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British Journal of Anaesthesia, 2004, Vol. 92, No. 2 218-222
© 2004 The Board of Management and Trustees of the British Journal of Anaesthesia


Clinical Investigations

Pharmacokinetics of levobupivacaine 0.25% following caudal administration in children under 2 years of age{dagger}

G. A. Chalkiadis*,1, R. L. Eyres1, N. Cranswick2, R. H. Taylor3 and S. Austin3

1 Department of Anaesthesia and Pain Management, and 2 Clinical Pharmacology, Department of General Paediatrics, University of Melbourne, Royal Children’s Hospital, Flemington Road, Parkville 3052, Victoria, Australia. 3 Department of Anaesthesia, Royal Belfast Hospital for Sick Children, 180 Falls Road, Belfast, BT12 6 BE, UK

*Corresponding author. E-mail:george.chalkiadis@rch.org.au
{dagger}Declaration of interest. This work was funded by Chiroscience Limited, Cambridge, UK.

Background. Levobupivacaine, the S(–)enantiomer of racemic bupivacaine is less cardiotoxic than racemic bupivacaine and the R(+)enantiomer dexbupivacaine, while retaining similar local anaesthetic properties and potency to racemic bupivacaine. The pharmacokinetic profiles of the two bupivacaine enantiomers differs and that of racemic bupivacaine may be age dependent. We examined the pharmacokinetics of levobupivacaine after its single shot caudal epidural administration in children.

Methods. An open-label phase 2 study was undertaken to examine the pharmacokinetics of levobupivacaine 0.25% 2 mg kg–1 in 49 children aged less than 2 yr, after single shot caudal epidural administration. Plasma concentrations were determined at intervals up to 60 min after caudal injection.

Results. Time to peak plasma concentration (Tmax) ranged between 5 and 60 min (median 30 min) and was reached later in children aged less than 3 months (P<0.005). Peak plasma concentration (Cmax) ranged between 0.41 and 2.12 µg ml–1 (median 0.80, mean (SD) 0.91 (0.40) µg ml–1).

Conclusion. After the caudal epidural administration of levobupivacaine 2 mg kg–1 in children less than 2 yr of age, Cmax was within the accepted safe range for racemic bupivacaine. Tmax varied and occurred later in some children, particularly those aged less than 3 months. Sampling in future pharmacokinetic studies in this age group should extend beyond 60 min.

Br J Anaesth 2004; 92: 218–22


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