Drug intelligence / Profile preview

amitriptyline

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intramuscular, Topical
01

Overview

Amitriptyline is a tricyclic antidepressant primarily used to treat major depressive disorder. It is also indicated for neuropathic pain syndromes (such as post-herpetic neuralgia), migraine and tension headache prophylaxis, and sometimes for eating disorders or nocturnal enuresis in children. Amitriptyline works by increasing the levels of certain neurotransmitters in the brain—mainly serotonin and norepinephrine—which helps regulate mood and pain perception[2][4][6]. The drug has strong anticholinergic effects, which contribute to its sedative properties but also increase side effects such as dry mouth, drowsiness, constipation, and weight gain[2][7]. Due to its side effect profile and toxicity risk in overdose, it is generally considered a second-line therapy for depression and pain conditions[2].

Brand names
ElavilEndepVanatrip
Other names
阿米替林
02

Targets

HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))NaV (Voltage-gated sodium channels)HRH1 (Histamine H1 Receptor)ADRA2A (α2A)M1 (Muscarinic acetylcholine receptor M1)MOR (Mu opioid receptor)ADRA1A (α1A)NMDAR (Glutamate receptor ionotropic, NMDA)NET (Norepinephrine Transporter)

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