Remimazolam

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Remimazolam[1] (CNS-7056) is a benzodiazepine derivative drug, developed by PAION, in collaboration with Japanese licensee Ono Pharmaceutical as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures. Remimazolam was found to be both faster acting and shorter lasting than midazolam, and human clinical trials showed a faster recovery time and predictable, consistent pharmacokinetics, suggesting some advantages over existing drugs for these applications.[2][3]

Trials[edit]

Remimazolam
Remimazolam structure.png
Systematic (IUPAC) name
methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate
Clinical data
Identifiers
308242-62-8 YesY
PubChem CID 9824461
ChemSpider 8043503 N
UNII 7V4A8U16MB YesY
Chemical data
Formula C21H19BrN4O2
439.304
 N (what is this?)  (verify)

Phase I[4] and Ib[5] dose-finding studies for procedural sedation with patients recovering faster from Remimazolam than midazolam. Phase II trials comparing Remimazolam to the standard anaesthesia protocols for cardiac surgery and colonoscopy were presented at major conferences in October 2014.[6]

A phase 2a trial comparing remimazolam to midazolam for upper endoscopy was published in December 2014, finding a similar safety profile.[7]

See also[edit]

References[edit]

  1. ^ EP Patent 1183243
  2. ^ Rogers WK, McDowell TS (December 2010). "Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures". IDrugs : the Investigational Drugs Journal 13 (12): 929–37. PMID 21154153. 
  3. ^ Saari TI, Uusi-Oukari M, Ahonen J, Olkkola KT (March 2011). "Enhancement of GABAergic activity: neuropharmacological effects of benzodiazepines and therapeutic use in anesthesiology". Pharmacological Reviews 63 (1): 243–67. doi:10.1124/pr.110.002717. PMID 21245208. 
  4. ^ "A placebo- and midazolam-controlled phase I single ascending-dose study evaluating the safety, pharmacokinetics, and pharmacodynamics of remimazolam (CNS 7056): Part I. Safety, efficacy, and basic pharmacokinetics.". Anesth Analg 115: 274–83. Aug 2012. doi:10.1213/ANE.0b013e31823f0c28. PMID 22190555. 
  5. ^ "A phase Ib, dose-finding study of multiple doses of remimazolam (CNS 7056) in volunteers undergoing colonoscopy.". Anesth Analg. 117: 1093–100. Nov 2013. doi:10.1213/ANE.0b013e3182a705ae. PMID 24108261. 
  6. ^ "Two Scientific Remimazolam Presentations Are Accepted for ASA and ACG Meeting in October 2014". MarketWired. Oct 1, 2014. Retrieved 2014-10-24. 
  7. ^ "A Phase IIa, Randomized, Double-Blind Study of Remimazolam (CNS 7056) Versus Midazolam for Sedation in Upper Gastrointestinal Endoscopy.". Anesthesia 120: 771–80. Dec 11, 2014. doi:10.1213/ANE.0000000000000548. PMID 25502841.