Abstract The International Association for the Study of Pain defines pain as ‘an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in such terms of such damage’. This definition of the pain experience thus combines both the phenomenon of nociception (the sensory nervous system's response to certain harmful or potentially harmful stimuli) and pain perception (process by which pain is recognized and interpreted by the brain). The Encyclopaedia Britannica defines an analgesic as any drug that relieves pains electively without blocking the conduction of nerve impulses, markedly altering sensory perceptions, or affecting consciousness. This selectivity is an important distinction between an anaesthetic and an analgesic drug. Analgesics can thus be broadly classified according to their role primarily on nociception as well as pain perception, both of which are intimately integrated to the pain experience. An understanding of the pain pathway is inherent to a good understanding of how therapeutic targets can act as analgesics. An overview of this is discussed in this article to understand rationale for therapeutic intervention. Opioids are substances that act on opioid receptors to produce morphine-like effects. Opioids have been used as a mainstay for pain management for centuries. As the problem of chronic pain has risen to epidemic proportions, so has the incidence of increase in opioid use as well as misuse and abuse of prescription opioids resulting in increasing morbidity and mortality. While being effective for acute pain and cancer pain management, opioids have not been very effective for the management of chronic pain or neuropathic pain. All other analgesics that do not produce analgesia through a primary effect on opioid receptors can be labelled as non-opioid analgesics (NOA). This article will aim to provide an overview of the pain pathway in relation to the therapeutic targets for providing analgesia, commonly used NAOs and their brief introduction.