Table 1.
Drugs with Effect on Neurotransmitter Receptors
| Trimetazidine | Noncompetitive EAA-R antagonist | Ischemia or conditions cursing with over-activation of the afferent input |
| Memantine | Noncompetitive NMDA-R antagonist. With serotonergic 5HT3-R, dopaminergic D2-R, and cholinergic mACh-R and nACh-R antagonism | Used to control acquired pendular nystagmus |
| Dizocilpine | NMDA-R antagonist | Neuroprotective agent in cases in which aminoglycoside use was required |
| Neramexane | Noncompetitive NMDA-R andα9α10-containing nACh-R antagonist | Phase III clinical trials for tinnitus control. ¿Can it be useful for ischemia or as neuroprotective for vestibular disorders? |
| Scopolamine and atropine | Competitive mACh-R antagonists | The most commonly used drug in vestibular disorders. Most effective drugs for the treatment of motion sickness |
| Diphenidol | Anticholinergic effect due to interactions with mACh-R | Prevention and symptomatic treatment of peripheral (labyrinthine) vertigo and associated nausea and vomiting. Control of nausea and vomiting of any origin |
| Betahistine | H3-R antagonistic and a partial, weak agonistic of H1 and H2 receptors | Most used drug in the Ménière's disease control in Europe. Reduces the incidence and severity of vertigo and the incidence of nausea and emesis |
| Diphenhydramine | Antagonist of H1 and of ACh receptors | Most used drug in the Ménière's disease control in USA |
| Meclizine and cyclizine | Antagonist of H1 and of ACh receptors | Commonly used in combination with betahistine or diphenhydramine in the Ménière's disease control |
| Promethazine | Antagonist of H1 and of ACh receptors | Treatment and prevention of vertigo |
| Diazepam, lorazepam and clonazepam | GABA-A receptor antagonists | Therapeutic effect in vertiginous syndromes, apart from their sedative and anxiolytic action that significantly contributes to the well-being of patients |
| Baclofen | GABA-B receptor antagonist | Used to control periodic alternating nystagmus |
| Gabapentin | GABA-A receptor agonist Slight Ca2+ channel block | Used to control pendular nystagmus |
| Phentanyl | Synthetic primary MOR agonist | Used in the treatment of Ménière's disease crises and vestibular neuronitis in combination with droperidol |
| Droperidol | Dopaminergic receptor antagonist | Usually an antipsychotic. Useful for treatment of acute peripheral vertigo |
| Sulpiride | Selective D2 receptor antagonist | Used as a vestibular sedative |
Excitatory amino acid receptor, EAA-R; N-methyl-D-aspartic acid receptor, NMDA-R; Type 3 serotonergic receptor, 5HT3-R; Type 2 dopamine receptor, D2-R; Nicotinc acetylcholine receptor, nACh-R; Muscarinic acetylcholine receptor, mACh-R; Type 1, 2 or 3 histamine receptor, H1-, H2- or H3; Type A or B γ-aminobutyric acid, GABA; µ-opioid receptor, MOR.