- Treatment of schizophrenia.
- Acute treatment of mania/mixed episodes due to bipolar I disorder.
Acts as a partial agonist at dopamine D2 receptors in the CNS and serotonin 5–HT1A; also acts an antagonist at 5–HT2A receptors.
- Decreased incidence and severity of symptoms of schizophrenia.
- Decreased occurrence and severity of mania associated with bipolar 1 disorder.
Absorption: Well absorbed following oral administration.
Protein Binding: 91–97%
Metabolism and Excretion: Two metabolites desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR) are have antipsychotic activity. Metabolism occurs mostly via the CYP3A4 enzyme system, with further metabolism resulting in inactive metabolites; 21% excreted urine, 1.2% as unchanged drug.
Half-life: Cariprazine–2–4 days; DDCAR–1–3 weeks.
TIME/ACTION PROFILE (improvement in symptoms)
|PO (schizophrenia)||within 1–2 wk||4–6 wk||2 wk†|
|PO (mania due to bipolar 1 disorder)||within 5–7 days||2–3 wk||2 wk†|
- Concurrent use of strong CYP3A4 inhibitors or inducers;
Use Cautiously in:
- Known cerebrovascular/cardiovascular disease, dehydration, concurrent use of diuretics/antihypertensives or syncope (↑ risk of orthostatic hypotension);
- Pre-existing ↓ WBC or ANC or history of drug-induced leukopenia/neutropenia;
- At risk of aspiration or falls;
- OB: Neonates exposed in the third trimester may experience extrapyramidal symptoms/withdrawal;
- Lactation: Consider maternal and fetal benefits against possible adverse effects in infant;
- Pedi: Safety and effectiveness not established;
- Geri: Elderly patients with dementia-related psychosis (↑ risk of adverse cardiovascular effects and death), consider age-related ↓ in renal/hepatic/cardiovascular function, concurrent disease states and medications (↓ initial dose recommended).
Adverse Reactions/Side Effects
CNS: drowsiness, headache, agitation, dizziness, fatigue, insomnia, restlessness.
EENT: blurred vision
CV: hypertension, orthostatic hypotension, tachycardia
GI: dyspepsia, nausea, ↓ appetite, constipation, diarrhea, dry mouth, dysphagia (↑aspiration risk), ↑ liver enzymes, vomiting
Derm: STEVENS-JOHNSON SYNDROME, rash
Hemat: AGRANULOCYTOSIS, leukopenia, neutropenia
Metabolic: dyslipidemia, hyperglycemia/diabetes mellitus, weight gain
MS: arthralgia, back pain, extremity pain
Neuro: akathisia, extrapyramidal symptoms, tardive dyskinesia
Misc: NEUROLEPTIC MALIGNANT SYNDROME, body temperature dysregulation, late-occurring adverse reactions (consider long half-life of active drug)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Levels, effects and risk of toxicity ↑ by concurrent use of strong CYP3A4 inhibitors including itraconazole and ketoconazole; concurrent use not recommended.
- Levels and effectiveness may be ↓ by concurrent use of strong CYP3A4 inducers including carbamazepine and rifampin; concurrent use not recommended.
- Concurrent use of diuretics or antihypertensives may ↑ risk of orthostatic hypotension/syncope.
PO: (Adults) Schizophrenia–1.5 mg/day initially, may be ↑ on second day to 3 mg, further increments of 1.5 mg or 3 mg may be made depending on response/tolerance up to maintenance dose of 1.5–6 mg/day; Bipolar mania–1.5 mg/day initially, may be ↑ on second day to 3 mg, further increments of 1.5 mg or 3 mg may be made depending on response/tolerance up to maintenance dose of 1.5–6 mg/day titrated up to 3–6 mg/day; Concurrent use of strong CYP3A4 inhibitors–↓ dose by 50%.
Capsules: 1.5 mg, 3 mg, 4.5 mg, 6 mg
- Assess mental status (orientation, mood, behavior) before and periodically during therapy.
- Assess weight and BMI initially and throughout therapy.
- Monitor BP (sitting, standing, lying), pulse, and respiratory rate before and periodically during therapy.
- Observe patient carefully when administering medication to ensure that medication is actually taken and not hoarded or cheeked.
- Monitor for adverse reactions and patient response for several wk after starting therapy and after each dose increase. Due to long action, may not occur for several wks. Consider reducing dose or discontinuing drug if severe adverse reactions occur.
- Monitor patient for onset of akathisia (restlessness or desire to keep moving) and extrapyramidal side effects (parkinsonian–difficulty speaking or swallowing, loss of balance control, pill rolling of hands, masklike face, shuffling gait, rigidity, tremors; and dystonic–muscle spasms, twisting motions, twitching, inability to move eyes, weakness of arms or legs) periodically throughout therapy. Report these symptoms.
- Monitor for tardive dyskinesia (uncontrolled rhythmic movement of mouth, face, and extremities; lip smacking or puckering; puffing of cheeks; uncontrolled chewing; rapid or worm-like movements of tongue). Notify health care professional immediately if these symptoms occur, as these side effects may be irreversible.
- Monitor for development of neuroleptic malignant syndrome (fever, muscle rigidity, altered mental status, respiratory distress, tachycardia, seizures, diaphoresis, hypertension or hypotension, pallor, tiredness, loss of bladder control). Notify health care professional immediately if these symptoms occur.
- Assess for skin reactions (rash, toxic skin reactions, bullous exanthema).
- Assess for falls risk. Drowsiness, orthostatic hypotension, and motor and sensory instability increase risk. Institute prevention if indicated.
Lab Test Considerations:
Monitor CBC frequently during therapy in patients with pre-existing or history of low WBC. May cause leukopenia, neutropenia, or agranulocytosis. Discontinue therapy if severe neutropenia (ANC <1000 mm3) occurs.
- Monitor fasting blood glucose and lipid profile initially and periodically during therapy.
- PO: Administer once daily without regard to meals.
- Advise patient to take medication as directed and not to skip doses or double up on missed doses. Take missed doses as soon as remembered unless almost time for the next dose. Do not stop taking cariprazine without consulting health care professional.
- Inform patient of possibility of extrapyramidal symptoms and tardive dyskinesia. Instruct patient to report these symptoms immediately.
- Advise patient to make position changes slowly to minimize orthostatic hypotension. Protect from falls.
- Medication may cause drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Advise patient and family to notify health care professional of new or worse depression; new or worse anxiety; feeling very agitated or restless; panic attacks; trouble sleeping; new or worse irritability; acting aggressive; being angry or violent; acting on dangerous impulses; an extreme increase in activity and talking; other unusual changes in behavior or mood or rash occur.
- Inform patient that cariprazine may cause weight gain. Advise patient to monitor weight periodically. Notify health care professional of significant weight gain.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any new medications. Caution patient to avoid taking alcohol or other CNS depressants concurrently with this medication.
- Advise patient that extremes in temperature should be avoided, because this drug impairs body temperature regulation.
- Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
- Advise female patients to notify health care professional if pregnancy is planned or suspected and to avoid breast feeding during therapy. Encourage pregnant patients to enroll in registry by contacting National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/.
- Decrease in excitable, paranoic, or withdrawn behavior.
- Decreased occurrence and severity of mania associated with bipolar 1 disorder.
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