Pharmacokinetics of lidocaine and bupivacaine and stable isotope labelled analogues: A study in healthy volunteers

✍ Scribed by A. G. L. Burm; J. W. Van Kleef; J. Spierdijk; A. G. De Boer; N. P. E. Vermeulen; L. G. J. De Leede; D. D. Breimer

• Publisher: John Wiley and Sons
• Year: 1988
• Tongue: English
• Weight: 477 KB
• Volume: 9
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bod.2510090109

✦ Synopsis

The pharmacokinetics of lidocaine and bupivacaine and tri-deuteromethyl-labelled lidocaine and bupivacaine were investigated in healthy volunteers. The deuteriumlabelled 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 F 5.9 min and 96 * 26 rnin for lidocaine, 9-2 * 7.0 rnin and 98 F 27 min for deuterium-labelled lidocaine, 15.3 t 9-9 min and 111 k 32 rnin for bupivacaine, and 15.2 f 10.9 min and 109 k 31 min for deuterium-labelled bupivacaine, respectively. The mean volumes of the central compartment and mean steady state volumes of distribution were: lidocaine 37 f 15 1 and 97 k 20 I, deuteriumlabelled lidocaine 39 & 16 I and 98 * 18 I, bupivacaine 27 & 11 1 and 66 * 23 I and deuterium-labelled bupivacaine 28 & 12 I, and 65 +-22 I, respectively. The respective mean plasma clearances were 0.88 k 0.181 min-', 0.87 * 0.181 min-', 0.61 k 0.151 min-', and 0.62 k 0.17 I min-'. 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.