aripiprazole

a·ri·pip·ra·zole (r-ppr-zl)

n.

An antipsychotic drug that functions as a partial dopamine receptor agonist and is used in the treatment of schizophrenia and other psychoses.

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aripiprazole,

an antipsychotic agent used to treat schizophrenia.

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aripiprazole

Abilify

Pharmacologic class: Quinolone-derived atypical antipsychotic agent

Therapeutic class: Antipsychotic, neuroleptic

Pregnancy risk category C

FDA Boxed Warning

• Drug increased mortality in elderly patients with dementia-related psychosis. Although causes of death were varied, most appeared to be cardiovascular or infectious. Drug isn't approved to treat dementia-related psychosis.

Action

Unclear. Thought to exert partial agonist activity at central dopamine D₂ and type 1A serotonin (5-HT_1A) receptors and antagonistic activity at serotonin 5-HT_2A receptors. Also has alpha-adrenergic and histamine₁-blocking properties.

Availability

Injection: 9.75 mg/1.3 ml (7.5 mg/ml)

Oral solution: 1 mg/ml

Tablets: 2 mg, 5 mg, 10 mg, 15 mg, 20 mg, 30 mg

Tablets (orally disintegrating): 10 mg, 15 mg

⊘Indications and dosages

➣ Schizophrenia

Adults: 10 to 15 mg P.O. daily. If needed, increase to 30 mg daily after 2 weeks.

➣ To maintain stability in schizophrenic patients

Adults: 15 mg P.O. daily. Therapy may continue for up to 26 weeks with periodic evaluations.

➣ Acute manic and mixed episodes associated with bipolar disorder

Adults: 30 mg P.O. daily for up to 3 weeks

➣ Agitation associated with schizophrenia or bipolar mania

Adults: Usual dosage, 5.25 to 15 mg I.M. as single dose. Recommended dosage is 9.75 mg I.M. as single dose. No additional benefit was demonstrated for 15 mg compared to 9.75 mg. Lower dosage of 5.25 mg may be considered when clinical factors warrant. If agitation warranting second dose persists following initial dose, cumulative dosages up to total of 30 mg/day may be given. However, efficacy of repeated doses in agitated patients hasn't been systematically evaluated in controlled clinical trials. Also, safety of total daily doses greater than 30 mg or injections given more frequently than every 2 hours hasn't been adequately evaluated in clinical trials. If ongoing aripiprazole therapy is clinically indicated, oral aripiprazole ranging from 10 to 30 mg/day P.O. should replace aripiprazole injection as soon as possible.

Dosage adjustment

• Concurrent use of potent CYP3A4 inhibitors (such as ketoconazole), CYP2D6 inhibitors (such as fluoxetine, paroxetine, quinidine), or CYP3A4 inducers (such as carbamazepine)

Contraindications

• Hypersensitivity to drug

Precautions

Use cautiously in:
• cerebrovascular disease, hypotension, seizure disorder, suicidal ideation
• high risk for aspiration pneumonia
• pregnant or breastfeeding patients
• children and adolescents (safety and efficacy not established).

Administration

• Give with or without food.
• Don't administer with grapefruit juice.

Route	Onset	Peak	Duration
P.O.	Slow	3-5 hr	Unknown

Adverse reactions

CNS: drowsiness, insomnia, akathisia, agitation, anxiety, headache, light-headedness, drowsiness, tremor, tardive dyskinesia, seizures, neuroleptic malignant syndrome, increased suicide risk

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

EENT: rhinitis

GI: nausea, vomiting, diarrhea, constipation, jaundice, abdominal pain, esophageal motility disorders

GU: urinary incontinence

Respiratory: cough

Skin: rash

Other: fever

Interactions

Drug-drug. CNS depressants: increased sedation

Drugs that induce CYP3A4: decreased aripiprazole effect

Drugs that inhibit CYP3A4 or CYP2D6: serious toxic effects

Other antipsychotic agents: increased extrapyramidal effects

Drug-herbs. Kava: increased CNS depression

Drug-behaviors. Alcohol use: increased sedation

Patient monitoring

☞ Watch for signs and symptoms of depression, and evaluate patient for suicidal ideation.
• Monitor neurologic status closely. Watch for tardive dyskinesia.
☞ Evaluate patient for neuroleptic malignant syndrome (fever, altered mental status, rigid muscles, arrhythmia, tachycardia, sweating). Stop drug and notify prescriber if these signs and symptoms occur.
• Monitor blood pressure, pulse, and weight.

Patient teaching

☞ Instruct patient to contact prescriber if he experiences depression or has suicidal thoughts.
• Advise patient to establish effective bedtime routine to minimize insomnia.
• Inform patient that symptoms will subside slowly over several weeks.
• Tell patient he may take drug with or without food.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient that drug may cause urinary incontinence.
• Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
• Caution patient to avoid strenuous exercise and hot environments whenever possible.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, herbs, and behaviors mentioned above.