Comparative canine pharmacokinetics-pharmacodynamics of fospropofol disodium injection, propofol emulsion, and cyclodextrin-enabled propofol solution following bolus parenteral administration

Journal of Pharmaceutical Sciences
Michelle P McIntosh, Roger A Rajewski

Abstract

The pharmacokinetics and pharmacodynamics of fospropofol (FP) disodium injection, propofol emulsion (PE), and cyclodextrin-enabled propofol (CDP) solution following bolus parenteral administration in dogs was evaluated. Three healthy male beagle dogs were treated in a three-way cross-over study (14 day washout period) with 6 mg/kg propofol equivalents. Blood samples were collected predose and at 16 points postdose through 1440 min and analyzed for propofol and FP, when appropriate. From 5 min predose to 30 min postdose, brain electrical activity [electroencephalography (EEG)] was recorded and analyzed by power spectrum analysis techniques. Each formulation appeared to be well tolerated with transient discomfort observed in the PE and CDP animals and minor excitability in the FP animals prior to loss of consciousness. Blood propofol followed three-compartment pharmacokinetic behavior and derived parameters were not statistically different except for elimination half-life from the CDP formulation and onset, and duration of anesthesia from the FP formulation. The effect site concentrations at 50% the maximum EEG effect for the FP and CDP formulations were approximately one-half that of the PE formulation. Onset and duration of ane...Continue Reading

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Citations

Jan 24, 2014·Journal of Zoo and Wildlife Medicine : Official Publication of the American Association of Zoo Veterinarians·Carrie A Schroeder, Rebecca A Johnson
Apr 27, 2017·Journal of Veterinary Emergency and Critical Care·Susan Blades Golubovic, John H Rossmeisl
Jun 11, 2015·The Journal of Pharmacy and Pharmacology·Thorsteinn LoftssonAngel Concheiro
Oct 19, 2020·Journal of Pharmaceutical Sciences·Thorsteinn Loftsson
May 5, 2021·Veterinary Anaesthesia and Analgesia·Nathaniel KapaldoEmily Klocke

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