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ANTIVERTIGINOUS DRUGS

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The drugs used in the management of vertigo icludes:

  1. Antihistamines,
  2. Benzodiazepines,
  3. Phenothiazines,
  4. Monoaminergic agents, and
  5. Anticholinergic agents.

ATIHISTAMINICS: Antihistamines prevent the histamine response in sensory nerve endings and blood vessels and are effective in treating vertigo.

melcizine

  • Meclizine: Meclizine decreases the excitability of the inner-ear labyrinth and blocks conduction in inner-ear vestibular-cerebellar pathways. Its effects are associated with therapeutic effects in relief of nausea and vomiting. It is most effective if used as needed for 2-3 days with episodes of true vertigo.
  • Cinnarizine

cinnerzine

  • Betahistine

dimenhydrinate

  • Dimenhydrinate: It is a 1:1 salt of 8-chlorotheophylline and diphenhydramine that is believed to be particularly useful in the treatment of vertigo. It diminishes vestibular stimulation and depresses labyrinthine function by means of its central anticholinergic activity.

ANXIOLYTICS (BENZODIAZEPINES) : By binding to specific receptor sites, benzodiazepines appear to potentiate the effects of gamma-aminobutyric acid (GABA) and facilitate inhibitory GABA neurotransmission and other inhibitory transmitters. These effects may prevent vertigo and emesis.

  • Diazepam is effective in treating vertigo, acute episodes in particular. It depresses all levels of the central nervous system (CNS), including the limbic system and the reticular formation, possibly by increasing the activity of GABA. Individualize the dosage, and cautiously increase it so as to avoid adverse effects. Discontinue as quickly as possible to maximize the cerebellar vestibular compensation process.

PHENOTHIAZINES: Phenothiazines are effective in treating emesis, possibly because of their effects in the dopaminergic mesolimbic system.

phenothiazines

  • Promethazine is an antidopaminergic drug that is effective in the treatment of emesis. It blocks postsynaptic mesolimbic dopaminergic receptors in the brain and reduces stimuli to the brainstem reticular system. Glycopyrrolate is safer and has fewer adverse effects. Promethazine is well tolerated by elderly patients and does not have the potential for causing extrapyramidal syndrome.

promethazine

 

  • Prochlorperazine (STEMETIL) is an antidopaminergic drug that blocks postsynaptic mesolimbic dopamine receptors. It has anticholinergic activity and can depress the reticular activating system (this effect may be responsible for relief of nausea and vomiting).

Prochlorperazine


ALPHA/ BETA ADRENERGIC AGONIST: Monoaminergic agents may be used to treat vertigo; their effect may involve modulation of the sympathetic system.

  • Ephedrine stimulates release of epinephrine stores, producing alpha- and beta-adrenergic receptors.

ephedrine


ANTICHOLINERGIC AGENTS: Anticholinergic agents are thought to work centrally by suppressing conduction in the vestibular-cerebellar pathways.

  • Glycopyrrolate blocks the action of acetylcholine at parasympathetic sites.

glycopyrrolate

 

  • Scopolamine blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands, and the CNS. It antagonizes the actions of histamine and serotonin. Transdermal application may be the most effective for motion sickness. Use of scopolamine in the treatment of vestibular neuronitis is limited by the drug’s slow onset of action. Severe adverse effects preclude its use in elderly. Glycopyrrolate is more effective and has fewer adverse effects, especially in elderly patients.

scopolamine

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