Iontophoresis is a non-invasive method of systemic and local drug delivery using an electric field. Iontophoresis enables diffusion of the selected drug via skin, mucosa, enamel, dentin, and other tissues. The amount of delivered therapeutic molecules is about 10–2000 times greater than conventional forms of delivery. Among other fields, this method is used in dentistry, ophthalmology, otorhinolaryngology, and dermatology. According to related literature, the most important drugs studied or administered by iontophoresis are: Local anesthetics, opioids, steroids, non-steroidal anti-inflammatory drugs, antibacterial drugs, antifungal drugs, antiviral drugs, anticancer drugs, fluorides, and vitamins. The present review covers current available data regarding the selected medicines used in iontophoresis. Furthermore, indications and conditions of iontophoresis application are reviewed.