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Aripiprazole

Aripiprazole is a second-generation (atypical) antipsychotic medication widely used for the treatment of schizophrenia, bipolar disorder, and as an adjunctive therapy for major depressive disorder (MDD). It is also approved for the treatment of irritability associated with autism spectrum disorder (ASD) in pediatric patients. Aripiprazole is known for its unique mechanism of action as a partial dopamine agonist, which differentiates it from other antipsychotics. This article provides a detailed overview of aripiprazole, including its mechanism of action, uses, dosage, side effects, precautions, drug interactions, and generic names, referencing authoritative sources such as the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.

Aripiprazole exerts its therapeutic effects through its action on multiple neurotransmitter systems in the brain. Its key mechanisms include:

  1. Dopamine Partial Agonism:
    • Aripiprazole acts as a partial agonist at dopamine D2 and D3 receptors. This means it stabilizes dopamine activity by acting as an agonist in areas with low dopamine levels (improving negative symptoms) and as an antagonist in areas with high dopamine levels (reducing positive symptoms).
    • This unique action contributes to its efficacy in treating schizophrenia and bipolar disorder with a lower risk of extrapyramidal side effects (EPS) and hyperprolactinemia.
  2. Serotonin Receptor Modulation:
    • Aripiprazole is a partial agonist at serotonin 5-HT1A receptors, which may contribute to its antidepressant and anxiolytic effects.
    • It is an antagonist at serotonin 5-HT2A receptors, which helps improve negative symptoms and reduce the risk of EPS.
  3. Other Receptor Interactions:
    • Aripiprazole has affinity for adrenergic α1 and histamine H1 receptors, which contributes to its side effect profile (e.g., sedation, orthostatic hypotension).
  4. Stabilization of Neurotransmitter Systems:
    • By modulating dopamine and serotonin activity, aripiprazole helps stabilize mood and reduce psychotic symptoms.

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