Pharmacokinetics of levobupivacaine 0.25% following caudal administration in children under 2 years of age.

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 (T(max)) 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 (C(max)) ranged between 0.41 and 2.12 micro g ml(-1) (median 0.80, mean (SD) 0.91 (0.40) micro g ml(-1)).

CONCLUSION

After the caudal epidural administration of levobupivacaine 2 mg kg(-1) in children less than 2 yr of age, C(max) was within the accepted safe range for racemic bupivacaine. T(max) 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.