Drug intelligence / Profile preview

dosulepin

Development stage
Phase 4
Lead developer
Spofa
Modality
Small Molecules
Administration
Oral
01

Overview

Dosulepin is a tricyclic antidepressant (TCA) primarily used for the treatment of major depressive disorder, and occasionally for certain types of nerve pain (such as fibromyalgia) and migraine prevention. It acts mainly as a serotonin–norepinephrine reuptake inhibitor, increasing the levels of these neurotransmitters in the synaptic cleft. Additionally, it exhibits antihistamine, anticholinergic, antiadrenergic, antiserotonergic, and sodium channel-blocking properties. Due to its relatively high toxicity in overdose and low therapeutic index compared to other TCAs, its use is generally reserved for patients unresponsive or intolerant to alternative therapies. Developed by SPOFA in the 1960s and first introduced in 1969 in the UK, dosulepin remains available in several European countries as well as Australia, South Africa, New Zealand, India and others but is not approved or marketed in the United States or Canada[1][3][4][5].

Brand names
ProthiadenDothiepinDopressDothepThadenAltapinDepresymDothapaxIdomPrepadineProtiadenProtiadeneXerenal
Other names
DosulepinaDosulépineDosulepinumDosulepin hydrochlorideDothiepin hydrochloride
02

Targets

ADRA1A (α1A)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)ADRA1 (Alpha-1 adrenergic receptor family)SCN5A (Sodium channel protein type 5 subunit alpha)

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