Drug intelligence / Profile preview

dextroamphetamine + venlafaxine

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

Overview

dextroamphetamine + venlafaxine is a combination of two pharmaceutical agents used off-label in certain neuropsychiatric contexts, particularly when both attention-deficit/hyperactivity disorder (ADHD) and major depressive disorder (MDD) are present. Dextroamphetamine is a central nervous system stimulant that increases synaptic concentrations of dopamine and norepinephrine by promoting their release and inhibiting reuptake. Venlafaxine is a serotonin-norepinephrine reuptake inhibitor (SNRI) antidepressant that increases levels of serotonin and norepinephrine in the brain, with some dopaminergic activity at higher doses. The combination may be considered for patients with comorbid ADHD and depression who have not responded to monotherapy; however, this use is not standard or widely approved due to safety concerns. The primary mechanism involves additive effects on monoaminergic neurotransmission—dopamine, norepinephrine, and serotonin—which can increase therapeutic efficacy but also raises the risk for adverse events such as serotonin syndrome or excessive CNS stimulation[3][4][8]. This combination should only be used under close medical supervision due to significant drug interaction risks.

02

Targets

SERT (Sodium-dependent serotonin transporter)VMAT2 (Vesicular monoamine transporter 2)DAT (Dopamine plasma membrane transport protein)TAAR1 (Trace amine-associated receptor 1)NET (Norepinephrine Transporter)

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