Cariprazine ($ Vraylar)

Second generation antipsychotic (dopamine, serotonin receptor partial agonist (D3/2, 5-HT1A), receptor antagonist (5-HT2B))

Dosing

Bipolar depression and antidepressant augmentation (1.5 mg/d)

Mania/mixed states (3-6 mg/d)

Schizophrenia (1.5-6 mg/d, avg 4.5 mg/d)

INTERACTIONS: Metabolized by 3A4. Raise 3-5x with carbamazepine. Lower 2x with nefazodone and grapefruit juice. May need to lower a little with non-pram SSRIs (fluoxetine, fluvoxamine, paroxetine, sertraline ≥ 150 mg/day).

LONG HALF-LIFE: 2-4 days (active metabolite 1-3 weeks).

Management

First line in schizophrenia: One of best tolerated antipsychotics overall, and only one that improves negative symptoms directly.

Less effective than other antipsychotics in bipolar and unipolar depression, but this varies by patient. Its potential to treat mania and depression makes it a good choice in bipolar I.

TOLERABILITY: Weight gain, sedation, akathisia, EPS (dystonia, stiffness), anticholinergic.

RISKS: Tardive dyskinesia (25% over 10 years, higher in elderly), metabolic, prolactinemia (can lead to breast cancer, osteopenia, sexual dysfunction), orthostasis (falls), QTc prolongation, temperature imbalance in elderly, NMS (muscle rigidity, fever, tachycardia).

EMR Text