Inhibitory effect of betahistine on polysynaptic neurons in the lateral vestibular nucleus

Unemoto, Hiroshi; Sasa, Masashi; Takaori, Shuji; Ito, Juichi; Matsuoka, Izuru

doi:10.1007/bf00454214

Cited by 28 publications

(15 citation statements)

References 13 publications

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“…Furthermore, there have been studies considering that it is effective on brain stem vestibular nuclei. Most of these studies indicate that betahistine has a suppressing effect on vestibular nuclei [17,20,22,24] . On the contrary, Serafin et al [2] reported that histamine increased the spontaneous arousal on vestibuler nuclei in an animal study.…”

Section: Groupmentioning

confidence: 99%

The Effects of Betahistine and Dimenhydrinate on Caloric Test Parameters; Slow-Phase Velocity of Nystagmus

Kıroğlu¹,

Dagkiran²,

Özdemir³

et al. 2014

Int Adv Otol

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OBJECTIVE:The aim of this study is to determine the effects of betahistine and dimenhydrinate on the slow phase velocity. MATERIALS and METHODS:Forty patients with complaints of vertigo and dizziness volunteered to be included in the study. All patients who were included the study were treated at the other medical centers. The patients were divided into two Groups. Patients in the first Group were given betahistine 24 mg three times per day. During this treatment, caloric testing was performed, and the dose was increased to 48 mg three times a day due to ongoing complaints. The test was then repeated four weeks after using this higher dosage. Patients in the second Group had caloric testing while using and four weeks after stopping dimenhydrinate. RESULTS:The study Group was comprised of 40 patients; 20 patients (13 female, 7 male, 18-68 years, median age 46) in the betahistine Group and 20 patients (14 female, 6 male, 24-74 years, median age 44.5) in the dimenhydrinate Group. The average slow phase maximum velocity in the first Group of patients was 18 -/+ 8.2 and 21.1 -/+ 10.8 deg/s at 24 mg betahistine three times a day and 48 mg three times a day, respectively. In the second Group of patients, the average slow phase velocity was 13.4 -/+ 5.1 and 18.2 -/+ 7.5 deg/s during and after stopping the treatment of dimenhydrinate, respectively. The caloric test-induced slow-phase velocity was decreased with dimenhydrinate and increased with the higher dosage of betahistine. CONCLUSION:To our knowledge, this is the first study to demonstrate that betahistine increases caloric-induced slow-phase velocity in humans. Dimenhydrinate and betahistine should not be used together because of their opposite effects on the vestibular system. Dimenhydrinate can be used to treat acute episodes of vertigo, whereas betahistine should not be used during the episode but may be used in the period between the attacks to stimulate the vestibular system.

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Section: Groupmentioning

confidence: 99%

The Effects of Betahistine and Dimenhydrinate on Caloric Test Parameters; Slow-Phase Velocity of Nystagmus

Kıroğlu¹,

Dagkiran²,

Özdemir³

et al. 2014

Int Adv Otol

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“…Diphenhydramine is widely used to prevent motion sickness. Our previous studies showed that the microiontophoretic application of betahistine and diphenhydramine inhibited the spike generation of polysynaptic neurons in the lateral vestibular nucleus (LVN) elicited by vestibular nerve stimulation (3,4). In addition, the inhibition by diphenidol of spike generation in the vestibular nucleus neuron with vestibular nerve stimulation has also been reported by Matsuoka et al (5).…”

mentioning

confidence: 70%

“…The interneurons in the LVN, probably including both neurons projecting to the spinal cord and the nuclei related with eye movements, were considered to be affected by these anti-vertigo drugs since the vestibular nerve contains both afferents from the semicircular canals and otolith (3,4). However, the finding that the MVN type I neurons activated by the horizontal rotation were inhibited by these drugs herein indicates that the neurons receiving input from the semicircular canal of the vestibule are affected by these drugs.…”

Section: Discussionmentioning

confidence: 91%

Effects of anti-vertigo drugs on medial vestibular nucleus neurons activated by horizontal rotation.

et al. 1991

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ABSTRACT-The effects of anti-vertigo drugs on medial vestibular nucleus (MVN) neurons were examined to assess the site and mode of action using cats anesthetized with a-chloralose. Single neuron activity in the MVN was extracellularly recorded using a silver wire microelectrode attached along a seven-barreled micropipette, each of which was filled with diphenhydramine, diphenidol, betahistine, glutamate or NaCl. Type I of the MVN neurons were identified according to the responses obtained when the animal placed on a turn-table was rotated sinusoidally. The effects of the drugs were examined on type I neurons which received impulses primarily from the labyrinth and sent them to the oculomotor nuclei. The microiontophoretic application of diphenhydramine, diphenidol and betahistine inhibited rotation-induced firing of type I MVN neurons. Diphenhydramine and diphenidol were more potent than betahistine. These results suggest that these drugs directly act on MVN neurons to reduce the responsiveness to rotatory stimulation.

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“…This effect occurs both in cramped and normal blood vessels (6)(7)(8). The antivertigo action of betahistine could also be explained as the result of an inhibition of massive impulses to the polysynaptic neurons of the lateral vestibular nucleus (9).…”

Section: Introductionmentioning

confidence: 99%

Preformulation Studies of Transdermal Therapeutic Systems Containing Betahistine

Şahbaz

Dortunç²

2015

mpj

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Betahistine has been used in the treatment of diseases accompanied by impaired peripheral circulation, e.g. Ménière's syndrome, to reduce the frequency of episodes of vertigo and tinnitus. The drug has a short half-life and should be taken three times daily. Its contraindication in patients with peptic ulcer history and the difficulty of frequently dosing requires administration ways other than the oral route. The aim of this study was to prepare transdermal therapeutic system formulations containing betahistine by using synthetic and FDA approved polymers, Eudragit RL 100 and Eudragit RS 100. All the ingredients were evaluated for their excipient-drug compatibility, using Differantial Scanning Calorimetry (DSC) tests. Formulations with different excipient ratios were prepared and evaluated for their macroscopic properties (general appearance, homogeneity, flexibility, transparency and color). Results indicated that there was no incompatibility between drug and excipients. Excipient ratios were optimised according to the macroscopic properties of the formulations.

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Inhibitory effect of betahistine on polysynaptic neurons in the lateral vestibular nucleus

Cited by 28 publications

References 13 publications

The Effects of Betahistine and Dimenhydrinate on Caloric Test Parameters; Slow-Phase Velocity of Nystagmus

The Effects of Betahistine and Dimenhydrinate on Caloric Test Parameters; Slow-Phase Velocity of Nystagmus

Effects of anti-vertigo drugs on medial vestibular nucleus neurons activated by horizontal rotation.

Preformulation Studies of Transdermal Therapeutic Systems Containing Betahistine

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