Functional magnetic resonance imaging (fMRI) was used to determine the acute blood oxygen level dependent effect (BOLD) of neuroleptic drugs in healthy male subjects. Using a robust simultaneous visuo-acoustic stimulation paradigm fMRI measurements were obtained prior to as well as 1 h and 24 h after intravenous infusion of 5 mg haloperidol to six healthy young men. After the administration, subjects showed significantly reduced BOLD contrast in the middle occipital gyrus while BOLD contrast was increased in the lingual gyrus. This pattern normalised within 24 h. Our results emphasise the necessity to control for interactions through acute medication and confirm fMRI as a non-invasive method for studying cerebral psychopharmacological effects.