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药品详细

Bromodiphenhydramine(溴二苯羟基胺)

化学结构式图
中文名
溴二苯羟基胺
英文名
Bromodiphenhydramine
分子式
C17H20BrNO
化学名
{2-[(4-bromophenyl)(phenyl)methoxy]ethyl}dimethylamine
分子量
Average: 334.251
Monoisotopic: 333.072826914
CAS号
1808-12-4
ATC分类
D04A 未知;D04A 未知;R06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Bromodiphenhydramine is an ethanolamine antihistamine with antimicrobial property. Bromodiphenhydramine is used in the control of cutaneous allergies. Ethanolamine antihistamines produce marked sedation in most patients

生产厂家
  • Parke davis div warner lambert co
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
  • Diphenhydramines
Substructures
  • Diphenhydramines
  • Benzyl Alcohols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Aryl Halides
  • Diphenylmethanes
  • Aromatic compounds
  • Halobenzenes
适应症
药理
Indication For management of symptoms related to hay fever and other types of allergy and used to help bring up phlegm, thin secretions, and make a cough productive.
Pharmacodynamics Bromodiphenhydramine is an 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, Bromodiphenhydramine competes with free histamine for binding at HA-receptor sites. Bromodiphenhydramine 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 Bromodiphenhydramine. This 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.
Mechanism of action Bromodiphenhydramine 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.
Absorption Well absorbed in the digestive tract.
Volume of distribution Not Available
Protein binding 96%
Metabolism
Hepatic (cytochrome P-450 system); some renal.
Route of elimination Not Available
Half life 1 to 4 hours
Clearance Not Available
Toxicity Signs of overdose include wheezing, tightness in the chest, fever, itching, bad cough, blue skin color, fits, swelling of face, lips, tongue, or throat.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 4 Not Available
Predicted Properties
Property Value Source
water solubility 3.45e-03 g/l ALOGPS
logP 4.16 ALOGPS
logP 4.42 ChemAxon
logS -5 ALOGPS
pKa (strongest basic) 8.87 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 87.55 ChemAxon
polarizability 33.48 ChemAxon
药物相互作用
Drug Interaction
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Bromodiphenhydramine, 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 Bromodiphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Bromodiphenhydramine, 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 Bromodiphenhydramine, 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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