section name header

Pronunciation

kar-IP-ra-zeen

Classifications

Therapeutic Classification: antipsychotics

Indications

BEERS REMS


Action

  • Acts as a partial agonist at dopamine D2 receptors in the CNS and serotonin 5–HT1A; also acts an antagonist at 5–HT2A receptors.
Therapeutic effects:
  • Decreased incidence and severity of symptoms of schizophrenia.
  • Decreased occurrence and severity of mania associated with bipolar 1 disorder.
  • Antidepressant action.

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 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 wk.

Time/Action Profile

(improvement in symptoms)

ROUTEONSETPEAKDURATION
PO (schizophrenia)within 1–2 wk4–6 wk2 wk
PO (mania due to bipolar 1 disorder)within 5–7 days2–3 wk2 wk



Plasma concentrations of drug and active metabolites following discontinuation.



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: hypertension, orthostatic hypotension, tachycardia

Derm: rash, STEVENS-JOHNSON SYNDROME

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, restlessness, SUICIDAL THOUGHTS/BEHAVIORS, tardive dyskinesia

Resp: cough

Misc: body temperature dysregulation

Interactions

Drug-drug:

Route/Dosage

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

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

Availability

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Vraylar