The effects of bupivacaine and pipecoloxylidide on platelet function in vitro.
The influence of bupivacaine and its major metabolite, pipecoloxylidide, on human platelet function was studied in vitro. Significant inhibition of ADP and collagen-induced platelet aggregation occurred only with concentrations of bupivacaine above 10 micrograms.ml-1. This concentration (10-25 micrograms.ml-1) is much higher than would be expected in routine clinical use of bupivacaine for epidural analgesia. The inhibition of platelet aggregation was associated with a significant decrease in beta-thromboglobulin secretion. In contrast, pipecoloxylidide had no effect on platelet aggregation or the beta-thromboglobulin release. We conclude that the previously reported 30-min time-lag between the maximal plasma concentration of bupivacaine and the inhibition of platelet aggregation is unlikely to be due to a metabolism of bupivacaine to pipecoloxylidide.
Odoom
J A
JA
Department of Anaesthesia, University of Amsterdam, The Netherlands.
Sturk
A
A
Dokter
P W
PW
Bovill
J G
JG
ten Cate
J W
JW
Oosting
J
J
D000328:Adult; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism / Q000502:physiology; D002045:Bupivacaine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D001620:beta-Thromboglobulin / Q000378:metabolism
D010975:Platelet Aggregation Inhibitors; D001620:beta-Thromboglobulin; C025149:2',6'-pipecoloxylidide; D002045:Bupivacaine