Drug intelligence / Profile preview

protriptyline

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

Overview

Protriptyline is a tricyclic antidepressant (TCA) used primarily for the treatment of depression and, in some cases, anxiety. It is classified as a secondary amine TCA and works by inhibiting the reuptake of norepinephrine and serotonin in the central nervous system, thereby increasing their levels in the brain[1][2][3][4][6]. This action enhances serotonergic neurotransmission, which is believed to underlie its antidepressant effects. Protriptyline also blocks histamine H1 receptor, alpha-1 adrenergic receptor, and muscarinic receptor—contributing to its side effect profile including anticholinergic effects such as dry mouth and urinary retention[4]. Compared to other TCAs, it tends to be less sedating[1]. Protriptyline has also been used off-label for conditions such as attention-deficit/hyperactivity disorder (ADHD), panic disorder, obsessive-compulsive disorder (OCD), enuresis (bedwetting), bulimia nervosa, cocaine dependency, bipolar depression phase, and as support in smoking cessation programs[5].

Brand names
Vivactil
Other names
protriptyline hydrochloride
02

Targets

ADRA1A (α1A)DAT (Dopamine plasma membrane transport protein)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)

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