Pharmacology of antipsychotics
Because clinical toxicity is often the result of exaggerated pharmacological activity, knowledge of an antipsychotic’s relative receptor binding can be used to predict adverse effects after therapeutic doses and overdose.
Antipsychotics bind to and antagonize presynaptic (autoreceptor) and postsynaptic D2-receptors, initially causing dopamine neurons to synthesize and release more dopamine. But with continued antipsychotic treatment, decreased production and release of dopamine occur along with continued postsynaptic D2-receptor antagonism.
For most antipsychotics, the affinity (potency) for the D2-receptor correlates with the dose required to treat schizophrenia and also the likelihood of producing EPS.
Antagonism . . .
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