ARIPIPRAZOLE

ARIPIPRAZOLe
(a-rip'-i-pra-zole)
Abilify
Classifications: psychotherapeutic; antipsychotic, atypical; dopamine system stabilizer;
Therapeutic: atypical antipsychotic

Prototype: Clozapine
Pregnancy Category: C

Availability

10 mg, 15 mg, 20 mg, 30 mg tablets; 1 mg/mL oral solution

Action

Efficacy of aripiprazole may be mediated through a combination of partial agonist activity at D2 and 5-HT1A receptors and antagonist activity at 5-HT2A receptors.

Therapeutic Effect

Partial dopaminergic agonist property of aripiprazole accounts for antipsychotic treatment of schizophrenic and bipolar individuals.

Uses

Treatment of schizophrenia, bipolar mania, maintenance in bipolar 1 disorder.

Unlabeled Uses

Depression with psychotic features.

Contraindications

Hypersensitivity to aripiprazole; dementia in elderly; QT prolongation; lactation; pregnancy (category C).

Cautious Use

History of seizures or conditions that lower seizure threshold (e.g., Alzheimer's dementia); suicidal ideation; brain tumor; dementia; diabetes mellitus; patients with known cardiovascular disease (history of MI or ischemic heart disease, heart failure, or conduction abnormalities), cerebrovascular disease, or conditions that predispose to hypotension (dehydration, hypovolemia, and treatment with antihypertensive medications); dysphagia; ethanol intoxication; hyperglycemia, hypothermia; obesity, elderly, children <18 y.

Route & Dosage

Schizophrenia
Adult: PO 10–15 mg once daily, may increase at 2-wk intervals to max of 30 mg/d if needed

Bipolar Mania
Adult: PO 30 mg once daily, may reduce to 15 mg/d

Administration

Oral
  • Note that dose should be reduced by 50% with concurrent treatment with ketoconazole, quinidine, fluoxetine, or paroxetine.
  • Store at 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

Body as a Whole: Headache, asthenia, fever, flu-like symptoms, peripheral edema, chest pain, neck pain, neck rigidity. CNS: Anxiety, insomnia, lightheadedness, somnolence, akathisia, tremor, extrapyramidal symptoms, depression, nervousness, increased salivation, hostility, suicidal thought, manic reaction, abnormal gait, confusion, cogwheel rigidity. CV: Hypertension, tachycardia, hypotension, bradycardia. Risk of stroke in elderly with dementia-related psychosis. GI: Nausea, vomiting, constipation, anorexia. Hematologic: Ecchymosis, anemia. Metabolic: Weight gain, weight loss, hyperglycemia, diabetes mellitus, increased creatine kinase. Musculoskeletal: Muscle cramp. Respiratory: Rhinitis, cough. Skin: Rash. Special Senses: Blurred vision.

Interactions

Drug: Carbamazepine will decrease aripiprazole levels (may need to double aripiprazole dose); ketoconazole, quinidine, fluoxetine, paroxetine may increase aripiprazole levels (reduce dose by ?); may enhance effects of antihypertensive agents. Herbal: St. John's wort may decrease aripiprazole levels. Food: High fat meals may delay time to peak plasma levels.

Pharmacokinetics

Absorption: 87% bioavailable. Peak: 3–5 h. Metabolism: In liver by CYP3A4 and 2D6. Major metabolite, has some activity. Elimination: 55% in feces, 25% in urine. Half-Life: 75 h (94 h for metabolite).

Nursing Implications

Assessment & Drug Effects

  • Monitor diabetics for loss of glycemic control.
  • Monitor cardiovascular status. Assess for and report orthostatic hypotension. Take BP supine then in sitting position. Report systolic drop of >15–20 mm Hg. Patients at increased risk are those who are dehydrated, hypovolemic, or receiving concurrent antihypertensive therapy.
  • Monitor body temperature in situations likely to elevate core temperature (e.g., exercising strenuously, exposure to extreme heat, receiving drugs with anticholinergic activity, or being subject to dehydration).
  • Monitor for and report signs of tardive dyskinesia.
  • Monitor for and immediately report S&S of neuroleptic malignant syndrome (NMS) that include: hyperpyrexia, muscle rigidity, altered mental status, irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia. Withhold drug if NMS is suspected.
  • Lab tests: Monitor periodically Hct & Hgb. Monitor periodically blood glucose. Monitor for elevated CPK and myoglobinuria if NMS is suspected.

Patient & Family Education

  • Carefully monitor blood glucose levels if diabetic.
  • Do not drive or engage in other potentially hazardous activities until reaction to drug is known.
  • Avoid situations where you are likely to become overheated or dehydrated.
  • Notify physician if you become pregnant or intend to become pregnant while taking this drug.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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