Introduction: Administrating local anesthetics with injections is associated with much pain and is known to lead to the development of edema of tissues that can negatively affect the surgical wound. The use of topical anesthetics has been increasing in several procedures due to its improved efficacy and decreased pain when compared to injected local anesthetics. Topical anesthetics are generally used in skin procedures, ophthalmological surgeries, minor procedures, and laser treatment modalities, along with other potential uses. Aim of work: In this review, we will discuss the most recent evidence on the use of topical anesthetics in medicine. Methodology: We did a systematic search for topical anesthesia use and updates in medicine, using PubMed search engine (http://www.ncbi.nlm.nih.gov/) and Google Scholar search engine (https://scholar.google.com). Our search also looked the mechanism of action and adverse effects. All relevant studies were retrieved and discussed. We only included full articles. Conclusions: Many mixtures have been developed and introduced for different uses. However, despite all developments and improvements in the use of topical local anesthetics, they are still associated with adverse events and toxicity that may be severe in some cases and cause death. Therefore, caution should be applied by physicians when they attempt to use topical local anesthetics along with careful attention to the proper doses and methods of application. In addition, strict caution should be applied with topical local anesthetics are applied in vulnerable patients like neonates, children, elderly, and pregnant females. Further studies are still required to improve the use of topical anesthetics and provide protocols with highest efficacy and minimal adverse events. Key words: Topical anesthetic, surgery, adverse effect