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| Title | Differential stereoselective effects of levobupivacaine, bupivacaine and dexbupivacaine on the heart in isolated rat hearts |
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| Subtitle | 原著 |
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| Authors | Kazuya Urashima*, Yoshiro Sohma**, Yoshio Ijiri***, Shiori Terai****, Takashi Umeda**, Yuka Kawakami*, Takako Nishihori*, Yoshihiko Hirotani*, Kazuhiko Tanaka* |
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| Authors(kana) | |
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| Organization | *Department of Clinical Pharmacy and Clinical Pharmacokinetics, Osaka University of Pharmaceutical Sciences, **Department of Physiology, Osaka Medical College, ***Department of Pharmacy, Osaka Medical College Hospital, *****Department of Hygienic Chemistry, Osaka University of Pharmaceutical Sciences, ******Department of Clinical Acupuncture, Kansai College of Oriental Medicine
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| Journal | Circulation Control |
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| Volume | 26 |
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| Number | 2 |
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| Page | 140-147 |
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| Year/Month | 2005/6 |
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| Article | Original article |
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| Publisher | Japan Society of Circulation Control |
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| Abstract | Bupivacaine (BUP) has an advantage over other local anesthetics because of its long-acting sensory anesthesia, but because of its high affinity for the myocardial Na+ channel it can be cardiotoxic. Levobupivacaine(LBUP) is an S(-)-isomer of the racemate BUP, and dexbupivacaine(DBUP) is an R(+) isomer. LBUP has less neuronal and cardiac toxiclty than BUP and DBUP, but DBUP induces more negative chronotropism and arrhythmogenic effects than either LBUP or BUP. We thus investigated the effects of LBUP, BUP and DBUP on the heart using isolated perfused rat hearts by measuring tissue ion contents. Using the Langendorff perfusion-system, each isolated rat heart was perfused with Krebs-Henseleit buffer containing varlous concentrations of LBUP, BUP and DBUP(0.5, 1.0, 5.0μg/ml) for 10 minutes. Thereafter, each heart was subjected to regional ischemia(11min) and reperfusion(3min). In other experiments using an atomic absorption spectrometer, we measured tissue Na+ Ca2+, and K+ contents in rat heart. There were significant differences in decreases of heart rate among the BUP formulations, showing reduction in the order LBUP>BUP>DBUP, and they had a protective effect agalnst reperfusion-induced arrhythmias. In the experiment on the total tissue ion contents, significant differences were observed, particularly in Na+ content, showing the reduction in the order LBUP>BUP>DBUP. It is suggested that there may be differences in Na+ channel-blocking action, whlch affects conduction systems and protective effects against reperfuslon-induced arrhythmias among the BUP formulations. |
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| Practice | Basic medicine |
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| Keywords | bupivacaine, levobupivacaine, dexbupivacaine, heart rate, ion |
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