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Palonosetron

帕洛諾司瓊
Mechanism of action:
Palonosetron 是一種第二代血清素 5-HT₃ 受體拮抗劑(second-generation 5-HT₃ receptor antagonist)。化療或放療會刺激腸道的腸嗜鉻細胞(enterochromaffin cell),導致釋放大量血清素(5-HT),血清素作用於腸道迷走神經末梢上的 5-HT₃ 受體,訊號傳入延腦嘔吐中樞,引起嘔吐。Palonosetron 的作用為高親和力結合 5-HT₃ 受體,誘導受體內化(internalization),使訊號長期受到抑制,以抑制嘔吐反射。
Reference(s):
1. De Leon A et al. (2006). Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting. Proc (Bayl Univ Med Cent).
2. Stoltz R et al. (2004). Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol.
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