Betahistine is used for treatment of several vestibular disorders. Despite
the accepted use of this histamine-like substance, its mechanism of action
is not well understood. The purpose of this study was to assess the possibi
lity that one of the activities of betahistine is increasing blood flow in
the peripheral vestibular end organs. Using a novel surgical approach, we i
dentified the posterior semicircular canal ampulla of guinea pigs and place
d a laser Doppler probe in position to obtain blood flow measurements from
the posterior semicircular canal ampulla, Blood pressure, heart rate, and v
estibular blood flow were continuously recorded, Concentration-response cur
ves were obtained for betahistine (2.5, 5, 7.5, and 10 mg/kg) and control-v
ehicle (0.15 mol/L NaCl) infusions, A separate group of subjects was pretre
ated with the competitive selective H3 agonist, thioperimide maleate, befor
e betahistine treatment. Increases in vestibular blood flow and decreases i
n blood pressure were observed in response to betahistine infusions. Pretre
atment with thioperamide maleate abolished these changes at low doses of be
tahistine and attenuated the responses at higher doses of betahistine, Thes
e results show that betahistine administration induces increases in vestibu
lar blood flow. These findings support the potential use of betahistine for
treatment of vestibular disorders, which may be caused by compromised circ
ulation.