Drug information of Cariprazine


It is used to treat schizophrenia and bipolar problems.

Mechanism of effect

Cariprazine is a second generation antipsychotic which displays partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors. It exhibits high affinity for dopamine (D2 and D3) and serotonin (5-HT1A) receptors and has low affinity for serotonin 5-HT2C and alpha1A-adrenergic receptors. Cariprazine functions as an antagonist for 5-HT2B (high affinity) and 5-HT2A receptors (moderate affinity), binds to histamine H1 receptors, and has no affinity for muscarinic (cholinergic) receptors


Extensively metabolized by CYP3A4 and, to a lesser extent, by CYP2D6 to active metabolites (desmethyl cariprazine [DCAR] and didesmethyl cariprazine [DDCAR]). DCAR is further metabolized into DDCAR by CYP3A4 and CYP2D6. DDCAR is then metabolized by CYP3A4 to a hydroxylated metabolite.
Urine (21%; 1.2% as unchanged drug cariprazine
Time to Peak
Plasma: Cariprazine: 3 to 6 hours
Half life
Cariprazine: 2 to 4 days; DCAR: 1 to 2 days; DDCAR: 1 to 3 weeks

Drug indications

Bipolar disorder: Acute treatment of manic or mixed episodes and major depression associated with bipolar I disorder

Schizophrenia: Treatment of schizophrenia


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 Disorder
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

Drug contraindications

Hypersensitivity to the active component or any of the ingredients

Safety and efficacy have not been established in patients younger than 18 years

Side effects

Central nervous system: Drug-induced extrapyramidal reaction, Parkinsonian-like syndrome, akathisia , headache, insomnia
Gastrointestinal: Nausea
 to 10%
Cardiovascular: Hypertension, tachycardia
Central nervous system: Drowsiness, restlessness, dizziness, anxiety, agitation, dystonia, fatigue, suicidal ideation
Dermatologic: Hyperhidrosis
Endocrine & metabolic: Weight gain, hyponatremia
Gastrointestinal: Vomiting, constipation, dyspepsia, abdominal pain , diarrhea, toothache, decreased appetite, xerostomia
Genitourinary: Pollakiuria
Hepatic: Increased serum transaminases, increased liver enzymes
Neuromuscular & skeletal: Increased creatine phosphokinase, limb pain, back pain , muscle rigidity, arthralgia
Ophthalmic: Blurred vision
<1%, postmarketing, and/or case reports: Cerebrovascular accident, dysphagia, gastritis, gastroesophageal reflux disease, hepatitis, leukopenia, neutropenia, rhabdomyolysis, Stevens-Johnson syndrome

Acetylcholinesterase Inhibitors (Central), Alcohol (Ethyl), Amifampridine, Amphetamines, Antidiabetic Agents, Anti-Parkinson Agents (Dopamine Agonist), Blood Pressure Lowering Agents, CNS Depressants, CYP3A4 Inducers (Moderate),
CYP3A4 Inducers (Strong), CYP3A4 Inhibitors (Moderate), CYP3A4 Inhibitors (Strong),
Dimethindene (Topical),
 Fosnetupitant , Iomeprol, Mequitazine, Opioid Agonists, Oxomemazine,
Selective Serotonin Reuptake Inhibitors, Serotonergic Agents (High Risk),
Tetrahydrocannabinol and Cannabidiol


There is a higher chance of death in older adults who take cariprazine for mental problems caused by dementia. Most of the deaths were linked to heart disease or infection. This medicine is not approved to treat mental problems caused by dementia

Drugs like this one have raised the chance of suicidal thoughts or actions in children and young adults. The risk may be greater in people who have had these thoughts or actions in the past. All people who take cariprazine need to be watched closely. Call the doctor right away if signs like low mood (depression), nervousness, restlessness, grouchiness, panic attacks, or changes in mood or actions are new or worse. Call the doctor right away if any thoughts or actions of suicide occur

Taking cariprazine in the third trimester of pregnancy may lead to uncontrolled muscle movements and withdrawal in the newborn

Some people may get a severe muscle problem called tardive dyskinesia. This problem may lessen or go away after stopping cariprazine, but it may not go away. The risk is greater with diabetes and in older adults, especially older women. The risk is greater with longer use or higher doses, but it may also occur after short-term use with low doses

Points of recommendation

What do I need to tell my doctor BEFORE I take Cariprazine
If you are allergic to cariprazine; any part of cariprazine; or any other drugs, foods, or substances
If you have any of these health problems: Kidney disease or liver disease
If you take any other drugs (prescription or OTC, natural products, vitamins). There are many drugs that interact with cariprazine, like certain drugs that are used for HIV, infections, or seizures

Avoid driving and doing other tasks or actions that call for you to be alert until you see how cariprazine affects you

To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs

Have blood work checked as you have been told by the doctor. Talk with the doctor

Be careful in hot weather or while being active. Drink lots of fluids to stop fluid loss

High blood sugar or diabetes, high cholesterol, and weight gain have happened with drugs like this one. These may raise the chance of heart and brain blood vessel disease

Low white blood cell counts have happened with drugs like this one. This may lead to a higher chance of infection. Rarely, infections have been deadly. Tell your doctor if you have ever had a low white blood cell count. Call your doctor right away if you have signs of infection like fever, chills, or sore throat

This medicine may cause seizures in some patients. Talk with the doctor

Dizziness, sleepiness, and feeling less stable may happen with cariprazine. These may lead to falling, which can cause broken bones or other health problems

Pregnancy level

Consult a physician before using

Neonates exposed to antipsychotic drugs during 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

Breast feeding warning

Unknown if distributed in human breast milk

Related drugs

Asenapine , Paliperidone , Blonanserin

Drug forms


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