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Indications

BEERS REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: cerebrovascular adverse reactions ( in elderly patients with dementia-related psychoses), orthostatic hypotension/syncope

EENT: blurred vision

Endo: hyperglycemia/diabetes

GI: abdominal pain, constipation, diarrhea, dry mouth, dysphagia, excess salivation, flatulence

Hemat: agranulocytosis, leukopenia, neutropenia

Metab: weight, appetite, dyslipidemia

Neuro: akathisia, abnormal dreams, cognitive impairment, dizziness, drowsiness, dystonia, extrapyramidal symptoms, headache, NEUROLEPTIC MALIGNANT SYNDROME, restlessness, sedation, SEIZURES, tardive dyskinesia, tremor, urges (eating, gambling, sexual, shopping)

Misc: body temperature dysregulation, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions

Drug-drug:

Drug-Natural Products:

Availability

(Generic available)

Route/Dosage

Schizophrenia

Renal Impairment

Hepatic Impairment

Major Depressive Disorder

Renal Impairment

Hepatic Impairment

Agitation Associated with Dementia Due to Alzheimer’s Disease

Renal Impairment

Hepatic Impairment

US Brand Names

Rexulti

Action

  • Psychotropic activity may be due to partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at the 5-HT2A receptor.
Therapeutic effects:
  • Decreased manifestations of schizophrenia, including excitable, paranoic, or withdrawn behavior.
  • Improvement in symptoms of depression with increased sense of well-being.
  • Decreased agitation associated with dementia due to Alzheimer's disease.

Classifications

Therapeutic Classification: antipsychotics, antidepressants

Pharmacologic Classification: serotonin-dopamine activity modulators (SDAM)

Pharmacokinetics

Absorption: Well absorbed (95%) following oral administration.

Distribution: Displays extravascular distribution.

Protein Binding: >99%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 and CYP2D6 isoenzymes; the CYP2D6 enzyme system exhibits genetic polymorphism (7% of population may be poor metabolizers and may have significantly brexpiprazole concentrations and an risk of adverse effects). 25% excreted in urine (<1% unchanged), 46% in feces (14% unchanged).

Half-Life: 91 hr.

Time/Action Profile

(improvement in symptoms)

ROUTEONSETPEAKDURATION
PO (schizophrenia)within 1–2 wk4–6 wkunknown
PO (depression)within 1 wk5 wkunknown



Patient/Family Teaching

Pronunciation

brex-PIP-ra-zole