Products
Aripiprazole is commercially available in tablet, meltable tablet, syrup, solution for injection, and sustained-release injection suspension forms (Abilify, Abilify Maintena, generics). It has been approved in many countries since 2004 and in the United States since 2002. Generics entered the market in 2015. Also used is the prodrug aripiprazollauroxil (Aristada).
Structure and properties
Aripiprazole (C23H27Cl2N3O2, Mr = 448.4 g/mol) is a piperazine and quinolinone derivative that differs structurally from previous neuroleptics. The active metabolite dehydroaripiprazole has a similar pharmacologic profile to the parent compound.
Effects
Aripiprazole (ATC N05AX12) has antipsychotic properties. Effects are attributed in part to partial agonism at dopamine D2 receptors and serotonin-5HT1a receptors and an antagonism at serotonin-5HT2a receptors. In addition, aripiprazole interacts with other neurotransmitter systems. It has a long half-life of 75 hours.
Indications
Aripiprazole is approved in many countries for the treatment of schizophrenia and manic or mixed episodes in bipolar disorder. In other countries, the range of indications is somewhat broader and additionally includes depression (adjunctive treatment), irritability in autism, and agitation in schizophrenia, among others. Other potential uses are mentioned in the literature.
Dosage
According to the drug label. Aripiprazole is taken independently of meals when administered perorally. Because of its long half-life, once-daily administration is sufficient.
Contraindications
- Hypersensitivity
Full details of precautions and interactions can be found in the drug label.
Interactions
Aripiprazole is metabolized by CYP3A4 and CYP2D6, and corresponding interactions with CYP inhibitors and inducers are possible. Other centrally acting drugs and alcohol may potentiate adverse effects. Aripiprazole is an alpha blocker and may potentiate blood pressure lowering when taken concomitantly with antihypertensive agents.
Adverse Effects
Headache, insomnia, and nausea are very common. Aripiprazole is an alpha blocker and therefore may lower blood pressure and often cause orthostatic hypotension and rapid heartbeat. Other common side effects include anxiety, agitation, weakness, fatigue, drowsiness, vomiting, constipation, increased salivation, visual disturbances, movement disorders, dizziness, dullness, tremor, and extrapyramidal symptoms.
