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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 interactions:
- strong CPY3AA4 inhibitors: reduce cariprazine dose in 1/2
- strong CPY3AA4 inducers: cariprazine not recommended
Mechanism of action:
- unknown
- partial agonist activity at central
- dopamine D2 receptors
- serotonin 5-HT1A receptors
- antagonist activity at serotonin 5-HT2A receptors
Interactions
drug adverse effects of antipsychotic agents
monitor with atypical antipsychotic agents
General
atypical antipsychotic agent; second generation antipsychotic
References
- Cassels C. Medscape. Sept 17, 2015s
FDA Okays New Atypical for Schizophrenia, Bipolar Disorder
http://www.medscape.com/viewarticle/851143