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cariprazine

Antipsychotic

Brand: VRAYLAR

Published 2026-02-05 · Last reviewed 2026-02-12 · 6 references

Content sourced from FDA labeling (DailyMed) and peer-reviewed literature.

Print sheet Review evidence

At a glance

Class: Antipsychotic·Typical dose: Schizophrenia: start 1.5 mg once daily; increase to 3 mg on day 2; adjust by 1.5–3 mg increments at ≥2-week intervals to 1.5–6 mg/day (max 6 mg).·PK (metabolism / half-life): Greater than 90% plasma protein bound with extensive tissue distribution.·LAI available: No

Class: Antipsychotic
Typical dose: Schizophrenia: start 1.5 mg once daily; increase to 3 mg on day 2; adjust by 1.5–3 mg increments at ≥2-week intervals to 1.5–6 mg/day (max 6 mg).
PK (metabolism / half-life): Greater than 90% plasma protein bound with extensive tissue distribution.
LAI available: No

Quick answers

What is cariprazine?: Cariprazine (brand Vraylar) is an second-generation antipsychotic (SGA) that preferentially targets dopamine D3 receptors, supporting efficacy across schizophrenia and bipolar disorder mood states.
What is VRAYLAR?: VRAYLAR is a brand name for cariprazine.
What is VRAYLAR (cariprazine) used for?: Label indications include: Schizophrenia; acute treatment of manic or mixed episodes and depressive episodes associated with bipolar I disorder; adjunctive therapy to antidepressants for major depressive disorder.
What drug class is VRAYLAR (cariprazine)?: Atypical Antipsychotic.
What is the mechanism of action of VRAYLAR (cariprazine)?: D3/D2 partial agonist (D3‑preferring); 5‑HT1A partial agonist; 5‑HT2A antagonist.
What strengths does VRAYLAR (cariprazine) come in?: Oral capsules (cariprazine hydrochloride / cariprazine HCl): 1.5 mg, 3 mg, 4.5 mg, 6 mg; blister and bottle packaging.
Is VRAYLAR (cariprazine) a controlled substance?: No — it is not scheduled as a controlled substance under U.S. federal law.
What is VRAYLAR (cariprazine) dosing for schizophrenia?: Schizophrenia: start 1.5 mg once daily; increase to 3 mg on day 2; adjust by 1.5–3 mg increments at ≥2-week intervals to 1.5–6 mg/day (max 6 mg).
What is the maximum dose of VRAYLAR (cariprazine) for major depressive disorder (clinical depression)?: Adjunctive major depressive disorder (clinical depression): start 1.5 mg once daily with an antidepressant; may increase to 3 mg/day (max 3 mg/day).
What is cariprazine hydrochloride (HCl)?: Oral capsules (cariprazine hydrochloride / cariprazine HCl): 1.5 mg, 3 mg, 4.5 mg, 6 mg; blister and bottle packaging.

General information

Cariprazine (brand Vraylar) is an second-generation antipsychotic (SGA) that preferentially targets dopamine D3 receptors, supporting efficacy across schizophrenia and bipolar disorder mood states.

This profile emphasizes its role in schizophrenia, bipolar I mania/mixed episodes, bipolar depression, and adjunctive major depressive disorder (MDD; clinical depression) as add-on therapy to antidepressants.

The cariprazine compare view, cariprazine evidence feed, and cariprazine print page can support counseling and shared decision-making around efficacy, akathisia risk, and titration timelines; the schizophrenia hub and bipolar disorder hub link to broader care pathways.

U.S. approvals

Schizophrenia (adults) (2015)
Bipolar I manic/mixed episodes (adults) (2015)
Bipolar I depression (adults) (2019)
Adjunctive treatment to antidepressants in major depressive disorder (adults) (2022)

Formulations & strengths

Oral capsules (cariprazine hydrochloride / cariprazine HCl): 1.5 mg, 3 mg, 4.5 mg, 6 mg; blister and bottle packaging.

Generic availability

No U.S. generics approved as of 2025; market exclusivity projected into the early 2030s.

Often chosen for negative-symptom improvement and bipolar depression coverage. Long-lived metabolites mean titration is slow and monitoring for akathisia and GI upset is important; metabolic impact is moderate.

