Cariprazine (Vraylar®) is a second-generation (atypical) antipsychotic. Here is basic information about this medication. Other articles on this website with more advanced information and tips related to this medication are linked to under Related Pages below.
FDA-approved indications
(last updated by us in September 2019)
1. Schizophrenia in adults
2. Acute treatment of manic or mixed episodes associated with bipolar I disorder in adults
3. Depressive episodes associated with bipolar I disorder (bipolar depression) in adults
Note: As of September 2019, cariprazine has not been approved by the FDA for adjunctive treatment of major depressive disorder.
Dosage
Schizophrenia
Starting dose: 1.5 mg/day
Recommended dose: 1.5 to 6 mg/day
Bipolar mania
Starting dose: 1.5 mg/day
Recommended dose: 3 to 6 mg/day
Bipolar depression
Starting dose: 1.5 mg/day
Recommended dose: 1.5 mg/day or 3 mg/day
Important! Please refer to the full Prescribing Information (see link below) before prescribing this medication.
Cariprazine Prescribing Information
Dosage forms and strengths
Capsules: 1.5 mg, 3 mg, 4.5 mg, and 6 mg
As of September 2019, cariprazine is not available in the USA in as either an injectable or a long-acting injectable form.
Potential side effects
Please see this page for a handout listing both the common and less common side effects of this medication along with the percentages of patients who report them.
Pharmacodynamics and mechanism of action
Cariprazine has the following main receptor effects:
– Partial agonist at dopamine D2 and D3 receptors
– Partial agonist at serotonin 1A (5-HT1A) receptors
– Antagonist at serotonin 2A (5-HT2A) and serotonin 2B (5-HT2B) receptors
Cariprazine also binds with low affinity to histamine H1, serotonin 2C (5-HT2C), and alpha 1A adrenergic receptors.
It has virtually no activity at cholinergic muscarinic receptors.
Pharmacokinetics
Cariprazine is extensively metabolized by CYP3A4 and, to a lesser extent, by CYP2D6, into two major active metabolites: desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR).
These two active metabolites have pharmacological activity identical to that of cariprazine.
Being a CYP2D6 poor metabolizer does not significantly affect the pharmacokinetics of cariprazine or of its active metabolites.
Drug interactions
If the person is on a strong inhibitor of CYP3A4, the dose of cariprazine should be reduced by half.
If the person is on an inducer of CYP3A4, the use of cariprazine is not recommended.
Cariprazine does not significantly induce or inhibit any cytochrome P450 enzyme or P-glycoprotein.
Related Pages
Cariprazine (Vraylar): Potential side effects
Activity of cariprazine (Vraylar®) on dopamine D3 and D2 receptors
Cariprazine (Vraylar®): Organized list of references
Second-Generation (“Atypical”) Antipsychotics (List)
Second-Generation Antipsychotics: Dose Equivalents
Dose adjustment for second-generation antipsychotics based on drug interactions
What should I be doing to monitor patients who are on an antipsychotic?
Is TD less likely with second-generation (“atypical”) antipsychotics?
Psychiatric medications with a long half-life
Dopamine receptors: A primer for clinicians
References
Vraylar (cariprazine Prescribing Information
Copyright 2016 to 2019, Rajnish Mago, MD, and Simple and Practical Medical Education, LLC. All rights reserved. May not be reproduced in any form without express written permission.
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