Psychopharmacological treatments for schizophrenia have always been a matter of debate and a very important issue in public health given the chronic, relapsing and disabling nature of the disorder. A thorough understanding of the pros and cons of currently available pharmacological treatments for schizophrenia is critical to better capture the features of treatment-refractory clinical pictures and plan the developing of new treatment strategies. This review focuses on brain functional changes induced by antipsychotic drugs as assessed by modern functional neuroimaging techniques (i.e. fMRI, PET, SPECT, MRI spectroscopy). The most important papers on this topic are reviewed in order to draw an ideal map of the main functional changes occurring in the brain during antipsychotic treatment. This supports the hypothesis that a network-based perspective and a functional connectivity approach are needed to fill the currently existing gap of knowledge in the field of psychotropic drugs and their mechanisms of action beyond neurotransmitter systems.