How do antidepressants affect serotonin receptors? The role of serotonin receptors in the therapeutic and side effect profile of the SSRIs.

The serotonin selective reuptake inhibitors (SSRIs) have proved to be an important development in the treatment of depression because of both their greater practical ease of use and their selective primary action on a single binding site. Their efficacy in depressive illness of a range of severities, but also in obsessive-compulsive disorder and panic, is largely established. The onset of action of the SSRIs may be delayed by autoinhibition at the cell bodies of raphe neurons. This suggests that blockade of autoreceptors may speed the onset of antidepressant action by SSRIs. The main unwanted effects of the SSRIs occur in relation to gastrointestinal, sleep, and orgasmic disturbances. However, the total side effect burden is less than that associated with the older, less selective compounds, and there are clear hypotheses for how the side effects that do occur may be mediated and hence how they may be reduced by either adjunctive treatment or design of new compounds.