Small molecule drug with a maximum clinical stage of Approval (across all indications), with 3 approved and 7 investigational indications.
targets Sodium-dependent dopamine transporter Sodium-dependent noradrenaline transporter
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trade names
Bupropion hydrochloride, Bupropion hydrochloride component of auvelity, Bupropion hydrochloride component of contrave, Forfivo xl, Wellbutrin, Wellbutrin 100
generic
BUPROPION HYDROCHLORIDE
MOA
12.1 Mechanism of Action Dextromethorphan is an uncompetitive antagonist of the NMDA receptor (an ionotropic glutamate receptor) and a sigma-1 receptor agonist. The mechanism of dextromethorphan in the treatment of MDD is unclear. The mechanism of action of bupropion in the treatment of MDD is unclear; however, it may be related to noradrenergic and/or dopaminergic mechanisms. Bupropion increases plasma levels of dextromethorphan by competitively inhibiting cytochrome P450 2D6, which catalyzes a major biotransformation pathway for dextromethorphan. Bupropion is a relatively weak inhibitor of the neuronal reuptake of norepinephrine and dopamine and does not inhibit monoamine oxidase or the reuptake of serotonin.
indication
1 INDICATIONS AND USAGE AUVELITY is indicated for the treatment of major depressive disorder (MDD) in adults. AUVELITY is a combination of dextromethorphan, an uncompetitive N -methyl D -aspartate (NMDA) receptor antagonist and sigma-1 receptor agonist, and bupropion, an aminoketone and CYP450 2D6 inhibitor, indicated for the treatment of major depressive disorder (MDD) in adults. ( 1 )
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