Showing posts with label Opioids. Show all posts
Showing posts with label Opioids. Show all posts

Wednesday, August 23, 2017

All You Need To Know About Opioids And Pain Treatment


Today's important post from ncbi.nlm.nih.gov (see link below) will be of interest to all neuropathy patients who's lives have been so disrupted by the disease and the pain that it brings, that they have had no alternative but to use opioids to quell the symptoms. We go to the doctors and 99% of us dread hearing that opioids are the only remaining option but we have to do it in order to live reasonable daily lives. However, the explanation generally ends there. We know they're the strongest analgesics and we're well aware of the dangers of addiction, let alone the potential side effects but if you're between a rock and a hard place, you accept the prescription in good faith! This comprehensive article tells us all we need to know about these drugs and for that reason it can remove much of the anxiety associated with opioids. More than that, it provides the knowledge we need to justify to ourselves and others that although it may not be the solution of choice, it can be a very effective one. We also sign an invisible contract with the doctor to make sure that we are monitored and controlled throughout our use and any potential dangers are dealt with when they begin and not when they've taken hold. Definitely worth a read then for anyone in this situation - it's amazing how much better you feel when you have knowledge in your armory.

Opioids and the Treatment of Chronic Pain: Controversies, Current Status, and Future Directions
Andrew Rosenblum,1,* Lisa A. Marsch,1 Herman Joseph,1 and Russell K. Portenoy2
Author information ► Copyright and License information ►
The publisher's final edited version of this article is available at Exp Clin Psychopharmacol
See other articles in PMC that cite the published article.

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Abstract

Opioids have been regarded for millennia as among the most effective drugs for the treatment of pain. Their use in the management of acute severe pain and chronic pain related to advanced medical illness is considered the standard of care in most of the world. In contrast, the long-term administration of an opioid for the treatment of chronic non-cancer pain continues to be controversial. Concerns related to effectiveness, safety, and abuse liability have evolved over decades, sometimes driving a more restrictive perspective and sometimes leading to a greater willingness to endorse this treatment. The past several decades in the United States have been characterized by attitudes that have shifted repeatedly in response to clinical and epidemiological observations, and events in the legal and regulatory communities. The interface between the legitimate medical use of opioids to provide analgesia and the phenomena associated with abuse and addiction continues to challenge the clinical community, leading to uncertainly about the appropriate role of these drugs in the treatment of pain. This narrative review briefly describes the neurobiology of opioids and then focuses on the complex issues at this interface between analgesia and abuse, including terminology, clinical challenges, and the potential for new agents, such as buprenorphine, to influence practice.
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Introduction

Opioids play a unique role in society. They are widely feared compounds, which are associated with abuse, addiction and the dire consequences of diversion; they are also essential medications, the most effective drugs for the relief of pain and suffering (Portenoy et al, 2004). Historically, concerns about addiction have apparently contributed to the undertreatment of disorders widely considered to be appropriate for opioid therapy, including cancer pain, pain at the end-of-life, and acute pain (Field and Cassel, 1997; Schnoll & Weaver, 2003; Portenoy & Lesage, 1999; Breitbart et al. 1998; Smith et al., 2008). The use of opioids for chronic non-malignant pain (CNMP) remains controversial (Manchikanti, 2008; McQuay, 1999). Following publication of reports on the safety and efficacy of opioids prescribed to small numbers of patients with CNMP (e.g., Portenoy and Foley, 1986; Nyswander and Dole, 1986) and the publication of a seminal article entitled “The Tragedy of Needless Pain”, (Melzack, 1990), the use of opioids to treat CNMP began to be more widely practiced and incorporated into clinical guidelines. Nevertheless, despite the advances in pain medicine and the wider use of opioids for various chronic pain conditions, there is still considerable controversy surrounding the type of conditions that should be treated, whether the treatment can be generally safe and effective in selected patients, and what the clinical goals should be (Ballantyne & Forge, 2007; Streltzer & Johansen, 2006; Stretzler & Kosten 2003).
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History of Opioids

The Sumerians in Mesopotamia were among the first people identified to have cultivated the poppy plant around 3400 BC. They named it Hul Gil, the “joy plant” (Booth, 1986). It eventually spread throughout the ancient world to every major civilization in Europe and Asia and was used to treat pain and many other ailments (Schiff, 2002; Askitopoulou, Ramoutsaki, & Konsolaki, 2002; Booth, 1986; Dikotter, Laaman, & Xun, 2004).


Developments in the 19th century transformed the practice of medicine and initiated the tension between the desire to make available the medicinal benefits of these drugs and recognition that the development of abuse and addiction can lead to devastating consequences for individuals and for society at large (Booth, 1986; Musto, 1999):
In 1803 morphine, an opioid analgesic, was extracted from opium by Friedrich Serturner of Germany;
Dr. Charles Wood, a Scottish physician, invented the hyperdermic needle and used it to inject morphine to relieve pain from neuralgia;
Dr. Eduard Livenstein, a German physician, produced the first accurate and comprehensive description of addiction to morphine, including the withdrawal syndrome and relapse, and argued that craving for morphine was a physiological response.
Diacetylmorphine (brand name heroin) was synthesized and briefly promoted as more effective and less addictive than morphine. In the early 20th century, when heroin was legally marketed in pill form, it was used by young Americans to elicit intense euphoria by crushing the heroin pills into powder for inhalation or injection (Katz et al., 2007, c.f. Meldrum, 2003; Hosztafi, 2001).

Beginning in the twentieth century, there were many research advances and major changes in the way opioids were used for the treatment of pain and addiction (Ballantyne, 2006; Corbett et al., 2006). These included attempts among several nations and international organizations to control the distribution and use of opioids (Musto, 1999); the introduction of opioid maintenance therapy for the treatment of opioid addiction (first with morphine and later with methadone, LAAM (levo-alpha acetyl methadol) and sublingual buprenorphine) (Courtwright, Joseph & Des Jarlais, 1989; Strain & Stitzer, 2006); the discovery of the endogenous opioids (Hughes, Smith, Kosterlitz, Fothergill, Morgan & Morris, 1975); and the recognition that pain is a debilitating and destructive disease and that opioids are essential for the treatment of many forms of acute and chronic pain.

