OBJECTIVEThis study aimed to comprehensively review the literature and provide a practical guide for optimizing drug regimens and supplementation related to orthognathic surgery.METHODSThe authors conducted a thorough review of the existing literature, following the PRISMA-ScR guidelines. Various types of studies except case reports and reviews were included. The study applied specific inclusion criteria, focusing on perioperative and/or postoperative drugs, medications, or supplementation related to orthognathic surgery.RESULTSThis guide included 78 studies on various medications in orthognathic surgery. It encompasses clinical trials, cohort studies, cross-sectional studies, prospective and retrospective studies. The topics covered include antibiotics, analgesics, corticosteroids, antiemetics, hemostatic agents, local anesthetics, herbal medicine, and botulinum toxin. Pain and edema control involved specific medications, while local anesthesia utilized ropivacaine and bupivacaine. The guide also discusses mineral and vitamin supplementation. The effectiveness of hemostatic agents and antiemetics was highlighted.CONCLUSIONPain management, reduced swelling, enhanced wound healing, and faster recovery are among the advantages. In addition to the standard drugs and medications, the inclusion of vitamin and mineral supplements, tranexamic acid, postoperative anesthetic blocks, and preemptive antiemetics is anticipated to offer various benefits in orthognathic surgery, despite the limited available evidence.