Sublingual dexmedetomidine: repurposing an anesthetic as an anti-agitation agent

Expert Rev Neurother. 2023 Feb;23(2):97-106. doi: 10.1080/14737175.2023.2174430. Epub 2023 Mar 2.

Abstract

Introduction: Especially when acutely ill, individuals with schizophrenia and bipolar disorder can present with agitated behavior. The initial approach to agitation management are non-pharmacologic strategies such as verbal de-escalation techniques; however, pharmacologic interventions may be needed. Dexmedetomidine is a selective alpha-2 adrenergic receptor agonist, and a sublingual formulation has been approved in the US for the treatment of agitation associated with schizophrenia and bipolar disorder in adults.

Areas covered: The authors review the published literature on sublingual dexmedetomidine using the US National Library of Medicine's PubMed.gov resource. Pharmacodynamics, pharmacokinetics, and efficacy and tolerability findings are summarized. The authors also provide a discussion to its potential place in the treatment armamentarium.

Expert opinion: Sublingual dexmedetomidine is an effective and well-tolerated pharmacologic option for the treatment of agitation associated with schizophrenia and bipolar disorder. The sublingual method of administration allows for a rapid onset of action with treatment effects beginning as early as 20 minutes after administration. Adverse effects include somnolence, hypotension, oral paresthesia, hypoesthesia, and dry mouth. Further study will be needed to evaluate sublingual dexmedetomidine in real-world patients receiving concomitant psychotropic medications.

Keywords: Schizophrenia; aggression; agitation; bipolar disorder; dexmedetomidine; pharmacodynamics; pharmacokinetics; psychopharmacology; sublingual.

MeSH terms

  • Adult
  • Anesthetics* / therapeutic use
  • Antipsychotic Agents* / therapeutic use
  • Dexmedetomidine* / therapeutic use
  • Humans
  • Psychomotor Agitation / drug therapy
  • Schizophrenia* / drug therapy

Substances

  • Antipsychotic Agents
  • Dexmedetomidine
  • Anesthetics