Drug intelligence / Profile preview

fluoxetine + imipramine

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Fluoxetine + imipramine is a combination of two antidepressant drugs, each with distinct mechanisms of action. Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) that increases synaptic serotonin levels by inhibiting its reuptake in the central nervous system. Imipramine is a tricyclic antidepressant (TCA) that inhibits the reuptake of both serotonin and norepinephrine, while also blocking histamine H1, α1-adrenergic, and muscarinic receptors. This combination may be considered in treatment-resistant depression but carries significant risk for adverse effects such as sedation, anticholinergic symptoms (dry mouth, blurred vision, constipation), and potentially life-threatening interactions like serotonin syndrome due to additive serotonergic activity[1][6][8]. The use of this combination should be closely monitored by healthcare professionals.

02

Targets

SERT allosteric site (Serotonin transporter allosteric site)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)ADRA1A (α1A)CHRM2 (M2)NET (Norepinephrine Transporter)

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