Formulary
Aripiprazole: Indications, Dosing, Side Effects and Interactions
Aripiprazole is a dopamine D 2 partial agonist with weak 5-HT 1a partial agonism and 5-HT 2A receptor antagonism.
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Aripiprazole: Indications, Dosing, Side Effects and Interactions
Aripiprazole is a dopamine D 2 partial agonist with weak 5-HT 1a partial agonism and 5-HT 2A receptor antagonism.
Drug action
Aripiprazole is a dopamine D 2 partial agonist with weak 5-HT 1a partial agonism and 5-HT 2A receptor antagonism.
Indications and dose
**Schizophrenia**
- **Adult** (By Mouth): 10-15 mg once daily; usual dose 15 mg once daily (max. per dose 30 mg once daily).
**Treatment and recurrence prevention of mania**
- **Adult** (By Mouth): 15 mg once daily, increased if necessary up to 30 mg once daily.
**Rapid control of agitation and disturbed behaviour in schizophrenia and mania**
- **Adult** (By Intramuscular Injection Using Immediate-Release Medicines): Initially 5.25-15 mg for 1 dose, alternatively usual dose 9.75 mg for 1 dose, followed by 5.25-15 mg after 2 hours if required, maximum 3 injections daily; maximum daily combined oral and parenteral dose 30 mg.
**Maintenance of schizophrenia in patients stabilised with oral aripiprazole who are CYP2D6 poor metabolisers [using once-monthly intramuscular depot injection]**
- **Adult** (By Deep Intramuscular Injection Using Depot Injection): 300 mg every month, minimum of 26 days between injections, treatment with prescribed daily dose of oral aripiprazole should be continued for 14 consecutive days after the first injection, for dose adjustment due to side-effects and for advice on missed doses-consult product literature, alternatively initially 600 mg for 1 dose, to be administered as 2 consecutive 300 mg injections, along with a single previously prescribed dose of oral aripiprazole, then maintenance 300 mg every month, minimum of 26 days between injections, for dose adjustment due to side-effects and for advice on missed doses-consult product literature.
**Maintenance of schizophrenia in patients stabilised with oral aripiprazole [using once-monthly intramuscular depot injection]**
- **Adult** (By Deep Intramuscular Injection Using Depot Injection): 400 mg every month, minimum of 26 days between injections, treatment with 10-20 mg oral aripiprazole daily should be continued for 14 consecutive days after the first injection, for dose adjustment due to side-effects and for advice on missed doses-consult product literature, alternatively initially 800 mg for 1 dose, to be administered as 2 consecutive 400 mg injections, along with a single dose of 20 mg oral aripiprazole, then maintenance 400 mg every month, minimum of 26 days between injections, for dose adjustment due to side-effects and for advice on missed doses-consult product literature.
**Maintenance of schizophrenia in patients stabilised with oral aripiprazole who are CYP2D6 poor metabolisers [using a two-month intramuscular depot injection]**
- **Adult** (By Deep Intramuscular Injection Using Depot Injection): 720 mg every 2 months, keep 56 days between injections (may be given up to 2 weeks before or 2 weeks after scheduled dose), treatment with prescribed daily dose of oral aripiprazole should be continued for 14 consecutive days after the first injection, for dose adjustments due to side-effects and for advice on missed doses-consult product literature, alternatively initially 1.02 g for 1 dose, to be administered consecutively using one 720 mg aripiprazole two-month intramuscular depot injection and one 300 mg aripiprazole once-monthly intramuscular depot injection, along with a single dose of 20 mg oral aripiprazole, then maintenance 720 mg every 2 months, keep 56 days between injections (may be given up to 2 weeks before or 2 weeks after scheduled dose), for dose adjustments due to side-effects and for advice on missed doses-consult product literature.
**Maintenance of schizophrenia in patients stabilised with aripiprazole once-monthly intramuscular depot injection who are CYP2D6 poor metabolisers [using a two-month intramuscular depot injection]**
- **Adult** (By Deep Intramuscular Injection Using Depot Injection): 720 mg every 2 months, keep 56 days between injections (may be given up to 2 weeks before or 2 weeks after scheduled dose), initial dose to be given a minimum of 26 days after previous 300 mg aripiprazole once-monthly intramuscular depot injection, for dose adjustments due to side-effects and for advice on missed doses-consult product literature.
