Ro48-6791

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Ro48-6791
Ro48-6791.svg
Systematic (IUPAC) name
3-{5-[(dipropylamino)methyl]- 1,2,4-oxadiazol-3-yl}- 8-fluoro- 5-methyl- 4,5-dihydro- 6H-imidazo[1,5-a] [1,4]benzodiazepin- 6-one
Clinical data
Legal status ?
Identifiers
ATC code ?
PubChem CID 9953485
Chemical data
Formula C21H25FN6O2 
Mol. mass 412.47
 YesY (what is this?)  (verify)

Ro48-6791 is a drug, a benzodiazepine derivative developed by Hoffman-LaRoche in the 1990s.[1]

Ro48-6791 was developed as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures. Ro48-6791 has properties similar to those of to midazolam, being water soluble, with a fast onset and short duration of action. It is 4-6x more potent than midazolam,[2] and slightly shorter acting,[3] and produces similar side effects such as sedation and amnesia.

It was tested up to Phase II human trials, but while it produced less respiratory depression than propofol, it had a longer recovery time and was deemed not to have any significant advantages over the older drug.[4] Similarly when Ro48-6791 was compared to midazolam, it had similar efficacy, higher potency and a shorter recovery time, but produced less of a synergistic effect on opioid-induced analgesia and produced more severe side effects such as dizziness after the procedure.[5] Consequently it was dropped from clinical development,[6] although it is still used in scientific research.[7]

See also[edit]

References[edit]

  1. ^ US Patent 5665718
  2. ^ Dingemanse, J; Van Gerven, JM; Schoemaker, RC; Roncari, G; Oberyé, JJ; Van Oostenbruggen, MF; Massarella, J; Segala, P et al. (1997). "Integrated pharmacokinetics and pharmacodynamics of Ro 48–6791, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects". British Journal of Clinical Pharmacology 44 (5): 477–86. doi:10.1046/j.1365-2125.1997.t01-1-00612.x. PMC 2042878. PMID 9384465. 
  3. ^ Hering, W; Ihmsen, H; Albrecht, S; Schwilden, H; Schüttler, J (1996). "Ro 48-6791 – ein kurzwirksames Benzodiazepin Untersuchungen zur Pharmakokinetik und Pharmakodynamik bei jungen und älteren Probanden im Vergleich mit Midazolam" [RO 48-6791--a short acting benzodiazepine. Pharmacokinetics and pharmacodynamics in young and old subjects in comparison to midazolam]. Der Anaesthesist (in German) 45 (12): 1211–4. doi:10.1007/s001010050360. PMID 9065257. 
  4. ^ Wrigley, PJ; Elliott, DW; Blake, D (1998). "A phase 2 clinical trial comparing Ro 48-6791, a new short-acting benzodiazepine, with propofol for induction of anaesthesia". Anaesthesia and intensive care 26 (5): 509–14. PMID 9807605. 
  5. ^ Tang, J; Wang, B; White, PF; Gold, M; Gold, J (1999). "Comparison of the sedation and recovery profiles of Ro 48-6791, a new benzodiazepine, and midazolam in combination with meperidine for outpatient endoscopic procedures". Anesthesia and Analgesia 89 (4): 893–8. doi:10.1097/00000539-199910000-00014. PMID 10512261. 
  6. ^ Gold, ME; Todd, SA; Spiegler, C; Gold, JA (1999). "When the drug trial fails: an approach to clinical drug studies". AANA journal 67 (6): 505–12. PMID 10876442. 
  7. ^ Ihmsen, H; Albrecht, S; Hering, W; Schüttler, J; Schwilden, H (2004). "Modelling acute tolerance to the EEG effect of two benzodiazepines". British Journal of Clinical Pharmacology 57 (2): 153–61. doi:10.1046/j.1365-2125.2003.01964.x. PMC 1884442. PMID 14748814.