PMID: 8968176Dec 1, 1996Paper

Pharmacokinetic-pharmacodynamic modeling of the new steroid hypnotic eltanolone in healthy volunteers

Anesthesiology
W HeringJ Schüttler

Abstract

In the last 4 y, several authors have reported largely satisfactory results using the new steroid intravenous anesthetic eltanolone (pregnanolone) to induce anesthesia. Until now, however, no investigations have addressed the infusion pharmacokinetics of eltanolone or used electroencephalographic effect data for full pharmacodynamic modeling. Thus the authors conducted a study to evaluate the pharmacokinetic and pharmacodynamic properties of eltanolone after infusion in healthy volunteers. Eltanolone emulsion was administered to 12 healthy men using a computer-controlled infusion device. Linearly increasing serum concentrations were generated for two consecutive infusions with an anticipated slope of 0.075 microgram.ml-1.min-1 and a targeted concentration of 2-2.5 micrograms/ml. During and after the infusion, electroencephalographic data were recorded as a continuous pharmacodynamic parameter to measure the hypnotic effect. In addition, blood pressure, heart rate, pulse oximetry, clinical signs of anesthesia, and any undesirable effects were recorded. The appearance of burst suppression periods in the raw electroencephalographic wave form was used as an end point for the infusion. Arterial blood samples were drawn frequently un...Continue Reading

References

Jun 10, 1988·European Journal of Pharmacology·E F Kirkness, A J Turner
Oct 1, 1988·British Journal of Anaesthesia·S HøgskildeM B Sørensen
Feb 1, 1988·British Journal of Anaesthesia·T KirkpatrickW S Nimmo
Jun 1, 1987·Journal of Pharmacokinetics and Biopharmaceutics·J SchüttlerL B Sheiner
Nov 1, 1984·Anesthesiology·S GancherW Krieger
Dec 1, 1984·British Journal of Anaesthesia·R L BarrattT A Torda
Dec 1, 1994·British Journal of Anaesthesia·Y MyintC S Reilly
Sep 1, 1994·Anesthesia and Analgesia·H KallelaK Korttila

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Citations

Jun 30, 2007·Clinical and Experimental Pharmacology & Physiology·Richard N Upton
Oct 31, 2002·Clinical Pharmacokinetics·William J Wight, Peter M C Wright
Jun 25, 2005·Alcoholism, Clinical and Experimental Research·Martin HillLuboslav Starka
May 20, 1998·European Journal of Anaesthesiology·J W Sear
Oct 22, 2002·The Journal of Pharmacology and Experimental Therapeutics·S A G VisserM Danhof
Jun 24, 2004·Molecular Pharmacology·Juha-Matti I AlakoskelaPaavo K J Kinnunen
Sep 25, 2020·Pediatric Research·Carlo V Bellieni
Dec 1, 2010·Physiological Research·M HillJ E Jirásek

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