Newer Drugs in Anaesthesia

REMIMAZOLAM: IMPORTANT POINTS

  • Its an ultra-short acting benzodiazepine that is currently under investigation in phase II and III clinical trials.
  • It is metabolized by tissue esterases in the blood to its inactive metabolite, carboxylic acid, which allows for rapid removal of the drug even with its use in prolonged infusions.
  • Remimazolam is eliminated by first-order pharmacokinetics, therefore with prolonged infusions or high doses, there is no problem with drug or metabolite accumulation .
  • It has been evaluated as a premedication drug prior to anesthesia; however due to its very short duration of action and the fact that it is not available as an oral formulation limits its use in this clinical situation.
  • It has been most studied as a drug for use in procedural sedation. It has been studied widely in sedation for endoscopic procedures like colonoscopies. Studies have shown doses of 0.1-0.2 mg/kg were effective sedative doses for patients undergoing endoscopic procedures. It allows for a faster onset and recover time when compared with midazolam. There is limited incidence of respiratory depression and it canability to be reversed with flumazenil without resedation
  • It is also currently being studied as a general anesthetic, using induction doses of 6 and 12 mg/kg/h and maintenance rates of 1 mg/kg/h.
  • Because its metabolism is organ-independent, it also has been evaluated for use as a sedative agent in the ICU setting. Its ultra-short acting nature would also make it an ideal agent to allow for neurological evaluation very soon after an infusion has been stopped .
  • The safety profile of remimazolam has been shown to be favorable overall, demonstrating less vasopressor use compared with patients sedated with propofol