Names and pronunciation
brex-pip′-ra-zole Rexulti
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Drug reference
brex-pip′-ra-zole Rexulti
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Func. class.: Antipsychotic, atypical
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ACTION: May exert its effects through a combination of partial agonist activity at dopaminergic D-2 receptors, serotonergic 5-HT1A receptors, antagonist activity at serotonergic 5-HT2A receptors
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USES: Adjunctive treatment of major depressive disorder, schizophrenia
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CONTRAINDICATIONS: Hyper sensitivity Precautions: Elderly patients, stroke, neuroleptic malignant syndrome, tardive dyskinesia, leukopenia, neutropenia, agranulocytosis, orthostatic hypotension, seizures, cognitive impairment
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Black Box Warning: Dementia-related psychosis, suicidal ideation in children, adolescents, young adults Black Box Warning: Suicidal ideation: provide close supervision and control; give the smallest quantity to reduce the risk of overdose. In those who exhibit changes in symptoms, worsening of depression, suici- dality, or other changes in mood or behavior, a decision should be made to change or dis- continue treatment. If discontinuing, taper as rapidly as possible, abrupt discontinua- tion of drug can cause adverse symptoms. Children and young adults <24 yr are at increased risk • Tardive dyskinesia: periodic evalua- tion for movement disorders (AIMS) is recommended. If signs and symptoms of B tardive dyskinesia appear, consider dis- continuation • Seizure disorder: use cautiously in pa- tients with history of seizure disorder or with conditions that may lower the sei- zure threshold. Conditions that lower the seizure threshold may be more prevalent in patients 65 yr or older • Orthostatic hypotension: dizziness, light headedness, tachycardia, and occa- sionally syncope. Risks are generally greatest at beginning of treatment and during dose escalation. Patients at higher risk include those with dehydration, hypo- volemia, treatment with antihypertensive medications, history of cardiac disease (HF, MI, CAD, ischemia, or conduction abnormalities), history of cerebrovascu- lar disease, and patients who are antipsy- chotic-naive. Monitor orthostatic vital signs, such as pulse and B/P. Complete fall risk assessments in at-risk patients on long-term antipsychotic therapy • Hematologic disease: those with a his- tory of clinically significant low WBC count or drug-induced leukopenia/neu- tropenia should have frequent CBC assessments in first few months of treat- ment. Discontinue in patients with ANC <1000/mm3 • Pregnancy/breastfeeding: use only when benefits outweigh fetal risks. Neo- nates exposed to antipsychotics in the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symp- toms after delivery. Enroll patient in Na- tional Pregnancy Registry for Psychiatric Medications (866-961-2388). Consider benefits/risks of breastfeeding
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SIDE EFFECTS CNS: Akathisia, fatigue, drowsiness, diz- ziness, tremor, sedation, insomnia, EPS EENT: Blurred vision, dry mouth, nasopharyngitis GI: Constipation, diarrhea, nausea, flatu- lence, abdominal cramping/pain GU: UTI MISC: Weight gain, myalgia
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INTERACTIONS Increase: temperature—anticholinergics Increase: CNS depression—other CNS depressants, use cautiously Increase: brexpiprazole effect—strong CYP2D6 inhibitors, strong CYP3A4 inhib- itors, may need dose reduction Drug/Herb: Decrease: brexpiprazole effect—St. John’s wort; may need to increase product dose Drug/Food: Increase: brexpiprazole effect—grape- fruit juice; avoid using together
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DOSAGE AND ROUTES Schizophrenia • Adult: PO Initially, 1 mg daily on days 1-4; increase to 2 mg daily on days 5-7, then increase to 4 mg daily on day 8 based on response and tolerability. Recommended dose range 2-4 mg/day (max: 4 mg/day) Adjunctive treatment of major de- pressive disorder • Adult: PO Initially, 0.5 to 1 mg daily; after titration to 1 mg/day, increase to target dose of 2 mg/day; titrate dosage at weekly intervals based on response and tolerability; max 3 mg/day Hepatic dose • Adult: PO Mild hepatic impairment: no change; moderate to severe hepatic im- pairment (Child-Pugh score ≥7): max 2 mg/day for major depressive disorder, 3 mg/day for schizophrenia Renal dose • Adult: PO CCr ≥60 mL/min: no change; CCr <60 mL/min, including end-stage re- nal disease (ESRD): max 2 mg/day for major depression, 3 mg/day for schizo- phrenia
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Available forms: Tablets 0.25, 0.50, 1, 2, 3, 4 mg
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Administer: • Initiate treatment at low end of dosage range in geriatric adults • Periodically reassess for need of con- tinued maintenance therapy • Give without regard to food • If dose is missed, give when remem- bered; if close to next dose, skip missed dose and give regular dose
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Assess: • Hypersensitivity: rash, facial swelling, urticaria, and anaphylaxis have been ob- served; discontinue immediately
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To use caution when driving or operat- ing machinery or performing other tasks that require mental alertness until the effects are known • To avoid ethanol ingestion during treatment. Somnolence could lead to falls with the potential for fractures and other injuries • To watch for suicidal behaviors or thoughts by family or impulsive urges • That dystonic reactions may occur • To rise slowly from sitting or lying, orthostatic hypotension may occur • To report if pregnancy is planned or suspected or if breastfeeding • To report all products taken to prevent drug interactions HIGH ALERT
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PHARMACOKINETICS Half-life 91 hr, onset unknown, peak 4 hr, duration unknown
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• Adult: PO Initially, 1 mg daily on days 1-4; increase to 2 mg daily on days 5-7, then increase to 4 mg daily on day 8 based on response and tolerability. Recommended dose range 2-4 mg/day (max: 4 mg/day) Adjunctive treatment of major de- pressive disorder
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• Adult: PO Initially, 0.5 to 1 mg daily; after titration to 1 mg/day, increase to target dose of 2 mg/day; titrate dosage at weekly intervals based on response and tolerability; max 3 mg/day Hepatic dose
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• Adult: PO Mild hepatic impairment: no change; moderate to severe hepatic im- pairment (Child-Pugh score ≥7): max 2 mg/day for major depressive disorder, 3 mg/day for schizophrenia Renal dose
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• Adult: PO CCr ≥60 mL/min: no change; CCr <60 mL/min, including end-stage re- nal disease (ESRD): max 2 mg/day for major depression, 3 mg/day for schizo- phrenia
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