During most of the twentieth century, the widely held perception among professionals in the United States was that the long-term use of opioid therapy to treat chronic pain was contraindicated by the risk of addiction, increased disability and lack of efficacy over time. During the 1990’s, a major change occurred, driven by a variety of medical and nonmedical factors (see below). The use of opioids for chronic pain began to increase, showing a substantial year-to-year rise that continues today. This increased use of opioids for legitimate medical purposes has been accompanied by a substantial increase in the prevalence of nonmedical use of prescription opioids (Zacny, et al., 2003). The National Survey on Drug Use and Health reported that the number of first time abusers of prescription opioids increased from 628,000 in 1990 to 2.4 million in 2004, that emergency room visits involving prescription opioid abuse increased by 45% from 2000 to 2002, and that treatment admissions for primary abuse of prescription opioids increased by 186% between 1997 and 2002 (SAMHSA, 2004a, 2004b). Opioid abuse indices rose most for two frequently prescribed opioids, hydrocodone and controlled-release (CR) oxycodone (Cicero, Inciardi, Munoz, 2005). Although the increase in prescription drug abuse is likely to be multifactorial, it is likely to reflect, in part, changes in available drug formulations and prescribing practices of opioid medication (Compton and Volkow, 2006). This link between increased medical use and increased abuse has driven some of the re-examination of the medical role of these drugs. The challenge, of course, is to reduce the likelihood of opioid misuse while not imposing barriers on the legitimate use of opioid medications, acknowledging both that increased abuse is probably inevitable when a psychoactive drug becomes more accessible and that attempts to control abuse can have the unintentional effects of discouraging treatment and placing severe restrictions on the medical profession.
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Brief Overview of Opioids: Neurobiology and Mechanism of Action

The term opioid refers to all compounds that bind to opiate receptors. Conventionally, the term opiate can be used to describe those opioids that are alkaloids, derived from the opium poppy; these include morphine and codeine. Opioids include semi-synthetic opiates, i.e., drugs that are synthesized from naturally occurring opiates (such as heroin from morphine and oxycodone from thebaine), as well as synthetic opioids such as methadone, fentanyl, and propoxyphene. The term narcotic is a legal designation and should not be used in the clinical setting; it refers to opioids and a few other drugs that are grouped with the opioids by law enforcement.

In the United States, numerous opioids have been commercialized for oral, transdermal and intravenous administration. Oral and transdermal formulations are usually administered for pain in the ambulatory setting. These include combination products, such as those containing hydrocodone and acetaminophen (Vicodin®, Lorset®) or ibuprofen (Vicoprofen®), tramadol and acetaminophen (Ultracet®), oxycodone and acetaminophen or aspirin (Percocet® or Percodan®), and those containing codeine and acetaminophen or aspirin. The single entity formulations on the market include those containing morphine (Avinza®, Kadian®, MS Contin®, MSIR®), oxycodone (OxyContin®), fentanyl (Duragesic®, Actiq®, Fentora®), hydromorphone (Dilaudid®), oxymorphone (Opana®), and methadone.

Opioids act by binding to specific proteins, called opioid receptors. Receptors are widely distributed. Those involved in pain modulation are situated in both the central nervous system and the peripheral nervous system. These receptors also bind endogenous opioid peptides (endorphins), which are involved in pain modulation and numerous other functions in the body. Among these functions are those mediated by deep structures of the brain, which are involved in the modulation of reinforcement and reward mechanisms, mood and stress. Opioid receptors are also found on cells from the immune system (Bidlack, 2000). In studies with rats, activation of these receptors with morphine is associated with varied effects, including sensitization of afferent nerves to noxious stimuli (Raghavendra, Rutkowski, & DeLeo, 2002).

When an opioid given for pain binds to receptors, analgesia may be accompanied by any of a diverse array of side effects related to the activation of receptors involved in other functions. These may include effects mediated by peripheral or by peripheral and central mechanisms, such as reduced peristalsis (leading to constipation) and itch, or primary central nervous system effects, such as miosis, (pupillary constriction) somnolence, mental clouding, and respiratory depression (Jaffe & Jaffe, 2004; Jaffe & Martin, 1990). Central mechanisms also lead to changes associated with hyperalgesia and decreased responsiveness to opioids (tolerance) and it has been speculated that opioid-induced hyperalgesia may be a clinically-relevant phenomenon leading to increased pain in some situations (Deleo, Tanga, & Tawfik, 2004). Activation of other central nervous system pathways by opioids also may produce mood effects, either dysphoria or euphoria.

Presumably, binding to those receptors involved in reinforcement and reward also occurs whenever an opioid is taken. In most individuals, when opioids are taken to treat pain, there appears to be no overt effect from change in these systems. In some cases, however, powerful reinforcement occurs, expressed as efforts to repeat the administration and these reinforcing outcomes may be associated with craving and with positive mood effects such as euphorigenic or pleasurable effects (Di Chiara, 2002; Koob & Bloom, 1988). These outcomes, which are uncommon but potentially serious when they occur (driving the development of an addictive pattern of use), can occur in the presence or absence of pain. Although these effects could be associated with iatrogenic addiction, they appear to be rare in patients who do not have risk factors suggesting the existence of the biological substrate for opioid-induced craving (see below).

Although several types of opioid receptors exist (e.g., mu, kappa and delta), opioid drugs largely produce their analgesic and reinforcing effects via activation of the mu opioid receptor; thus, opioids used for pain are often described as, “mu agonists”. Mu drugs that have the ability to fully activate opioid receptors (e.g., higher doses produce greater receptor activation in a dose-dependent manner) are referred to as opioid agonists or full mu agonists (such as morphine, oxycodone and methadone). Those opioids that occupy, but do not activate, receptors are referred to as opioid antagonists (e.g., naltrexone, naloxone); they can reverse the effects of mu opioid agonists. Those opioids that either have a low intrinsic activity at the mu receptor, or are agonists at another receptor and antagonists at the mu receptor are called agonist-antagonist drugs. Those with a low intrinsic activity are called partial opioid agonists and are characterized by a ceiling on most agonist activity, such that increases in dose will increase the drug’s physiological and subjective effects only to a certain level and further dose increases produce no additional effects (Jaffe & Martin, 1990).

These differences in mu receptor interactions are clearly related to the clinical use of opioid drugs and their abuse liability. Agonist-antagonist drugs are less attractive than pure mu agonists to individuals with addiction and no pain. Although other biochemical and molecular processes are presumably relevant to variation in these effects, relatively little is known about the interactions among these processes in humans.

The clinical use of opioid drugs is influenced by a variety of other characteristics, including pharmacokinetics. With the notable exception of methadone and buprenorphine, most opioids have relatively short half-lives and this has necessitated the development of new delivery systems designed to provide prolonged effects and a longer dosing interval.

Clinically-relevant physical dependence and tolerance (see below) may occur with short-term or long-term use of an opioid compound, particularly a pure mu agonist. These phenomena, which vary greatly in the clinical setting, represent neuroadaptational processes. The neurophysiology of physical dependence and tolerance are closely related to each other and to the phenomenon of opioid-induced hyperalgesia (Mao, 2002). The possibility that opioid administration, particularly at relatively high doses, may lead to increased pain has contributed to the controversy about opioid therapy for non-cancer pain, notwithstanding the limited evidence that this phenomenon occurs in clinical settings.
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Brief Overview of Chronic Pain

Chronic pain has been described as pain that has persisted for at least 1 month following the usual healing time of an acute injury, pain that occurs in association with a nonhealing lesion, or pain that recurs frequently over a period of months. In most clinical and research reports, chronic pain is typically defined as pain that has persisted for at least 3 months (Verhaak, Kerssens, Dekker, Sorbi, & Sensing, 1998).

