Ro48-6791

Drugbox
IUPAC_name = 3-(5-dipropylaminomethyl-1,2,4-oxadiazol-3-yl) -8-fluoro-5-methyl-5,6-dihydro-4H-imidazo [1,5-a] [1,4] benzodiazepin-6-one

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C=21 | H=25 | F=1 | N=6 | O=2
molecular_weight = 412.47
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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, [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. [http://www.ncbi.nlm.nih.gov/pubmed/9384465 PMID 9384465] ] and slightly shorter acting, [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. [http://www.ncbi.nlm.nih.gov/pubmed/9065257 PMID 9065257] ] 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. [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. [http://www.ncbi.nlm.nih.gov/pubmed/9807605 PMID 9807605] ] 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. [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. [http://www.ncbi.nlm.nih.gov/pubmed/10512261 PMID 10512261] ] Consequently it was dropped from clinical development, [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. [http://www.ncbi.nlm.nih.gov/pubmed/10876442 PMID 10876442] ] although it is still used in scientific research. [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. [http://www.ncbi.nlm.nih.gov/pubmed/14748814 PMID 14748814] ]

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