Drug intelligence / Profile preview

bupropion + mirtazapine

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

Overview

Bupropion + mirtazapine is a combination of two antidepressant medications used together, primarily for the treatment of major depressive disorder (MDD), especially in cases resistant to monotherapy. Bupropion is an aminoketone class antidepressant that acts as a norepinephrine and dopamine reuptake inhibitor, resulting in increased levels of these neurotransmitters in the brain. It is considered activating and may be particularly effective for patients with depression characterized by hypersomnia, fatigue, increased appetite, or weight gain. Mirtazapine is a tetracyclic antidepressant that works mainly as an antagonist at central presynaptic alpha-2 adrenergic inhibitory autoreceptors and heteroreceptors (increasing noradrenergic and serotonergic activity), as well as antagonizing certain serotonin receptors (5-HT2 and 5-HT3) and histamine H1 receptors. This profile gives it sedative properties and makes it more effective for patients with insomnia, decreased appetite, or weight loss associated with depression. The combination has been studied from treatment initiation in randomized controlled trials; results suggest higher remission rates compared to monotherapy with selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine. The combination may be considered when rapid symptom control or broader symptom coverage is needed[3][7]. However, there are potential drug interactions between bupropion and mirtazapine that require careful monitoring due to the risk of adverse effects[1].

02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)ADRA2C (α2C)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)HTR2A (Serotonin receptor 5-HT2A)HRH1 (Histamine H1 Receptor)ADRA2A (α2A)ADRA2B (α2B)HTR2C (5-hydroxytryptamine 2C receptor)DAT (Dopamine plasma membrane transport protein)α3β2 nAChR (α3β2 nicotinic receptor)NET (Norepinephrine Transporter)

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