The prevalence of chronic pain in the general population is believed to be quite high, although published reports have varied greatly. Cautious cross-national estimates of chronic pain range from 10% (Verhaak et al., 1998) to close to 20% (Gureje, Simon, & Von Korff, 2001), which would represent 30 to 60 million Americans. A national survey of 35,000 households in the US, conducted in 1998, estimated that the prevalence among adults of moderate to severe non-cancer chronic pain was 9% (American Pain Society, 1999). A large survey (N=18,980) of general populations across several European countries reported that the prevalence for chronic painful physical conditions was 17.1% (Ohayon & Schatzberg, 2003).

Chronic pain is a highly complex phenomenon, which may or may not be primarily driven by tissue injury. Conventionally, the most common forms of chronic pain are divided into those labeled “nociceptive”, or pain caused by ongoing stimulation of pain receptors by tissue damage, and those labeled “neuropathic”, or pain presumed to be related to damage to or dysfunction of the peripheral or central nervous system. These categories of pain simplify a complex reality in which both acute and chronic pain are induced by multiple peripheral and central mechanisms, which continually interact with each other and with numerous pain modulating systems. The perturbations that ultimately results in pain perception are caused by neurophysiological processes and other related systems. For example, recent evidence has begun to highlight the role of neuroimmune activation following a tissue injury as an important mechanism in the development of chronic pain (DeLeo, 2006). The role of cytokines and other inflammatory mediators is obvious in inflammatory nociceptive pains, such as some types of arthritis, but new data suggest an equally salient role in the development of chronic neuropathic pain associated with central sensitization of neural pathways following peripheral injury (Deleo, 2006).

All chronic pain is profoundly influenced by psychological processing and responses (Turk & Melzack, 2001). Pain severity and pain-related functional impairment are often found to be associated with psychological and social factors, and patients with identical diseases associated with pain, such as degenerative disk disease, may vary greatly in their reports of pain severity and pain behaviors (Aronoff, 1999). There is an extensive literature documenting the importance of operant conditioning factors (Fordyce, 1976) and cognitive-behavioral factors (Turk, Meichenbaum, & Genest, 1983) in the maintenance of chronic pain behaviors.

Chronic pain also is influenced by psychosocial and psychiatric disturbances, such as cultural influences, social support, comorbid mood disorder, and drug abuse (Gatchel, Peng, Peters, Fuchs & Turk, 2007). Classic studies of pain behavior indicate that cultural differences in the beliefs and attitudes towards pain (e.g., Zbrowski, 1969) and the social/environmental context of the pain (e.g., Beecher, 1959) have a significant impact on pain behaviors.

The contribution of psychological, social and psychiatric factors should not lead to the conclusion that a pain syndrome is primarily psychogenic. Pain related exclusively or primarily to psychological factors occurs, but is far less prevalent than pain associated with organic processes that are powerfully influenced by psychosocial mediators and psychiatric comorbidities (Portenoy, Payne, & Passik, 2004).

The “pattern of suffering” or the pain-related disability that often occurs in concert with persistent pain commonly touches on all domains of function. Patients with chronic pain may demonstrate pain-related interference with ability to perform usual activities at home, work, or school; maladaptive or dysfunctional behaviors, social isolation, and poor sleep patterns; and frequent health care utilization (Dworkin & Sherman, 2001). The recognition that acute pain can compromises health has led major medical associations and accreditation committees to designate pain severity as a “fifth vital sign”, along with blood pressure, temperature, heart rate, and respiration (Fishman, 2005). Further recognition of the increased interest in the assessment and management of pain is underscored by the U.S. Federal Law (Pain Relief Promotion Act of 2000) that declared the first decade of the 21st century as the Decade of Pain Control and Research (Gatchel et al., 2007).

Chronic pain is a major public health problem, which is associated with devastating consequences to patients and families, a high rate of health care utilization, and huge society costs related to lost work productivity. The existing treatments for chronic pain are unable to address the problem and better therapies are urgently needed. The need for these therapies is the backdrop for the expanding use of opioid drugs. An extensive clinical experience indicates that long-term opioid therapy is able to help selected patients have a better quality of life, less use of health care, and improved productivity. The medical community is no longer debating the reality of these outcomes, but rather, is now focused on a more fruitful debate about patient selection and the benefits and burdens of these drugs in varied subpopulations. Whether the frame of reference is the individual patient and family, or society-at-large, the issue is about balancing the potential benefits of these drugs in the large and diverse population with chronic pain with its potential risks.
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Terminology of Opioid Abuse: Dependence, Tolerance, Addiction

Concerns that addiction is a frequent iatrogenic consequence of the medical use of opioids may partially be attributed to confusion over terminology, as a well as failure to recognize that both addiction and chronic pain have a multifactorial etiology. In an effort to develop universal agreement on terminology related to addiction, the American Academy of Pain Medicine (AAPM), the American Pain Society (APS), and the American Society of Addiction Medicine (ASAM) approved a consensus document that clarified this terminology (ASAM, 2001; Savage, 2003).

According to the consensus document, tolerance is defined as a decreased subjective and objective effect of the same amount of opioids used over time, which concomitantly requires an increasing amount of the drug to achieve the same effect. Although tolerance to most of the side effects of opioids (e.g., respiratory depression, sedation, nausea) does appear to occur routinely, there is less evidence for clinically significant tolerance to opioids– analgesic effects (Collett, 1998; Portenoy et al., 2004). For example, there are numerous studies that have demonstrated stable opioid dosing for the treatment of chronic pain (e.g., Breitbart, et al., 1998; Portenoy et al., 2007) and methadone maintenance for the treatment of opioid dependence (addiction) for extended periods (Strain and Stitzer, 2006). However, despite the observation that tolerance to the analgesic effects of opioid drugs may be an uncommon primary cause of declining analgesic effects in the clinical setting, there are reports (based on experimental studies) that some patients will experience worsening of their pain in the face of dose escalation (Ballantyne, 2006). It has been speculated that some of these patients are not experiencing more pain because of changes related to nociception (e.g. progression of a tissue-injuring process), but rather, may be manifesting an increase in pain as a result of the opioid-induced neurophysiological changes associated with central sensitization of neurons that have been demonstrated in preclinical models and designated opioid-induced hyperalgesia (Mao, 2002; Angst & Clark, 2006). Analgesic tolerance and opioid-induced hyperalgesia are related phenomena, and just as the clinical impact of tolerance remains uncertain in most situations, the extent to which opioid-induced hyperalgesia is the cause of refractory or progressive pain remains to be more fully investigated. Physical dependence represents a characteristic set of signs and symptoms (opioid withdrawal) that occur with the abrupt cessation of an opioid (or rapid dose reduction and/or administration of an opioid antagonist). Physical dependence symptoms typically abate when an opioid is tapered under medical supervision. Unlike tolerance and physical dependence which appear to be predictable time-limited drug effects, addiction is a chronic disease that “represents an idiosyncratic adverse reaction in biologically and psychosocially vulnerable individuals” (ASAM, 2001).

The distinction between physical dependence and addiction is not always made clear in the pain literature (Ferrell, McCaffery, Rhiner, 1992). Most patients who are administered opioids for chronic pain behave differently from patients who abuse opioids and do not ever demonstrate behaviors consistent with craving, loss of control or compulsive use (e.g., Cowan et al., 2001). Of course, pain and addiction are not mutually exclusive and some patients who are treated for pain do develop severe behavioral disturbances indicative of a comorbid addictive disorder.

