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[Pharmacology](https://durgical.com/en/pharmacology/) · [Second-generation antipsychotics](https://durgical.com/en/pharmacology/classes/second-generation-antipsychotics/)

# Aripiprazole

An atypical antipsychotic that is a partial agonist at D2: little prolactin rise and lower metabolic risk, but frequent restlessness (akathisia).

Updated 2026-11-01

- Class: [Second-generation antipsychotics](https://durgical.com/en/pharmacology/classes/second-generation-antipsychotics/)
- Receptor: Dopamine D2 receptor (partial agonist); serotonin 5-HT1A receptor shown
- ATC code: N05AX12

◎**Dopamine D2 receptor (partial agonist); serotonin 5-HT1A receptor shown**Aripiprazole

ⓘ The figure shows aripiprazole bound to the human serotonin 5-HT1A receptor (with its G protein), where it is also a partial agonist; no aripiprazole-bound D2 structure exists.

**Target in 3D:** Dopamine D2 receptor (partial agonist); serotonin 5-HT1A receptor shown. PDB structure 7E2Z (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/7E2Z) · Drag to rotate · pinch to zoom

## Mechanism of action

Aripiprazole is a partial agonist at D2 and 5-HT1A receptors and an antagonist at 5-HT2A. Where dopamine is in excess (mesolimbic) it acts as a brake; where it is low it gives some stimulation. So it raises prolactin little and causes less sedation and weight gain, but akathisia is common.

- Aripiprazole partly activates D2 and 5-HT1A receptors
- With excess dopamine it lowers the signal: less psychosis
- Some D2 signal remains: prolactin stays near normal
- Common side effect: akathisia (inner restlessness)

## Pharmacokinetics

**Absorption**
Taken by mouth; long-acting injections exist

**Metabolism**
Liver, by CYP2D6 and CYP3A4, to an active metabolite (dehydro-aripiprazole)

**Half-life**
Long: about 75 hours (about 94 hours for the active metabolite), longer in CYP2D6 poor metabolisers

## Indications

- Schizophrenia
- Manic and mixed episodes of bipolar I disorder
- Irritability associated with autistic disorder
- Tourette's disorder

## Adverse effects

### Common

- Akathisia and restlessness
- Nausea, headache and insomnia
- Less weight gain and prolactin rise than other atypicals

### Serious (rare, important)

- Compulsive urges: gambling, shopping, binge eating, sexual urges
- Worsening or new suicidal thoughts, watched for as with antidepressants
- Hyperglycaemia (less often than other atypicals)
- Neuroleptic malignant syndrome
- Tardive dyskinesia (may be irreversible)
- Higher mortality in older people with dementia-related psychosis (boxed warning)

## Contraindications

- Hypersensitivity to aripiprazole

## Key interactions

**Strong CYP2D6 inhibitors (fluoxetine, paroxetine) or CYP3A4 inhibitors (ketoconazole)**
Higher aripiprazole exposure

**Strong CYP3A4 inducers (carbamazepine, rifampicin)**
Lower levels and loss of effect

## What is monitored

- Restlessness and akathisia
- New compulsive behaviours
- Weight, glucose and lipids
- Mood and suicidal thoughts in young people

## Administration and safety

- Oral and long-acting injectable forms are different products and are not interchanged one-for-one
- Its long half-life means effects and side effects fade slowly after stopping

## Nursing care

- Asks about inner restlessness and the urge to keep moving (akathisia), which can be mistaken for worsening agitation
- Teaches the patient and family to report new urges to gamble, shop or binge eat
- Records weight, waist, glucose and lipids at baseline and during treatment
- Watches for fever, rigidity and confusion (neuroleptic malignant syndrome) and for abnormal movements; reports them at once

## Pregnancy and breastfeeding

Newborns exposed in the third trimester may have extrapyramidal or withdrawal symptoms (agitation, abnormal tone, tremor, feeding problems); use weighs benefit and risk.

## Memory aid

Aripiprazole is the «thermostat»: it turns dopamine down where it is too high and up where it is too low, but it makes the legs restless.

## Test yourself

Think of the answer, then tap the question to see it.

## Why does aripiprazole raise prolactin less than risperidone?

As a D2 partial agonist it keeps some dopamine signalling at the pituitary, so prolactin stays near normal.

## Which movement side effect is especially common with aripiprazole?

Akathisia: an inner restlessness with an urge to keep moving.

## Which unusual behavioural side effects are listed for aripiprazole?

Compulsive urges such as gambling, shopping, binge eating and sexual urges.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/aripiprazole/)

## Related drugs

- [Risperidone](https://durgical.com/en/pharmacology/risperidone/)
- [Quetiapine](https://durgical.com/en/pharmacology/quetiapine/)

[← Back to the class: Second-generation antipsychotics](https://durgical.com/en/pharmacology/classes/second-generation-antipsychotics/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - ARIPIPRAZOLE tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=abb8ad7e-7998-4485-a09f-a2892190f4ad) (DailyMed (U.S. National Library of Medicine), 2026); [Aripiprazole: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a603012.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/?query=aripiprazole) (World Health Organization, 2025); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 19 (McGraw Hill, 2023).

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Representative model, for educational purposes only.

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