Ro48-6791
| 200px | |
| Systematic (IUPAC) name | |
|---|---|
|
3-{5-[(dipropylamino)methyl]- 1,2,4-oxadiazol-3-yl}- 8-fluoro- 5-methyl- 4,5-dihydro- 6H-imidazo[1,5-a] [1,4]benzodiazepin- 6-one | |
| Identifiers | |
| PubChem | CID 9953485 |
| Chemical data | |
| Formula | C21H25FN6O2 |
| Molar mass | 412.47[[Script error: No such module "String".]] |
Ro48-6791 is a drug, 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 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,[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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See also
References
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<references />, or <references group="..." />- ↑ Dingemanse, J; Van Gerven, JM; Schoemaker, RC; Roncari, G; Oberyé, JJ; Van Oostenbruggen, MF; Massarella, J; Segala, P; Zell, M (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 2042878 Freely accessible. PMID 9384465.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ 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 1884442 Freely accessible. PMID 14748814.
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