Some patients who are treated with opioids for pain display problematic behaviors that, on careful assessment, do not reflect addiction, but rather, appear to relate to a different process. This may be another psychiatric disorder associated with impulsive drug-taking, an unresolved family issue, a disorder of cognition, or criminal intention. In addition, there appear to be some patients who engage in problematic behaviors related specifically to desperation about unrelieved pain. The term pseudoaddiction was coined to describe the latter phenomenon (Weissman & Haddox, 1989).

Behaviors that may represent pseudoaddiction and behaviors that reflect addiction or some other serious psychopathology can occur simultaneously, and presumably, one type of phenomenon may incite the others. The diagnosis of these and other conditions may be challenging and requires a careful assessment of clinical phenomenology, specifically a range of drug-related behaviors during treatment with a potentially abusable drug (Portenoy, 1994, Lue, Passik, & Portenoy, 1998).

The term aberrant drug-related behaviors has been used to indicate the broad array of problematic nonadherence behaviors (Passik, Kirsh, Donaghy, & Portenoy, 2006), the nature of which is uncertain until a diagnosis can be developed based on astute clinical assessment. Some aberrant drug-related behavior strongly suggests the existence of addiction. These may include the use of alternative routes of administration of oral formulations (e.g., injection or sniffing), concurrent use of alcohol or illicit drugs, and repeated resistance to changes in therapy despite evidence of adverse effects; examples of aberrant behavior less suggestive of addiction are drug hoarding during periods of reduced symptoms, occasional unsanctioned dose escalation, and aggressive complaining about the need for more drugs (Portenoy, 1994).
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Distinction between Withdrawal and Chronic Pain

Because addiction is associated with psychological distress and physical discomfort in the form of opioid withdrawal symptoms, it may be difficult to distinguish primary chronic pain complaints from withdrawal pain. Withdrawal also may have the potential to increase baseline pain related to other processes. For example, based on anecdotal evidence from chronic pain patients, withdrawal from opioids can greatly increase pain in the original pain site. These phenomena suggest the need to carefully assess the potential for withdrawal during long-term opioid therapy (e.g, at the end of a dosing interval or during periods of medically-indicated dose reduction).

These phenomena notwithstanding, there also is evidence that experienced drug abusers are able to distinguish withdrawal pain from chronic pain. For example in studies of methadone maintenance patients, both the phenomenology and correlates of chronic pain were different than for withdrawal pain (Karasz et al., 2004; Rosenblum et al., 2003). Chronic pain is typically localized (e.g., back pain, headache) and persists (although with varying degrees of severity) for long periods of time (Gureje, Von Korff, Simon & Gater, 1998). Although certain subjective experiences of withdrawal (e.g., muscle ache) are similar to some distinct pain syndromes, other withdrawal experiences such as yawning, sweating and hot and cold flashes are likely to be more commonly associated with subjective drug withdrawal than with primary pain conditions. Moreover, the constellation of words used to describe withdrawal pain is likely to be different than words used to describe other painful disorders. Qualitative studies of addicts going through withdrawal typically refer to the experience as “being sick” (similar to a moderate to severe flu-like illness) and not as representing a distinct pain (Farrell, 1994). The subjective experience of withdrawal can be validly measured with an instrument such as the Subjective Opiate Withdrawal Scale (SOWS; Handelsman, et al., 1987). Withdrawal from short-acting opioids, such as heroin, is typically short-lived; physical symptoms are likely to reach their maximum intensity over a 36–72 hour period and to reduce in intensity after that (Farrell, 1994).
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Co-occuring Chronic Pain and Opioid Addiction

The prevalence of addictive disorders among chronic pain patients is difficult to determine (Covington and Kotz 2003). One 1992 literature review found only seven studies that utilized acceptable diagnostic criteria and reported that estimates of substance use disorders among chronic pain patients ranged from 3.2% – 18.9% (Fishbain, Rosomoff, & Rosomoff, 1992). A Swedish study of 414 chronic pain patients reported that 32.8% were diagnosed with a substance use disorder (Hoffmann, Olofsson, Salen, & Wickstrom, 1995). In two US studies, 43 to 45% of chronic pain patients reported aberrant drug-related behavior; the proportion with diagnosable substance use disorder is unknown (Katz et al., 2003; Passik et al., 2004). All these studies evaluated patients referred to pain clinics and may overstate the prevalence of substance abuse in the overall population with chronic pain.

A relatively high prevalence of substance abuse disorders among persons with chronic pain can also be inferred by the high co-occurrence of these two disorders. There have been several reports that the prevalence of chronic pain among persons with opioid and other substance use disorders is substantially higher than the pain prevalence found in the general population (Breitbart, et al., 1996; Brennan, Schutte, & Moos, 2005; Jamison, Kauffman, & Katz, 2000; Rosenblum et al., 2003; Sheu, et al., 2008).
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Opioid Treatment for Chronic Pain

Opioid therapy is the mainstay approach for the treatment of moderate to severe pain associated with cancer or other serious medical illnesses (Patt & Burton, 1998; World Health Organization, 1996). Although the use of opioid analgesics for the treatment of CNMP has been increasing in recent years (Joranson, Ryan, Gilson & Dahl, 2000) and has been endorsed by numerous professional societies (AAPM, APS, 1997; American Geriatric Society, 1998; Pain Society, 2004), the use of opioids remains controversial due to concerns about side effects, long-term efficacy, functional outcomes, and the potential for drug abuse and addiction. The latter concerns are especially evident in the treatment of CNMP patients with substance use histories (Savage, 2003).

Other concerns that may contribute to the hesitancy to prescribe opioids may be related to perceived and real risks associated with regulatory and legal scrutiny during the prescribing of controlled substances (Office of Quality Performance, 2003). These concerns have propelled extensive work to develop predictors of problematic behaviors or frank substance abuse or addiction during opioid therapy. Questionnaires to assist in this prediction and monitoring have been developed and used in research and field trials. Examples include the Prescription Drug Use Questionnaire (PDUQ; Compton et al., 1998); the Pain Assessment and Documentation Tool (PADT; Passik et al., 2004) and the Current Opioid Misuse Measure (COMM; Butler et al., 2007). These instruments are not used in practice settings at this time.

