Drug intelligence / Profile preview

citalopram + nortriptyline

Development stage
Preclinical
Lead developer
Lundbeck
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Citalopram + nortriptyline is a combination of two antidepressant medications used together, primarily studied for the treatment of moderate-to-severe major depressive disorder. Citalopram is a selective serotonin reuptake inhibitor (SSRI) that increases serotonin levels in the brain by inhibiting its reuptake at the synaptic cleft. Nortriptyline is a tricyclic antidepressant (TCA) that inhibits the reuptake of both norepinephrine and serotonin, and also has antimuscarinic effects through action on acetylcholine receptors. The rationale for combining these agents is to achieve synergistic enhancement of serotonergic and noradrenergic neurotransmission, which may provide greater efficacy than monotherapy with either agent alone. Clinical studies have shown this combination can be more effective than citalopram alone in reducing depressive symptoms in patients with major depression[2][3]. However, this combination carries an increased risk for adverse effects such as serotonin syndrome and should be used with caution under specialist supervision[1][5].

02

Targets

mAChR (Muscarinic acetylcholine receptors)SERT allosteric site (Serotonin transporter allosteric site)NET (Norepinephrine Transporter)

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