|Chemical and physical data|
|3D model (JSmol)|
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, and slightly shorter acting, 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. 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. Consequently, it was dropped from clinical development, although it is still used in scientific research.
- US Patent 5665718
- 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 . PMID 9384465.
- 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.
- 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.
- 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.
- 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.
- 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 . PMID 14748814.