Narrative reports on the use of opioids for CNMP have underscored the effectiveness of opioid therapy for selected populations of patients and there continues to be a consensus among pain specialists that some patients with CNMP can benefit greatly from long-term therapy (Ballantyne & Mao, 2003; Trescot et al., 2006). This consensus, however, has received little support in the literature. Systematic reviews on the use of opioids for diverse CNMP disorders report only modest evidence for the efficacy of this treatment (Trescot et al., 2006; 2008). For example, a review of 15 double-blind, randomized placebo-controlled trials reported a mean decrease in pain intensity of approximately 30% and a drop-out rate of 56% only three of eight studies that assessed functional disturbance found improvement (Kalso, Edwards, Moore, & McQuay, 2004). A meta-analysis of 41 randomized trials involving 6,019 patients found reductions in pain severity and improvement in functional outcomes when opioids were compared with placebo (Furlan, Sandoval, Mailis-Gagnon, & Tunks, 2006). Among the 8 studies that compared opioids with non-opioid pain medication, the six studies that included so-called “weak” opioids (e.g., codeine, tramadol) did not demonstrate efficacy, while the two that included the so-called “strong” opioids (morphine, oxycodone) were associated with significant decreases in pain severity. The standardized mean difference (SMD) between opioid and comparison groups, although statistically significant, tended to be stronger when opioids were compared with placebo (SMD = 0.60) than when strong opioids where compared with non-opioid pain medications (SMD = 0.31). Other reviews have also found favorable evidence that opioid treatment for CNMP leads to reductions in pain severity, although evidence for increase in function is absent or less robust (Chou, Clark, & Helfand, 2003; Eisenberg, McNicol, & Carr, 2005). Little or no support for the efficacy of opioid treatment was reported in two systematic reviews of chronic back pain (Deshpande, Furlan, Mailis-Gagnon, Atlas, & Turk, 2007; Martell, et al., 2007). Because patients with a history of substance abuse typically are excluded from these studies, they provide no guidance whatsoever about the effectiveness of opioids in these populations.

Adding further to the controversy over the utility of opioid analgesics for CNMP is the absence of epidemiological evidence that an increase in the medical use of opioids has resulted in a lower prevalence of chronic pain. Noteworthy is a Danish study of a national random sample of 10,066 respondents (Eriksen, Sjøgren, Bruera, Ekholm, & Rasmussen, 2006). Denmark is known for having an extremely high national usage of opioids for CNMP and this use has increased by more than 600% during the past two decades (Eriksen, 2004). Among respondents reporting pain (1,906), 90% of opioid users reported moderate to very severe pain, compared with 46% of non-opioid users; opioid use was also associated with poor quality of life and functional disturbance (e.g., unemployment).

Although this epidemiological study may be interpreted as demonstrating that opioid treatment for CNMP has little benefit, the authors acknowledge that these disquieting findings do not indicate causality and could be influenced by the possibility of widespread undertreatment, leading to poorly managed pain. This latter interpretation is supported by a commentary on the Ericksen et al. study (Keane, 2007). Keane notes that among the 228 pain patients receiving opioids only 57 (25%) were using strong opioids, while the remainder was using weak opioids. European (as well as United States) clinical guidelines generally recommend long-acting formulations of strong opioids for the treatment of chronic moderate to severe pain, which may be supplemented with short-acting opioids for breakthrough pain (Pain Society, 2004; OQP, 2003; Gourlay, 1998; Vallerand, 2003; Fine & Portenoy, 2007).

The possibility of inappropriate opioid treatment is further supported by another Danish study that assigned pain patients who were on opioid therapy to either a multidisciplinary pain center (MPC) or to general practitioners (GP) who had received initial supervision from the MPC staff (Eriksen, Becker, & Sjegren, 2002). At intake, a substantial number of patients in both groups were apparently receiving inappropriate opioid therapy for chronic pain (60% were being treated with short-acting opioids and 49% were taking opioids on demand). At the 12 month follow-up, 86% of MPC patients were receiving long-acting opioids and 11% took opioids on demand. There was no change in the administration pattern in the GP group. These findings suggest that a significant proportion of opioid-treated CNMP patients may be receiving inappropriate opioid treatment and that educating general practitioners in pain medicine may require more than initial supervision.

It is generally acknowledged that there is a wide degree of variance in the prescribing patterns of opioids for chronic pain (Lin, Alfandre, & Moore, 2007; Trescot et al., 2006). Some opioid treatment practices persist despite evidence that they might be harmful or have little benefit, such as the over-prescribing of propoxyphene among the elderly (Barkin, Barkin, & Barkin, 2006; Singh, Sleeper, & Seifert, 2007). Nursing home patients being treated with opioids have been found to be inadequately assessed for pain and to be more likely treated with short-acting rather than long acting opioids (Fujimoto & Coluzzi, 2000). A substantial number of physicians are reluctant or unwilling to prescribe long-acting opioids to treat CNMP, even when it may be medically appropriate (Nwokeji, et al., 2007).

Controversy about the long-term effectiveness of opioid treatment also has focused on the potential clinical implications of opioid-induced hyperalgesia. As noted earlier, exposure to opioids can result in an increased sensitivity to noxious stimuli in animals, and an increased perception of some types of experimental pain in humans (c.f., Koppert & Schmeltz, 2007; Angst & Clark, 2006). Anecdotal reports of hyperalgesia occurring with very high or escalating doses of opioids (Angst & Clark, 2006) has been viewed as a clinical correlate of these experimental findings. The extent to which this phenomenon is relevant to the long-term opioid therapy administered to most patients with chronic pain is unknown. Although experimental evidence suggests that opioid-induced hyperalgesia might limit the clinical utility of opioids in controlling chronic pain (Chu, Clark, & Angst., 2006), there have been no reports of observations in the clinical literature to suggest that it should be a prominent problem. More research is needed to determine whether the physiology underlying opioid-induced hyperalgesia may be involved in a subgroup of patients who develop problems during therapy, such as loss of efficacy (tolerance) or progressive pain in the absence of a well defined lesion.

Outcome studies of long term use of opioids are compromised by methodological limitations which make it difficult to acquire evidence of efficacy (Noble, Tregear, Treadwell, & Schoelles, 2007). Methodological limitations may be unavoidable because of the ethical and practical challenges associated rigorous studies such as randomized controlled trials. Guidelines for opioid therapy must now be based on limited evidence; future evidence may be acquired by utilizing other study designs (Noble et al., 2007) such as practical clinical trials (Tunis, Stryer, & Clancy, 2003). These studies should include at least three criteria to reflect a positive treatment response: i.e., reduction of pain severity (derived from subjective reports or scores on pain scales), recovery of function (improved scores on instruments that measure some aspect of function), and quality of life.

Guidelines for the use of opioids for the treatment of chronic pain have been published (AAFP et al., 1996–2002; OQP, 2003), and recent guidelines have emphasized the need to initiate, structure and monitor therapy in a manner that both optimizes the positive outcomes of opioid therapy (analgesia and functional restoration) and minimize the risks associated with abuse, addiction and diversion (Portenoy et al., 2004). These guidelines discuss patient selection (highlighting the likelihood of increased risk among patients with prior histories of substance use disorders), the structuring of therapy to provide an appropriate level of monitoring and a presumably lessened risk of aberrant drug-related behavior, the ongoing assessment of drug-related behaviors and the need to reassess and diagnose should these occur, and strategies that might be employed in restructuring therapy should aberrant behaviors occur and the clinician decide to continue treatment. They also note that therapy should be undertaken initially as a trial, which could lead to the decision to forego more therapy, and that an “exit strategy” must be understood to exist should the benefits in the individual be outweighed by the burdens of treatment.

