cariprazine (Vraylar)

Indications

• schizophrenia
• bipolar disorder
• adjunctive therapy to antidepressants for treatment of major depressive disorder in adults

Dosage

• QD dosing
  • starting dose 1.5 mg
  • max dose: 6 mg schizophrenia, biopolar mania,
  • max dose: 3 mg bipolar depression or adjunctive treatment of depression

Capsules: 1.5, 3 mg, 4,5 mg 6 mg.

Pharmacokinetics

• metabolized by CYP3A4 &, to a lesser extent, by CYP2D6
• two major active metabolites
  • desmethylcariprazine (DCAR)
  • didesmethylcariprazine (DDCAR)

Adverse effects

• extrapyramidal symptoms
  • tremor, slurred speech, involuntary muscle movements
• akathisia, dyspepsia, vomiting, somnolence, restlessness
• does not prolong the QTc interval

• drug adverse effects of antipsychotic agents
• drug adverse effects of atypical antipsychotic agents
• drug adverse effects of psychotropic agents

Drug interactions

• strong CPY3AA4 inhibitors: reduce cariprazine dose in 1/2
• strong CPY3AA4 inducers: cariprazine not recommended

• drug interaction(s) of antipsychotics & dopamine receptor agonists
• drug interaction(s) of antipsycotics with benzodiazepines

Mechanism of action

• unknown
  • partial agonist activity at central
    • dopamine D2 receptors
    • serotonin 5-HT1A receptors
  • antagonist activity at serotonin 5-HT2A receptors

More general terms

• atypical antipsychotic agent; second generation antipsychotic