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ANESTHETIC PHARMACOLOGY

Sedation with GPI 15715, a Water-Soluble Prodrug of Propofol, Using Target-Controlled Infusion in Volunteers

Jörg Fechner, MD^*, Harald Ihmsen, PhD^*, Christine Schiessl, MD^*, Christian Jeleazcov, MD^*, James J. Vornov, MD, PhD, Helmut Schwilden, MD, PhD^*, and Jürgen Schüttler, MD^*

*Department of Anesthesiology, University of Erlangen-Nuremberg, Erlangen, Germany; and Guilford Pharmaceuticals Inc., Baltimore, Maryland

Address correspondence and reprint requests to Jörg Fechner, MD, Department of Anesthesiology, University of Erlangen-Nuremberg, Krankenhausstrasse 12, 91054 Erlangen, Germany. Address e-mail to joerg.fechner{at}kfa.imed.uni-erlangen.de.

GPI 15715 is the first water-soluble propofol prodrug that has been studied in humans. Present propofol lipid formulations have well known undesirable properties, for example, pain on injection and increased triglyceride concentrations. We investigated whether GPI 15715 is suitable to achieve and maintain moderate sedation for 2 h. Six male and six female volunteers received a target-controlled infusion of GPI 15715, with an initial propofol target concentration of 1.8 µg/mL and the possibility to adjust the propofol target once after 1 h. Propofol concentrations, the bispectral index, and modified Observer’s Assessment of Alertness/Sedation Scale (MOAA/S) scores were monitored. The median MOAA/S score was 4 during the first hour and was 3 during the second hour of infusion. The propofol target had to be changed to 2.4 µg/mL in seven volunteers and to 3.0 µg/mL in two volunteers. A propofol concentration of 1.9 µg/mL had the highest probability to result in an MOAA/S score of 3, which corresponds with moderate sedation. We observed no serious side effects. We conclude that GPI 15715 produces excellent sedation.

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Anesthesia & Analgesia® is published for the International Anesthesia Research Society® by Lippincott Williams & Wilkins with the assistance of Stanford University Libraries' HighWire Press®. Copyright 2006 by the International Anesthesia Research Society. Online ISSN: 1526-7598   Print ISSN: 0003-2999