The relatively recent recognition that guidelines for the opioid treatment of chronic pain must incorporate both the principles of prescribing as well as approaches to risk assessment and management may represent an important turning point for this approach to pain management. Acknowledging that prescription drug abuse has increased during the past decade, a period during which the use of opioid therapy by primary care physicians and pain specialists has accelerated, pain specialists and addiction medicine specialists now must collaborate to refine guidelines, help physicians identify the subpopulations that can be managed by primary care providers, and discover safer strategies that may yield treatment opportunities to larger numbers of patients.
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Treating Patients with Addictive Disorders

Safe and effective pain treatment is especially important for persons with a drug use history because inadequate treatment or lack of treatment for pain may have problematic consequences, such as illicit drug use (e.g., heroin), misuse of prescription opioids and other pain medications (e.g., benzodiazipines), psychiatric distress, functional impairment and a tendency for health providers to attribute pain complaints and requests for pain medication to an addictive disorder rather than to a pain disorder (Gureje, et al., 2001; Scimeca, Savage, Portenoy, & Lowinson, 2000). Undertreatment of pain among addicted persons may lead to the adverse medical, social and personal consequences associated with continued drug-seeking behavior (Savage, 1996). Pain complaints may be most problematic among persons with opioid addiction, as this group may have lower tolerance for pain than other addicted populations (Compton, 1994; Compton, Charuvastra, & Ling, 2001). Pain and opioid addiction may be further intertwined among persons who have a history of abusing controlled opioid pain medications, such as oxycodone or hydrocodone.
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A Possible Role on the use of Buprenorphine for the Treatment of Chronic Pain

Increasing interest in developing clinical protocols for opioid treatment of chronic pain in the population with substance abuse histories has highlighted the role of opioid medications that may have lower abuse potential. One medication that is beginning to be examined is buprenorphine, a partial opioid mu agonist that is well recognized as an analgesic (Johnson, Fudala, & Payne, 2005). In 2002, a sublingual tablet (both in mono form – Subutex® - and combined with naloxone - Suboxone®) was approved by the U.S Food and Drug Administration as a Schedule III medication for the treatment of opioid dependence. In numerous controlled clinical trials, it has been demonstrated to be highly efficacious in reducing illicit opioid use and promoting treatment retention among opioid abusers (e.g., Johnson, Strain, & Amass, 2003; Kakko, Svanborg, Kreek, Heilig, 2003; O'Connor et al., 1998; Fudala et al., 2003). In opioid addicts, it suppresses the craving and withdrawal symptoms associated with opioid use and also blocks the euphoric effects of subsequent opioid use (See Bickel & Amass, 1995 for a review).

As a partial mu-agonist, buprenorphine has a ceiling effect on its agonist activity (Lewis, 1985; Walsh, Preston, Bigelow & Stitzer, 1995). It is less likely than a full agonist to cause respiratory depression in opioid-naïve patients (Cowan, Lewis & Macfarlane, 1977). This property of buprenorphine increases its safety profile by reducing the risk of accidental overdose (Walsh, Preston, Stitzer, Cone & Bigelow, 1994). The partial agonism of buprenorphine would presumably yield a ceiling effect for analgesia as well, which would limit the clinical use of the drug in pain management, but there is some question about the extent of this ceiling effect in practice (Dahan, et al., 2006).

Although the combination buprenorphine/naloxone tablet (Suboxone) may precipitate withdrawal in opioid-tolerant persons if it is injected, making it relatively unattractive for diversion (CSAT, 2004), there is nevertheless evidence of diversion, as would be expected with any psychoactive drug that has hedonic properties (Cicero & Inciadi, 2005; Smith, Bailey, Woody, & Kleber, 2007). Rates of abuse are relatively low compared to full mu agonists and buprenorphine rarely is endorsed as a primary drug of abuse (Cicero, Suratt, & Inciardi, 2007; Rosenblum et al., 2007; SAMHSA, 2006).

In Europe, a transdermal formulation of buprenorphine has been approved for the treatment of chronic pain (e.g., Griessinger, Sittl, & Likar, 2005; Sittl, 2005). In post-marketing surveillance studies and in a multicenter randomized controlled clinical trial, the transdermal patches were reported to be effective and well-tolerated in the treatment of cancer and non-cancer chronic pain (Griessinger et al., 2005; Sittl, 2005; Sorge and Stittl, 2004; Sittl, Nuijten, & Nautru, 2006). A transdermal formulation of buprenorphine is not presently available in the United States.

The off-label use of sublingual buprenorphine tablets to treat chronic pain has been described in two clinical reports, one describing its use in a series of chronic pain patients who were responding poorly to other opioid analgesics (Malinoff et al., 2005) and the other describing the response of patients with both pain and addiction (Heit & Gourlay, 2008). In both of these reports, the authors reported that their patients were successfully treated with buprenorphine, e.g., pain relief and improved mood and functioning.

In a similar manner, two earlier publications describe the open-label use of the parenteral formulation of buprenorphine administered sublingually to treat patients with chronic pain (Adriaensen, Mattelaer, & Vanmeenen, 1985; Nasar, McLeavy, & Knox, 1986). Although most patients were followed up for less than one month, both studies reported good analgesia and low incidence or time-limited unwanted side effects. There is also evidence from several preclinical studies and one study with human subjects that, in contrast to pure mu-agonists, buprenorphine exerts a lasting anti-hyperalgesic effect (Hans, 2007; Koppert, et al., 2005). The transdermal trials conducted in Europe, the anecdotal reports of sublingual administration in North America, and buprenorphine’s comparatively high safety profile suggest that it would be valuable to systematically study buprenorphine as a treatment of pain in patients with substance use disorders.
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Conclusion

Opioids are among the most effective medications for moderate to severe pain. Although there is a consensus on their utility as a treatment for chronic cancer pain, their long-term use for chronic non-malignant pain remains controversial. Several medical professional organizations acknowledge the utility of opioid therapy and many case series and large surveys report satisfactory reductions in pain, improvement in function and minimal risk of addiction. However, the clinical trials that have been conducted do not provide adequate evidence of long-term effectiveness. Despite the consensus of pain specialists, and the eminently ethical and medically justified commentaries to consider opioid therapy in the armamentarium of treatments for moderate to severe pain (Brennan, Carr, & Cousins, 2007), there is concern that the pendulum has swung from undertreatment to overtreatment (White & Kehlen, 2007). This controversy is enhanced by the increased prevalence of prescription opioid abuse, which has developed concomitantly with an increase in opioid administration in the clinic. The resolution of this controversy will require much more research and the acceptance of treatment guidelines that recognize the dual obligations of the prescriber: to optimize the balance between analgesia and side effects, and promote other favorable outcomes, while concurrently assessing and managing the risks associated with abuse, addiction and diversion. At this juncture, it is important that the opioid treatment debate evolve from a discussion focused on “too little” or “too much” to one focused on identification and training of best treatment practices. Improvement in opioid therapy can occur through research and training to aid practitioners to determine the appropriate patient subpopulations and treatment protocols to achieve satisfactory outcomes.

