Abstract

Physicians continue to struggle with the clinical management of pain, in part because of the large interindividual variability in the efficacy, occurrence of side effects and undesired severe adverse drug reactions from the prescribed analgesics. Pharmacogenomics, the study of how an individual's genetic inheritance affects the body's response to medications, has an important role and can explain some of this interindividual variability. Genetic identification of known variant alleles that affect the pharmacokinetics or pharmacodynamics of medications used for pain management can enable physicians to select the appropriate analgesic drug and dosing regimen for an individual patient, instead of empirical selection and dosing escalation. In this article, clinically relevant pharmacogenomic targets for the management of opioid pain, including efflux transporters, proteins that metabolize drugs, enzymes that regulate the neurotransmitters that modulate pain, and opioid receptors, will be reviewed.

Highlights

  • Physicians continue to struggle with the clinical management of pain, in part because of the large interindividual variability in the e cacy, occurrence of side e ects and undesired severe adverse drug reactions from the prescribed analgesics

  • The use of opioids in pain management requires careful dose escalation and empirical adjustments based on clinical response and the presence of side effects or adverse drug reactions (ADRs)

  • Pharmacogenomic approaches offer insight into the genetic variables that can affect a drug’s uptake, transport, activation of its target, metabolism, interaction with other medications and excretion. e use of pharmacogenomics in patients requiring pain management can lead to more efficient opioid selection, dose optimization and minimization of ADRs to improve patient outcome

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Summary

Introduction

Physicians continue to struggle with the clinical management of pain, in part because of the large interindividual variability in the e cacy, occurrence of side e ects and undesired severe adverse drug reactions from the prescribed analgesics. The use of opioids in pain management requires careful dose escalation and empirical adjustments based on clinical response and the presence of side effects or adverse drug reactions (ADRs). Genetic variants (such as 3435C>T) in P-glycoprotein have been associated with variability of pain relief in cancer patients treated with morphine [6].

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