cariprazine

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

Known cerebrovascular/cardiovascular disease, dehydration, concurrent use of diuretics/antihypertensives or syncope (↑ risk of orthostatic hypotension);
May ↑ risk of suicide attempt/ideation, especially during early treatment or dose adjustment; risk may be greater in children or adolescents;
Pre-existing ↓ WBC or ANC or history of drug-induced leukopenia/neutropenia;
At risk of aspiration or falls;
OB: Neonates exposed in the 3rd trimester may experience extrapyramidal symptoms/withdrawal;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established;
Geri:
Appears on Beers list. ↑ risk of stroke, cognitive decline, and mortality in older adults with dementia. Avoid use in older adults, except for schizophrenia, bipolar disorder, or adjunctive treatment of major depressive disorder (not indicated for dementia-related psychosis)
.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, orthostatic hypotension, tachycardia

Derm: rash, STEVENS-JOHNSON SYNDROME (SJS)

EENT: blurred vision

Endo: hyperglycemia/diabetes mellitus

GI: dyspepsia, nausea, ↑liver enzymes, constipation, diarrhea, dry mouth, dysphagia (↑ aspiration risk), vomiting

Hemat: AGRANULOCYTOSIS, leukopenia, neutropenia

Metab: ↓appetite, dyslipidemia, weight gain

MS: arthralgia, back pain, extremity pain

Neuro: akathisia, drowsiness, extrapyramidal symptoms, headache, agitation, dizziness, fatigue, insomnia, NEUROLEPTIC MALIGNANT SYNDROME (NMS), restlessness, SUICIDAL THOUGHTS/BEHAVIORS, tardive dyskinesia

Resp: cough

Misc: body temperature dysregulation

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including itraconazole and ketoconazole, and moderate CYP3A4 inhibitors, including erythromycin and fluconazole, may ↑ levels and risk of toxicity; ↓ cariprazine dose.
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.

Availability ⬆ ⬇

Capsules: 1.5 mg; 3 mg; 4.5 mg; 6 mg

Route/Dosage ⬆ ⬇

Schizophrenia or Acute Treatment of Mania/Mixed Episodes Associated With Bipolar I Disorder

PO (Adults ): 1.5 mg once daily; may ↑ to 3 mg once daily on Day 2; further dosage adjustments can be made in increments of 1.5 mg or 3 mg depending on response/tolerability (max dose = 6 mg once daily). Initiation of strong CYP3A4 inhibitor while on stable dose of cariprazine: If current dose 1.5–3 mg once daily: Change to 1.5 mg every 3 days. If current dose 4.5–6 mg once daily: Change to 1.5 mg every other day. Initiation of moderate CYP3A4 inhibitor while on stable dose of cariprazine: If current dose 1.5–3 mg once daily: Change to 1.5 mg every other day. If current dose 4.5–6 mg once daily: Change to 1.5 mg once daily. Initiation of cariprazine while on stable dose of strong CYP3A4 inhibitor: 1.5 mg every 3 days; may ↑ to 1.5 mg every other day if needed. Initiation of cariprazine while on stable dose of moderate CYP3A4 inhibitor: 1.5 mg every other day; may ↑ to 1.5 mg once daily, if needed.

Depressive Episodes Associated With Bipolar I Disorder or Adjunctive Treatment of Major Depressive Disorder

PO (Adults ): 1.5 mg once daily; may ↑ to 3 mg once daily on Day 15 depending on response/tolerability (max dose = 3 mg once daily); Initiation of strong CYP3A4 inhibitor while on stable dose of cariprazine: If current dose 1.5–3 mg once daily: Change to 1.5 mg every 3 days. If current dose 4.5–6 mg once daily: Change to 1.5 mg every other day. Initiation of moderate CYP3A4 inhibitor while on stable dose of cariprazine: If current dose 1.5–3 mg once daily: Change to 1.5 mg every other day. If current dose 4.5–6 mg once daily: Change to 1.5 mg once daily. Initiation of cariprazine while on stable dose of strong CYP3A4 inhibitor: 1.5 mg every 3 days. Initiation of cariprazine while on stable dose of moderate CYP3A4 inhibitor: 1.5 mg every other day.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a partial agonist at dopamine D₂ receptors in the CNS and serotonin 5-HT_1A; also acts an antagonist at 5-HT_2A receptors.

Therapeutic effects:

Decreased incidence and severity of symptoms of schizophrenia.
Decreased occurrence and severity of mania associated with bipolar I disorder.
Antidepressant action.

Classifications ⬆ ⬇

Therapeutic Classification: antipsychotics

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: 91–97%.

Metabolism/Excretion: Two metabolites, desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR), have antipsychotic activity. Metabolism occurs mostly via the CYP3A4 isoenzyme, with further metabolism resulting in inactive metabolites; 21% excreted urine, 1.2% as unchanged drug.

Half-Life: Cariprazine: 2–4 days; DDCAR: 1–3 wk.

