Products
Cariprazine was approved in the United States in 2015 and in many countries and the EU in 2018 in capsule form (Reagila, some countries: Vraylar).
Structure and properties
Cariprazine (C21H32Cl2N4O, Mr = 427.4 g/mol) is a piperazine and dimethylurea derivative. It is present in the drug as cariprazine hydrochloride, a white powder. Active metabolites are involved in the effects of the compound.
Effects
Cariprazine (ATC N05AX15) has antipsychotic properties. The effects are attributed to partial agonism at dopamine D2/D3– and serotonin-5-HT1A receptors, as well as antagonism at serotonin-5-HT2B-, serotonin-5-HT2A– and histamine H1 receptors in the central nervous system. Cariprazine has a long half-life of 2 to 4 days. The half-life of the active metabolites is as long as 3 weeks.
Indications
For the treatment of schizophrenia in adult patients. Also used in some countries for the acute treatment of manic or mixed episodes in type I bipolar disorder.
Dosage
According to the SmPC. Capsules are taken once daily, independent of meals. Always administer at the same time of day.
Contraindications
- Hypersensitivity
- Combination with strong or moderate CYP3A4 inhibitors or CYP3A4 inducers.
Refer to the drug label for complete precautions.
Interactions
Cariprazine is a substrate of CYP3A4 and of CYP2D6, and corresponding drug-drug interactions are possible.
Adverse effects
The most common possible adverse effects include extrapyramidal disturbances (parkinsonism) and akathisia (sitting restlessness).
