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New benzodiazepines for sedation. | LitMetric

New benzodiazepines for sedation.

Best Pract Res Clin Anaesthesiol

Department of Anesthesiology, LSU Health New Orleans, 1542 Tulane Ave., New Orleans, LA, 70112, USA. Electronic address:

Published: June 2018

AI Article Synopsis

  • New drugs with benzodiazepine-like properties, including remimazolam and clonazolam, are being explored for their medical use.
  • All benzodiazepines bind to proteins and are moderately lipid soluble, and they can be metabolized into active forms in the body.
  • The review discusses their mechanism of action involving GABA and chloride channels, their primary use in sedation and anesthesia, and provides insights into their pharmacologic profiles, side effects, and recent clinical trials.

Article 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.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bpa.2018.06.007DOI Listing

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