Abstract

Publisher Summary This chapter discusses the dosage of antischizophrenic drugs and the affinity for muscarinic cholinergic receptor sites in the brain to predict extrapyramidal effects. The dopamine hypothesis of schizophrenia is predicated in large part upon the interactions of the antischizophrenic phenothiazines and butyrophenones with brain catecholamines, especially dopamine. Besides accounting for their antischizophrenic effects, blockade by phenothiazines and butyrophenones of dopamine receptors can explain their extrapyramidal side effects including akathisia, abnormal movements, and parkinsonian-like symptoms. If dopamine receptors throughout the brain respond similarly to various phenothiazines, at therapeutic antischizophrenic doses similar receptor blockade should occur in all the dopamine systems. The therapeutic antischizophrenic dopamine receptor blockade requires almost ten times higher brain levels of thioridazine than of trifluoperazine.

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