The Sound of Evolution
Amitriptyline
阿米替林
Mechanism of action:
Amitriptyline 是一種三環抗憂鬱劑（tricyclic antidepressant，TCA）。Amitriptyline 的作用機制尚未完全清楚，其可能抑制突觸前神經末梢對正腦上腺素（norepinephrine）與血清素（serotonin）的回收，使這些神經傳導物質在突觸間濃度上升，增強其在中樞神經的神經傳導活性，進而影響與情緒調節及疼痛調控相關的神經路徑。Amitriptyline 亦可能拮抗多種受體，比如組織胺 H₁ 受體、毒蕈鹼型乙醯膽鹼受體（muscarinic acetylcholine receptor）、α₁-腎上腺素受體等。
Reference(s):
1. Grauer MT et al. (2004). P-glycoprotein reduces the ability of amitriptyline metabolites to cross the blood brain barrier in mice after a 10-day administration of amitriptyline. J Psychopharmacol.
2. O'Brien FE et al. (2013). Human P-glycoprotein differentially affects antidepressant drug transport: relevance to blood-brain barrier permeability. Int J Neuropsychopharmacol.
3. Abaut AY et al. (2007). Oral bioavailability and intestinal secretion of amitriptyline: Role of P-glycoprotein? Int J Pharm.