Abstract
Pain is extremely multifaceted in nature, with physical injury being just one of its causes. The most commonly prescribed therapeutic intervention for acute as well as chronic pain (postoperative or otherwise) is Opioids. Opioid analgesics act via the opioid receptors (G protein coupled), that are widely distributed in the central and peripheral nervous system as well as the gastrointestinal tract, producing pain relief. The opioid analgesics are divided into distinct categories depending on the receptor type and their potency. Three major types of receptors mediate analgesic effects, namely, mu (μ), delta (δ) and kappa (κ). These are also further subdivided into different subtypes depending on the duration and onset as rapid-onset, short-acting and long-acting. The neurobiology behind opioid analgesia involves the mesolimbic (midbrain) reward system. There is also increasing scientific evidence that plasma pharmacokinetics, along with the CNS distribution of opioids, is greatly influenced by the P-glycoprotein (P-gp) efflux transporter. The ABCB1 gene is responsible for coding P-gp hence it was postulated that variability in the ABCB1 gene could potentially play an important role in determining why there is interindividual variability towards opioids therapeutic interventionsHence the primary purpose of this review was to compile and understand the research regarding the mechanisms of opioid actions and the effect of genetic variability (ABCB1 gene), on the P-gp transporters regarding their expression/function while also examining the opioid use, abuse and dependence and possibly coming up with some strategies to use pharmacogenomics as a potential tool for solving these issues
Highlights
Pain is extremely multifaceted in nature, with physical injury being just one of its causes
It can be observed that the mutations resulting in functional changes in ABCB1 genetic variants are relatively moderate and substrate dependent
Genetic variability in the ABCB1 may be important in determining morphine exposure during the administration of illegal opioids, ABCB1 variants are expected to increase opioid exposure during the initial stages or opioid use as well as abuse, which in turn can increase the risk or dependence
Summary
Pain is extremely multifaceted in nature, with physical injury being just one of its causes. The development of any diseases is often a multifaceted affair. Scientific research and modern advances in medicine have revealed that the level of pain experienced is a combination of psychological and physiological factors. It is of vital importance that the patients experience pain relief, especially after surgical procedures. Adequate pain relief is often deemed to be an important measurement of patient satisfaction and it helps prevent any post-surgical chronic pain. The most commonly prescribed therapeutic intervention for acute as well as chronic pain (postoperative or otherwise) is Opioids
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