Value Source
melting point < 25 °C PhysProp
boiling point 160 °C at 1.00E-01 mm Hg PhysProp
logP 2.6 Not Available
Predicted Properties
Property Value Source
water solubility 2.28e-01 g/l ALOGPS
logP 3.03 ALOGPS
logP 3.27 ChemAxon
logS -3.1 ALOGPS
pKa (strongest basic) 8.87 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 25.36 ChemAxon
rotatable bond count 6 ChemAxon
refractivity 82.13 ChemAxon
polarizability 31.7 ChemAxon
药物相互作用
Drug Interaction
Benzylpenicilloyl Polylysine Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Treatment with systemic histamine H1 antagonists such as carbinoxamine should be suspended for benzylpenicilloyl-polylysine skin testing to minimize the potential for false negative results. Delay skin testing until the systemic effects of the antihistamine have dissipated. A histamine skin test may be used to assess residual antihistaminic effects.
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Pramlintide Pramlintide may enhance the anticholinergic effect of Anticholinergics such as carbinoxamine. These effects are specific to the gastrointestinal tract. Use caution during concomitant therapy with pramlintide and anticholinergics. Additive effects on reduced gastrointestinal motility may occur.
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Carbinoxamine, 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 Carbinoxamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Carbinoxamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Trospium Trospium and Carbinoxamine, 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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