Document Detail

Comparison of the effects of bupivacaine and ropivacaine on heart cell mitochondrial bioenergetics.
MedLine Citation:
PMID:  9605695     Owner:  NLM     Status:  MEDLINE    
BACKGROUND: High lipophilic local anesthetics interfere with mitochondrial energy metabolism. These metabolic effects could in part explain some of the toxic effects of local anesthetics, such as bupivacaine-induced myocardial depression. The aim of this study was to compare the bioenergetic effects of the local anesthetics bupivacaine and ropivacaine. METHODS: The effects of both local anesthetics on mitochondrial energy metabolism were studied in rat heart isolated mitochondria and in saponin-skinned left ventricle fibers. Oxygen consumption, adenosine triphosphate synthesis, and enzymatic activities of the complexes of the respiratory chain were measured. RESULTS: Bupivacaine and ropivacaine acted, in isolated mitochondria, as uncouplers between oxygen consumption and phosphorylation of adenosine diphosphate. Further, an inhibitory effect of mitochondrial respiration was evidenced with both anesthetics during maximal respiration and was assigned to a direct inhibition of complex I of the respiratory chain. Mitochondrial adenosine triphosphate synthesis was decreased by both mechanisms. However, both in isolated mitochondria and in permeabilized heart fibers, ropivacaine was less potent than bupivacaine. Adenosine triphosphate synthesis was completely suppressed at 3 mM (approximately 0.1%) bupivacaine, whereas 3 mM ropivacaine induced only about a 40% inhibition. CONCLUSIONS: Ropivacaine disturbs mitochondrial energy metabolism less than bupivacaine does. The lower lipid solubility of ropivacaine may be responsible for the lesser dose-dependent effects of this drug on mitochondrial bioenergetics.
F Sztark; M Malgat; P Dabadie; J P Mazat
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Publication Detail:
Type:  Comparative Study; In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anesthesiology     Volume:  88     ISSN:  0003-3022     ISO Abbreviation:  Anesthesiology     Publication Date:  1998 May 
Date Detail:
Created Date:  1998-06-16     Completed Date:  1998-06-16     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1300217     Medline TA:  Anesthesiology     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1340-9     Citation Subset:  AIM; IM    
Laboratoire d'Anesthésiologie (C.J.F. INSERM 9705), Université Victor Segalen Bordeaux 2 and Hôpital Pellegrin, France.
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MeSH Terms
Amides / pharmacology*
Anesthetics, Local / pharmacology*
Bupivacaine / pharmacology*
Dose-Response Relationship, Drug
Energy Metabolism / drug effects
Mitochondria, Heart / drug effects*,  enzymology,  metabolism,  ultrastructure
Oxidative Phosphorylation / drug effects
Oxygen Consumption / drug effects
Rats, Wistar
Reg. No./Substance:
0/Amides; 0/Anesthetics, Local; 2180-92-9/Bupivacaine; 84057-95-4/ropivacaine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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