An atypical antipsychotic which is used in the treatment of schizophrenia and bipolar mania.
Brand name Vraylar.
It acts primarily as a D3 receptor and D2 receptor partial agonist.
It has a high selectivity for the D3 receptor.
It is also useful as an add-on therapy in major depressive disorder.
Oral agent.
Has high bioavailability.
Can cross the blood brain barrier because it is lipophilic.
Protein binding 91–97%.
Hepatic metabolism via CYP3A4 and to a lesser extent CYP2D6.
Elimination half-life 2–5 days and 2–3 wks for active metabolite, desmethylcariprazine.
Excretion by urine and bile.
Side effects include: akathisia, insomnia, and weight gain, sedation, nausea, dizziness, vomiting, anxiety, and constipation.
Does not alter prolactin levels. . Does not increase the QT interval on the electrocardiogram (ECG).
It is a D2 and D3 partial agonist.
Has a higher affinity for D3 receptors.
The D2 and D3 receptors are important targets for the treatment of schizophrenia.
The overstimulation of dopamine receptors has been implicated as a possible cause of schizophrenia.
It acts to inhibit overstimulated dopamine receptors, therefore acting as an antagonist.
It stimulates the same receptors when the endogenous dopamine levels are low.
Its high selectivity towards D3 receptors could associated with reduced side effects associated with the other antipsychotic drugs, because D3 receptors are mainly located in the ventral striatum and would not incur the same motor extrapyramidal symptoms as drugs that act on dorsal striatum dopamine receptors.
Also acts on 5-HT1A receptors.
It has partial agonist as well as antagonist properties depending on the endogenous dopamine levels.
It is suspected that in schizophrenia endogenous dopamine levels are high, and it acts as an antagonist by blocking dopamine receptors.
When endogenous dopamine levels are low, it acts more as an agonist, increasing dopamine receptor activity.