Propofol and flurazepam act synergistically to potentiate GABAA receptor activation in human recombinant receptors

European Journal of Pharmacology
J N Reynolds, R Maitra

Abstract

The intravenous general anaesthetic propofol (2,6-di-isopropylphenol) is frequently combined with a benzodiazepine. There are clinical reports of synergism between these two agents for induction of general anaesthesia. To investigate a possible mechanism of this synergistic interaction between propofol and benzodiazepines, the effect of propofol and flurazepam on GABAA receptor function was examined in Xenopus oocytes expressing recombinant alpha 1 beta 2 gamma 2L and alpha 2 beta 2 gamma 2L receptor constructs. Potentiation of GABA receptor-activated current by low (1-10 microM) concentrations of propofol together with flurazepam (0.25-0.5 microM) was significantly greater than predicted by an additive response. Isobolographic analysis indicated a strong synergistic interaction between propofol and flurazepam at either of the receptor constructs examined. In contrast, the cyclopyrrolone derivative zopiclone, which produced a similar facilitation of GABA receptor-activated current compared to flurazepam, produced a less than additive potentiation when combined with propofol. Flurazepam significantly decreased the EC50 concentration of propofol for potentiation of GABA responses. Thus, flurazepam, in addition to facilitating GAB...Continue Reading

References

Nov 1, 1991·British Journal of Anaesthesia·T G Short, P T Chui
Sep 1, 1994·Naunyn-Schmiedeberg's Archives of Pharmacology·A ConcasG Biggio

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Citations

Mar 11, 2000·Brain Research·S M O'SheaN L Harrison
May 14, 2003·European Journal of Pharmacology·Mansoureh EghbaliBryndis Birnir
Feb 26, 2008·Pharmacology, Biochemistry, and Behavior·Stephanie C Licata, James K Rowlett
Feb 4, 1999·Critical Care Clinics·S M Lowson, S Sawh
Jan 18, 2011·European Journal of Pharmacology·Janet L Fisher
Jul 30, 2016·The European Journal of Neuroscience·Jaspreet KaurAndrea Nistri
Mar 14, 2017·Journal of Pain & Palliative Care Pharmacotherapy·John Bodnar
Sep 8, 2018·Journal of Intensive Care Medicine·John Bodnar
Jul 20, 2002·The Journal of Pharmacology and Experimental Therapeutics·Mark W Fleck
Dec 17, 1997·Annals of Emergency Medicine·T R Coomes, S W Smith

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