Classics in Chemical Neuroscience: Risperidone

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Abstract
After identifying the influence of serotonergic receptors in ameliorating the negative symptoms associated with schizophrenia, atypical antipsychotics were developed incorporating dopamine and serotonin antagonism. Risperidone, sold under the trade name Risperdal, was the second atypical antipsychotic developed following clozapine, but quickly became a first-line treatment for acute and chronic schizophrenia due to its preferential side effect profile. Despite initial FDA-approval 25 years ago, risperidone continues to be a fundamental treatment in schizophrenia, bipolar I disorder, and autism-related irritability. It is on the World Health Organization’s List of Essential Medicines for its balance of efficacy, safety, tolerability, and cost-effectiveness. In this review, we highlight the history and importance of risperidone as an atypical antipsychotic, in addition to its chemical synthesis, manufacturing, drug metabolism and pharmacokinetics, pharmacology, structure-activity relationship, indications, and adverse effects.
Funding Information
  • National Institute of Mental Health (MH082867)

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