The 5-HT1B/D agonist sumatriptan has been used in a number of studies as a
neuroendocrine challenge agent. Whether its neuroendocrine effects are cent
rally mediated is unclear, however, since sumatriptan shows minimal penetra
tion of the central nervous system. Zolmitriptan shows a greater penetratio
n into the central nervous system than sumatriptan, and has recently been s
hown to be an effective challenge agent. In order to determine the neuroend
ocrine, temperature and side effects of a 2.5 mg oral dose of zolmitriptan,
17 healthy volunteers underwent a placebo controlled, repeated measures, d
ouble blind neuroendocrine challenge. Zolmitriptan or placebo were administ
ered, and cortisol, growth hormone, prolactin, blood pressure and temperatu
re, were measured over four hours after the dose of zolmitriptan. Zolmitrip
tan at this dose was well tolerated by all subjects, with minimal side effe
cts and only minor effects on blood pressure. There was a significant incre
ase in serum growth hormone after zolmitriptan compared to placebo, however
there were no significant effects on cortisol, prolactin or oral temperatu
re. The neuroendocrine effects of 2.5 mg of orally administered zolmitripta
n are similar to previously reported effects of sumatriptan, with minimal s
ide effects. (C) 2000 Elsevier Science Ltd. All rights reserved.