Codeine is metabolized by the cytochrome P450 2D6 (CYP2D6) to morphine. Codeine is a much weaker agonist at mu opioid receptors than morphine. Therefore, codeine analgesia is highly dependent on CYP2D6 activity. Large prospective studies in the clinical environment do not exist, but it appears reasonable to avoid codeine use in CYP2D6 poor metabolizers (PMs). CYP2D6 metabolizes other opioid ana...

Deaths involving opioid analgesics have increased dramatically in the United States. Approximately 4,000 such deaths were documented in 1999, increasing to 16,235 in 2013, reflecting a nearly quadrupled death rate from 1.4 to 5.1 deaths per 100,000. To investigate this increase in New York state, trends in poisoning deaths involving opioid analgesics from 2003 to 2012 were examined. Data source...

The discovery of the opioid receptors began in the 1970s and three (μ, δ and κ) are now recognised. Most current opioid analgesics interact preferentially with μ receptors, although some have actions at δ and κ receptors. The revelation that opioid receptors are present on peripheral sensory neurones and immune system cells, has led to the realisation that the opioid system is involved in a hos...

The opioid receptors (ORs) are known to be distributed widely in the central nervous system (CNS) and in peripheral sensory and autonomic nerves. Activation of ORs by endogenous and exogenous ligands results in a multitude of physiological functions and behaviors, e.g. pain and analgesia, stress and social status, tolerance and dependence, learning and memory, eating and drinking, and many more...

The peer-reviewed literature yields a plethora of examples of variability in patient's responses to medications. The rapidly progressing field of pharmacogenetics offers insight into the variation in responses observed clinically, and in particular for the variability observed among patients administered mu opioid analgesics. Genetic variation leads to interperson variability in drug absorption...

Prescription Drug Monitoring Programs (PDMP) are statewide databases that collect data on prescription of controlled substances. New York State mandates prescribers to consult the PDMP registry before prescribing a controlled substance such as opioid analgesics. The effect of mandatory PDMP on opioid drug prescriptions by dentists is not known. This study investigates the impact of mandatory PD...

Recently, the outcomes were published of the Global Opioid Policy Initiative, evaluating the availability, cost of opioid medicines and the regulatory barriers that are possibly impeding access for the management of cancer pain in developing countries. Other studies have shown that the vast majority of the world population has no access to opioid analgesics. This study shows by country which op...

.................................................................................................viii CHAPTER 1 – INTRODUCTION.........................................................................1 OPIOID ANALGESICS IN ABORTION CARE................................................2 NON-OPIOID ORAL ANALGESICS IN ABORTION CARE................................4 PREDICTORS OF PAIN DURING ABORTION....

One of the most important functions of the opioid system is the control of pain. Among the three main opioid receptor classes (μ, δ, κ), the μ (MOR) is the main type targeted for pharmacotherapy of pain. Opioid analgesics such as morphine, oxycodone and fentanyl are agonists at the MOR and are the mainstay for the treatment of moderate-to-severe pain. However, adverse effects related to opioid ...

PURPOSE Since 1990, numerous jurisdictions in the United States (US) have reported increases in drug poisoning mortality. During the same time period, the use of opioid analgesics has increased markedly as part of more aggressive pain management. This study documented a dramatic increase in poisoning mortality rates and compared it to sales of opioid analgesics nationwide. METHODS Trend analy...