N

Figure 8 5HT1A agonist anxiolytics.

Buspirone

Figure 8 5HT1A agonist anxiolytics.

Gepirone

Tandospirone nonsedating anxiolytic approved for the treatment of GAD. Despite its clinical efficacy buspirone is not widely prescribed mainly because of a delay in onset of action compared to BZs and also because it is ineffective in patients who have previously taken BZs for their anxiety.93

Gepirone (Figure 8) is an azapirone that is structurally similar to buspirone, but is more selective for the 5HT1A receptor. Initial studies of gepirone in depressed patients using an immediate release formulation resulted in good antidepressant efficacy but this was limited by tolerability issues at higher doses.93 An extended release formulation of gepirone (Gepirone ER) is under development for treatment of depression. In addition to major depression, gepirone may have utility in patients with anxious depression94 as well as GAD.95 Another second-generation azapirone, tandospirone, was launched in Japan (1996) and China (2004) for treatment of GAD (Figure 8).

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