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Ropivacaine

羅哌卡因
Mechanism of action:
Ropivacaine 主要作用於阻斷神經細胞膜上的電壓門控鈉離子通道(voltage-gated Na⁺ channels)。Ropivacaine 在未離子化狀態下可穿越神經細胞膜,進入神經元內部後再轉為離子化型態,結合於鈉離子通道的內側結合位點,尤其偏好開啟或失活狀態(open/inactivated state)的通道,使鈉離子無法內流,神經細胞膜無法去極化(depolarization),導致動作電位無法產生與向前傳導。
Reference(s):
1. Liu BG et al. (2000). The effects of ropivacaine on sodium currents in dorsal horn neurons of neonatal rats. Anesth Analg.
2. Arlander E et al. (1998). Metabolism of ropivacaine in humans is mediated by CYP1A2 and to a minor extent by CYP3A4: an interaction study with fluvoxamine and ketoconazole as in vivo inhibitors. Clin Pharmacol Ther.
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