Drug intelligence / Profile preview

amisulpride + citalopram

Development stage
Preclinical
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Amisulpride + citalopram is a combination of two pharmaceutical agents used off-label in the management of depressive disorders, particularly in cases where monotherapy with citalopram (a selective serotonin reuptake inhibitor, SSRI) has failed to achieve adequate clinical response. Amisulpride is an atypical antipsychotic that acts primarily as a selective dopamine D2 and D3 receptor antagonist, with preferential activity in the limbic system. At low doses, it can enhance dopaminergic transmission by blocking presynaptic receptors, which may help alleviate negative symptoms or augment antidepressant effects. Citalopram is an SSRI that increases serotonergic neurotransmission by inhibiting the reuptake of serotonin at synaptic clefts. The rationale for combining these drugs lies in their complementary mechanisms—serotonergic enhancement from citalopram and dopaminergic modulation from amisulpride—which may provide benefit for treatment-resistant depression[1][7]. However, this combination carries a significant risk of QT interval prolongation and potentially life-threatening cardiac arrhythmias; thus, it should only be considered under close medical supervision[2][3][4].

02

Targets

HTR7 (5-hydroxytryptamine receptor 7)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)SERT allosteric site (Serotonin transporter allosteric site)SERT (Sodium-dependent serotonin transporter)

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