New benzodiazepines for sedation

Best Pract Res Clin Anaesthesiol. 2018 Jun;32(2):149-164. doi: 10.1016/j.bpa.2018.06.007. Epub 2018 Jul 3.

Abstract

There are currently new drugs being developed that have benzodiazepine properties. This review will examine remimazolam, 3-hydroxyphenazapam, adinazolam, clonazolam, and deschloroetizolam as well as other novel agents. All benzodiazepines are protein bound and only moderately lipid soluble. In addition to their baseline properties, they can be enzymatically broken down into active metabolites. The mechanism of action of these medications is related to polysynaptic pathway inhibition via direct interaction with GABA and modifiable chloride channels. The main neurological areas of involvement are primarily the amygdala and reticular activating system. Benzodiazepines are used for sedation and for adjuvants to general anesthetics and not as primary induction agents. We describe the characteristics of newer drugs being developed, including their pharmacologic profile, side effects and efficacy, as well as the most recent clinical trials and future directions in benzodiazepine development.

Keywords: benzodiazepines; derivatives; non-benzodiazepine; novel benzodiazepines; sedation.

Publication types

  • Review

MeSH terms

  • Anesthesia / methods*
  • Anesthesia / trends
  • Benzodiazepines / administration & dosage*
  • Benzodiazepines / metabolism
  • Humans
  • Hypnotics and Sedatives / administration & dosage*
  • Hypnotics and Sedatives / metabolism

Substances

  • Hypnotics and Sedatives
  • Benzodiazepines