**Maintenance of schizophrenia in patients stabilised with oral aripiprazole [using a two-month intramuscular depot injection]**
- **Adult** (By Deep Intramuscular Injection Using Depot Injection): 960 mg every 2 months, keep 56 days between injections (may be given up to 2 weeks before or 2 weeks after scheduled dose), treatment with 10-20 mg oral aripiprazole daily should be continued for 14 consecutive days after the first injection, for dose adjustments due to side-effects and for advice on missed doses-consult product literature, alternatively initially 1.36 g for 1 dose, to be administered consecutively using one 960 mg aripiprazole two-month intramuscular depot injection and one 400 mg aripiprazole once-monthly intramuscular depot injection, along with a single dose of 20 mg oral aripiprazole, then maintenance 960 mg every 2 months, keep 56 days between injections (may be given up to 2 weeks before or 2 weeks after scheduled dose), for dose adjustments due to side-effects and for advice on missed doses-consult product literature.
**Maintenance of schizophrenia in patients stabilised with aripiprazole once-monthly intramuscular depot injection [using a two-month intramuscular depot injection]**
- **Adult** (By Deep Intramuscular Injection Using Depot Injection): 960 mg every 2 months, keep 56 days between injections (may be given up to 2 weeks before or 2 weeks after scheduled dose), initial dose to be given a minimum of 26 days after previous 400 mg aripiprazole once-monthly intramuscular depot injection, for dose adjustments due to side-effects and for advice on missed doses-consult product literature.
**Schizophrenia for aripiprazole**
- **Child 15-17 years (under expert supervision)** (By mouth): Initially 2 mg once daily for 2 days, increased to 5 mg once daily for 2 days, then increased to 10 mg once daily, then increased in steps of 5 mg if required; maximum 30 mg per day.
**Treatment of mania (under expert supervision) for aripiprazole**
- **Child 13-17 years** (By mouth): Initially 2 mg once daily for 2 days, increased to 5 mg once daily for 2 days, then increased to 10 mg once daily, increased in steps of 5 mg if required, maximum duration of treatment 12 weeks, doses above 10 mg daily should only be used in exceptional cases; maximum 30 mg per day.
Cautions
For all antipsychotic drugs Blood dyscrasias; cardiovascular disease; conditions predisposing to seizures; depression; diabetes (may raise blood glucose); epilepsy; history of jaundice; myasthenia gravis; Parkinson's disease (may be exacerbated); photosensitisation (may occur with higher dosages); prostatic hypertrophy; severe respiratory disease; susceptibility to angle-closure glaucoma Cautions, further information Cardiovascular disease An ECG may be required, particularly if physical examination identifies cardiovascular risk factors, personal history of cardiovascular disease, or if the patient is being admitted as an inpatient. Elderly Screening Tool of Older Persons' potentially inappropriate Prescriptions (STOPP) criteria to aid medication reviews (see Prescribing in the elderly for information). Potentially inappropriate: for all antipsychotics (other than quetiapine and clozapine) in patients with parkinsonism or Lewy Body Disease (risk of severe extrapyramidal symptoms) in behavioural and psychological symptoms of dementia (BPSD), unless symptoms are severe and other non-pharmacological treatments have failed (increased risk of stroke) for use as a hypnotic, unless sleep disorder is due to psychosis or dementia (risk of confusion, hypotension, extrapyramidal side-effects, and falls) in patients prone to falls (may cause gait dyspraxia, parkinsonism) if prescribed a phenothiazine (other than prochlorperazine for nausea, vomiting, or vertigo; chlorpromazine for relief of persistent hiccups; levomepromazine as an antiemetic in palliative care) as first-line treatment (sedative, significant antimuscarinic (anticholinergic) toxicity in older people, and safer and more efficacious alternatives exist) if prescribed an antipsychotic drug with moderate or marked antimuscarinic effects (e.g. chlorpromazine, clozapine, flupenthixol, fluphenazine, pipothiazine, promazine, and zuclopenthixol) in patients with a history of prostatism or urinary retention (high risk of urinary retention) Cautions For aripiprazole Cerebrovascular disease; elderly (reduce initial dose); risk of aspiration pneumonia
Side effects
