Cariprazine

Cariprazine is a prescription medication used to treat Schizophrenia and Bipolar I Disorder

• Cariprazine is available under the following different brand names: Vraylar

Adult dosage

Capsule

• 1.5mg
• 3mg
• 4.5mg
• 6mg

Schizophrenia

Adult dosage

• 1.5 mg orally once daily initially; may increase to 3 mg/day on Day 2. 
• Depending upon clinical response and tolerability, further dose adjustments can be made in 1.5 to 3-mg increments; the dosing range is 1.5-6 mg orally once daily. 

Bipolar I Disorder

Adult dosage

Manic or mixed episodes

• Day 1: 1.5 mg orally
• Day 2: Increase to 3 mg orally
• Day 3 and thereafter: Depending on clinical response and tolerability, further dose adjustments can be made in 1.5 to 3-mg increments; the dosing range is 3-6 mg orally once daily; not to exceed 6 mg/day. 

Depressive episodes

• 1.5 mg orally once daily initially
• Depending upon clinical response and tolerability, the dosage can be increased to 3 mg once daily on Day 15; not to exceed 3 mg once daily. 

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”.

Common side effects of Cariprazine include:

• involuntary muscle movements, 
• upset stomach, 
• vomiting, 
• drowsiness, and 
• restlessness 

Serious side effects of Cariprazine include:

• hives, 
• difficulty breathing, 
• swelling of the face, lips, tongue, or throat, 
• sudden numbness or weakness (especially on one side of the body), 
• problems with vision or speech, 
• lightheadedness, 
• severe distress, 
• agitation, 
• seizure, 
• uncontrolled muscle movements in the face (chewing, lip-smacking, frowning, tongue movement, blinking or eye movement), 
• trouble swallowing, 
• accidentally inhaling food or drink, 
• fever, 
• chills, 
• sore throat, 
• mouth sores, 
• skin sores, 
• sore throat, 
• cough, 
• increased thirst, 
• increased urination, 
• dry mouth, 
• fruity breath odor, 
• very stiff (rigid) muscles, 
• high fever, 
• sweating, 
• confusion, 
• fast or uneven heartbeats, and
• tremors

Rare side effects of Cariprazine include:

• none 

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them.  Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Cariprazine has severe interactions with at least 22 other drugs. 
• Cariprazine has serious interactions with at least 19 other drugs.
• Cariprazine has moderate interactions with at least 85 other drugs.
• Cariprazine has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drugs interactions. Therefore, before using this drug, tell your doctor or pharmacist of all the drugs you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Contraindications

• Hypersensitivity to Cariprazine 

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Cariprazine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Cariprazine?”

Cautions

• Antipsychotic drugs increase the all-cause risk of death in elderly patients with dementia-related psychosis; a higher incidence of stroke and TIA, including fatal stroke, was also observed (see Black Box Warnings)
• Hypersensitivity reactions reported ranging from rash, pruritus, urticaria, and events suggestive of angioedema (eg, swollen, tongue, lip swelling, face edema, pharyngeal edema, facial swelling)
• Neuroleptic malignant syndrome reported; monitor for hyperpyrexia, muscle rigidity, delirium, and autonomic instability; other signs include increased CPK, myoglobinuria (rhabdomyolysis), and acute renal failure; if NMS is suspected, immediately discontinue treatment
• Tardive dyskinesia, a potentially irreversible, involuntary, dyskinetic movement syndrome, may develop in patients treated with antipsychotics
• Adverse effects may first appear several weeks after initiating treatment, as drug and metabolite levels accumulate; monitor for extrapyramidal symptoms or akathisia
• Leukopenia and neutropenia reported; agranulocytosis (including fatal cases) reported with other atypical antipsychotics; discontinue Cariprazine in patients with an absolute neutrophil count less than 1000/mm³ and follow WBC until recovery
• May cause orthostatic hypotension and syncope; caution in patients vulnerable to hypotension (eg, elderly, dehydration, hypovolemia, concomitant antihypertensive drugs, cardiovascular or cerebrovascular disease)
• May cause seizures; risk is greatest with history of seizures or conditions that lower seizure threshold
• May cause cognitive and motor impairment
• Body temperature dysregulation reported; may disrupt the ability to reduce core body temperature; caution with strenuous exercise, exposure to extreme heat, dehydration, and coadministration with anticholinergic medications
• Esophageal dysmotility and aspiration were reported with antipsychotic drug use
• May cause somnolence, postural hypotension, motor and sensory instability, which may lead to falls and, consequently, fractures or other injuries; for patients with diseases, conditions, or medications that could exacerbate these effects, complete fall risk assessments when initiating antipsychotic treatment and recurrently for patients on long-term antipsychotic therapy

Drug interactions overview

• Coadministration with a strong CYP3A4 inhibitor increases the exposures of Cariprazine and its major active metabolite, didesmethylcariprazine (DDCAR), compared to the use of Cariprazine alone (see Dosage Modifications)
• The effect of CYP3A4 inducers on the exposure of Cariprazine has not been evaluated, and the net effect is unclear

Metabolic changes

• Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, reported; assess fasting plasma glucose before or soon after initiation of antipsychotic medication, and monitor periodically
• Lipids alteration has occurred; obtain a fasting lipid profile at baseline and monitor periodically during treatment before or soon after initiation of antipsychotic medication
• Weight gain observed; monitor weight at baseline and frequently thereafter

Suicidal thoughts or behaviors

• Pooled analyses of placebo-controlled trials of anti-depressive drugs showed an increased risk of suicidal thoughts or behavior in patients aged 24 years or younger taking these drugs for any indication; monitoring for emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior
• Inform patients, their caregivers, and families of the increased the risk of suicidal thoughts and behavior; advice to be alert for the emergence or worsening of signs and symptoms

Pregnancy and Lactation

• Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk for extrapyramidal symptoms or withdrawal symptoms after delivery; these complications vary in severity, with some being self-limited and others requiring ICU support and prolonged hospitalization

Pregnancy exposure registry

• Report exposure during pregnancy to the National Pregnancy Registry for Atypical Antipsychotics 1-866-961-2388 OR, http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/. 
• Unknown if distributed in human breast milk.  
• Present in rat milk. 
• Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or the underlying maternal condition.