Guanfacine

胍法辛
Mechanism of action:
Guanfacine 是一種選擇性 α₂A-腎上腺素受體促效劑(selective α₂A-adrenergic receptor agonist)。Guanfacine 對 α₂A 次型具有高度選擇性,特別作用於前額葉皮質(prefrontal cortex)和腦幹血管運動中樞的突觸後 α₂A 受體。當 guanfacine 活化 α₂A 受體後,對於前額葉皮質可調節前額葉神經網路的訊號傳遞並降低過度雜訊,增強與執行功能相關的神經活動效率;對於腦幹血管運動中樞,會透過抑制交感神經的神經元活性,抑制正腎上腺素(norepinephrine)的釋放,進而降低交感神經輸出。
Reference(s):
1. Cruz MP et al. (2010). Guanfacine Extended-Release Tablets (Intuniv), a Nonstimulant Selective Alpha(2A)-Adrenergic Receptor Agonist For Attention-Deficit/Hyperactivity Disorder. P T.
2. Kirch W et al. (1980). Elimination of guanfacine in patients with normal and impaired renal function. Br J Clin Pharmacol.
3. Minns AB et al. (2010). Guanfacine overdose resulting in initial hypertension and subsequent delayed, persistent orthostatic hypotension. Clin Toxicol (Phila).
