Chapter 4

Antidepressant Drugs

Horrick Sharma, Michaela Leffler and M. O. Faruk Khan

Abstract

This chapter is a comprehensive account of the medicinal chemistry of the antidepressant drugs. It provides the mechanism of drug action and details of the structure-activity relationships (SAR) of the antidepressant and related drugs to give the knowledge base for pharmacists. After a study of this chapter, students will be able to:

• Relate principles of affective disorders including the biogenic amine hypothesis and depression.

• Describe the roles of dopamine, serotonin and norepinephrine in depression and how these roles relate to the mechanism of action of antidepressant drugs.

• Describe different classes of antidepressant drugs with examples.

• Compare the chemical structures of all the classes of antidepressant drugs and relate their action with structures.

• Illustrate the mechanism of action, SAR, metabolites, and clinical considerations of: ▪ Serotonin and norepinephrine reuptake inhibitors

o Tricyclic antidepressants (TCAs)

o Phenylalkylamines

▪ Selective serotonin reuptake inhibitors (SSRIs)

o Phenoxyphenylalkyl amines

o Phenylalkylamine

▪ Monoamine oxidase inhibitors (MAOIs)

▪ Miscellaneous antidepressant drugs

Total Pages: 163-206 (44)

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