We studied the effect of the tricyclic antidepressant lofepramine (140
-210 mg daily for 16 days) on 5-hydroxytryptamine 1A (5-HT1A) receptor
sensitivity in healthy volunteers, using a buspirone neuroendocrine c
hallenge paradigm (30 mg orally). We also studied the effect of lofepr
amine on platelet 5-HT content and sleep architecture. Lofepramine tre
atment did not alter the hypothermic, endocrine or amnesic effects of
buspirone but significantly lowered platelet 5-HT content and decrease
d rapid eye movement sleep. Our findings suggest that at clinically us
ed doses, lofepramine inhibits the uptake of 5-HT and produces changes
in sleep architecture characteristic of tricyclic antidepressants. Ho
wever, lofepramine does not appear to alter the sensitivity of 5-HT1A
receptors.