Cariprazine (Vraylar) is an antipsychotic used to treat schizophrenia, specific types of bipolar I disorder, and as an add-on treatment for major depressive disorder (MDD). Cariprazine is from the drug class atypical antipsychotics.

Cariprazine is thought to work by managing chemicals in the brain (neurotransmitters), including serotonin and dopamine. Although the mechanism of action of cariprazine is unknown, its effect may be from a combination of partial agonist activity at central dopamine D₂ and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors.

Cariprazine is specifically indicated to treat adults with:

• Schizophrenia
• Acute manic or mixed episodes associated with bipolar I
• Depressive episodes associated with bipolar I disorder (bipolar depression) 
• Adjunctive treatment with an antidepressant therapy (ADT) for major depressive disorder (MDD).

Cariprazine, under the brand name Vraylar, became an FDA-approved medicine on September 17, 2015.

Cariprazine is not approved for use in older adults with dementia-related psychosis.  It may increase the risk of death in older adults with dementia-related psychosis and is not approved for this use.

Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric and young adult patients. All antidepressant-treated patients should be closely monitored for clinical worsening and emerging of suicidal thoughts and behaviors. The safety and effectiveness of this medicine have not been established in pediatric patients. 

Cariprazine may disrupt the body’s ability to reduce core body temperature. Exposure to extreme heat, strenuous exercise, dehydration, and anticholinergic medications may cause an increase in body temperature. Use this medicine with caution in these circumstances.

Take cariprazine exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose.

Cariprazine capsules are taken once daily and can be taken with or without food.

It may take several weeks before your symptoms improve. Keep using the medication as directed, and tell your doctor if your symptoms do not improve.

Tell your doctor if you have any changes in weight while taking this medicine.

Your blood pressure and heart rate will need to be checked often. You may also need frequent blood tests.

Taking this medicine at high doses or for a long time can cause a serious movement disorder that may not be reversible. The longer you use this medicine, the more likely you are to develop this disorder, especially if you are an older adult. Symptoms of this disorder include tremors or other uncontrollable muscle movements.

Usual Adult Dose for Schizophrenia:

Initial dose: 1.5 mg orally once a day
Titration regimen: The dose may be increased to 3 mg once a day on Day 2; further dose adjustments should be made in 1.5 to 3 mg increments based on efficacy and tolerability.
Maintenance dose: 1.5 to 6 mg orally once a day
Maximum dose: 6 mg/day.
 

Usual Adult Dose for Bipolar I with Manic or Mixed Episodes:

Initial dose: 1.5 mg orally once a day
Titration regimen: The dose should be increased to 3 mg once a day on Day 2; further dose adjustments should be made in 1.5 to 3 mg increments based on efficacy and tolerability.
Maintenance dose: 3 to 6 mg orally once a day
Maximum dose: 6 mg/day

Usual Adult Dose for Bipolar Depression:

Initial dose: 1.5 mg orally once a day
Titration regimen: The dose can be increased to 3 mg once a day on Day 15 based on efficacy and tolerability.
Maintenance dose: 1.5 mg to 3 mg orally once a day
Maximum dose:  3 mg/day

Usual Adult Dose for Adjunctive Therapy to Antidepressants for MDD:

Initial dose: 1.5 mg orally once a day
Titration regimen: The dose can be increased to 3 mg once a day on Day 15 based on efficacy and tolerability. In clinical trials, dosage titration at intervals of less than 14 days resulted in a higher incidence of adverse reactions.
Maintenance dose: 1.5 mg to 3 mg orally once a day
Maximum dose:  3 mg/day.

General Comments on dosing

Comments:

• Due to the long half-life, changes in dose will not be fully reflected in plasma for several weeks; monitor for adverse reactions and treatment response several weeks after beginning therapy and after each dose adjustment.
• Doses above 6mg once a day have not shown increased effectiveness sufficient to outweigh dose-related adverse reactions.
• Dosage Adjustments will be needed for CYP3A4 Inhibitors and Inducers.
• Click the link below for more detailed information on cariprazine dosing.

You should not use cariprazine if you are allergic to it or any ingredients contained in this medicine. Click here for a full list of Vraylar ingredients

Cariprazine is not approved for use by anyone younger than 18 years old.

To make sure cariprazine is safe for you, tell your doctor if you have:

• high cholesterol or triglycerides (a type of fat in the blood);
• a stroke or blood clot;
• heart disease;
• have or had a low white blood cell count;
• high blood pressure;
• liver or kidney disease;
• diabetes; 
• have or had seizures (convulsions) or
• if you are dehydrated.

Pregnancy

Tell your healthcare provider if you plan to become pregnant, are pregnant or become pregnant. Taking cariprazine while pregnant may cause harm to your unborn baby. Taking antipsychotic medicine in the last 3 months of pregnancy may cause withdrawal symptoms, breathing problems, feeding problems, fussiness, tremors, and limp or stiff muscles in the newborn. If you get pregnant, tell your doctor right away. Do not stop taking this medicine without your doctor's advice.

If you are pregnant, your name may be listed on a pregnancy registry to track the effects of cariprazine on the baby.

Breastfeeding

It may not be safe to breastfeed while using this medicine. Talk to your healthcare provider about the best way to feed your baby while being treated with cariprazine.

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA's Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Unless your doctor tells you otherwise, continue your normal diet.

Avoid driving or hazardous activity until you know how this medicine will affect you. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Dizziness or drowsiness can cause falls, accidents, or severe injuries.

While you are taking cariprazine, you may be more sensitive to temperature extremes such as very hot conditions. Avoid becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise.

Common cariprazine side effects may include:

• involuntary muscle movements;
• upset stomach, vomiting;
• drowsiness; or
• feeling restless.

Serious cariprazine side effects

Get emergency medical help if you have signs of an allergic reaction to cariprazine: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• sudden numbness or weakness (especially on one side of the body);
• problems with vision or speech,
• a light-headed feeling, like you might pass out;
• severe distress or agitation;
• a seizure;
• uncontrolled muscle movements in your face (chewing, lip smacking, frowning, tongue movement, blinking or eye movement);
• trouble swallowing, or accidentally inhaling food or drink;
• low white blood cell counts - fever, chills, sore throat, mouth sores, skin sores, sore throat, cough, trouble breathing, feeling light-headed;
• high blood sugar - increased thirst, increased urination, dry mouth, fruity breath odor; or
• severe nervous system reaction - very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, feeling like you might pass out.

Cariprazine can have long-lasting effects on your body. Some side effects could occur for several weeks after you stop using this medicine. You may also have new side effects whenever your dose is changed.

This is not a complete list of side effects, and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.

Taking cariprazine with other drugs that make you sleepy or slow your breathing can cause dangerous side effects or death. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

Medicines that are strong CYP3A4 Inhibitors or are CYP3A4 Inducers interact with cariprazine, tell your healthcare provider if your are on these medications. Click on the link below to check for interactions with this medicine.

Many drugs can interact with cariprazine. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed here. Tell your doctor about all your current medicines and any medicine you start or stop using.

Keep all appointments with your doctor and the laboratory. Your doctor may order certain lab tests to check your body's response to cariprazine.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.