Drug intelligence / Profile preview

dosulepin + sertraline

Development stage
Unknown
Lead developer
Spofa
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two antidepressant drugs, dosulepin (also known as dothiepin) and sertraline. Dosulepin is a tricyclic antidepressant (TCA) that acts primarily as a serotonin–norepinephrine reuptake inhibitor, with additional antihistamine, anticholinergic, antiadrenergic, antiserotonergic, and sodium channel-blocking effects[2][5]. Sertraline is a selective serotonin reuptake inhibitor (SSRI) that increases serotonergic activity in the central nervous system by inhibiting the presynaptic reuptake of serotonin[3]. Both are used for the treatment of depression; sertraline is also indicated for obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, social anxiety disorder, and premenstrual dysphoric disorder. The combination does not have an established unique indication or brand formulation; co-administration may be considered in rare clinical scenarios but carries significant risk due to pharmacokinetic interactions—SSRIs like sertraline can increase plasma levels of TCAs like dosulepin—and increased risk of side effects including serotonin syndrome[4][6][7].

Other names
dosulepin and sertralinedothiepin and sertraline
02

Targets

SERT (Sodium-dependent serotonin transporter)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)M1 (Muscarinic acetylcholine receptor M1)SCN5A (Sodium channel protein type 5 subunit alpha)NET (Norepinephrine Transporter)

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