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Chemical Compound Review

Aequamen     N-methyl-2-pyridin-2-yl- ethanamine

Synonyms: Mersilon, Ribrain, Vasomotal, Betaistina, betahistine, ...
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Disease relevance of Vasomotal

  • To test the effectiveness of betahistine HC1 in reducing the frequency of transient ischemic attacks (TIAs) caused by vertebral-basilar artery insufficiency, we randomly assigned 26 patients with a typical history of the condition to a placebo-drug or a drug-placebo sequence, each sequence lasting two months [1].
  • In Ménière's disease treatment strategies range from low-salt diet, diuretics, and betahistine, to intratympanic injection of corticosteroids or gentamicin [2].
  • Betahistine is a structural analogue of histamine that is prescribed for the treatment of vestibular disorders such as M??ni??re's disease and the symptomatic treatment of vertigo [3].
  • A clinical intolerance to betahistine that gave rise to asthma or bronchospasm was only reported in eight ADRs [3].
  • In this review we analyse the safety profile of betahistine based on data obtained during >35 years of worldwide postmarketing surveillance.Until 31 December 2005, 554 adverse drug reaction (ADR) reports with 994 individual signs and symptoms were received by the marketing authorisation holder from worldwide sources and were reviewed and evaluated [3].

Psychiatry related information on Vasomotal


High impact information on Vasomotal


Chemical compound and disease context of Vasomotal


Biological context of Vasomotal


Anatomical context of Vasomotal

  • 2-Methylhistamine, N alpha,N alpha-dimethylhistamine and betahistine were partial agonists in both cerebellum and cerebral cortex, but all produced a greater percentage of the maximum response to histamine in cerebellar slices [17].
  • The present data show that the inhibitory action of the afferent neurons discharge previously described for BH is not restricted to this molecule but is also shared by other H3 antagonists [18].
  • Extracellular single-unit activity was recorded from the caudal, spinal-projecting region of the vestibular nuclei during tilt of the animal, before and after i.p. injection of betahistine [19].
  • [3H]Mepyramine binding to H1-receptors in membranes from guinea-pig cerebellum was inhibited by betahistine with a Ki value of 31 microM [15].
  • Betahistine-induced vascular effects in the rat cochlea [20].

Associations of Vasomotal with other chemical compounds


Gene context of Vasomotal


Analytical, diagnostic and therapeutic context of Vasomotal

  • This review provides new insights into the basic mechanisms by which betahistine improves vestibular compensation in animal models of unilateral vestibular dysfunction, and elucidates particularly the mechanisms of action of this substance at the level of the CNS [27].
  • Also, beta-histine was capable of significantly reducing the size of developing infarcts for up to 120 min after ligation [28].
  • Each individual received, in a randomized double-blind study, 3 different single oral dosages of betahistine (8, 16 and 32 mg) on 3 different occasions [29].
  • The cerebellar region, which is the most important area involved in vertigo patients with vascular pathology, showed almost complete normalisation of perfusion following Betahistine therapy [30].
  • Pre and post betahistine therapy 99m Tc - HMPAO brain spect studies in patients with vertigo [30].


