Aripiprazole: 7 things you should know

Medically reviewed by Carmen Fookes, BPharm. Last updated on April 4, 2022.

1. How it works

• Aripiprazole may be used to treat psychotic symptoms.
• Experts aren't sure exactly how aripiprazole works to relieve the symptoms of schizophrenia but suggest it may partially activate dopamine 2 and serotonin 1A receptors and block serotonin 2A receptors. It does appear to have some activity at other receptors, which may account for its side effects (for example its tendency to cause low blood pressure on standing may be due to its blocking effect on adrenergic alpha1 receptors).
• Aripiprazole belongs to the class of medicines known as atypical antipsychotics. Atypical means it is less likely than older antipsychotics to cause side effects, such as extrapyramidal symptoms (EPS). EPS are drug-induced movement disorders and include tremors, Parkinson's-like symptoms (walking with a shuffle, mask-like facial features), and tardive dyskinesia (this describes abnormal, repetitive facial movements such as lip-smacking or poking the tongue out).

2. Upsides

• Used orally and intramuscularly to relieve symptoms of psychosis (such as delusions and hallucinations) and agitation associated with schizophrenia. Considered a first-line agent by the American Psychiatric Association (APA).
• Used alone or in conjunction with lithium or valproate to treat manic or mixed episodes of bipolar I disorder with or without psychotic features.
• May also be used in addition to other medications in the treatment of depression.
• May be used to reduce irritability associated with autistic disorder. The dosage range in children and adolescents aged 6 to 17 years is 5 to 15 mg/day.
• Reduces tic severity in Tourette's syndrome. The recommended dosage in children is 5 to 20 mg/day starting at 2 mg/day and increasing slowly over at least a week.
• Available as a tablet, an orally disintegrating tablet, an oral solution, and an extended-release intramuscular (IM) injection. The IM injection is approved for the treatment of agitation associated with schizophrenia or bipolar mania.
• The recommended starting dosage is 10-15 mg/day for schizophrenia or bipolar disorder. Dosages up to 30 mg/day have been used; however, they have not been shown to be any more effective than 10-15 mg/day. Allow at least 2 weeks between dosage increases.
• May be used in adolescent patients with schizophrenia, aged 13 to 17 years. The recommended target dose is 10 mg/day.
• May be given with or without food.
• Available in six tablet strengths: 2mg, 5mg, 10mg, 15mg, 20mg, and 30mg.
• Orally disintegrating tablets are available as 10mg and 15mg strengths. The oral solution is 1mg/mL.
• The dosage of the oral solution can be substituted for the tablets on an mg per mg basis up to 25mg. For people receiving 30mg tablets, substitute 25mg (25mL) of solution.
• Aripiprazole is generic. Also available the branded version Abilify.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Akathisia (an inner restlessness), sedation, headache, insomnia, agitation, anxiety, nausea, tremor. Other reasonably common side effects include constipation, vomiting, dry mouth, stomach upsets, and extrapyramidal symptoms (such as restlessness, tremor, and uncontrolled muscle contractions). May also cause difficulty swallowing.
• Should not be used for the treatment of dementia-related psychosis in elderly people as associated with a higher risk of death.
• If being used as an adjunct therapy in the treatment of depression, monitor for worsening depression, agitation, or mood changes. May increase the risk of suicidal thoughts or behavior in young adults (similar to other antidepressants and antipsychotics).
• May cause a drop in blood pressure on standing, particularly during the initial dose-titration period; dosage may need reducing. May not be suitable for people with known cardiovascular disease (history of a heart attack, angina, heart failure, or arrhythmia), stroke, seizure disorders, and people at risk of dehydration.
• Blood levels may need monitoring as aripiprazole can cause numbers of white blood cells to decrease.
• May increase blood sugar levels. People with a history of diabetes or at risk of diabetes should be monitored closely. Less likely than some other antipsychotics to cause undesirable changes in blood cholesterol and lipid levels or to cause weight gain.
• Potentially irreversible tardive dyskinesia can develop, even with low dosages used short-term. Symptoms include facial grimacing, repetitive chewing, and tongue thrusting.
• Rarely, may cause Neuroleptic Malignant Syndrome; symptoms include high body temperature, muscle rigidity, and mental disturbances; discontinue immediately and seek urgent medical advice.
• May interact with several drugs, including benzodiazepines, carbamazepine, fluoxetine, and itraconazole. See prescribing information for a full list of interactions.
• There have been several substitution and dispensing errors reported between the two different extended-release IM forms of aripiprazole lauroxil, Aristada Initio, and Aristada. Aristada Initio is for single-dose administration only. Do not substitute Aristada Initio for Aristada.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Aripiprazole is an antipsychotic used in the treatment of schizophrenia and several other disorders. Aripiprazole is less likely than some other antipsychotics to cause weight gain.

