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Pharmacokinetics of Intravenous Procaine Infusion in Humans

Astride B. Seifen, MD^*, Alfredo A. Ferrari, MD, Ernst E. Seifen, MD, Dola S. Thompson, MD, and John Chapman, BS^||

Department of Anesthesiology, University of Arkansas for Medical Sciences, 4301 West Markham, Little Rock, Arkansas 72201.

Abstract

Pharmacokinetic data during and following the continuous intravenous infusion of procaine are lacking. We studied 12 women undergoing hysterectomy during N₂O-O₂ and narcotic anesthesia. A constant infusion of 2% procaine was administered at a rate of 1 mg/kg/min to six patients (group I) and at a rate of 1.5 mg/kg/min to the other six (group II). Procaine plasma levels were determined by flame ionization gas-liquid chromatography. Using a two-compartment pharmacokinetic model, disposition kinetics were studied. Steady-state plasma levels were achieved within 20 to 30 minutes after commencement of the infusion. Following termination of the infusion the drug disappeared with a distribution half-life (t ) of 2.49 ± 0.36 minutes and an elimination half-life (tß) of 7.69 ± 0.99 minutes at both infusion rates. In group I, the fraction of drug in the central compartment was 65%, the volume of distribution at steady-state was 0.79 ± 0.14 L/kg, and total body clearance 0.08 ± 0.01 L/kg/min. In group II, the fraction of drug in the central compartment was 82%, the volume of distribution at steady-state 0.34 ± 0.07 L/kg, and the total body clearance 0.04 ± 0.01 L/kg/min. These data indicate that procaine is a drug of limited distribution and tissue uptake with a short duration of action.

Key Words: ANESTHETICS, Local: procaine • PHARMACOKINETICS: intravenous procaine

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