For all antipsychotic drugs Common or very common Agitation; amenorrhoea; arrhythmias; constipation; dizziness; drowsiness; dry mouth; erectile dysfunction; fatigue; galactorrhoea; gynaecomastia; hyperglycaemia; hyperprolactinaemia; hypersalivation; hypotension (dose-related); insomnia; leucopenia; movement disorders; muscle rigidity; neutropenia; parkinsonism; postural hypotension (dose-related); QT interval prolongation; rash; seizure; tremor; urinary retention; vomiting; weight increased Uncommon Agranulocytosis; confusion; neuroleptic malignant syndrome (discontinue-potentially fatal) Rare or very rare Sudden death; withdrawal syndrome neonatal Side-effects, further information For depot antipsychotics-side-effects may persist until the drug has been cleared from its depot site. Overdose Phenothiazines cause less depression of consciousness and respiration than other sedatives. Hypotension, hypothermia, sinus tachycardia, and arrhythmias may complicate poisoning. For details on the management of poisoning see Antipsychotics under Emergency treatment of poisoning . Side-effects For aripiprazole General side-effects: Common or very common Anxiety; appetite abnormal; diabetes mellitus; gastrointestinal discomfort; headache; musculoskeletal stiffness; nausea; vision disorders; weight decreased Uncommon Alopecia; depression; diarrhoea; hiccups; hypertension; sexual dysfunction; suicidal behaviours; thrombocytopenia Frequency not known Cardiac arrest; diabetic hyperosmolar coma; diabetic ketoacidosis; dysphagia; embolism and thrombosis; generalised tonic-clonic seizure; hepatic disorders; hyperhidrosis; hyponatraemia; laryngospasm; oropharyngeal spasm; pancreatitis; pathological gambling; peripheral oedema; photosensitivity reaction; pneumonia aspiration; rhabdomyolysis; serotonin syndrome; speech disorder; syncope; temperature regulation disorder; urinary incontinence Specific side-effects: Uncommon With intramuscular use Altered smell sensation; anaemia; asthenia; behaviour abnormal; breast tenderness; chest discomfort; cough; drooling; dyslipidaemia; eye pain; fever; gait abnormal; gastrointestinal disorders; glycosuria; hyperinsulinaemia; joint disorders; muscle complaints; muscle tone increased; nephrolithiasis; oculogyric crisis; pain; skin reactions; sleep disorder; taste altered; thirst; vulvovaginal dryness Frequency not known With intramuscular use Binge eating; drug reaction with eosinophilia and systemic symptoms (DRESS); poriomania; psychiatric disorders With oral use Aggression; chest pain; myalgia
Interactions
**Severe interactions:**
- Valproate and lithium When either valproate or lithium was administered concomitantly with aripiprazole, there was no clinically significant change in aripiprazole concentrations and therefore no...
- Potential for aripiprazole to affect other medicinal products In clinical studies, 10 mg/day to 30 mg/day doses of aripiprazole had no significant effect on the metabolism of substrates of CYP2D6...
**Other interactions (23):**
- Due to its 1 -adrenergic receptor antagonism, aripiprazole has the potential to enhance the effect of certain antihypertensive medicinal products.
- Given the primary CNS effects of aripiprazole, caution should be used when aripiprazole is administered in combination with alcohol or other CNS medicinal products with overlapping adverse reactions...
- If aripiprazole is administered concomitantly with medicinal products known to cause QT prolongation or electrolyte imbalance, caution should be used.
- Potential for other medicinal products to affect aripiprazole A gastric acid blocker, the H 2 antagonist famotidine, reduces aripiprazole rate of absorption but this effect is deemed not clinically...
- Aripiprazole is metabolised by multiple pathways involving the CYP2D6 and CYP3A4 enzymes but not CYP1A enzymes.
- Quinidine and other CYP2D6 inhibitors In a clinical trial in healthy subjects, a strong inhibitor of CYP2D6 (quinidine) increased aripiprazole AUC by 107 %, while C max was unchanged.
Pregnancy
For all antipsychotic drugs Extrapyramidal effects and withdrawal syndrome have been reported occasionally in the neonate when antipsychotic drugs are taken during the third trimester of pregnancy. Following maternal use of antipsychotic drugs in the third trimester, neonates should be monitored for symptoms including agitation, hypertonia, hypotonia, tremor, drowsiness, feeding problems, and respiratory distress. Pregnancy For aripiprazole Use only if potential benefit outweighs risk.
Breast feeding
For all antipsychotic drugs There is limited information available on the short- and long-term effects of antipsychotic drugs on the breast-fed infant. Animal studies indicate possible adverse effects of antipsychotic medicines on the developing nervous system. Chronic treatment with antipsychotic drugs whilst breast-feeding should be avoided unless absolutely necessary. Phenothiazine derivatives are sometimes used in breast-feeding women for short-term treatment of nausea and vomiting. Breast feeding For aripiprazole Manufacturer advises avoid-present in milk.
Hepatic impairment
Manufacturer advises caution in severe impairment (oral treatment preferred to intramuscular administration; limited information available).
Medicinal forms
Solution,Tablet,Tablet,Solution,Solution,Suspension,Injection
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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