5. Tips

• May be administered with or without food.
• Several brands of aripiprazole are available. Formulations include oral tablets, orally-disintegrating tablets, and an oral solution. Disintegrating tablets should not be removed from their blister until ready to administer. Dry hands should be used to peel back the foil on the blister rather than attempting to pop the tablet through the foil. The tablet should then be placed on the tongue. May be taken with or without liquid, but do not attempt to split the tablet.
• May cause sedation or impair judgment skills and affect your ability to drive or operate machinery. Avoid alcohol.
• Avoid overheating and dehydration.
• Seek urgent medical advice if you develop unusual body movements, confusion, high fever, lightheadedness, fainting, seizures, have problems controlling your body temperature, or difficulty swallowing.
• Aripiprazole may make you feel dizzy when going from a sitting or lying down position to standing. This may increase your risk of falls. Stand up slowly and remove any fall hazards from your home (such as loose rugs).
• Talk with your doctor if you develop any worrying side effects such as uncontrollable facial grimacing, restlessness, severe dizziness, or severe abdominal discomfort.
• Tell your doctor if you are intending to become pregnant and you are taking aripiprazole as your doctor may wish to change you to a different medication. Aripiprazole is incompatible with breastfeeding.

6. Response and effectiveness

• Peak blood levels are reached within three to five hours of taking oral aripiprazole. Effects are long-lasting, so aripiprazole is usually taken once daily.
• May take up to two weeks to achieve stable blood concentrations.
• Target dosages of 10-15mg per day of aripiprazole are recommended for schizophrenia; dosages above 15 mg/day are not more effective than 15 mg/day.
• Dosage reductions may be needed for people known to be poor metabolizers of drugs like aripiprazole, or in people taking other medications known to interfere with the hepatic enzymes CYP2D6 and CYP3A4. Conversely, a dosage increase of aripiprazole may be needed when given with medications that induce CYP3A4.

7. Interactions

Medicines that interact with aripiprazole may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with aripiprazole. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with aripiprazole include:

• anti-anxiety medications such as diazepam and oxazepam
• anticonvulsants, such as phenytoin
• antidepressants, such as amitriptyline, imipramine, nortriptyline
• antifungals, such as itraconazole or ketoconazole
• antihistamines that cause sedation, such as diphenhydramine
• bupropion
• CYP2D6 strong inhibitors (such as bupropion, fluoxetine, paroxetine, quinidine, or terbinafine. Administer half the usual dosage
• CYP3A4 strong inhibitors (such as clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal, or grapefruit). Administer half the usual dosage
• CYP3A4 strong inducers (such as carbamazepine or rifampin). Double the usual dosage over 1 to 2 weeks
• duloxetine
• HIV medications such as indinavir and ritonavir
• ipratropium
• grapefruit juice and products
• lithium
• methylphenidate
• migraine treatments, such as rizatriptan and sumatriptan
• monoamine oxidase inhibitors, such as selegiline, isocarboxazid, or phenelzine
• opioid analgesics such as oxycodone and morphine
• muscle relaxants such as cyclobenzaprine
• quinidine
• serotonin modulators, such as nefazodone and trazodone
• sleeping pills, such as zolpidem
• some chemotherapy treatments
• some heart medications, such as doxazosin and prazosin
• other medications used to treat mental illness, such as clozapine and thioridazine.

Alcohol may worsen the side effects of aripiprazole such as drowsiness, dizziness, and liver toxicity.

Note that this list is not all-inclusive and includes only common medications that may interact with aripiprazole. You should refer to the prescribing information for aripiprazole for a complete list of interactions.

References

• Aripiprazole. Revised 02/2022. Bionpharma Inc. https://www.drugs.com/pro/aripiprazole-odt.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use aripiprazole only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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