From the FDA Drug Label
The active ingredient of VRAYLAR is cariprazine, an atypical antipsychotic, in hydrochloride salt form.
- Classification: Vraylar (cariprazine) is classified as an atypical antipsychotic 1.
- Key characteristics: It has partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors 1.
From the Research
Vraylar (cariprazine) is classified as an atypical antipsychotic medication, specifically a dopamine D3-preferring D3/D2 receptor partial agonist, with a preference for the D3 receptor, and also acts as a partial agonist at serotonin 5-HT1A receptors.
Key Characteristics
- Vraylar functions as a partial agonist at dopamine D2 and D3 receptors, with higher affinity for D3 receptors
- It is FDA-approved for the treatment of schizophrenia, acute manic or mixed episodes associated with bipolar I disorder, and bipolar depression
- The typical dosing range is 1.5-6 mg once daily for schizophrenia and bipolar mania, and 1.5-3 mg once daily for bipolar depression
- Vraylar has a uniquely long half-life (approximately 2-4 days for the parent compound and up to 3 weeks for its active metabolite)
Common Side Effects
- Akathisia (restlessness)
- Extrapyramidal symptoms
- Weight gain (though less than some other atypicals)
- Sedation
Metabolic Profile
- Unlike some other antipsychotics, Vraylar has a relatively neutral metabolic profile, making it a consideration for patients with metabolic concerns, as noted in studies such as 2 and 3.
Clinical Efficacy
- Cariprazine has demonstrated efficacy in improving schizophrenia symptoms, including improvements in Positive and Negative Syndrome Scale (PANSS) total scores, as seen in studies like 2 and 3.
- It was associated with a significantly longer time to relapse than placebo in a long-term, phase III, relapse-prevention study, as reported in 2.
- Cariprazine was also significantly more efficacious than risperidone in improving PANSS Factor Score for Negative Symptoms in a phase III trial in patients with predominantly negative symptoms of schizophrenia, as noted in 3.
Tolerability
- Cariprazine was generally well tolerated in clinical trials, with most adverse events being of mild to moderate severity, and metabolic changes observed were considered generally not clinically significant, as seen in studies such as 2 and 3.
- The most commonly encountered adverse events (incidence ≥5% and at least twice the rate of placebo) are extrapyramidal symptoms and akathisia, as reported in 2.
- Short-term weight gain appears small, with approximately 8% of patients receiving cariprazine 1.5-6 mg/d gaining ≥7% body weight from baseline, compared with 5% for those randomized to placebo, resulting in an NNH of 34, as noted in 2.
- Cariprazine is associated with no clinically meaningful alterations in metabolic variables, prolactin, or the ECG QT interval, as reported in 2.