Aripiprazole; Indications/Uses, Dosage, Side effects, Drug Interaction, Pregnancy

Aripiprazole
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Aripiprazole is a quinoline derivate and atypical antipsychotic agent. Aripiprazole has partial agonistic activity at dopamine D2 receptors and serotonin 5-HT1A receptors, as well as potent antagonistic activity on serotonin 5-HT2A receptors. This drug stabilizes dopamine and serotonin activity in the limbic and cortical system. Aripiprazole is used in managing symptoms of schizophrenia and of acute manic and mixed episodes associated with bipolar I disorders.

Aripiprazole is an atypical antipsychotic & it is recommended and primarily used in the treatment of schizophrenia and bipolar disorder. It is used to treat the symptoms of psychotic conditions such as schizophrenia and bipolar I disorder(manic depression). It is not known if aripiprazole is safe or effective in children younger than 13 with schizophrenia, or children younger than 10 with bipolar disorder.

Mechanism of Action of Aripiprazole

Aripiprazole’s antipsychotic activity is likely 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. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole’s antagonism of histamine H1 receptors may explain the somnolence observed with this drug.

Indications of Aripiprazole

Contra-Indications of Aripiprazole

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Dosages of Aripiprazole

Strengths:  2 mg; 5 mg; 10 mg; 15 mg; 20 mg; 30 mg;300 mg; 400 mg; 1 mg/mL; 9.75 mg/1.3 mL;

Schizophrenia

Oral
Immediate-Release

  • Initial dose: 10 or 15 mg orally once a day
  • Target dose: 10 to 15 mg per day; effective dose range 10 to 30 mg per day; however, clinical trials have not found doses exceeding 10 or 15 mg per day to be more effective.
  • Maximum dose: 30 mg/day

Parenteral
Aripiprazole Extended-Release IM Suspension

  • Initial dose: 400 mg IM once; continue aripiprazole 10 to 20 mg orally once a day for 14 days
  • Maintenance dose: 300 to 400 mg IM once a month; should not be given sooner than 26 days after the previous injection.

Aripiprazole Lauroxil Extended-Release IM Suspension

  • Patients stable on oral aripiprazole 10 mg/day: Initial dose 441 mg IM once; continue aripiprazole 10 mg orally once a day for 21 days.
  • Patients stable on oral aripiprazole 15 mg/day: Initial dose 662 mg IM once; continue aripiprazole 15 mg orally once a day for 21 days.
  • Patients stable on oral aripiprazole at least 20 mg/day: Initial dose 882 mg IM; continue oral aripiprazole once a day for 21 days.
  • Maintenance doses: 441 mg, 662 mg, or 882 mg IM monthly, 882 mg IM every 6 weeks, or 1064 mg IM every 2 months; this drug should not be given sooner than 14 days after the previous injection.

 Bipolar Disorder

Oral
Immediate-Release

  • Initial dose: 15 mg orally once a day
  • Target dose: 15 mg orally once a day; may increase dose based on clinical response. Dose increases, if needed, should be at 2-week intervals to allow time to achieve steady state.
  • Maximum dose: 30 mg/day

Adjunctive Therapy with Lithium or Valproate

  • Initial dose: 10 to 15 mg orally once a day
  • Target dose: 15 mg orally once a day; may increase dose based on clinical response.
  • Maximum dose: 30 mg/day

Parenteral
Aripiprazole Extended-Release IM Suspension

  • Initial dose: 400 mg IM once; continue aripiprazole 10 to 20 mg orally once a day for 14 days
  • Maintenance dose: 300 to 400 mg IM once a month; should not be given sooner than 26 days after the previous injection
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Depression

Oral
Immediate-Release

  • Initial dose: 2 to 5 mg orally once a day
  • Doses may be adjusted in increments up to 5 mg per day at intervals of no less than 1 week.
  • Maintenance dose: 2 to 15 mg once a day
  • Maximum dose: 15 mg/day

 Agitated State

Parenteral formulation

Immediate-Release

  • Initial dose: 9.75 mg IM once
  • Maintenance dose: 5.25 to 15 mg IM once
  • Maximum dose: 30 mg/day

Side Effects

The most common

More common

Rare

Drug Interactions

Aripiprazole may interact with following drug, ssupplements & may change the efficacy of drug

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Pregnancy Catagory of Aripiprazole

FDA Pregnancy Category C

Pregnancy

This medication falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Lactation

Aripiprazole has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from aripiprazole, a choice should be made whether to stop nursing or to stop use of this medication. The importance of the drug to the mother should be considered.

References

 

Aripiprazole

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