Cariprazine

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 D 2 and serotonin 5-HT 1A receptors and antagonist activity at serotonin 5-HT 2A receptors.

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• . CONTRAINDICATIONS VRAYLAR is contraindicated in patients with history of a hypersensitivity reaction to cariprazine.contraindicated

. DOSAGE AND ADMINISTRATION Administer VRAYLAR orally once daily with or without food ( 2 ) Starting Dose Recommended Dose Schizophrenia in Adults ( 2.2 ) 1.5 mg daily 1.5 mg to 6 mg daily Schizophrenia in Pediatric Patients (13-17 years) ( 2.2 ) 0.5 mg daily 1.5 mg to 4.5 mg daily Bipolar Mania in Adults ( 2.3 ) 1.5 mg daily 3 mg to 6 mg daily Bipolar Mania in Pediatric Patients (10-17 years) ( 2.3 ) 0.5 mg daily 3 mg or 4.5 mg daily Bipolar Depression in Adults ( 2.4 ) 1.5 mg daily 1.5 mg or 3 mg daily Adjunctive therapy to antidepressants for MDD in Adults ( 2.5 ) 1.5 mg daily 1.5 mg or 3 mg daily Adults with Schizophrenia and Bipolar Mania: Maximum recommended daily dosage is 6 mg. Dosages above 6 mg daily do not confer significant benefit, but increase the risk of dose-related adverse reactions ( 2.2 , 2.3 ) Pediatric patients with Schizophrenia and Bipolar Mania: Maximum recommended daily dosage is 4.5 mg. Adults with Bipolar Depression: Maximum recommended daily dosage is 3 mg ( 2.4 ) Adjunctive therapy for treatment of MDD in Adults: Maximum recommended daily dosage is 3 mg ( 2.5 ) 2.1 General Dosing Information VRAYLAR is given orally once daily and can be taken with or without food. Because of the long half-life of cariprazine and its active metabolites, changes in dose will not be fully reflected in plasma for several weeks. Prescribers should monitor patients for adverse reactions and treatment response for several weeks after starting VRAYLAR and after each dosage change [see Warnings and Precautions ( 5.6 ) , Clinical Pharmacology ( 12.3 )] .

. WARNINGS AND PRECAUTIONS Cerebrovascular Adverse Reactions in Elderly Patients with Dementia-Related Psychosis: Increased incidence of cerebrovascular adverse reactions (e.g., stroke, transient ischemic attack) ( 5.3 ) Neuroleptic Malignant Syndrome: Manage with immediate discontinuation and close monitoring ( 5.4 ) Tardive Dyskinesia : Discontinue if appropriate ( 5.5 ) Late-Occurring Adverse Reactions: Because of VRAYLAR’s long half-life, monitor for adverse reactions and patient response for several weeks after starting VRAYLAR and with each dosage change ( 5.6 ) Metabolic Changes : Monitor for hyperglycemia/diabetes mellitus, dyslipidemia and weight gain ( 5.7 ) Leukopenia, Neutropenia, and Agranulocytosis : Perform complete blood counts (CBC) in patients with pre-existing low white blood cell counts (WBC) or history of leukopenia or neutropenia. Consider discontinuing VRAYLAR if a clinically significant decline in WBC occurs in absence of other causative factors ( 5.8 ) Orthostatic H ypotension and Syncope : Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope ( 5.9 ) Seizures: Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold ( 5.11 ) Potential for Cognitive and Motor Impairment: Use caution when operating machinery ( 5.12 ) 5.1 Increased Mortality in Elderly Patients with Dementia-Related Psychosis Antipsychotic drugs increase the all-cause risk of death in elderly patients with dementia-related psychosis.

The following adverse reactions are discussed in more detail in other sections of the labeling: Increased Mortality in Elderly Patients with Dementia-Related Psychosis [see Boxed Warning and Warnings and Precautions ( 5.1 )] Suicidal Thoughts and Behaviors [see Boxed Warning and Warnings and Precautions ( 5.2 )] Cerebrovascular Adverse Reactions, Including Stroke, in Elderly Patients with Dementia-Related Psychosis [see Warnings and Precautions ( 5.3 )] Neuroleptic Malignant Syndrome [see Warnings and Precautions ( 5.4 )] Tardive Dyskinesia [see Warnings and Precautions ( 5.5 )] Late Occurring Adverse Reactions [see Warnings and Precautions ( 5.6 )] Metabolic Changes [see Warnings and Precautions ( 5.7 )] Leukopenia, Neutropenia, and Agranulocytosis [see Warnings and Precautions ( 5.8 )] Orthostatic Hypotension and Syncope [see Warnings and Precautions ( 5.9 )] Falls [see Warnings and Precautions ( 5.10 )] Seizures [ see Warnings and Precautions ( 5.11 )] Potential for Cognitive and Motor Impairment [see Warnings and Precautions ( 5.12 )] Body Temperature Dysregulation [see Warnings and Precautions ( 5.13 )] Dysphagia [see Warnings and Precautions ( 5.14 )] Most common adverse reactions in adults (incidence ≥ 5% and at least twice the rate of placebo) were ( 6.1 ) : Schizophrenia: extrapyramidal symptoms and akathisia Bipolar mania: extrapyramidal symptoms, akathisia, dyspepsia, vomiting, somnolence, and restlessness Bipolar depression: nausea, akathisia, restlessness, and extrapyramidal symptoms Adjunctive treatment of MDD: akathisia, restlessness, fatigue, constipation, n…

Pregnancy : Based on animal data, may cause fetal harm. ( 8.1 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to VRAYLAR during pregnancy. For more information, contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/. Risk Summary Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery (see Clinical Considerations). There are no available data on VRAYLAR use in pregnant women to inform any drug-associated risks for birth defects or miscarriage. The major active metabolite of cariprazine, DDCAR, has been detected in adult patients up to 12 weeks after discontinuation of VRAYLAR [see Clinical Pharmacology ( 12.3 )]. Based on animal data, VRAYLAR may cause fetal harm. Administration of cariprazine to rats during the period of organogenesis caused malformations, lower pup survival, and developmental delays at drug exposures less than the human exposure at the maximum recommended human dose (MRHD) of 6 mg/day. However, cariprazine was not teratogenic in rabbits at doses up to 4.6 times the MRHD of 6 mg/day [see Data] .

