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Meclizine

美克洛嗪
Mechanism of action:
Meclizine 是一種第一代 H₁ 受體拮抗劑(H₁ receptor antagonist),並具有抗膽鹼(anticholinergic)特性。Meclizine 阻斷中樞神經系統中的 H₁ 受體,特別是前庭核(vestibular nuclei)與延腦嘔吐中樞,減弱來自內耳前庭器官的異常刺激傳入,從而降低前庭相關訊號對嘔吐中樞的驅動。Meclizine 亦可輕度拮抗毒蕈鹼型乙醯膽鹼受體(muscarinic acetylcholine receptor),進一步抑制前庭系統對嘔吐中樞的刺激,加強其對暈動/嘔吐反射的抑制作用。
Reference(s):
1. Amini A et al. (2015). Histamine Antagonists for Treatment of Peripheral Vertigo: A Meta-Analysis. J Int Adv Otol.
2. Wang Z et al. (2012). Meclizine metabolism and pharmacokinetics: formulation on its absorption. J Clin Pharmacol.
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