Remimazolam

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Remimazolam
Identifiers
  • methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H19BrN4O2
Molar mass439.304 g/mol g·mol−1
3D model (JSmol)
  • c4cccnc4C1=NC(CCC(=O)OC)c(ncc2C)n2-c(cc3)c1cc3Br
  • InChI=1S/C21H19BrN4O2/c1-13-12-24-21-17(7-9-19(27)28-2)25-20(16-5-3-4-10-23-16)15-11-14(22)6-8-18(15)26(13)21/h3-6,8,10-12,17H,7,9H2,1-2H3/t17-/m0/s1 ☒N
  • Key:CYHWMBVXXDIZNZ-KRWDZBQOSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

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

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 anesthesia protocols for cardiac surgery and colonoscopy were presented at major conferences in October 2014.[6]

A phase IIa trial comparing remimazolam to midazolam for upper endoscopy was published in December 2014, finding a similar safety profile.[7] Remimazolam was originally discovered in the late 1990s at Glaxo Wellcome in their labs in Research Triangle Park, NC.

See also

References

  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.


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