Lichenoid drug reaction is termed as a condition of the oral cavity having an identifiable etiology, which is clinically and histologically similar to oral lichen planus. A number of drugs have been described as a causative factor of those reactive lesions. The aim of this study is to conduct a systematic review on the role of causative drugs in oral lichenoid lesions (OLLD) and the clinicopathological features of this entity which still has uncertainty in diagnosis. Bibliographic searches were carried out to identify articles published in English on PubMed (R) Online electronic databases from 1993 to 2013. Available clinical, histological and treatment methods were recorded. A total of 25 articles fulfilled the inclusion criteria with 37 patients. OLLD were detected frequently in patients with a history of zidovudine and imatinib mesylate medication. OLLD occurred significantly in subjects over the age of 30 (p<0.01), mostly on buccal mucosa (42.37%). The most preferable treatment is withdrawal of the drugs and administering a topical steroid regimen. Thirty OLLD cases were confirmed by biopsies which were characterized by diffuse inflammatory infiltrate through the deep side of the lamina propria. Medical history and histological features are the two basic criteria for the differential diagnosis of OLLD.