Drug intelligence / Profile preview

amitriptylinoxide

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral
01

Overview

Amitriptylinoxide is a tricyclic antidepressant (TCA) introduced in Europe in the 1970s for the treatment of depression. It is both an analogue and metabolite of amitriptyline and exhibits similar antidepressant efficacy but with a faster onset of action and fewer adverse effects compared to its parent compound. Amitriptylinoxide acts primarily as a serotonin and norepinephrine reuptake inhibitor, serotonin receptor antagonist, and H1 receptor antagonist. It has significantly lower affinity for α1-adrenergic receptors (about 60-fold less than amitriptyline) and shows the weakest affinity among TCAs for muscarinic acetylcholine receptors, resulting in reduced anticholinergic side effects such as dry mouth or dizziness. Amitriptylinoxide may also function as a prodrug of amitriptyline[2][5][6].

Brand names
AmioxidAmbivalonEquilibrin
Other names
amitriptyline N-oxideamitriptylinoxide
02

Targets

NET (Norepinephrine Transporter)5-HT (Serotonin receptors)SERT (Sodium-dependent serotonin transporter)

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