From the FDA Drug Label
The mechanism of action of cariprazine is unknown. However, the efficacy of cariprazine could be mediated through a combination of partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors Cariprazine acts as a partial agonist at the dopamine D3 and D2 receptors with high binding affinity (Ki values 0.085 nM, and 0.49 nM (D2L) and 0. 69 nM (D2S), respectively) and at the serotonin 5-HT1A receptors (Ki value 2.6 nM). Cariprazine acts as an antagonist at 5-HT2B and 5-HT2A receptors with high and moderate binding affinity (Ki values 0.58 nM and 18.8 nM respectively)
Vraylar Mechanism of Action:
- The exact mechanism of action of Vraylar (cariprazine) is unknown.
- However, it is believed to work through a combination of:
- Partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors.
- Antagonist activity at serotonin 5-HT2A receptors.
- Cariprazine also has high binding affinity for dopamine D3 and D2 receptors, and serotonin 5-HT1A receptors.
- It has moderate to high binding affinity for 5-HT2B and 5-HT2A receptors, and lower binding affinity for other receptors 1, 1, 1.
From the Research
Vraylar (cariprazine) works by acting as a partial agonist at dopamine D2 and D3 receptors and serotonin 5-HT1A receptors, while also blocking 5-HT2A receptors in the brain, as evidenced by the most recent and highest quality study 2. This medication is primarily used to treat schizophrenia and bipolar disorder, including bipolar depression and manic or mixed episodes. Key points about Vraylar's mechanism of action and use include:
- Unique mechanism involves preferential binding to D3 receptors, which distinguishes it from other antipsychotics and may contribute to its effectiveness for both mood and psychotic symptoms 3
- Helps regulate neurotransmitter activity in brain regions associated with thought processes, mood regulation, and behavior
- Typical dosing ranges from 1.5 to 6 mg once daily for various conditions, with gradual titration often recommended to minimize side effects 4
- Full therapeutic effects may take several weeks to develop Common side effects include:
- Restlessness
- Movement disorders
- Weight gain (though less than some other antipsychotics)
- Digestive issues Regular monitoring by a healthcare provider is essential to assess effectiveness and manage potential side effects, as noted in studies such as 2 and 5.