This chapter is a comprehensive account of the medicinal chemistry of antipsychotic drugs. It provides the mechanism of drug action and detail structureactivity relationships of the first- and second-generation antipsychotic and related drugs to give the knowledge base for pharmacists. Upon completion of this chapter, students will be able to:
• Describe the historical background about the development of antipsychotic therapeutics.
• Apply the principles of fundamental pathophysiology of schizophrenia and other psychotic disorders and receptors associated with it to their pharmacological action.
• Recognize the dopamine and its chemical analogues and identify the essential structural features to become an antipsychotic agent.
• Differentiate between the positive and negative symptoms and extrapyramidal side effects and distinguish between the typical and atypical classes of antipsychotics.
• Apply the principles of structure-activity relationships to the antipsychotic drugs.
• Delineate the clinical significance of all classes of antipsychotic drugs and their therapeutic indications.
• Identify the therapeutic use, side effects and metabolic pathways of selected first- and second-generation antipsychotic agents.
Keywords: Antipsychotic Drugs, Antianxiety Drugs, Drug-Receptor Interaction, Dopamine, First-Generation Antipsychotics, Structure-Activity Relationship, Second-Generation Antipsychotics, Typical And Atypical Antipsychotic Agents.