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药品详细

Betahistine(倍他司汀)

化学结构式图
中文名
倍他司汀
英文名
Betahistine
分子式
C8H12N2
化学名
methyl[2-(pyridin-2-yl)ethyl]amine
分子量
Average: 136.1943
Monoisotopic: 136.100048394
CAS号
5638-76-6
ATC分类
N07C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Betahistine is an antivertigo drug first used for treating vertigo assosicated with Ménière’s disease. It is also commonly used for patients with balance disorders.

生产厂家
  • Abbott products inc
  • Teva Pharmaceuticals
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Health Canada
剂型
规格
化合物类型
Type small molecule
Classes
  • Pyridines and Derivatives
Substructures
  • Aliphatic and Aryl Amines
  • Pyridines and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Imines
适应症
药理
Indication For the reduction of episodes of vertigo association with Ménière's disease.
Pharmacodynamics Betahistine primarily acts as a histamine H1-agonist with 0.07 times the activity of histamine. Stimulating the H1-receptors in the inner ear causes a vasodilatory effect and increased permeability in the blood vessels which results in reduced endolymphatic pressure. Betahistine is believed to act by reducing the asymmetrical functioning of sensory vestibular organs as well as by increasing vestibulocochlear blood flow. Doing so aids in decreasing symptoms of vertigo and balance disorders. Betahistine also acts as a histamine H3-receptor antagonist which causes an increased output of histamine from histaminergic nerve endings which can further increase the direct H1-agonist activity. Furthermore, H3-receptor antagonism increases the levels of neurotransmitters such as serotonin in the brainstem, which inhibits the activity of vestibular nuclei, helping to restore proper balance and decrease in vertigo symptoms.
Mechanism of action Not Available
Absorption When given orally, betahistine is rapidly absorbed from the gastrointestinal tract.
Volume of distribution Not Available
Protein binding Very low.
Metabolism
Betahistine is metabolized primarily into 2-pyridylacetic acid and is subsequently excreted in the urine.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Betahistine
    		2-pyridylacetic acid Details
    Route of elimination Renal
    Half life 3-4 hours
    Clearance Not Available
    Toxicity Symptoms of overdose (< 640 mg) include mild to moderate nausea, dry mouth, dyspepsia, abdominal pain and somnolence. More serious complications such as convulsions, pulmonary or cardiac complications, may occur with higher intentional overdoses (> 640 mg).
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    logP 0.68 YOUNG,RC ET AL. (1993)
    pKa 10.1 (at 10 °C) PERRIN,DD (1965)
    Predicted Properties
    Property Value Source
    water solubility 4.93e+01 g/l ALOGPS
    logP 0.59 ALOGPS
    logP 0.63 ChemAxon
    logS -0.44 ALOGPS
    pKa (strongest basic) 9.77 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 2 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 24.92 ChemAxon
    rotatable bond count 3 ChemAxon
    refractivity 41.33 ChemAxon
    polarizability 15.85 ChemAxon
    药物相互作用
    食物相互作用
    • Take with food.

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