Betahistine

Betahistine
ATC Code N07CA01
Formula C8H12N2
Molar Mass (g·mol−1) 136,19
Physical State solid
Density (g·cm−3) 0,98
Melting Point (°C) 113–114
PKS Value 3,5
CAS Number 5638-76-6
PUB Number 2366
Drugbank ID DB06698
Solubility sparingly soluble in water

Basics

Betahistine is a drug used to treat vertigo. It is often prescribed for balance disorders or to relieve symptoms of vertigo, such as those associated with Ménière's disease. It was first approved in Europe in 1970 for the treatment of Ménière's disease. Betahistine is a histamine analogue.

Pharmacology

Pharmacodynamics

Betahistine has two mechanisms of action. Primarily, it is a weak agonist at H1 receptors located on blood vessels in the inner ear. Stimulation of H1 receptors in the inner ear causes vasodilation, which leads to increased blood vessel permeability and a reduction in endolymphatic pressure; this action prevents rupture of the labyrinth, which may contribute to the hearing loss associated with Ménière's disease. Betahistine also acts by reducing asymmetric vestibular sensory function and increasing vestibulocochlear blood flow, which relieves symptoms of vertigo. In addition, betahistine also acts as a histamine H3 receptor antagonist by increasing the turnover of histamine from postsynaptic histaminergic nerve receptors, which subsequently leads to an increase in H1 agonist activity.

Pharmacokinetics

Betahistine is available in both tablet and solution form and is taken orally. It is rapidly and completely absorbed. The mean plasma elimination half-life is 3 to 4 hours, and excretion is virtually complete in the urine within 24 hours. Plasma protein binding is very low. Betahistine is converted to aminoethylpyridine and hydroxyethylpyridine in the liver and excreted in the urine as pyridylacetic acid.

Toxicity

Side effects

Patients taking betahistine may experience the following side effects:

  • Headache
  • Minor side effects in the gastrointestinal tract
  • Nausea
  • Hypersensitivity and allergic reactions

Hypersensitivity reactions resolve quickly after betahistine is stopped.

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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