![]() ![]() Here, we review current antihistamine use in managing vertigo, focusing on efficacy, side effects and impact on central compensation. The nonselective nature of many of these agents imposes clinical limitations, with most antivertigo agents acting principally through sedation or reduction of nausea rather than addressing the cause of the vertigo itself. 11 Vestibular suppressants cover 3 main drug groups, anticholinergics, antihistamines and benzodiazepines. They are primarily represented by vestibular suppressants which reduce vertigo and nystagmus evoked by vestibular imbalance or motion sickness, while antiemetics are used to combat nausea and vomiting. While vestibular rehabilitation is recommended by many international clinical practice guidelines, 8, 9, 10 pharmacological approaches form the backbone of vertigo management, composed of agonists and antagonists of neurotransmitters and neuromodulators that modulate vestibular afferent/efferent synaptic input. 6, 7 Nonetheless, in‐depth knowledge of the pathophysiology of vertigo is lacking and a thorough understanding is currently hampered by nonstandardised definitions. ![]() This highly complex process is orchestrated by peripheral and central neurons, which rely on a range of neurotransmitters (glutamate, acetylcholine, γ‐aminobutyric acid and glycine), further modulated by histamine, adrenaline and noradrenaline. Sensory hair cell damage, synaptic uncoupling and neuronal damage disturb the balance of vestibular signalling. Sense of balance and position are derived from input from the 3 semicircular canals and otolith organs in the peripheral vestibular system, integrated with proprioceptive and visual information in the vestibular nuclei. Vertigo may arise centrally following injury to the balance centres of the central nervous system (CNS), or be of peripheral origin linked to disorders of the vestibule located in the inner ear. 3, 4 While the occupational impact is poorly qualified, it represents a substantial economic cost to society. 2 Vertigo is associated with a wide range of pathologies, including inner ear diseases such as benign paroxysmal positional vertigo (BPPV), vestibular migraine, Ménière's disease, acute unilateral vestibulopathy (AUV) and labyrinthitis. The 12‐month prevalence of vertigo ranges from 2 to 5%, with incidence linked to age. Vertigo is principally characterised by an erroneous sensation of spinning motion, frequently accompanied by vestibulo‐oculomotor symptoms of oscillopsia, nystagmus, postural imbalance, and falling, 1 along with neurovegetative effects, notably nausea and vomiting. With an excellent safety profile and notable absence of sedation, encouraging outcomes in an induced vertigo model in healthy volunteers have led to ongoing clinical studies in acute unilateral vestibulopathy, with the hope that H 4 antagonists will offer new effective therapeutic options to patients suffering from vertigo. The preclinical potential of SENS‐111 (Seliforant), an oral first‐in‐class selective H 4 antagonist is the only such molecule to date to be translated into the clinical setting. A number of novel selective H 4 antagonists are active in vestibular models in vivo. Recently demonstrated expression of H 4 receptors in the peripheral vestibular system represents a new potential drug target for treating vestibular disorders. Other approaches include antihistamine combination studies, devices, physical therapy and behavioural interventions. To address these issues, the timing of administration of betahistine, the mainstay H 3 antihistamine, can be fine‐tuned, while bioavailability is also being improved. Additionally, the primary and limiting side effect of sedation is counterproductive to normal functioning and the natural recovery process occurring via central compensation. Nonetheless, effective management of vertigo proves elusive as many treatments largely address only associated symptoms, and with questionable efficacy. Agents targeting the H 1 and H 3 receptors have been in clinical use for several decades as single agents. ![]() Antihistamines represent the largest class of agents used to combat vestibular vertigo symptoms. Solutions include vestibular suppressants and vestibular rehabilitation, which form the mainstay of therapy. It increasingly affects the elderly, with a high cost to society. ![]() Vertigo is associated with a wide range of vestibular pathologies. ![]()
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