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Korean Journal of Anesthesiology 1988;21(1):102-116.
DOI: https://doi.org/10.4097/kjae.1988.21.1.102   
Effects of Bupivacaine on Calcium Transport Across Biological Membranes and Its Cardiotoxicity .
Byoung Youn Jeoung, Ku Ja Kim
1Department of Anesthesiology, Catholic University, School of Medicine, Seoul, Korea.
2Department of Anesthesiology, Ewha Womans University, College of Medicine, Seoul, Korea.
Abstract
A new local anesthetic, bupivacaine, is widely used for regional anesthesia because of its high potency and long duration of action. However, bupivacaine is reported to result in cardiovascular collapse associated with convulsion at a plasma concentration above the normal one, while other local anesthetics do not. Also resuscitation is very difficult. Although the mechanism of this action is not known, bupivacaine seems to have an influence on Ca2+ transport across cell membranes via various pathways. The present study was designed to evaluate the effects of bupivacaine on Ca2+ transport across cell membranes. The results are as follows: 1) Bupivacaine inhibites Ca2+ uptake by SR of skeletal muscle. 2) Bupivacaine suppressed the Bowditch and Woodworth staircase phenomena in a guines pig's left auricle, however this was reversible even at convulsant doses. 3) Bupivacaine also suppressed the Na+-Ca2+ exchange pump on guines pig's left auricle. 4) Bupivacaine increased the Ca2+-ATPase activity by SR of skeletal muscle. 5) At concentrations above 3ug/ml, bupivacaine induced cardiac arrhythmia. These findings suggest that bupivacaine-induced cardiotoxicity is possibly due to a Ca2+- channel blockade, depression of the Na+-Ca2+ pump, inhibition of Ca2+ uptake by SR and subsequent decrease of intracellular Ca2+ concentration.
Key Words: Anesthetics-local; bupivacaine; Ca2+ transport; Cardiotoxicity


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