Aripiprazole

Trade Names:
Abilify
- Tablets 2 mg
- Tablets 5 mg
- Tablets 10 mg
- Tablets 15 mg
- Tablets 20 mg
- Tablets 30 mg
- Solution, oral 1 mg/mL
- Injection 7.5 mg/mL

Trade Names:
Abilify Discmelt
- Tablets, orally disintegrating 10 mg
- Tablets, orally disintegrating 15 mg

Pharmacology

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Partial agonist at dopamine D ₂ and serotonin 5-HT _1A receptors, and antagonist at serotonin 5-HT _2A receptor.

Pharmacokinetics

Absorption

Well absorbed; steady state is attained within 14 days. T _max is 3 to 5 h and bioavailability is 87%.

T _max is 1 to 3 h and absolute bioavailability is 100%.

Distribution

More than 99% is protein bound, primarily to albumin. Vd is 404 L or 4.9 L/kg.

Metabolism

Hepatic metabolism (dehydrogenation, hydroxylation, N-dealkylation) involves CYP2D6 and CYP3A4. Major metabolite is dehydro-aripiprazole (active).

Elimination

Approximately 25% excreted in urine (less than 1% unchanged) and 55% in feces (approximately 18% as unchanged drug). Elimination t _½ is 75 h (aripiprazole) and 94 h (dehydro-aripiprazole).

Special Populations

In severe renal function impairment (Ccr less than 30 mL/min), C _max increased 36% (parent drug) and 53% (metabolite), but AUC was 15% lower for aripiprazole and 7% higher for metabolite. No dosage adjustment needed.

AUC increased 31% in mild hepatic function impairment, increased 8% in moderate impairment, and decreased 20% in severe impairment. No dosage adjustment required.

Cl was 20% lower. No dosage adjustment required.

C _max and AUC are 30% to 40% higher in women than in men. No dosage adjustment required.

Indications and Usage

Treatment of schizophrenia; treatment of acute manic and mixed episodes associated with bipolar disorder.

Treatment of agitation associated with schizophrenia or bipolar disorder, manic or mixed.

Contraindications

Standard considerations.

Dosage and Administration

PO Start with 10 or 15 mg/day on a daily schedule. The effective dose range is 10 to 30 mg/day. Do not increase dosage before 2 wk.

PO Start with 30 mg once daily. Approximately 15% of patients had dose decreased to 15 mg/day based on tolerability.

IM Recommended dose is 9.75 mg. A lower dose of 5.25 mg may be considered based on clinical factors. If agitation persists, cumulative doses up to 30 mg/day may be given.

PO Reduce the usual dose of aripiprazole 50%. Increase the dose when the CYP3A4 or CYP2D6 inhibitor is discontinued.

PO Double the usual dose of aripiprazole (to 20 to 30 mg). Base additional increases on clinical evaluation. Decrease the dose (to 10 to 15 mg) when the CYP3A4 inducer is discontinued.

No evidence is available from controlled trials. Periodically reassess patient to determine need for maintenance treatment.

Storage/Stability

Store at 59° to 86°F. Oral solution: Store at 59° to 86°F. Opened bottle can be used for up to 6 months after opening.

Store at 59° to 86°F. Protect from light by storing in carton until use.

Drug Interactions

Avoid while taking aripiprazole.

May elevate aripiprazole plasma levels, increasing the adverse reactions.

May reduce aripiprazole plasma levels, decreasing the therapeutic effect.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension, tachycardia (2%); hypotension (at least 1%).

CNS

Headache (30%); anxiety (20%); insomnia (19%); akathisia (15%); dizziness, sedation (11%); tremor (8%); somnolence (7%); extrapyramidal disorder, fatigue, restlessness (6%); aggression, appetite decreased, asthenia, confusional state, delusion, depression, dyskinesia, gait disturbance, hallucination, irritability, lethargy, mania, mood altered, paranoia, pyrexia, schizophrenia, suicidal ideation (at least 1%); generalized tonic-clonic seizure (postmarketing).

Dermatologic

Contusion, skin laceration (at least 1%).