Time/Action Profile ⬆ ⬇

(improvement in symptoms)

ROUTE	ONSET	PEAK	DURATION
PO (schizophrenia)	within 1–2 wk	4–6 wk	2 wk‡
PO (mania due to bipolar I disorder)	within 5–7 days	2–3 wk	2 wk‡

‡Plasma concentrations of drug and active metabolites following discontinuation.

Patient/Family Teaching ⬆ ⬇

Explain the purpose and side effects of cariprazine. 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. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
Emphasize the importance of routine follow-up exams and continued participation in psychotherapy as indicated.
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, family, and caregivers to look for suicidality, especially during early therapy or dose changes. Notify health care professional immediately if thoughts about suicide or dying, attempts to commit suicide, new or worse depression or anxiety, agitation or restlessness, panic attacks, insomnia, new or worse irritability, aggressiveness, acting on dangerous impulses, mania, or other changes in mood or behavior 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 patients with diabetes to report worsening of glucose control due to potential for hyperglycemia.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected during therapy or if breastfeeding. 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/. May cause extrapyramidal and/or withdrawal symptoms (agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, feeding disorder) in neonates whose mothers were exposed to antipsychotic drugs during 3rd trimester of pregnancy. Symptoms vary in severity. Some neonates recover within hours or days without specific treatment; others required prolonged hospitalization. Monitor neonates of women pregnant while taking cariprazine for extrapyramidal and/or withdrawal symptoms and manage symptoms appropriately.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

14501- MSN Laboratories Private Limited
- 14501-0035-
  - 14501-0035-2- 50 kg in 1 DRUM (14501-0035-2)

57741- Maprimed S.A.
- 57741-3700-
  - 57741-3700-1- 25 kg in 1 DRUM (57741-3700-1)

57741- Maprimed S.A.
- 57741-4100-
  - 57741-4100-1- 25 kg in 1 DRUM (57741-4100-1)

61874- Allergan, Inc.
- 61874-115- Vraylar
  61874-115-07- 7 CAPSULE, GELATIN COATED in 1 BLISTER PACK (61874-115-07)

61874- Allergan, Inc.
- 61874-115- Vraylar
  - 61874-115-17- 1 BLISTER PACK in 1 CARTON (61874-115-17) / 7 CAPSULE, GELATIN COATED in 1 BLISTER PACK

61874- Allergan, Inc.
- 61874-115- Vraylar
  - 61874-115-20- 2 BLISTER PACK in 1 CARTON (61874-115-20) / 10 CAPSULE, GELATIN COATED in 1 BLISTER PACK (61874-115-11)

61874- Allergan, Inc.
- 61874-115- Vraylar
  - 61874-115-30- 30 CAPSULE, GELATIN COATED in 1 BOTTLE (61874-115-30)

61874- Allergan, Inc.
- 61874-116-
  - 61874-116-00- 1 BAG in 1 DRUM (61874-116-00) / 65000 CAPSULE, GELATIN COATED in 1 BAG

61874- Allergan, Inc.
- 61874-130- Vraylar
  61874-130-07- 7 CAPSULE, GELATIN COATED in 1 BLISTER PACK (61874-130-07)

61874- Allergan, Inc.
- 61874-130- Vraylar
  - 61874-130-20- 2 BLISTER PACK in 1 CARTON (61874-130-20) / 10 CAPSULE, GELATIN COATED in 1 BLISTER PACK (61874-130-11)

61874- Allergan, Inc.
- 61874-130- Vraylar
  - 61874-130-30- 30 CAPSULE, GELATIN COATED in 1 BOTTLE (61874-130-30)

61874- Allergan, Inc.
- 61874-131-
  - 61874-131-00- 1 BAG in 1 DRUM (61874-131-00) / 65000 CAPSULE, GELATIN COATED in 1 BAG

61874- Allergan, Inc.
- 61874-145- Vraylar
  61874-145-07- 7 CAPSULE, GELATIN COATED in 1 BLISTER PACK (61874-145-07)

61874- Allergan, Inc.
- 61874-145- Vraylar
  - 61874-145-30- 30 CAPSULE, GELATIN COATED in 1 BOTTLE (61874-145-30)

61874- Allergan, Inc.
- 61874-146-
  - 61874-146-00- 1 BAG in 1 DRUM (61874-146-00) / 65000 CAPSULE, GELATIN COATED in 1 BAG

61874- Allergan, Inc.
- 61874-160- Vraylar
  61874-160-07- 7 CAPSULE, GELATIN COATED in 1 BLISTER PACK (61874-160-07)

61874- Allergan, Inc.
- 61874-160- Vraylar
  - 61874-160-30- 30 CAPSULE, GELATIN COATED in 1 BOTTLE (61874-160-30)

61874- Allergan, Inc.
- 61874-161-
  - 61874-161-00- 1 BAG in 1 DRUM (61874-161-00) / 65000 CAPSULE, GELATIN COATED in 1 BAG

76055- Sionc Pharmaceutical Private Limited
- 76055-0042-
  76055-0042-1- 60 kg in 1 DRUM (76055-0042-1)

82708- HOSTER LABS PRIVATE LIMITED
- 82708-0003-
  82708-0003-1- 1 kg in 1 DRUM (82708-0003-1)

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