CHRONOPHARMACOKINETIC STUDY OF LIDOCAINE IN THE RAT

  • 1 January 1982
    • journal article
    • research article
    • Vol. 13  (1) , 65-76
Abstract
The influence of the hour of administration on lidocaine [a local anesthetic and antiarrhythmic agent] kinetics was studied in the rat. A single 50-mg/kg dose of lidocaine was given i.m., at 4 different fixed time points of a 24-h period (i.e., 1000, 1600, 2200 and 0400 h) to 70 rats. AT each specified time point blood samples were taken 5, 15, 30 min, 1, 2, 4 and 6 h after the drug administration. Lidocaine plasma levels (free and bound) were determined according to a specific gas chromatographic method. Lidocaine-free fraction varied with time, and the protein binding of lidocaine showed a circadian variation. The observed variations may be related to daily fluctuations of absorption or binding of the drug, diurnal variation of the hepatic drug metabolizing enzymes responsible for the inactivation of the drug and/or diurnal variations in excretion rate of lidocaine.

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