Date of Award

5-14-2011

Degree Type

Thesis

Department

Pharmacy

First Advisor

Kimberly Beck

Abstract

Opioid analgesics are a class of medications with affinity for receptors in the brain which are naturally targeted by endogenous opioid peptides to exert neuromodulatory action.' Long before this target pathway was ever elucidated, ancient cultures had documented use of a naturally occurring plant derivative, opium, which provided the same effects as opioid drugs today. The active alkaloid constituent of opium is morphine. The human body's equivalents of these substrates interact with multiple types of opioid receptors which produce the effects responsible for pain relief. In addition, there are also unwanted side effects including constipation, nemesis, and respiratory depression. Contributing to those undesirable factors, are receptor-induced responses such as euphoria, tolerance, and physical dependence which provide a causal link to medication abuse.2 While there have been multiple studies done which evaluate the efficacy of opioids in chronic pain, that determine the pain relief achieved by opioids versus placebo, and those relating structural modifications to potency and receptor specificity, an initial literature search of the relationship of chemical changes to the opioid ring system to over utilization of the analgesics shows a lack of information. The rate of use among the general public is growing at a rapid pace, with certain opioid prescriptions experiencing an 800% rise in fill rate over the past decade alone.' It has been asserted that this class of medications is the most commonly prescribed in the entire US.' Although that may be true in terms of prescription volume, just greater than 3% of adults are on chronic opioid therapy for treatment of pain not related to 2 malignancies,s with chronic treatment being defined as consecutive usage for greater than three months time.