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KMID : 0378120030300010001
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Chungnam Medical Journal
2003 Volume.30 No. 1 p.1 ~ p.8
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Effects of Bupivacaine and Ropivacaine on HERG Current Expressed in Xenopus Oocyte
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Kim Cuk-Seong
Lee Kyoo-Seong
Kim Hyo-Shin
Son Sook-Jin
Lee Sang-Do
Kim Kwang-Jin
Jeon Byeong-Hwa
Kim Yoon-Hee
Park Jin-Bong
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Abstract
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Bupivacaine is an amide-type local anesthetic widely used for regional anesthesia. Ropivacaine is developed as a less cardiotoxic alternatives to bupivacaine. In the present study, we have analyzed the effects of bupivacaine and ropivacaine on HERG currents expressed in Xenopus oocytes.
Bupivacaine and ropivacaine(3∼1,000μM) blocked HERG currents in a concentration dependent manner. EC_(50) was 26.1±3.1μM(n_(R) 0.65±0.04) and 43.5±7.9μM(n_(H) 0.99±0.13) in bupivacaine and ropivacaine, respectively. Bupivacaine and ropivacaine did not affect the activation and deactivation kinetics of HERG channels. However, the drugs decreased the slope conductance measured from fully activated current-voltage relationship curves. These results suggest that bupivacaine and ropivacaine have a similarinhibitory effect on HERG channels, which could be a possible cellular mechanism of LQT or ventricular arrythmia by the drugs.
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KEYWORD
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Bupivacaine, Ropivacaine, HERG
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