Finally, it is imperative to advance a research agenda that leads to the identification of methods that would enhance pain relief while reducing the likelihood of addiction and other adverse events when opioids are selected for therapy. This should include the testing of novel medications that may be safer or more differentially effective for select treatment populations (as the proposal to test buprenorphine with high risk patients, discussed above) and the evaluation of treatment protocols incorporating risk management techniques.
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Acknowledgments

The authors wish to thank two anonymous reviewers who provided extremely thoughtful and helpful comments on an earlier version of this paper. Acknowledgement: Development of this paper was partially supported by a National Institute on Drug Abuse grant R21 DA022675.

References:

In order to find the references for this piece, you'll need to go to the original site - there are far too many to feature here (Ed.)


https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2711509/

Sunday, August 6, 2017

Opioids To Manage Chronic Pain Another Perspective


Today's post from paulchristomd.com (see link below) is a well-balanced and thoughtful look at the current debate about opioid prescription for chronic pain (naturally including neuropathic pain). So many of us have been forced to take opioids to keep our neuropathy symptoms under control; simply because nothing else has worked. It's not as if our doctors have prescribed opioids as a first-line treatment - we've generally been through the mill of other medications and their lack of effectiveness and side-effects and opioids are a last resort treatment but we need them. We're not rabid junkies preying on the helpless to get out fix; we're genuine pain patients who have been left with no choice. The fact that we're now stigmatised as being social pariahs is not our fault and has left us fuming with anger at the hysterical reactions of media and politicians. This article looks at the problem calmly and puts the debate into perspective - worth a read.

Opioids in Pain Management 
Dr Paul Christo MD Posted on July 14, 2016

As we all know, opioids are commonly prescribed for pain. The news has portrayed some scary stories, highlighting celebrity opioid overdoses and stories of addiction. Although opioids have definite risks, they can be quite effective for certain patients with chronic non-cancer pain In patients with cancer pain or those experiencing pain at the end of life, opioids are critical. About 20% of patients going to physician offices with non-cancer pain symptoms or pain-related diagnoses (including acute and chronic pain) receive an opioid prescription.*

Opioids are powerful painkillers that remain the gold standard for easing postoperative pain. Since the 1990s, more pain specialists and especially primary care doctors have prescribed opioids for patients with persistent pain. Unfortunately, we’ve seen an escalating number of people die from opioid related overdoses. However, opioid related deaths are now beginning to plateau. When examining the literature, there are no studies that compare opioids to other possible treatments with respect to long term outcomes (greater than a year) in pain, function, or quality of life. The Centers for Disease Control (CDC) has responded by recently issuing their opioid prescribing guideline. Their recommendations focus on incorporating non opioid therapies and non-pharmacological therapies (exercise, weight loss, procedures like nerve blocks, and psychological therapies like cognitive behavioral therapy) as therapies for chronic pain instead of opioids.

On the other hand, many of these deaths resulted from combining opioids with alcohol or drugs called benzodiazepines. Some pain experts and patients feel that the “War on Opioids” is hurting patients who need them, saying that the majority of people becoming addicted to opioids are not chronic pain patients. Rather, they are people using opioids non-medically to get “high”, or treat other medical problems like anxiety or depression. As the debate continues, we are seeing more physicians and healthcare providers prescribe fewer opioids primarily due to the FDA’s recommendation to limit the supply, the CDC’s guideline, and fear of media scrutiny. Opioids can produce significant side effects, including constipation, nausea, mental clouding, and respiratory depression, which can sometimes lead to death*. As a patient, it’s important to make sure the prescriber is well versed in opioids as a therapy before initiating them.

Some of the lesser known side effects of opioids include decrease in testosterone and estrogen levels, worsening pain (opioid induced hyperalgesia), and sleep disordered breathing. In fact, there is mounting evidence that long term opioid use for pain can actually produce a chronic pain state, whereby patients find themselves in a vicious cycle of using opioids to treat pain caused by previous opioid use*. Due to the uncommon, but serious risk of respiratory depression and the number of unintentional opioid overdoses, both the American Medical Association and Substance Abuse and Mental Health Administration recommend co-prescribing naloxone to patients at risk who are taking opioids. Naloxone is an opioid antagonist (reversal agent for opioids) and is FDA approved as a nasal spray (Narcan® made by Adapt Pharma) and a subcutaneous or intramuscular injection (Evzio® made by Kaleo). Naloxone is intended to be used by first responders, relatives, or friends of people taking prescribing opioids or using heroin in order to reverse sedation, respiratory depression, and lowered blood pressure.

Pain continues to be a substantial public health problem worldwide. Despite advances, opioids are still needed for pain after trauma or surgery. They are needed for cancer pain, palliative care, and in select situations can be effective for chronic pain. There are an array of options available instead of opioids. For instance, antiepileptic drugs, antidepressants, and NSAIDS can be effective analgesics along with spinal cord stimulation, peripheral nerve stimulation, nerve blocks, pain pumps, psychology, holistic approaches, and integrative therapies. Don’t be afraid to ask about these therapies and to try them. Pain therapies are customized because each person’s pain is unique. A pain treatment that is successful for one patient may not offer than same relief in another. I have spoken about many of these therapies on my radio show, Aches and Gains.

Education is important. Be aware of the side effects of opioids. Keep in contact with your doctor or healthcare provider who can monitor the safe use of opioids if that therapy is chosen.

For more in-depth insight on opioids, listen to my radio show War on Opioids.

http://www.paulchristomd.com/opioids-pain-management/
*NIH.gov “The Role of Opioids in the Treatment of Chronic Pain”
*CDC.gov “CDC Guideline for Prescribing Opioids for Chronic Pain – United States 2016”


http://www.paulchristomd.com/opioids-pain-management/

Friday, August 4, 2017

Opioids And Chronic Nerve Pain


Today's post from medicine.ox.ac.uk (see link below) may seem enormously long but if you have been prescribed, or feel that you may end up being prescribed, opioids then it's in your own interests to learn as much as you can about these drugs with such a socially bad image. The image comes from recreational abuse but there is no doubt that opioids can be very useful for neuropathic pain - in fact they are often a welcome but last resort. The problems (possible addiction and the idea that you'll always need more) arise from personal misuse and doctors who send you away with a prescription and let you get on with it. You need to take them as prescribed and only as prescribed and you need to have the sort of partnership with your doctor that allows monitoring and awareness of how they are affecting you. They are excellent drugs for controlling chronic pain (especially nerve pain) but you need to feel secure in taking them and not fearful of the consequences. Close contact with your doctor is essential, especially during the initial period. He or she will begin with a low dose and build up if necessary until the best effect is achieved but that sometimes means patience on both sides. You may need more, you may even need less but either way if you remain aware that they are strong medications and listen to your body, you will be fine. Doctor/patient communication is essential for opioids to work best. This article may be a hefty chunk for breakfast reading and sometimes difficult to understand but remember, it's your health and your body and the more knowledge you have of what opioids will do and how they work, the faster you will obtain the relief from pain that you need. Remember also, there are many sorts of opioids - if one doesn't suit you another probably will. Checking out the alphabetical list to the right of this blog will reveal many more articles on opioids and neuropathy.

