Ro48-6791 Explained

Ro48-6791 is a drug, an imidazobenzodiazepine 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 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

• Benzodiazepine

Notes and References

1. US . 5665718 .
2. Dingemanse J, van Gerven JM, Schoemaker RC, Roncari G, Oberyé JJ, van Oostenbruggen MF, Massarella J, Segala P, Zell M, Cohen AF . 6 . 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 . November 1997 . 9384465 . 2042878 . 10.1046/j.1365-2125.1997.t01-1-00612.x .
3. Hering W, Ihmsen H, Albrecht S, Schwilden H, Schüttler J . [RO 48-6791--a short acting benzodiazepine. Pharmacokinetics and pharmacodynamics in young and old subjects in comparison to midazolam] . German . Der Anaesthesist . 45 . 12 . 1211–4 . December 1996 . 9065257 . 10.1007/s001010050360 . 29508 . RO 48-6791--a short acting benzodiazepine. Pharmacokinetics and pharmacodynamics in young and old subjects in comparison to midazolam .
4. Wrigley PJ, Elliott DW, Blake D . 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 . October 1998 . 9807605 . 10.1177/0310057X9802600506 . free .
5. Tang J, Wang B, White PF, Gold M, Gold J . 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 . October 1999 . 10512261 . 10.1097/00000539-199910000-00014 .
6. Gold ME, Todd SA, Spiegler C, Gold JA . When the drug trial fails: an approach to clinical drug studies . AANA Journal . 67 . 6 . 505–12 . December 1999 . 10876442 .
7. Ihmsen H, Albrecht S, Hering W, Schüttler J, Schwilden H . Modelling acute tolerance to the EEG effect of two benzodiazepines . British Journal of Clinical Pharmacology . 57 . 2 . 153–61 . February 2004 . 14748814 . 1884442 . 10.1046/j.1365-2125.2003.01964.x .