Patients with chronic non-malignant pain report impairment of physical and social life along with psychological state affecting their overall quality of life. The purpose of managing pain is to reduce the trauma and improve the patient comfort with better quality of life. Tramadol is a centrally acting weak μ-opioid receptor analgesic and is a racemic mixture of (+)-tramadol and (−)-tramadol enantiomers. Tramadol is used worldwide and is listed in many medical guidelines for pain management. The (+)-tramadol has greater affinity for μ-opioid receptor and provides additional prevention of 5- hydroxy tryptamine reuptake, while the (-)-tramadol is a successful noradrenaline reuptake inhibitor and intensifies its release by activating the auto receptor. Tramadol is prescribed to relieve moderate to severe pain management in patients. Tramadol does not show much serious adverse effects without any dependency potential in therapeutic doses as seen in other opioids, like morphine. Tramadol metabolite M1 also has μ-opioid receptor agonist activity, but it faces poor blood brain barrier permeability. In this review, we report the complete updated status of Tramadol along with its chemistry, synthesis, pharmacology, medicinal uses, adverse effects and its combinations available in the market. We have also covered Tramadol patents so that a complete overview provides a broader perspective for future designing of its derivatives and increase their potential use for pain management in terminal cancer patients.