Bupivacaine kinetic changes induced by diltiazem in mice.

Abstract:

:This study was designed to document possible changes in bupivacaine and its main metabolite, des-butyl-bupivacaine (PPX) kinetics in mice after a single 5 mg/kg injection of diltiazem. After a single 20 mg/kg i.p. dose of bupivacaine, kinetic parameters of bupivacaine were not statistically different but the ratio AUC PPX/AUC bupivacaine was significantly lower when bupivacaine was associated with diltiazem: thus, it may indicate an influence of diltiazem on bupivacaine metabolism i.e. an inhibition. Diltiazem also seems to increase the free fraction of bupivacaine and thus to decrease the percentage of protein binding. These effects may contribute to the enhanced toxicity previously observed.

journal_name

Life Sci

journal_title

Life sciences

authors

Bruguerolle B,Lorec AM

doi

10.1016/0024-3205(94)00601-6

subject

Has Abstract

pub_date

1994-01-01 00:00:00

pages

PL315-9

issue

19

eissn

0024-3205

issn

1879-0631

pii

0024-3205(94)00601-6

journal_volume

54

pub_type

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