Mechanism of Action and Clinical Benefits of Aripiprazole

Primary Mechanism and Receptor Activity

• The American Academy of Sleep Medicine suggests that aripiprazole's efficacy for positive and negative symptoms results from the combination of D2 partial agonism and 5-HT1A partial agonism, in patients with schizophrenia 1
• The unique pharmacological profile of aripiprazole translates to clinical benefits, including a better tolerability profile compared to olanzapine and other atypicals, in patients with psychiatric disorders 1, 2, 3

Clinical Translation and Important Caveats

• The American Academy of Pediatrics notes that aripiprazole is described as the first "third-generation" antipsychotic, specifically because of its partial dopamine receptor agonist activity, which distinguishes it from second-generation "atypical" antipsychotics, in the treatment of psychiatric disorders 4
• Aripiprazole may cause paradoxical activation or agitation in some patients due to its partial agonist properties, as documented in PTSD nightmare treatment studies, in patients with post-traumatic stress disorder 1, 2, 3