In the treatment of pain management, physicians employ a variety of drugs, ranging from low-impact to highly potent, and to maximize patient health, urine toxicology analyses can significantly improve the delivery of pain treatment. Drugs such as opioids that are used for pain management are peculiar in that they provide effective pain relief and have a high risk of addiction. The use of illicit drugs in the general population has been on the rise; however, self-reporting and close monitoring of patient behavior are insufficient means to detect drug abuse and confirm compliance. Therefore, in order to create more effective drug treatment plans, physicians must understand and account for the implications of patient drug use history. Urine toxicology analysis is an important tool for pain physicians because it is more sensitive than most alternative blood tests, more efficient and cost-effective. Urine testing in addition to improving patient pain management also has forensic and legal implications. There are however limitations to urine toxicology methods as they can produce false-positive and false-negative results and are prone to human error and sample contamination There is also a need for more specific and rapid urine drug testing. Healthcare professionals should therefore be familiar with the limitations of various urine drug testing methods, and possess skills necessary to properly interpret these results. This review suggests that the overall benefits incurred by both the patients short-term and long-term health support the routine integration of urine toxicology analysis in routine clinical care. In addition to improving health care and patient health, it has a strong potential to improve patient-physician relationships and protects the interest of involved healthcare practitioners.