Receptor-Binding Profiles of Antipsychotics: Clinical Strategies When Switching Between Agents
J Clin Psychiatry 2007;68(suppl 6):5-9
© Copyright 2015 Physicians Postgraduate Press, Inc.
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In spite of apparent improvements in the pharmacotherapy of schizophrenia, many patients still
demonstrate an incomplete therapeutic response to antipsychotic medication and/or intolerable adverse
effects, necessitating a change in their medication regimen. The switch from one antipsychotic
to another, however, is not without challenges and can be complicated by withdrawal-emergent adverse
effects that prompt the patient or the clinician to abort the switch. The extent to which these
adverse events can be predicted by comparing the effects of the old and new antipsychotic medications
on various receptor systems, including dopaminergic, muscarinic, and histaminergic receptors,
is of considerable clinical and research interest. For example, patients receiving a sedating antipsychotic
with high affinity for histamine H1 receptors could experience rebound insomnia if switched to
a less sedating agent with a low affinity for H1 receptors. An understanding of the differential receptorbinding
profiles of the various antipsychotics can help clinicians anticipate and manage potential
clinical issues that may be encountered when switching antipsychotic therapy.