EENT

Pharyngolaryngeal pain (4%); blurred vision, nasal congestion (3%); conjunctivitis (at least 1%).

GI

Nausea (16%); constipation (13%); vomiting (12%); dyspepsia (10%); dry mouth (5%); abdominal discomfort, stomach discomfort (3%); salivary hypersecretion (2%); loose stools (at least 1%).

Hepatic

Jaundice (postmarketing).

Metabolic-Nutritional

Weight gain (3%); blood CPK increased, dehydration, weight loss (at least 1%).

Musculoskeletal

Arthralgia (5%); pain in extremity (4%); stiffness (1%); fracture, muscle cramp, muscle pain, muscle rigidity, musculoskeletal pain (at least 1%).

Respiratory

Cough (3%); dyspnea, pneumonia, upper and lower respiratory tract infection (at least 1%)

Miscellaneous

Pain (3%); peripheral edema (2%); chest pain, fall (at least 1%); allergic reaction including anaphylactic reaction, angioedema, laryngospasm, oropharyngeal spasm, pruritus, urticaria (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Aspiration pneumonia

Antipsychotics have been associated with esophageal dysmotility and aspiration; use with caution in patients at risk for aspiration pneumonia.

Cerebrovascular adverse reactions

The risk of cerebrovascular adverse reactions (eg, stroke, transient ischemic attack) may be increased.

Cognitive and motor skills

Cognitive and motor skills may be impaired; caution patients about operating hazardous machinery or driving until they are reasonably certain that therapy does not affect them adversely.

Dosage adjustment

Adjust dosage when aripiprazole is used concomitantly with potential CYP3A4 inhibitor or inducer, or with potential CYP2D6 inhibitor.

Hyperglycemia and diabetes mellitus

Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, may occur.

Neuroleptic malignant syndrome (NMS)

NMS has occurred with antipsychotics and is potentially fatal. Signs and symptoms are altered mental status, diaphoresis, hyperpyrexia, irregular BP, irregular pulse, muscle rigidity, and tachycardia.

Orthostatic hypotension

May occur.

Seizures

Seizures may occur; use with caution in patients with a history of seizures or with conditions that potentially lower the seizure threshold.

Suicide

Closely supervise high-risk patients; do not give excessive quantities.

Tardive dyskinesia

A potentially irreversible syndrome of involuntary body and facial movements may occur.

Temperature regulation

Antipsychotics can disrupt the body's ability to reduce core temperature.

Overdosage

Symptoms

Somnolence, tremor, vomiting.

Patient Information

• Explain name, dose, action, and potential adverse reactions of drug, including risk of developing tardive dyskinesia.
• Instruct patient to take prescribed dose once daily without regard to meals but to take with food if stomach upset occurs.
• Instruct patient not to open blister for orally disintegrating tablet until ready to administer.
• Inform patient that orally disintegrating tablet should be placed on the tongue and that disintegration occurs rapidly in saliva. It may be taken without water.
• Advise phenylketonuric patients that orally disintegrating tablet contains phenylalanine.
• Instruct patient not to stop taking aripiprazole when feeling better.
• Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Instruct diabetic patient to monitor blood glucose more frequently when drug is started or dose is changed and to inform health care provider of significant changes in readings.
• Tell patient to immediately report high fever, muscle rigidity, altered mental status, irregular or rapid pulse, sweating, racing thoughts, mood swings, irritability, unquenchable thirst, frequent urination, seizures, or rash to health care provider.
• Advise patient to avoid strenuous activity during periods of high temperature or humidity.
• Instruct patient to avoid alcoholic beverages while taking aripiprazole.
• Instruct patient to get up slowly from lying or sitting position and to avoid sudden position changes to prevent postural hypotension. Advise patient to report dizziness with position changes to health care provider. Caution patient that hot tubs, or hot showers or baths may make dizziness worse.
• Advise patient taking antihypertensives to monitor BP at regular intervals.
• Advise patient that drug may impair judgment, thinking, or motor skills, or cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
• Advise patient to notify health care provider of the following symptoms: constipation, excessive drowsiness, increased agitation or anxiety, involuntary body or facial movements, nausea, vomiting.

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