Nefazodone—A novel antidepressant— May increase REM sleep

Abstract

Nefazodone, an analogue of the antidepressant drug trazodone, has a pharmacological profile distinct from that of tricyclic antidepressants (TCAs) and selective 5-hydroxytryptamine (5HT) uptake inhibitors. Biochemical and behavioral studies indicate that nefazodone possesses 5-HT2 receptor antagonist properties with little affinity for histamine H~ receptors and ott-adrenoceptors (Taylor et al 1982). In addition, nefazodone is moderately active as an inhibitor of the synaptic uptake of noradrenaline (NA) and 5-HT (Yocca et al 1985). Nefazodone has two active metabolites, hydroxy-nefazodone (which pharmacologically resembles nefazodone) and m-chlorophenylpiperazine (mCPP). The pharmacological properties of mCPP appear to include agonist properties at 5-HTIA and 5-HT~c receptors with antagonist effects at 5-HT2 and 5-HTa receptors (Hamik and Peroutka 1989). Controlled trials indicate that the clinical efficacy of nefazodone is superior to placebo and equivalent to that of TCAs in the treatment of rr,ajor depression (Feighner et ai 1989; Fontaine et al 1991; Weise et al 1991). It is well established that antidepressant drugs produce characteristic changes in sleep architecture that almost invariably include a reduction in the amount