Bioavailability, pharmacokinetics, and analgesic activity of ketamine in humans

J. A. Clements, W. S. Nimmo, I. S. Grant

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    241 Citations (Scopus)


    The pharmacokinetics of ketamine in analgesic doses after intravenous, intramuscular, and oral administration was investigated in healthy volunteers. Plasma ketamine concentration-time curves were fitted by a two-compartment open model with a terminal half-life of 186 min. Absorption after intramuscular injection was rapid and the bioavailability was 93%. However, only 17% of an oral dose was absorbed because of extensive first-pass metabolism. Simultaneous measurements of the elevation of pain threshold in an ischemic exercise test showed a marked effect for 15-60 min after intramuscular injection, but little or no effect after the oral solution. Pain threshold elevation occurred at plasma ketamine concentrations above 160 mg/ml.

    Original languageEnglish
    Pages (from-to)539-542
    Number of pages4
    JournalJournal of Pharmaceutical Sciences
    Issue number5
    Publication statusPublished - 1982


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