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Cariprazine (Vraylar®): Basic Information

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

1. Treatment of schizophrenia in adults

2. Acute treatment of manic or mixed episodes associated with bipolar I disorder in adults

3. Treatment of depressive episodes associated with bipolar I disorder (bipolar depression) in adults

4. Adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults. 


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

Adjunctive therapy to antidepressants for major depressive disorder

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 the 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

Cariprazine is not available 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. It binds with high affinity to both of them but its affinity for D3 receptors is greater than that for D2 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 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®)

Cariprazine (Vraylar®): Basic Information

Cariprazine (Vraylar): Potential side effects

Activity of cariprazine (Vraylar®) on dopamine D3 and D2 receptors

Cariprazine (Vraylar®): Organized list of references


Second-Generation Antipsychotics—General articles

Second-generation (“atypical”) antipsychotics (List)

Second-generation antipsychotics: Dose equivalents

Dose adjustment for second-generation antipsychotics based on drug interactions

Do adolescents have more metabolic side effects with second-generation antipsychotics?

Does weight gain with second-generation (atypical) antipsychotics plateau after the first few months?

Do adolescents have more metabolic side effects with second-generation antipsychotics?

What should I be doing to monitor patients who are on an antipsychotic?

The patient who “demands” TWO antipsychotics

Long-acting injectable antipsychotics: Overview

Dose equivalents of long-acting injectable second-generation antipsychotics 


References

Cariprazine Prescribing Information


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Disclaimer: The material on this website is provided as general education for medical professionals. It is not intended or recommended for patients or other laypersons or as a substitute for medical advice, diagnosis, or treatment. Patients must always consult a qualified healthcare professional regarding their diagnosis and treatment. Healthcare professionals should always check this website for the most recently updated information.

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