Tramadol is the most widely used analgesic in the world. Indications for the general administration of tramadol in dentistry and oral surgery are restricted to cases with moderate to severe pain. However, new evidence supports the peripheral use of this well-known drug. The unique properties of this atypical opioid, including its impact on neuronal conduction, attenuation of inflammation, and antimicrobial effects, together with its possible beneficial influence on the wound healing process, have been observed after local administration in human and animal research. The paper focuses on the local administration of tramadol within orofacial tissues, with particular consideration given to its possible use in dentistry.