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药品详细

Tripelennamine(曲吡那敏)

化学结构式图
中文名
曲吡那敏
英文名
Tripelennamine
分子式
C16H21N3
化学名
N-benzyl-N-[2-(dimethylamino)ethyl]pyridin-2-amine
分子量
Average: 255.358
Monoisotopic: 255.173547687
CAS号
91-81-6
ATC分类
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

A histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation. It is used to treat asthma; HAY fever; urticaria; and rhinitis; and also in veterinary applications. Tripelennamine is administered by various routes, including topically. [PubChem]

生产厂家
  • Anabolic inc
  • Barr laboratories inc
  • Heather drug co inc
  • Impax laboratories inc
  • Lannett co inc
  • Novartis pharmaceuticals corp
  • Nylos trading co inc
  • Parke davis div warner lambert co
  • Watson laboratories inc
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
  • Pyridines and Derivatives
  • Benzene and Derivatives
  • Aminopyridines and Derivatives
Substructures
  • Aliphatic and Aryl Amines
  • Pyridines and Derivatives
  • Benzene and Derivatives
  • Aminopyridines and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
适应症
药理
Indication Used for the symptomatic relief of hypersensitivity reactions, coughs, and the common cold.
Pharmacodynamics Used to treat the effects of colds and allergies. Tripelennamine is an antihistamine. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Tripelennamine is a histamine H1 antagonist. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. 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 Tripelennamine 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 Well absorbed in the digestive tract.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hepatic
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Symptoms of overdose include clumsiness or unsteadiness, convulsions, drowsiness, dryness of mouth, nose, or throat, feeling faint, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath or troubled breathing, shuffling walk, tic-like movements of head and face, trembling and shaking of hands and trouble in sleeping.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility 587 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 3.3 Not Available
logS -2.64 ADME Research, USCD
Predicted Properties
Property Value Source
water solubility 2.84e+00 g/l ALOGPS
logP 3.05 ALOGPS
logP 3.2 ChemAxon
logS -1.9 ALOGPS
pKa (strongest basic) 8.76 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 19.37 ChemAxon
rotatable bond count 6 ChemAxon
refractivity 81.27 ChemAxon
polarizability 29.86 ChemAxon
药物相互作用
Drug Interaction
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
食物相互作用
Not Available

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