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药品详细

Brompheniramine(溴苯那敏)

化学结构式图
中文名
溴苯那敏
英文名
Brompheniramine
分子式
C16H19BrN2
化学名
[3-(4-bromophenyl)-3-(pyridin-2-yl)propyl]dimethylamine
分子量
Average: 319.239
Monoisotopic: 318.073161265
CAS号
86-22-6
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

Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria. [PubChem]

生产厂家
  • Alpharma us pharmaceuticals division
  • Barr laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Kv pharmaceutical co
  • Newtron pharmaceuticals inc
  • Nexgen pharma inc
  • Par pharmaceutical inc
  • Pharmaceutical assoc inc div beach products
  • Pioneer pharmaceuticals inc
  • Sandoz inc
  • Usl pharma inc
  • Vitarine pharmaceuticals inc
  • Watson laboratories inc
  • Wyeth ayerst laboratories
  • Wyeth consumer healthcare
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
  • Pheniramines
Substructures
  • Pheniramines
  • Pyridines and Derivatives
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Aryl Halides
  • Heterocyclic compounds
  • Aromatic compounds
  • Phenylpropylamines
  • Imines
  • Halobenzenes
适应症
药理
Indication For the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing.
Pharmacodynamics Brompheniramine is an antihistaminergic medication of the propylamine class. It is a first-generation antihistamine. In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Brompheniramine is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Mechanism of action Brompheniramine works by acting as an antagonist of the H1 histamine receptors. It also functions as a moderately effective anticholingeric agent, likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine. Its effects on the cholinergic system may include side-effects such as drowsiness, sedation, dry mouth, dry throat, blurred vision, and increased heart rate.
Absorption Antihistamines are well absorbed from the gastrointestinal tract after oral administration.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hepatic (cytochrome P-450 system), some renal.
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Oral, rat: LD50 = 318 mg/kg. Signs of overdose include fast or irregular heartbeat, mental or mood changes, tightness in the chest, and unusual tiredness or weakness.
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 149.5 °C at 5.00E-01 mm Hg PhysProp
water solubility Freely soluble (maleate salt) Not Available
logP 3.4 Not Available
Predicted Properties
Property Value Source
water solubility 1.27e-02 g/l ALOGPS
logP 3.63 ALOGPS
logP 3.75 ChemAxon
logS -4.4 ALOGPS
pKa (strongest basic) 9.48 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 16.13 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 83.67 ChemAxon
polarizability 32.08 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, Brompheniramine, 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 Brompheniramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Brompheniramine, 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 Brompheniramine, 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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