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Chapter 14. Sertraline

David R. Block, M.D.; Kimberly A. Yonkers, M.D.; Linda L. Carpenter, M.D.
DOI: 10.1176/appi.books.9781585623860.411109

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Excerpt

Research has implicated dysregulation of serotonin (5-HT) in mood and anxiety disorders. Despite the effectiveness of the monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants (TCAs), which exert their effects by inhibiting the enzymatic degradation and reuptake of monoamines, respectively, side effects and potential serious adverse events limited their utility. Researchers thus identified compounds that are selective in blocking neurotransmitter reuptake and yet have little agonist and antagonist activity at receptors thought to be associated with adverse effects. Sertraline [(+)-cis-(1S,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthylamine], a naphthylamino compound that is structurally different from MAOIs and TCAs (Figure 14–1), is one of this class of drugs (Guthrie 1991; Heym and Koe 1988).

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FIGURE 14–1. Chemical structure of sertraline.

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Sample questions:
1.
Compared with other selective serotonin reuptake inhibitors (SSRIs), sertraline has a 10-fold increase in antagonism of which of the following receptors?
2.
Which of the following statements regarding sertraline’s pharmacokinetic properties is true?
3.
Sertraline is approved by the U.S. Food and Drug Administration (FDA) for the treatment of all of the following disorders except
NOTE:
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