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Aripiprazole

Aripiprazole, sold under the brand name Abilify among others, is an atypical antipsychotic. It is recommended and primarily used in the treatment of schizophrenia and bipolar disorder. More

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Description

Aripiprazole, sold under the brand name Abilify among others, is an atypical antipsychotic. It is recommended and primarily used in the treatment of schizophrenia and bipolar disorder.

Generic Name

Aripiprazole

Chemical names

Aripiprazole, Abilitat, Abilify, Abilify Discmelt

Brand names

Arena, Aria, Aridus, Arip-MT, Arilan, Aripat-MD, Arisun, Aripra-MT, Arive, Arpicin, Arize, Arpit, Arza, Arpizol, Asprito, Arzu, Elrip, Real One, Pipra-A, Schizopra.

IUPAC name

7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-1,2,3,4-tetrahydroquinolin-2-one

Pharmacokinetics

  • Absorption: Well absorbed by oral route
  • Distribution: 99% protein binding
  • Metabolism: Hepatic
  • Excretion: Approximately  55% in feces and 25 % through urine

Actions

Aripiprazole's acts as antipsychotic due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.

Dosage/Dosage form

Oral dosage forms

  • Initial dose: 10-15 mg once daily.
  • Max dose: 30 mg once daily.
  • Usual maintenance dose: 15 mg once daily.

Therapeutic uses

Schizophrenia and related psychotic disorders.

Adverse effects/Side effects

Headache, insomnia, agitation, somnolence; constipation, dyspepsia, pain, vomiting, nausea, dizziness, dry mouth; abdominal pain; anxiety, orthostatic hypotension; akathisia; tremor, hypertonia and blurred vision.

Interaction

  • Inhibitors of CYP2D6 (e.g. fluoxetine or quinidine or paroxetine) or CYP3A4 (e.g. ketoconazole) can inhibit aripiprazole elimination and cause increased blood levels. 
  • Ingestion with a high-fat meal delays time to peak plasma level
  • Drugs that induce CYP3A4 (e.g. carbamazepine) could cause an increase in aripiprazole clearance and lower blood levels.
  • Increased CNS depression with ethanol.

Contraindications

Contraindicated in lactation, Hypersensitivity. 

Storage

Store at 59° to 86°F.

Information

Molecular weight

448.385

Molecular formula

C23H27Cl2N3O2

CAS number

129722-12-9

Precautions

  • Prevent overdose
  • Closely observe patients who are started on therapy for clinical worsening, suicidality, or unusual changes in behavior.
  • Caution when operating hazardous machinery