section name header

Pronunciation

a-ri-PIP-ra-zole

Classifications

Therapeutic Classification: antipsychotics, mood stabilizers

Pharmacologic Classification: serotonin-dopamine activity modulators (SDAM)

Indications

BEERS REMS


Action

  • Psychotropic activity may be due to agonist activity at dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at the 5-HT2A receptor.
  • Also has alpha1 adrenergic blocking activity.
Therapeutic effects:
  • Decreased manifestations of schizophrenia.
  • Decreased mania in bipolar patients.
  • Decreased symptoms of depression.
  • Decreased agitation associated with schizophrenia or bipolar disorder.
  • Decreased emotional and behavioral symptoms of irritability.
  • Decreased incidence of tics.

Pharmacokinetics

Absorption: Well absorbed (87%) following oral administration; 100% following IM injection.

Distribution: Extensive extravascular distribution.

Protein Binding: >99%.

Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A4 and CYP2D6 isoenzymes; the CYP2D6 enzyme system exhibits genetic polymorphism; 7% of population may be poor metabolizers (PMs) and may have significantly aripiprazole concentrations and an risk of adverse effects ( dose by 50% in PMs); one metabolite (dehydro-aripiprazole) has antipsychotic activity. 18% excreted unchanged in feces; <1% excreted unchanged in urine.

Half-Life: Aripiprazole: 75 hr; dehydro-aripiprazole: 94 hr; ER injectable suspension: 30–46 days (Abilify Maintena); 29–35 days (Aristada)

Time/Action Profile

(antipsychotic effect)

ROUTEONSETPEAKDURATION
POunknown2 wkunknown
ER-IMunknownunknownunknown





Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: bradycardia, chest pain, edema, hypertension, orthostatic hypotension, tachycardia

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), dry skin, ecchymosis, skin ulcer, sweating

EENT: blurred vision, conjunctivitis, ear pain

Endo: prolactin, hyperglycemia

GI: constipation, salivation, anorexia, nausea, vomiting

GU: urinary incontinence

Hemat: AGRANULOCYTOSIS, anemia, leukopenia, neutropenia

Metab: dyslipidemia, weight gain, weight loss

MS: muscle cramps, neck pain

Neuro: drowsiness, extrapyramidal reactions, tremor, abnormal gait, akathisia, confusion, depression, fatigue, hostility, impaired cognitive function, impulse control disorders (eating/binge eating, gambling, sexual, shopping), insomnia, lightheadedness, manic reactions, nervousness, restlessness, sedation, SEIZURES, SUICIDAL THOUGHTS, tardive dyskinesia

Resp: dyspnea

Misc: heat regulation, HYPERSENSITIVITY REACTIONS, injection site reactions, NEUROLEPTIC MALIGNANT SYNDROME

Interactions

Drug-drug:

Route/Dosage

Schizophrenia

Acute Manic or Mixed Episodes Associated with Bipolar I Disorder

Maintenance Treatment of Bipolar I Disorder

Depression

Irritability Associated with Autistic Disorder

Tourette's Disorder

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Abilify, Abilify Asimtufii, Abilify Maintena, Abilify Mycite, Aristada, Aristada Initio

Pill Image

aripiprazole_195-8584.jpg