View labelExact

Mechanism of action

Refer to the Glossary entry on Neurotransmitters for background on receptor systems involved in serious mental illness.

Cariprazine stabilizes dopamine and serotonin activity via partial agonism at D3/D2 and 5-HT1A receptors coupled with 5-HT2 antagonism, balancing mesolimbic and mesocortical pathways.

Preferential D3 occupancy may contribute to negative-symptom gains and cognitive benefits highlighted in clinical trials.

Partial agonist at dopamine D3>D2 receptors.
Partial agonist at serotonin 5-HT1A; antagonist at 5-HT2A/5-HT2B receptors.
Antagonist at adrenergic α1B and histamine H1 receptors.
Minimal muscarinic receptor binding.

Metabolism & pharmacokinetics

Oral bioavailability ~50%; Tmax 3–6 hours; food has negligible effect on exposure.
Greater than 90% plasma protein bound with extensive tissue distribution.
Metabolized by CYP3A4 (major) and CYP2D6 (minor) to active metabolites desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR).
Terminal half-life 2–4 days for parent, 1–2 days for DCAR, and up to 1–3 weeks for DDCAR; effective half-life ~7 days at steady state.
Eliminated primarily in feces (~70%) with <10% renal excretion.

Dosing & administration

Schizophrenia: start 1.5 mg once daily; increase to 3 mg on day 2; adjust by 1.5–3 mg increments at ≥2-week intervals to 1.5–6 mg/day (max 6 mg).
Bipolar I mania/mixed: initiate 1.5 mg once daily, increase to 3 mg on day 2, then titrate by 1.5 mg increments up to 6 mg/day.
Bipolar I depression: 1.5 mg once daily for at least 14 days; may increase to 3 mg/day based on response.
Adjunctive major depressive disorder (clinical depression): start 1.5 mg once daily with an antidepressant; may increase to 3 mg/day (max 3 mg/day).
Label recommends halving the dose with strong CYP3A4 inhibitors; coadministration with strong CYP3A4 inducers is generally avoided; not recommended in severe hepatic impairment.

Adverse effects

FDA boxed warnings

Increased mortality in elderly patients with dementia-related psychosis (antipsychotic class warning).
Suicidal thoughts and behaviors in children, adolescents, and young adults treated with antidepressants (applies to adjunctive MDD indication).

Common side effects (≥10%)

Akathisia: Occurs in up to 20% depending on dose; most frequent cause of discontinuation.
Extrapyramidal symptoms (EPS): Overall 6–10%, predominantly akathisia and tremor.
Nausea: Approximately 10% of patients.
Somnolence: Around 10% across indications.
Weight gain: ≥7% increase in roughly 7–13% over 6–12 months.

Other notable effects

Modest metabolic shifts—continue routine monitoring of weight, fasting glucose, and lipids.
Orthostatic hypotension during initiation due to α1 antagonism.
Impulse-control problems reported rarely; counsel patients to report new urges.
Prolactin changes are minimal but assess if symptoms appear.

Interactions

Strong CYP3A4 inhibitors (ketoconazole, clarithromycin) increase exposure; label recommends reducing cariprazine dose by half and monitoring for akathisia or sedation.
Strong CYP3A4 inducers (rifampin, carbamazepine, St. John’s wort) substantially lower exposure; coadministration is generally avoided.
Moderate CYP3A4 inhibitors often warrant slower titration and closer monitoring.
Additive CNS depression with alcohol, benzodiazepines, or opioids.
May blunt efficacy of dopamine agonists (e.g., levodopa); this combination is often avoided when dopaminergic therapy is needed.

Other useful information

Long-lived metabolites mean clinical response to dose changes can be delayed; allowing several weeks before adjusting again is common.
Patients and caregivers can be advised on early akathisia; clinicians often manage it with dose adjustments, beta-blockers, or benzodiazepines.
Low impact on QTc, but a baseline ECG is often considered in patients with cardiac risk or polypharmacy.
Once-daily dosing at a consistent time (with or without food) helps maintain steady exposure.
Metabolic monitoring typically includes baseline, 12 weeks, then annually.
Comparing dopamine partial agonists side-by-side using the cariprazine compare view can help select alternatives when akathisia, cost, or residual symptoms prompt a switch.

References

Related hubs:Schizophrenia hub·Bipolar hub