Drug intelligence / Profile preview

Imipramine oxide

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Imipramine oxide (also known as imipraminoxide or imipramine N-oxide) is a tricyclic antidepressant (TCA) that was introduced in Europe in the 1960s for the treatment of depression. It is both an analogue and a metabolite of imipramine and shares similar pharmacological effects. Compared to its parent compound, clinical trials have shown that it has a faster onset of action, slightly higher efficacy, and fewer or less pronounced side effects—particularly reduced orthostatic hypotension and anticholinergic symptoms such as dry mouth, sweating, dizziness, and fatigue. The precise pharmacology is not fully elucidated but is presumed to be similar to that of imipramine; it likely acts as an inhibitor of serotonin and norepinephrine reuptake while antagonizing serotonin, adrenergic (adrenaline), histamine, and muscarinic acetylcholine receptors with weaker antiadrenergic and anticholinergic actions than its parent drug. Imipraminoxide has also been described as a prodrug for imipramine[1].

Brand names
ImiprexElepsin
Other names
imipraminoxideimipramine N-oxide
02

Targets

AR (Adrenergic receptors)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)NET (Norepinephrine Transporter)5-HT (Serotonin receptors)SERT (Sodium-dependent serotonin transporter)H (Histamine receptors)

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