1999
DOI: 10.1097/00000542-199903000-00027
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Interaction of Bupivacaine and Tetracaine with the Sarcoplasmic Reticulum Ca2+Release Channel of Skeletal and Cardiac Muscles 

Abstract: Bupivacaine's ability to enhance Ca2+ release channel-ryanodine receptor activity of skeletal muscle sarcoplasmic reticulum most likely contributes to the myotoxicity of this local anesthetic. Thus, the pronounced myotoxicity of bupivacaine may be the result of this specific effect on Ca2+ release channel-ryanodine receptor superimposed on a nonspecific action on lipid bilayers to increase the Ca2+ permeability of sarcoplasmic reticulum membranes, an effect shared by all local anesthetics. The specific action … Show more

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Cited by 67 publications
(42 citation statements)
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“…30,31 Alteration of the SR by LAAs may occur at the level of the SR Ca 2+ release channelryanodine receptor (RyR) or with the calcium reuptake, 30,[32][33][34] and could be responsible for a decrease in amplitude of contraction and/or increase in the duration of contraction. 34 We observed an increase in time-to-peak-shortening (isotony) and time-to-peakforce (isometry) that were compatible with alteration of RyR (increase time to release Ca 2+ ). This result is in agreement with the findings of Mio et al 31 who described an increase in time-to-peak-light by measuring variation of calcium content with aequorin light intensity measurements.…”
Section: Discussionmentioning
confidence: 99%
“…30,31 Alteration of the SR by LAAs may occur at the level of the SR Ca 2+ release channelryanodine receptor (RyR) or with the calcium reuptake, 30,[32][33][34] and could be responsible for a decrease in amplitude of contraction and/or increase in the duration of contraction. 34 We observed an increase in time-to-peak-shortening (isotony) and time-to-peakforce (isometry) that were compatible with alteration of RyR (increase time to release Ca 2+ ). This result is in agreement with the findings of Mio et al 31 who described an increase in time-to-peak-light by measuring variation of calcium content with aequorin light intensity measurements.…”
Section: Discussionmentioning
confidence: 99%
“…In addition, local anesthetics can either decrease [22,23] or increase Ca 2+ mobilization [24] from the sarcoplasmic reticulum and also decrease the sensitivity of myofilaments to Ca 2+ [25]. The stereoselective effects induced by the bupivacaine isomers, R(+) and S(−), have been intensively studied to determine which causes less cardiotoxicity while still providing potent nerve blockade.…”
Section: Discussionmentioning
confidence: 99%
“…Die kanalvermittelte Ca 2+ -Freisetzung dominiert quantitativ: Dieses Wissen beruht v. a. auf den Beobachtungen, dass zum einen die Inkubation von SR-Vesikeln mit Rutheniumrot, einem potenten Inhibitor des Ca 2+ -Freisetzungskanals, die lokalanästhetikainduzierte Ca 2+ -Release aus diesen Organellen nicht vollständig verhindern kann [40]. Zum anderen konnten Komai [27]. Gestützt werden diese Befunde durch die Tatsache, dass höher konzentriertes Bupivacain (10 mM) kultivierte Myozyten irreversibel schädigt; dagegen werden keine derartigen Effekte bei der Verwendung niedrigerer Konzentrationen (≤0,75 mM) beobachtet [27].…”
Section: Subzelluläre Aspekteunclassified