Explore the Pharmacodynamics of Brexpiprazole With Dr Jain
Dr Rakesh Jain: My name is Dr Rakesh Jain, and today we're going to discuss how REXULTI is thought to work. REXULTI and antidepressants both interact with some of the same neurotransmitter systems implicated in depression, but in different ways.
Some antidepressants, such as SSRIs, SNRIs, and NDRIs, are reuptake inhibitors that are thought to work on 1 or 2 types of neurotransmitter receptors. SSRIs inhibit the reuptake of serotonin. SNRIs inhibit the reuptake of both serotonin and norepinephrine, while NDRIs inhibit the reuptake of norepinephrine and dopamine. Reuptake inhibitors, such as SSRIs, work by blocking the presynaptic reabsorption of serotonin. SNRIs and NDRIs function in similar ways for other neurotransmitter transporters.
REXULTI is thought to work differently than reuptake inhibitors as a partial agonist and antagonist. REXULTI has high binding affinity to 3 types of neurotransmitter receptors—norepinephrine, serotonin, and dopamine. REXULTI binds directly to the receptor and acts as a partial agonist across some dopamine and serotonin receptors and as an antagonist across some norepinephrine and serotonin receptors. REXULTI acts as an antagonist at norepinephrine ɑ1B, ɑ2C, ɑ1D, and ɑ1A receptors. REXULTI acts as a partial agonist at serotonin 5-HT1A receptors but also as an antagonist at serotonin 5-HT2A, 5-HT2B, and 5-HT7 receptors. REXULTI acts as a partial agonist at both dopamine D2 and D3 receptors. These neurotransmitters exert their effects not only individually, but also by modulating each other's activity.
REXULTI and antidepressants may work together, but in different ways, on some of the same neurotransmitter receptors implicated in depression. Most antidepressants work through reuptake inhibition, while REXULTI is both a direct partial agonist and antagonist of these systems. Please continue listening for additional important safety information.