Metabolism

VRAYLAR activity is thought to be mediated by cariprazine and its two major active metabolites, desmethylcariprazine (DCAR) and didesmethylcariprazine (DDCAR), which are pharmacologically equipotent to cariprazine. After multiple dose administration of VRAYLAR, mean cariprazine and DCAR concentrations reached steady state at around Week 1 to Week 2 and mean DDCAR concentrations appeared to be approaching steady state at around Week 4 to Week 8 in a 12-week study (Figure 1).

10.1 Human Experience In pre-marketing clinical trials involving VRAYLAR in approximately 5000 patients or healthy subjects, accidental acute overdosage (48 mg/day) was reported in one patient. This patient experienced orthostasis and sedation. The patient fully recovered the same day. 10.2 Management of Overdosage No specific antidotes for VRAYLAR are known. In managing overdose, provide supportive care, including close medical supervision and monitoring, and consider the possibility of multiple drug involvement. In case of an overdose, consult a Certified Poison Control Center (1-800-222-1222) for up-to-date guidance and advice.

• Sep 17, 2015NDANDA204370Abbvie

1. 1Off Label Use1,03712%
2. 2Drug Ineffective5155.8%
3. 3Weight Increased4535.1%
4. 4Akathisia4064.6%
5. 5Anxiety3624.1%
6. 6Tardive Dyskinesia3604.0%
7. 7Nausea3443.9%
8. 8Tremor3383.8%
9. 9Fatigue3343.8%
10. 10Insomnia3333.7%
11. 11Suicidal Ideation3113.5%
12. 12Depression2743.1%
13. 13Dizziness2723.1%
14. 14Somnolence2392.7%
15. 15Feeling Abnormal2192.5%

The 10 most recently updated of 50 ClinicalTrials.gov registrations naming Cariprazine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Assess Change in Disease Activity and Adverse Events (AEs) With Cariprazine in the Treatment of Depressive Episodes in Pediatric Participants Participants (10 to 17 Years of Age) With Bipolar I Disorder.
  Recruiting · Phase 3 · Interventional · 380 enrolled · AbbVie
  NCT04777357updated 2026-06-12
• Pharmacokinetics, Safety, Tolerability and Efficacy of a Subcutaneous Long-Acting Injection of Cariprazine (Cariprazine Depot) in Subjects Eligible for Treatment With Oral Cariprazine
  Recruiting · Phase 1 · Phase 2 · Interventional · 24 enrolled · Mapi Pharma Ltd.
  NCT07185815updated 2026-05-01
• Dopamine D3 Receptor Occupancy in Bipolar Depression
  Withdrawn · Phase 4 · Interventional · 0 enrolled · New York State Psychiatric Institute
  NCT05060549updated 2026-04-14
• Evaluate Pharmacokinetics, Safety, and Tolerability of AX251 LAI in Patients With Schizophrenia
  Not yet recruiting · Phase 1 · Interventional · 48 enrolled · Anxo Pharmaceutical Co., Ltd.
  NCT07484204updated 2026-03-20
• An Exploratory Analysis of Immune and Inflammatory Response Associated With Clozapine
  Terminated · Phase 4 · Interventional · 5 enrolled · Ohio State University
  NCT05741502updated 2026-02-25
• Observational Study of Oral Cariprazine Capsules to Assess Change in Disease Activity in Adult Participants With Bipolar I Disorder
  Completed · Observational · 120 enrolled · AbbVie
  NCT06256367updated 2026-02-24
• RNA Editing as a Biomarker of Antidepressant Response in Unipolar and Bipolar Depression (EDIT-ANDRE)
  Recruiting · Phase 4 · Interventional · 120 enrolled · Mayo Clinic
  NCT07266545updated 2026-02-23
• Cariprazine for Comorbid Cocaine and Opioid Use Disorder
  Completed · Phase 2 · Interventional · 26 enrolled · Kyle Kampman
  NCT05063201updated 2026-01-23
• Lithium Versus Cariprazine in the Acute Phase Treatment of Bipolar Depression (DUAG9)
  Recruiting · Phase 4 · Interventional · 122 enrolled · Aalborg University Hospital
  NCT05913947updated 2026-01-21
• Safety, Pharmacokinetics and Efficacy Study of MP-214 in Patients With Schizophrenia
  Completed · Phase 2 · Interventional · 34 enrolled · Tanabe Pharma Corporation
  NCT00862992updated 2026-01-05

Frequently asked questions

How does Cariprazine work?

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 D 2 and serotonin 5-HT 1A receptors and antagonist activity at serotonin 5-HT 2A receptors.

What is Cariprazine used for?

According to FDA labeling, Cariprazine carries indications including: .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Cariprazine?

Cariprazine is classified as Other antipsychotics, Atypical Antipsychotic, Dopamine Agonists, Serotonin Receptor Interactions.

What are the brand names for Cariprazine?

Cariprazine is marketed under brand names including Vraylar.

What are the contraindications for Cariprazine?

Cariprazine labeling lists contraindications including: . CONTRAINDICATIONS VRAYLAR is contraindicated in patients with history of a hypersensitivity reaction to cariprazine.. Always consult the full prescribing information and a clinician.