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Bupivacaine

布比卡因
Mechanism of action:
Bupivacaine 是一種醯胺類(amide)衍生物。Bupivacaine 進入神經細胞後,會在軸突內部轉化為帶正電的離子型,此離子型藥物會結合在電壓門控鈉離子通道(voltage-gated Na⁺ channel)的內側結合位點(S6 segment),穩定通道的不活化狀態,使動作電位無法產生與傳導,導致感覺、運動與自主神經訊號暫時中斷。
Reference(s):
1. Rosenblatt MA et al. (2006). Successful use of a 20% lipid emulsion to resuscitate a patient after a presumed bupivacaine-related cardiac arrest. Anesthesiology.
2. Picard J et al. (2006). Lipid emulsion to treat overdose of local anaesthetic: the gift of the glob. Anaesthesia.
3. Zhang H et al. (2014). Voltage-dependent blockade by bupivacaine of cardiac sodium channels expressed in Xenopus oocytes. Neurosci Bull.
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