Aripiprazole, or Abilify, is a drug used mainly to treat schizophrenia and bipolar disorder. It is sold under a number of names, including Abilify

This article will look at the uses, modes of action, side effects, and precautions of this drug.

Fast facts on aripiprazole

Here are some key points about aripiprazole. More detail and supporting information is in the main article.

  • Aripiprazole is an atypical antipsychotic that is used schizophrenia and other conditions.
  • The exact mode of action for aripiprazole is still unclear.
  • Side effects can include aching limbs, dizziness and seizures.
  • Aripiprazole was first approved for use in schizophrenia in 2002.
  • It is being investigated for a potential role in the treatment of cocaine addiction.

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Aripiprazole is an antipsychotic that works at a number of receptors and transporters.

Aripiprazole is classed as an atypical (second-generation) antipsychotic. It works at a large number of sites, including receptors and transporters.

Its chemical name is C23H27Cl2N3O2

The drug mediates its action by either blocking receptors (antagonist) or by binding to them and inducing an opposite response to receptor's normal role (inverse agonist).

Aripiprazole exerts its impact via various receptors including multiple subtypes of serotonin, dopamine, adrenergic, muscarinic acetylcholine and histamine receptors. It also works on serotonin, norepinephrine and dopamine transporter proteins.

The drug was first approved by the US Food and Drug Administration (FDA) for use in schizophrenia in 2002.

Aripiprazole is used predominantly for the treatment of schizophrenia and bipolar disorder but can also be used as an add-on treatment for major depressive disorder, tic disorders, obsessive-compulsive disorders (OCD), and irritability associated with autism.

Schizophrenia

Schizophrenia was the first illness to be targeted by aripiprazole. The decision by the FDA to approve its use was based on clinical trials that showed aripiprazole's ability to lessen psychotic episodes and reduce relapses when compared to a placebo.

The current consensus of scientific opinion is that aripiprazole's effect is comparable to a number of other typical and atypical antipsychotics. It has fewer side effects than some, but more than others. Aripiprazole is considered a middle-range antipsychotic regarding its effectiveness.

Bipolar disorder

Aripiprazole can be effective in treating the acute manic episodes of bipolar disorder in adults, adolescents and children.

However, its effect is only useful for the manic phases with little or no effect on the depressive phases. For this reason, aripiprazole is often used in conjunction with mood stabilizers. This dual approach is effective, but it increases the risk of movement disorders (extrapyramidal symptoms).

Major depression

Some patients are prescribed aripiprazole in conjunction with antidepressants, however, as above, this increases the risk of movement disorders; there is also an additional risk of weight gain.

Autism

Aripiprazole can be useful in reducing some aspects of autistic behavior. Studies show that it can reduce irritability, hyperactivity and repetitive movements (stereotypy) in autistic children and youths.

The side effects include weight gain, drooling, tremors and sleepiness.

Obsessive-compulsive disorder

There is some evidence that low doses of aripiprazole can yield positive results in obsessive-compulsive disorders (OCD) that are resistant to selective serotonin reuptake inhibitors (SSRI) alone.

As with other atypical antipsychotics, the exact method of action for aripiprazole is not known. The design of the drug was based on the dopamine hypothesis.

The dopamine hypothesis predicts that dopamine hyperactivity in the mesolimbic pathways of the brain (also known as reward pathways) causes delusions, hallucinations and disorganized thoughts.

Dopamine inactivity in the mesocortical pathways (involved in cognitive control, motivation and emotional response) and the prefrontal cortex (an area implicated in planning complex cognitive behavior and moderating social behavior) leads to an impairment in linguistic ability, an inability to experience pleasure, and autism.

Aripiprazole's effects at dopamine receptors are thought to decrease dopamine production and stabilize the dopamine system.

As with any pharmacological intervention, there will be side effects. These can range from subtle to major.

Minor side effects include:

  • pain in the limbs or joints
  • headache
  • nervousness
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Aripiprazole could be dangerous if taken by elderly patients with dementia-related psychosis.

More serious side effects include:

  • irregular heart beat
  • breathing difficulties
  • tightening of neck muscles and throat
  • swelling of the eyes, face, mouth, throat, hands, ankles, feet, lower legs
  • hives, rashes and general itching
  • chest pain
  • seizures
  • sweating
  • stiffness
  • confusion
  • changes in vision
  • unusual movements
  • fever
  • stiff muscles

The use of aripiprazole involves some risks.

Elderly people with dementia-related psychosis

Research has found an increased risk of death with use of aripiprazole in patients aged 77 to 88 years with dementia-related psychosis, due to cerebrovascular events, or adverse effects on the circulatory system in the brain.

Neuroleptic malignant syndrome

Aripiprazole might induce neuroleptic malignant syndrome (NMS). NMS is a potentially life-threatening neurological disorder consisting of muscle rigidity, fever, delirium or coma and autonomic instability.

People with depression

During clinical trials, a small number of depressed children, teenagers, and young adults taking aripiprazole reported an increase in suicidal thoughts.

At this stage, the prevalence of this side effect in younger people is not known.

As with any drug that acts at a variety of different sites, research into its full capabilities is ongoing. Below are two areas of current research.

Potential role in cocaine addiction

Aripiprazole is known to stabilize mesocorticolimbic dopamine activity. This pathway is implicated in addictive behavior. A study in rats showed that aripiprazole reduced cocaine-seeking behavior. As such, it has implications for use in the treatment of cocaine addicts in the future.

Negative implications for methamphetamine addicts

Aripiprazole may be counter-productive as a treatment for methamphetamine addiction. It was found to increase methamphetamine's stimulant and euphoric effects. Aripiprazole also appeared to increase the desire for the drug.

Antipsychotics and gray matter

Antipsychotic medications are the most common treatment for individuals with schizophrenia, helping to relieve some of the debilitating symptoms caused by the disorder. But according to a study published in 2015, long-term use of these drugs may also negatively impact brain structure.