Autism Spectrum Disorder Medication

Updated: Sep 30, 2019
  • Author: James Robert Brasic, MD, MPH; Chief Editor: Caroly Pataki, MD  more...
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Medication

Medication Summary

The established therapies for autistic disorder are nonpharmacologic. These therapies may include behavioral, educational, and psychological treatment. No pharmacologic agent is effective in the treatment of the core behavioral manifestations of autistic disorder. However, medication may be effective in the treatment of comorbid disorders, including self-injurious behaviors and movement disorders.

Simultaneous treatment with two or more antipsychotics may be beneficial to treat agitation/irritability, physical aggression, and self-injurious behaviors of patients with ASD, particularly moderately to severely ill males with autism and intellectual disability. Generally these treatment regimens are well tolerated without serious adverse events. [182]

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Second-Generation Antipsychotics

Class Summary

The atypical antipsychotic agents risperidone and aripiprazole have been approved by the FDA for irritability associated with autistic disorders.

Risperidone (Risperdal, Risperdal Consta, Risperdal M-Tab)

Risperidone is an atypical antipsychotic agent that is indicated for irritability associated with autistic disorder in children and adolescents aged 5-16 years. Risperidone is a mixed serotonin-dopamine antagonist that binds to 5-HT2 with very high affinity and binds to the dopamine D2 receptor with less affinity. Affinity for the dopamine D2 receptor is 20 times lower than that for the 5-HT2 receptor. Risperidone is FDA approved for irritability and aggression in children with ASD, 5 years and older. 

The combination of serotonin antagonism and dopamine antagonism is thought to improve negative symptoms of psychoses and reduce the incidence of extrapyramidal side effects in comparison with conventional antipsychotics.

Aripiprazole (Abilify, Abilify MyCite)

Aripiprazole is indicated for irritability associated with autistic disorder in children and adolescents aged 6-17 years. Aripiprazole is thought to be a partial dopamine (D2) and serotonin (5-HT1A) agonist, and to antagonize serotonin (5-HT2A). Aripiprazole is available as a tablet, an orally disintegrating tablet, or an oral solution.

Ziprasidone (Geodon)

Ziprasidone, a second-generation antipsychotic drug, is used off-label to treat serious behavior disorders associated with autism, such as self-injurious behavior. It elicits its effects through antagonism of D2, D3, 5-HT2A, 5-HT2C, 5-HT1A, 5-HT1D, and alpha1-adrenergic receptors. In addition, it has a moderate antagonistic effect for histamine H1. It moderately inhibits the reuptake of serotonin and norepinephrine.

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SSRI Antidepressants

Class Summary

SSRIs are widely prescribed for children with autism or a related condition. These agents are used off-label to help with intractable repetitive behaviors, such as compulsion.

Fluoxetine (Prozac)

Fluoxetine selectively inhibits presynaptic serotonin reuptake, with minimal or no effect on the reuptake of norepinephrine and dopamine.

Citalopram (Celexa)

Citalopram enhances serotonin activity by selective reuptake inhibition of serotonin at the neuronal membrane. Dose-dependent QT prolongation has been reported with citalopram. [149, 150] . This agent is contraindicated in patients with congenital long QT syndrome.

Escitalopram (Lexapro)

Escitalopram is an S-enantiomer of citalopram. The mechanism of action is thought to be potentiation of serotonergic activity in the central nervous system (CNS), resulting from the inhibition of CNS neuronal reuptake of serotonin.

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Stimulants

Class Summary

Stimulants may be effective for treating hyperactivity associated with autism. The magnitude of response, however, is less than that seen in developmentally normal children with attention deficit hyperactivity disorder

Methylphenidate (Ritalin, Quillivant XR, Ritalin LA, Concerta)

Methylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. Methylphenidate is a racemic mixture composed of the d- and l-enantiomers. The d-enantiomer is more pharmacologically active than the l-enantiomer.

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Alpha-2-adrenergic agonists

Class Summary

Alpha-2-adrenergic agonists may facilitate the management of inattention, hyperactivity, and impulsivity in children with ASD.

Clonidine (Catapres, Catapres-TTS, Kapvay)

Clonidine stimulates alpha2-adrenoreceptors in the brain stem, activating an inhibitory neuron, which in turn results in reduced sympathetic outflow. These effects result in a decrease in vasomotor tone and heart rate. May aid in the treatment of agression in children and adolescents.

Guanfacine (Intuniv)

Guanfacine, an alpha2 agonist, may preferentially bind postsynaptic alpha2A adrenoreceptors in the prefrontal cortex, and this preferential binding may improve delay-related firing of prefrontal cortex neurons. As a result, guanfacine may affect behavioral inhibition. It has been used off label to reduce hyperactivity in children.

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