Effect of lofepramine on 5-HT function and sleep.
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 challenge paradigm (30 mg orally). We also studied the effect of lofepramine on platelet 5-HT content and sleep architecture. Lofepramine treatment did not alter the hypothermic, endocrine or amnesic effects of buspirone but significantly lowered platelet 5-HT content and decreased rapid eye movement sleep. Our findings suggest that at clinically used doses, lofepramine inhibits the uptake of 5-HT and produces changes in sleep architecture characteristic of tricyclic antidepressants. However, lofepramine does not appear to alter the sensitivity of 5-HT1A receptors.
Herdman
J R
JR
MRC Unit of Clinical Pharmacology, Littlemore Hospital, Oxford, UK.
Cowen
P J
PJ
Campling
G M
GM
Hockney
R A
RA
Laver
D
D
Sharpley
A L
AL
D000328:Adult; D001792:Blood Platelets / Q000737:chemistry* / Q000187:drug effects; D002065:Buspirone / Q000097:blood / Q000494:pharmacology; D004569:Electroencephalography; D006801:Humans; D008127:Lofepramine / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D008297:Male; D008568:Memory / Q000187:drug effects; D011388:Prolactin / Q000097:blood; D011985:Receptors, Serotonin / Q000187:drug effects*; D012701:Serotonin / Q000032:analysis* / Q000097:blood; D012890:Sleep / Q000187:drug effects*; D012895:Sleep, REM / Q000187:drug effects
D011985:Receptors, Serotonin; D012701:Serotonin; D011388:Prolactin; D008127:Lofepramine; D002065:Buspirone