• Karin P W Schoenmakers, Tom B Vree, Nigel T M Jack, Bart van den Bemt, Jacques van Limbeek, and Rudolf Stienstra.
• Department of Anesthesiology, Sint Maartenskliniek, Hengstdal 3, 6574 NA, Nijmegen, The Netherlands.
• Br J Clin Pharmacol. 2013 May 1;75(5):1321-7.

AimsNo pharmacokinetic data exist on doses of ropivacaine larger than 300 mg for peripheral nerve block in man, although in clinical practice higher doses are frequently used. The purpose of the present study was to describe the pharmacokinetic profile in serum of 450 mg ropivacaine with and without epinephrine in patients undergoing anterior cruciate ligament reconstruction.MethodsTwelve patients were randomly allocated to receive a single shot combined sciatic/femoral nerve block with 60 ml of either ropivacaine 0.75% alone (group R, n = 6) or ropivacaine 0.75% plus epinephrine 5 μg ml(-1) (group RE, n = 6). Venous blood samples for total and free ropivacaine serum concentrations were obtained during 48 h following block placement. Pharmacokinetic parameters were calculated using a non-compartmental approach.ResultsResults are given as mean (SD) for group R vs. group RE (95% CI of the difference). Total Cmax was 2.81 (0.94) μg ml(-1) vs. 2.16 (0.21) μg ml(-1) (95% CI -0.23, 1.53). tmax was 1.17 (0.30) h vs. 1.67 (0.94) h (95% CI -1.40, 0.40). The highest free ropivacaine concentration per patient was 0.16 (0.08) μg ml(-1) vs. 0.12 (0.04) μg ml(-1) (95% CI -0.04, 0.12). t(1/2) was 6.82 (2.26) h vs. 5.48 (1.69) h (95% CI -1.23, 3.91). AUC was 28.35 (5.92) μg ml(-1)  h vs. 29.12 (7.34) μg ml(-1)  h (95% CI -9.35, 7.81).ConclusionsFree serum concentrations of ropivacaine with and without epinephrine remained well below the assumed threshold of 0.56 μg ml(-1) for systemic toxicity. Changes in pharmacokinetics with epinephrine co-administration did not reach statistical significance.© 2012 The Authors. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society.

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