section name header

Pronunciation

kar-IP-ra-zeen

Classifications

Therapeutic Classification: antipsychotics

Indications

BEERS REMS

Action

Therapeutic Effects:

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