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Pharmacokinetics of lidocaine and bupivacaine and stable isotope labelled analogues: A study in healthy volunteers
Author(s) -
Burm A. G. L.,
Van Kleef J. W.,
Spierdijk J.,
De Boer A. G.,
Vermeulen N. P. E.,
De Leede L. G. J.,
Breimer D. D.
Publication year - 1988
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bod.2510090109
Subject(s) - lidocaine , bupivacaine , pharmacokinetics , chemistry , local anesthetic , chromatography , deuterium , anesthesia , pharmacology , medicine , physics , quantum mechanics
The pharmacokinetics of lidocaine and bupivacaine and tri‐deuteromethyl‐labelled lidocaine and bupivacaine were investigated in healthy volunteers. The deuterium‐labelled and the unlabelled form of the drug to be investigated were simultaneously infused in 10 min. Plasma concentrations were determined using a combination of capillary gas chromatography and mass fragmentography. Bi‐exponential functions were fitted to the plasma concentration‐time data. The mean distribution and elimination half‐lives were 8.4±5.9 min and 96±26 min for lidocaine, 9.2±7·0 min and 98±27 min for deuterium‐labelled lidocaine, 15.3±9·9 min and 111±32 min for bupivacaine, and 15.2 ± 10.9 min and 109±31 min for deuterium‐labelled bupivacaine, respectively. The mean volumes of the central compartment and mean steady state volumes of distribution were: lidocaine 37±151 and 97±201, deuterium‐labelled lidocaine 39±161 and 98±181, bupivacaine 27±111 and 66±231 and deuterium‐labelled bupivacaine 28±121, and 65±221, respectively. The respective mean plasma clearances were 0.88±0181 min −1 , 0.87±0.181 min −1 , 0.61±0.151 min −1 , and 0.62±0.171 min −1 . The results of the study indicate that substitution of a deuterated methyl group does not alter the pharmacokinetics of lidocaine and bupivacaine in healthy subjects.