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Antipsychotics: The Essentials Module 2 Mechanism of Action of Aripiprazole

Learn about aripiprazole as a partial agonist on dopamine pathways, its impact on schizophrenia, and how it differs from other antipsychotics in managing symptoms and risks. Understand its effects on dopamine systems and why it's favored for its lower side effect profile.

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Antipsychotics: The Essentials Module 2 Mechanism of Action of Aripiprazole

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  1. Antipsychotics: The EssentialsModule 2Mechanism of Action of Aripiprazole FlavioGuzmán, MD

  2. Aripiprazole is a partial agonist that acts on mesolimbic and mesocortical dopamine pathways.

  3. What is an partial agonist?

  4. Aripiprazole as partial agonist

  5. Partial agonism in the mesolimbic pathway

  6. Dopamine Activity in Healthy Individuals Dopaminergic neurotransmission Maximal Activity Normal Activity Basal Activity log [drug] Courtesy of Richard Mailman, modified from Mailman RB, Murthy V. Current pharmaceutical design 2010;16:488-501.

  7. Schizophrenia: overactivity of the mesolimbic pathway Dopaminergic neurotransmission Maximal Activity Schizophrenia Basal Activity log [drug] Courtesy of Richard Mailman, modified from Mailman RB, Murthy V. Current pharmaceutical design 2010;16:488-501.

  8. Aripiprazole therapy Dopaminergic neurotransmission Dotted sigmoidal line: actions of partial agonist in the presence of endogenous concentrations of dopamine. Maximal Activity Schizophrenia Basal Activity log [drug] Courtesy of Richard Mailman, modified from Mailman RB, Murthy V. Current pharmaceutical design 2010;16:488-501.

  9. Partial agonism in the mesocortical pathway

  10. Dopamine Activity in Normal Circumstances Dopaminergic neurotransmission Maximal Activity Normal Activity Basal Activity log [drug] Courtesy of Richard Mailman, modified from Mailman RB, Murthy V. Current pharmaceutical design 2010;16:488-501.

  11. Dopamine System in Schizophrenia Maximal Activity Normal Activity Schizophrenia Basal Activity log [drug] Courtesy of Richard Mailman, modified from Mailman RB, Murthy V. Current pharmaceutical design 2010;16:488-501.

  12. Aripiprazole Therapy Dopaminergic neurotransmission Maximal Activity Normal Activity Schizophrenia Basal Activity log [drug] Courtesy of Richard Mailman, modified from Mailman RB, Murthy V. Current pharmaceutical design 2010;16:488-501.

  13. Aripiprazole effects on other dopamine pathways Tuberoinfundibular Pathway Nigrostriatal Pathway Less risk of hyperprolactinemia Less risk of EPS

  14. Other pharmacological properties

  15. Key Points • Aripiprazole is a partial agonist at D2 receptors. • It may act as an antipsychotic by: • Lowering dopaminergic neurotransmission in the mesolimbic pathway. • Enhancing dopaminergic activity in the mesocortical pathway. • It has a lower risk of EPS and hyperprolactinemia than other antipsychotics.

  16. References and further reading • Mailman RB, Murthy V. Third generation antipsychotic drugs: partial agonism or receptor functional selectivity? Current pharmaceutical design 2010;16:488-501. • Brunton LB, Lazo JS, Parker KL, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw-Hill; 2010. • Stahl, S M. Stahl's Essential Psychopharmacology: Neuroscientific Basis and Practical Applications. 3rd ed. New York: Cambrigde University Press; 2008

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