  1. A comparison of betahistine hydrochloride with placebo for vertebral-basilar insufficiency: a double-blind study. Spruill, J.H., Toole, J.F., Kitto, W., Miller, H.E. Stroke (1975) [Pubmed]
  2. Pharmacological advances in the treatment of neuro-otological and eye movement disorders. Strupp, M., Brandt, T. Curr. Opin. Neurol. (2006) [Pubmed]
  3. Betahistine : a retrospective synopsis of safety data. Jeck-Thole, S., Wagner, W. Drug safety : an international journal of medical toxicology and drug experience. (2006) [Pubmed]
  4. Rheoencephalographic and other studies of betahistine in humans. IV. Prolonged administration with improvement in arteriosclerotic dementia. Seipel, J.H., Fisher, R., Blatchley, R.J., Floam, J., Bohm, M. Journal of clinical pharmacology. (1977) [Pubmed]
  5. Effect of the H1-histamine receptor agonist betahistine on drinking and eating behavior in pygmy goats. Rossi, R., Del Prete, E., Scharrer, E. Physiol. Behav. (1999) [Pubmed]
  6. Evaluation of betahistine for the prevention of seasickness: effect on vestibular function, psychomotor performance and efficacy at sea. Gordon, C.R., Doweck, I., Nachum, Z., Gonen, A., Spitzer, O., Shupak, A. Journal of vestibular research : equilibrium & orientation. (2003) [Pubmed]
  7. Comparative responses of the carotid and vertebral arterial systems of rhesus monkeys to betahistine. Tomita, M., Gotoh, F., Sato, T., Amano, T., Tanahashi, N., Tanaka, K., Yamamoto, M. Stroke (1978) [Pubmed]
  8. Distribution of cardiac output in dogs during intravenous infusion of betahistine. Smith, K.A., Meyer, M.W. Stroke (1976) [Pubmed]
  9. Drugs affecting the inner ear. A review of their clinical efficacy, mechanisms of action, toxicity, and place in therapy. Norris, C.H. Drugs (1988) [Pubmed]
  10. Betahistine-induced bronchospasm. Jiménez, I., Antón, E., Picáns, I., Jerez, J. Allergy (1996) [Pubmed]
  11. Postmarketing study of the use of flunarizine in vestibular vertigo and in migraine. Verspeelt, J., De Locht, P., Amery, W.K. Eur. J. Clin. Pharmacol. (1996) [Pubmed]
  12. A double-blind crossover study comparing betahistine and cinnarizine in the treatment of recurrent vertigo in patients in general practice. Deering, R.B., Prescott, P., Simmons, R.L., Downey, L.J. Current medical research and opinion. (1986) [Pubmed]
  13. Influence of histamine receptor antagonists on the dynamics of the cutaneous hypersensitivity reaction in patients infected with schistosoma haematobium. Snyman, J.R., Sommers, D.K., Gregorowski, M.D. Eur. J. Clin. Pharmacol. (1993) [Pubmed]
  14. Histamine-induced inhibition of neutrophil chemotaxis and T-lymphocyte proliferation in man. Bury, T.B., Corhay, J.L., Radermecker, M.F. Allergy (1992) [Pubmed]
  15. Actions of betahistine at histamine receptors in the brain. Arrang, J.M., Garbarg, M., Quach, T.T., Dam Trung TuongM, n.u.l.l., Yeramian, E., Schwartz, J.C. Eur. J. Pharmacol. (1985) [Pubmed]
  16. Effect of positively and negatively charged liposomes on skin permeation of drugs. Ogiso, T., Yamaguchi, T., Iwaki, M., Tanino, T., Miyake, Y. Journal of drug targeting. (2001) [Pubmed]
  17. Regional variation in the characteristics of histamine H1-agonist mediated breakdown of inositol phospholipids in guinea-pig brain. Carswell, H., Young, J.M. Br. J. Pharmacol. (1986) [Pubmed]
  18. Histamine (H3) receptors modulate the excitatory amino acid receptor response of the vestibular afferents. Chávez, H., Vega, R., Soto, E. Brain Res. (2005) [Pubmed]
  19. Effects of betahistine on the spatiotemporal response properties of vestibulospinal neurons to labyrinthine volleys. Barresi, M., Bruschini, L., Li Volsi, G., Manzoni, D. Eur. J. Pharmacol. (2005) [Pubmed]
  20. Betahistine-induced vascular effects in the rat cochlea. Laurikainen, E.A., Miller, J.M., Quirk, W.S., Kallinen, J., Ren, T., Nuttall, A.L., Grénman, R., Virolainen, E. The American journal of otology. (1993) [Pubmed]
  21. Rheoencephalographic and other studies of betahistine in humans: I. The cerebral and peripheral circulatory effects of single doses in normal subjects. Seipel, J.H., Floam, J.E. Journal of clinical pharmacology. (1975) [Pubmed]
  22. The influence of betahistine on the dynamics of the cutaneous hypersensitivity reaction in patients with grass pollen allergy. Snyman, J.R., Sommers, D.K., van Wyk, M., Gregorowski, M.D. Immunopharmacology (1995) [Pubmed]
  23. Effects of anti-vertigo drugs on medial vestibular nucleus neurons activated by horizontal rotation. Kawabata, A., Sasa, M., Kishimoto, T., Takaori, S. Jpn. J. Pharmacol. (1991) [Pubmed]
  24. Synergy among agents inhibiting granulocyte aggregation. Hammerschmidt, D.E., Flynn, P.J., Coppo, P.A., Skubitz, K.M., Jacob, H.S. Inflammation (1982) [Pubmed]
  25. Comparison of the effects of histamine H1- and H2-receptor agonists on large and small airways in normal and asthmatic subjects. White, J.P., Mills, J., Eiser, N.M. British journal of diseases of the chest. (1987) [Pubmed]
  26. The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Poyurovsky, M., Pashinian, A., Levi, A., Weizman, R., Weizman, A. International clinical psychopharmacology. (2005) [Pubmed]
  27. Histamine and betahistine in the treatment of vertigo: elucidation of mechanisms of action. Lacour, M., Sterkers, O. CNS drugs. (2001) [Pubmed]
  28. Modification of the size of developing infarcts in the ligated dog heart by betahistine-HCL. Terracio, L., Kubicek, W.G. Acta anatomica. (1978) [Pubmed]
  29. Effect of betahistine dihydrochloride on induced vestibular nystagmus: a double blind study. Oosterveld, W.J. Clinical otolaryngology and allied sciences. (1987) [Pubmed]
  30. Pre and post betahistine therapy 99m Tc - HMPAO brain spect studies in patients with vertigo. Krishna, B.A., Kirtane, M.V., Sangeeta, T., Gopinath, G. Neurology India. (2000) [Pubmed]
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