What is Aripiprazole?
Aripiprazole is an active ingredient used in the treatment of schizophrenia, bipolar disorder, autism and depression.
The brand names of Aripiprazole in the United States are: Abilify, Abilify Maintena, Aristada and Abilify MyCite.
Mechanism of action (MOA) Aripiprazole
Antipsychotic. Partial dopamine D2 receptor agonist and serotonin 5-HT1a and serotonin 5-HT2a receptor antagonist.
Therapeutic indications, uses and benefits of Aripiprazole
Oral use: schizophrenia in adults and adolescents >15 years.
Moderate or severe manic episodes in bipolar disorder I in adults and adolescents >13 years and in relapse prevention.
Intramuscular normal release: rapid control of agitation and behavioural alterations in schizophrenia, when oral treatment is not adequate.
Intramuscular prolonged release: maintenance treatment in schizophrenia in adult patients stabilized with oral aripiprazole.
Dosage of Aripiprazole
– Oral:
Adults.
Schizophrenia: initial, 10-15 mg/day; maintenance, 15 mg/day as a single daily dose. Manic episodes in bipolar disorder I: start, 15 mg as a single daily dose.
For the prevention of relapses of manic episodes continue with the same dose.
Consider daily dose adjustments, including reduction, according to clinical status. Effective dose range: 10-30 mg/day
Children.
Schizophrenia in adolescents 15 years and older and manic episodes in bipolar disorder I in adolescents 13 years and older: start with 2 mg for 2 days, increasing to 5 mg for 2 days to reach recommended dose, 10 mg/day.
The duration of treatment for manic episodes should be the minimum necessary for symptom control and should not exceed 12 weeks.
Irritability associated with autistic disorder: safety and efficacy in children and adolescents has not yet been established < 18 years with current data no posological recommendation can be made. The same is true for tics associated with Tourette’s disorder in children and adolescents between 6 and 18 years of age.
– Intramuscular adults:
Normal release: 9.75 mg as a single injection (into deltoid or gluteus major muscle). Effective dose range: 5.25-15 mg as a single injection.
Max. daily dose in all formulations: 30 mg .
Prolonged release: 400 mg as a single injection (buttock or deltoid) once a month (not earlier than 26 days after previous injection).
After the first injection, continue treatment with 10 to 20 mg of oral aripiprazole for 14 consecutive days to maintain therapeutic concentrations of aripiprazole during the onset of treatment. If adverse reactions occur with the 400 mg dose, a dose reduction to 300 mg once a month should be considered.
In slow metabolizers of CYP2D6, the starting and maintenance dose should be 300 mg. With potent CYP3A4 inhibitors, the dose should be reduced to 200 mg.
Method of administration
Oral use: oral-dispersible tablets or oral solution should be taken as an alternative to tablets in patients who have difficulty swallowing.
The buccodispersible tablet should be placed in the mouth, on the tongue, where it will quickly disperse with saliva. It can be taken with or without liquid. It can be dissolved in water and drink the resulting suspension.
Parenteral use:
– Normal release: administered via IM. In order to increase absorption and minimize variability, it is recommended to perform the injection in the deltoid or gluteus maximus muscle avoiding adipose areas.
– prolonged release: only via IM The suspension should be injected immediately after reconstitution, but can be kept in the vial at a temperature below 25 ºC for 4 hours.
The suspension should be injected slowly into the buttocks or deltoids, in a single administration.
Contraindications of Aripiprazole
Hypersensitivity to aripiprazole.
Warnings and Precautions with Aripiprazole
Severe liver failure, under 15 in schizophrenia and 13 in manic episodes; elderly.
Known cardiovascular disease (history of myocardial infarction or ischemic heart disease, heart failure, or conduction abnormalities), cerebrovascular disease, diseases that may predispose to hypotension (dehydration, hypovolaemia, and concomitant with antihypertensive drugs) or hypertension, including accelerated or malignant hypertension.
Identify all possible risk factors for VTE before and during treatment. Family history of prolonged QT interval. If signs of tardive dyskinesia appear, reduce dose or discontinue; in case of other extrapyramidal symptoms, close monitoring.
Stop treatment if signs and symptoms indicative of MNS develop, or have unexplained high fever without additional clinical manifestations of MNS. Epilepsy or history of seizures.
In elderly people with dementia-related psychosis, treatment is not indicated. Diabetes mellitus or with risk factors for diabetes mellitus, regular control. Hypersensitivity reactions.
Weight control (especially in adolescents), if the increase is significant, reduce the dose.
Dysphagia, aripiprazole should be used with caution in patients at risk of aspiration pneumonia. Pathological addiction to gambling, vigilance. Risk of suicidal tendencies.
Intramuscular normal release: with benzodiazepines by parenteral route (risk of excessive sedation and cardiorespiratory depression), monitor orthostatic hypotension; not evaluated efficacy and safety in alcohol or drug intoxication.
After the evaluation of the pharmacovigilance data it has been observed: risk of falls, since it can cause drowsiness, postural hypotension, motor and sensory instability.
Liver failure
Caution in severe hepatic insufficiency, adjust dose.
Interactions with Aripiprazole
- Increased plasma concentration with: quinidine, fluoxetine, paroxetine, ketoconazole, itraconazole and HIV protease inhibitors.
- Decreased plasma concentration with: carbamazepine, rifampicin, rifabutin, phenytoin, phenobarbital, primidone, efavirenz, nevirapine, St. John’s wort.
- Increases the effect of: certain antihypertensive agents.
- Caution with: alcohol or other substances of central action, substances that produce prolongation of the QT interval or electrolytic disorders.
- Concomitant with ISRS/IRSN risk of s. serotonergic.
Pregnancy and Aripiprazole
Due to insufficient human safety information and problems identified in animal reproduction studies, it should not be used in pregnancy, unless the expected benefit clearly justifies the potential risk to the foetus.
Breastfeeding
Aripiprazole is excreted in human breast milk. Patients should be warned not to breastfeed if they are taking aripiprazole.
Effects on driving ability
Aripiprazole acts on the central nervous system and can produce: drowsiness, dizziness, visual alterations and decreased ability to react. These effects as well as the disease itself make it advisable to be cautious when driving vehicles or operating dangerous machinery, especially until each patient’s particular sensitivity to the medication has been established.
Adverse reactions and side effects of Aripiprazole
Diabetes mellitus; insomnia, agitation, anxiety; headache, akathisia, drowsiness/sedation, tremor, extrapyramidal disorder, dizziness; blurred vision; nausea, vomiting, dyspepsia, constipation, salivary hypersecretion; fatigue; tachycardia; orthostatic hypotension; aggression; hiccup.
After the evaluation of the pharmacovigilance data it has been observed: oculogenic crisis.
⭐⭐⭐⭐⭐ VIDEO OF ABILIFY/ARIPIPRAZOLE (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: 82VFR53I78
ChemIDplus
DrugPortal
PubChem CID: 60795
NCI Thesaurus: C47403