Document Detail

Disposition of bupivacaine and its metabolites in the maternal, placental, and fetal compartments in rats.
MedLine Citation:
PMID:  11020763     Owner:  NLM     Status:  MEDLINE    
BACKGROUND: This study was designed to determine the disposition of bupivacaine and its metabolites in the maternal, placental, and fetal compartments, using multiple sampling time points in chronically prepared awake pregnant rats. METHODS: All animals received an intravenous infusion of bupivacaine at a rate of 0.33 mg. kg-1. min-1 over a period of 15 min. The fetuses were delivered either at the end of infusion or at 2 or 4 h after dosing. Maternal and fetal blood and tissue samples were obtained for the assays of bupivacaine and its metabolites using capillary gas chromatography-mass spectrometry. RESULTS: The elimination half-life of bupivacaine was 37.7 min. The major metabolite was 3'-hydroxybupivacaine. Bupivacaine and 3'-hydroxybupivacaine were present in all samples at the end of administration. The fetal to maternal concentration ratio of bupivacaine in plasma was 0.29, and in the placenta was 0.63. The amnion contained the highest bupivacaine concentration: threefold higher in the maternal and 11-fold higher than in the fetal plasma. At 4 h after dosing, bupivacaine was no longer detectable in any maternal and fetal samples, whereas 3'-hydroxybupivacaine was still present in all tissues except the fetal plasma and heart. CONCLUSIONS: These data indicate that a considerable amount of bupivacaine is taken up by both sides of the placenta, as well as the amnion and myometrium. 3'-Hydroxybupivacaine was present in all tissues except the fetal plasma and heart samples, even after the parent compound became no longer detectable. Whether this slow elimination of 3'-hydroxybupivacaine causes any adverse effects on the fetus-newborn needs to be explored.
H O Morishima; A Ishizaki; Y Zhang; R A Whittington; R F Suckow; T B Cooper
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Anesthesiology     Volume:  93     ISSN:  0003-3022     ISO Abbreviation:  Anesthesiology     Publication Date:  2000 Oct 
Date Detail:
Created Date:  2000-10-13     Completed Date:  2000-10-27     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  1300217     Medline TA:  Anesthesiology     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1069-74     Citation Subset:  AIM; IM    
Departments of Anesthesiology and Psychiatry, College of Physicians and Surgeons, Columbia University, New York, New York, USA.
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MeSH Terms
Amnion / metabolism
Anesthetics, Local / metabolism,  pharmacokinetics*,  pharmacology
Blood Pressure / drug effects
Bupivacaine / analogs & derivatives*,  metabolism,  pharmacokinetics*,  pharmacology
Fetus / metabolism*
Heart Rate / drug effects
Maternal-Fetal Exchange*
Myometrium / metabolism
Placenta / metabolism*
Rats, Sprague-Dawley
Tissue Distribution
Grant Support
Reg. No./Substance:
0/3-hydroxybupivacaine; 0/Anesthetics, Local; 2180-92-9/Bupivacaine

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