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Cariprazine

VRAYLAR

What it isD3-preferring D2/D3 partial agonist with serotonergic activity; schizophrenia, bipolar disorder, and adjunctive depression.

Why this oneIts unusually broad mood labeling spans bipolar mania, bipolar depression, and adjunctive unipolar depression.

What limits itAkathisia is dose-limiting; long-lived active metabolites delay steady response and make adverse effects linger after stopping.

FDA-approved for

FDA label

BOXED WARNING Increased mortality in elderly with dementia-related psychosis; increased suicidal thoughts/behaviors in pediatric and young adult patients
FDA dosingPopulationStartTargetMax
SchizophreniaAdults1.5 mg QD1.5–6 mg QD6 mg/day
SchizophreniaAdolescents 13–17 yr0.5 mg QD1.5–4.5 mg QD4.5 mg/day
Bipolar I mania/mixedAdults1.5 mg QD3–6 mg QD6 mg/day
Bipolar I mania/mixedChildren 10–17 yr0.5 mg QD3 or 4.5 mg QD4.5 mg/day
Bipolar depressionAdults1.5 mg QD1.5 or 3 mg QD3 mg/day
MDD, adjunct to antidepressantAdults1.5 mg QD1.5 or 3 mg QD3 mg/day

Titration Bipolar depression & adjunctive MDD: wait ≥14 days before increasing to 3 mg (titration <14 days raises adverse reactions)

Renal CrCl ≥30 mL/min: no adjustment; CrCl <30 mL/min: not evaluated

Hepatic Mild–moderate (Child-Pugh 5–9): no adjustment; severe (10–15): not recommended

Long half-life — dose changes not fully reflected in plasma for several weeks

Instructions

Cautions

Adverse reactions

Pregnancy May cause fetal harm (animal data); pregnancy registry available; third-trimester exposure risks EPS/withdrawal in neonate

Lactation No human data; present in rat milk — weigh benefits vs. risk

⚠ BOXED WARNING

Cost, est. cash$200–$1,200/month

Generic entry2029 est.

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability1 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.

Active metabolites

Mechanism of action: Cariprazine ballicule

Cariprazine ballicule: receptor binding, kinetics and half-life diagram

Open Cariprazine in the interactive console ↗

Memory aids: mascots and interaction avatars

Cariprazine VRAYLAR mascot mnemonic cartoon
“Car ripper seen (going) Vroom!”
Antipsychotics are represented with spooky mascots
Vroom! → potentially activating, not sedating
Engine running → akathisia
Jaw clenched → dystonia
V-forming headlights are “V-Rays”
Bright headlight → possibly sharpened cognition
Long headlights → extremely long half-life
Cariprazine CYP3A4 substrate avatar
CYP3A4 substrate

Open Cariprazine in the interactive console ↗