Multifocal electroretinography (mfERG) is an objective, noninvasive examination for the assessment of visual function. It enables the stimulation of multiple retinal areas simultaneously and recording of each response independently, providing a topographic measure of retinal electrophysiological activity in the central 40-50° of the retina. A clinical application of mfERG represents the assessment of retinal toxicity associated with systemic medications. Drug-induced retinopathy represents a disease that, although not common, requires early recognition: if not detected early, it may progress and cause irreversible retinal dysfunction with subsequent visual impairment. This review aims to evaluate the use of mfERG in the assessment of retinal dysfunction associated with various systemic pharmacological agents based on the currently available literature. The most commonly recognized systemic medications affecting retinal function are included, such as chloroquine and hydroxychloroquine, vigabatrin, deferoxamine, ethambutol, interferon-α, tamoxifen, digoxin, sildenafil, canthaxanthin, amiodarone and nefazodone. The role of mfERG in the early diagnosis of retinal toxicity and the evaluation of disease severity is reviewed, as well as its clinical value in monitoring disease progression or recovery after drug cessation.