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Unfortunately, astemizole does not appear to be generally useful as it is ineffective in preventing motion sickness (Kohl et al, 1987) and because it has significant potential toxicity.There is evidence for involvement of several types of histamine receptors.Histamine agonists that act on receptor subtypes are also used for treatment of vertigo (e.g. This can sometimes result in a peculiar situation where individuals take both antihistamines and histamine agonists at the same time.Benzodiazepines are GABA modulators, acting centrally to suppress vestibular responses. They increase the affinity of chloride channel opening (Soto et al, 2013).
Most antihistamines also have calcium channel blocking effect (according to Timmerman, 1994).
Cholinergic agonists that cross into the brain, such as physostigmine, can cause a motion-sickness syndrome (Soto et al, 2013).
Cholinergic agonists that do not cross into the brain such as neostigmine, do not produce motion sickness. While the precise role of histamine in central vestibular processing is uncertain, there are data indicating that centrally acting antihistamines prevent motion sickness and reduce the severity of its symptoms even if taken after the onset of symptoms (Takeda et al, 1989).
Addiction, the biggest problem, can usually be avoided by keeping the dose to 0.5 mg BID or less. Fall risk is increased in the elderly by roughly the same proportions.
Other problems include higher incidence of car accidents (risk x1.5), and hip fractures (risk x 1.8) (Ray, Griffin et al. Similarly, low doses of diazepam (Valium) (2 mg) can be quite effective for dizziness.