Pharmaco-electroencephalography (pharmaco-EEG) has never gained great popularity in epilepsy research. Nevertheless, the electroencephalogram (EEG) is the most important neurological examination technique in this patient population. Development and investigation of antiepileptic drugs (AEDs) involves EEG for diagnosis and outcome evaluation. In contrast to the common use of the EEG for documenting the effect of AEDs on the presence of interictal epileptiform activities or seizures, quantitative analysis of drug responses in the EEG are not yet standard in pharmacological studies. We provide an overview of dedicated pharmaco-EEG studies with AEDs in humans. A systematic search in PubMed yielded 43 articles, which were reviewed for their relevance. After excluding studies according to our exclusion criteria, nine studies remained. These studies plus the retrieved references from the bibliographies of the identified studies yielded 37 studies to be included in the review. The most prominent method in pharmaco-EEG research for AEDs was analysis of the frequency content in response to drug intake, often with quantitative methods such as spectral analysis. Despite documenting the effect of the drug on brain activity, some studies were conducted in order to document treatment response, detect neurotoxic effects, and measure reversibility of AED-induced changes. There were some attempts to predict treatment response or side effects. We suggest that pharmaco-EEG deserves more attention in AED research, specifically because the newest drugs and techniques have not yet been subject to investigation.