Ro48-6791

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Ro48-6791
Ro48-6791.svg
Identifiers
E number{{#property:P628}}
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Chemical and physical data
FormulaC21H25FN6O2
Molar mass412.47

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]


Ro48-6791 is a drug which is a benzodiazepine derivative developed by Hoffman-LaRoche in the 1990s.

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 similar properties to midazolam, being water soluble, with a fast onset and short duration of action. It is 4-6x more potent than midazolam,[1] and slightly shorter acting,[2] 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.[3] 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.[4] Consequently it was dropped from clinical development,[5] although it is still used in scientific research.[6]



References

  1. Dingemanse J, van Gerven JM, Schoemaker RC, Roncari G, Oberyé JJ, van Oostenbruggen MF, Massarella J, Segala P, Zell M, Cohen AF. 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. 1997 Nov;44(5):477-86. PMID 9384465
  2. 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. Anaesthesist. 1996 Dec;45(12):1211-4. PMID 9065257
  3. 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. 1998 Oct;26(5):509-14. PMID 9807605
  4. 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. 1999 Oct;89(4):893-8. PMID 10512261
  5. Gold ME, Todd SA, Spiegler C, Gold JA. When the drug trial fails: an approach to clinical drug studies. AANA Journal. 1999 Dec;67(6):505-12. PMID 10876442
  6. 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. 2004 Feb;57(2):153-61. PMID 14748814



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