Ro48-6791
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Ro48-6791
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| Systematic (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 | |
| Identifiers | |
| CAS number | ? |
| ATC code | ? |
| PubChem | ? |
| Chemical data | |
| Formula | C21H25FN6O2 |
| Mol. mass | 412.47 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
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| Legal status | |
| Routes | ? |
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]
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[edit] References
- ^ 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
- ^ 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
- ^ 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
- ^ 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
- ^ 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
- ^ 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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