 
OPIOID USE IN CHRONIC PAIN
H J McQuay DM, Clinical Reader in Pain Relief

Pain Research; Nuffield Department of Anaesthetics, University of Oxford, Oxford UK 


Abstract

Many of the important questions for those who prescribe opioids in chronic pain, and important for those who take the drugs, still have to be answered with inadequate evidence, because we lack randomised trials on these topics

Two of the principal reasons for 'failure' of opioids to relieve pain, incident pain and neuropathic pain, are discussed. Some specific adverse effect problems are addressed, and the paper concludes with a section on the vexed issue of opioid prescription in non-cancer pain.

If we take in our hands any volume ... let us ask, "Does it contain any abstract reasoning concerning quantity or number?" No. "Does it contain any experimental reasoning concerning matter of fact and existence?" No. Commit it then to the flames, for it can contain nothing but sophistry and illusion."
David Hume (1711-76)


Much of our prescribing of opioids is based on opinion rather than on evidence. In part this is because opioid use in chronic non-cancer pain is an orphan area, in part because trial design and conduct is not easy in this patient group, and in part it is historic - many opioids are old drugs, and the registration trials required for new drugs have therefore not been done. It is remarkable how little new evidence on oral and intramuscular opioid use has emerged since earlier reviews [1, 2, 3]. An added complication is that there is a plethora of routes by which these drugs can be given. The fact "that it can be done" very often pre-empts the more important question "should it be done?". Enthusiasts for the new route carry it into practice without adequate comparison of risk and benefit with 'established' routes. Again these arguments have been well rehearsed [4]. Much of the 'new' evidence for spinal or transdermal opioids does not answer the real clinical questions. 


Clinical aspects
Effectiveness
Success


Just how effective are opioids in managing chronic pain, cancer or non-cancer? The assumption from audits of applying WHO guidelines (Figure 1) in cancer pain is that two-thirds of patients achieve good or moderate pain relief.



The adequacy of these audits has been challenged on process grounds [5]. In practical terms we have refrained from detailed questioning of the adequacy of our methods because of a wider public health political goal, which is to achieve better coverage of the world population with implemented WHO guidelines (and sufficient drug supplies).

In attempting to update the WHO guidelines questions emerge such as whether a second stage is necessary and whether a fourth stage should be added [6], and yet again there is the problem that little research evidence answers these clinically relevant questions. Both existing guidelines and the updated versions are based necessarily on non-optimal levels of evidence. Only 2% of the randomised controlled trials in pain relief study cancer pain directly [7].

Beyond trying to determine just how good the good and moderate relief is for the two-thirds of patients, there are two obvious problem areas, neuropathic pain and incident pain.
 

 NEUROPATHIC PAIN

There are 2 extreme positions on opioid sensitivity. One suggests that opioid sensitivity is a relative phenomenon and therefore that any pain can be controlled by opioids provided that there is an adequate dose escalation and control of adverse effects [8]. The other extreme insists that some pains are intrinsically insensitive to opioids and that this insensitivity can be predicted from the clinical characteristics of the pain [9]. Nociceptive pain is thought to be sensitive to opioids while neuropathic pain is regarded as insensitive. If neuropathic pain shows an analgesic response with opioid then this has been attributed to mood improvement rather than to a direct effect on pain pathways [10].

Both extremes of this controversy are supported by a very small number of controlled trials each of which has methodological limitations. These studies have used either single doses [10, 11], infusions of different opioids [8, 9] or have measured pain without simultaneous assessment of adverse effects [9, 10, 11, 12]. The flaw with studies which use a single (fixed) dose or infusion rate is that they may underestimate responses in patients with previous opioid exposure. These patients may need more opioid to achieve analgesic effect than the opioid naive.

Using patient-controlled analgesia (PCA) with simultaneous nurse observer measurement of analgesia and adverse effects we gave two concentrations of morphine in a double-blind randomised cross-over fashion and compared the clinical responses produced by both concentrations of morphine [13].

The results did not support the assumption that neuropathic pains are always opioid insensitive. Half of the pains judged as neuropathic achieved a good response. Nociceptive pains, however, collectively showed a better analgesic response, because all of them achieved a good response in at least one of the sessions. No nociceptive pain had a poor response in this study.

Secondly, it had been suggested that the analgesic response of neuropathic pains to opioids can be explained by the changes in mood induced by the opioids [10]. When the results of patients with consistent responses were compared, changes in mood reflected changes in pain intensity and relief regardless of the clinical character of the pain, nociceptive or neuropathic. Mood improved when pain intensity decreased or pain relief increased. No patient had a change in mood in the absence of a change in pain intensity or pain relief, and patients with nociceptive pains in fact showed a greater change in mood than those with neuropathic pain. Therefore, the theory that relief of neuropathic pains by opioids is due to changes in mood was not supported by our findings.

INCIDENT PAIN

The problem with incident pain is that the analgesia necessary to control episodic incident pain is usually far more than is required when it is absent. The patient between bouts of incident pain may then suffer all the adverse effects of an 'overdose'. Optimal analgesic regimes should restore normal function. The reality, however, is that with sub-optimal regimes, or when the incident pain cannot be controlled satisfactorily despite an optimal regime, function and quality of life may have to be reduced to cope with the pain. In this delicate balance between adequate control of the incident pain and adverse effects between times the patient often opts to 'accept' the incident pain rather than to endure the adverse effects.

 
Classifying incident pain


The overlap in conventional use between the terms incident pain and breakthrough pain is unfortunate. Breakthrough pain describes an inadequate analgesic regime [14], and is therefore an operational definition of pain which is not controlled, but is 'breaking through' the analgesic regime. The regime may be adequate to control background pain but inadequate to control incident pain.

Incident pain is used commonly to describe pain on movement. Conventionally the widest definition is pain which comes on when the patient is not resting. This may be pain caused by deep breathing or coughing, or pain caused by walking, turning or lifting. These pains on activity or movement may, to an extent, be controlled by the patient, by not moving. Incident pain thus describes some characteristics of the pain, such as its relationship to coughing or movement, and describes those characteristics independent of the presence or absence of an analgesic regime. Breakthrough pain is one type of incident pain.

Complicating matters further there is a third kind of incident pain, which is an intermittent pain which can occur even when the patient is resting, and can occur with no known triggering process. The patient has no control over these pains. Complete description of the pain would also include whether or not the patient has background pain which is present at rest. The problem with restricting the definition of incident pain to pain related to movement or to activity is that excluding the intermittent, unpredictable pain excludes a considerable proportion of these difficult pains (see under prevalence below).  


Figure 2 summarises the definition problems.



The simplest definition is that incident pain is characterised by episodic increases in pain intensity.

Another characteristic is the patient's ability to suppress or avoid the incident pain; the pain may be defined as "volitional" or "non-volitional" [14]. Volitional pain should be predictable. 


Characteristics of incident pain

Pain on movement may be predictable, occurring each time the patient moves in a particular way. It may be brief or it may be prolonged. It may be acute, as a result of a recent change in disease or due to treatment. It may be chronic. These three axes, predictability, time course of the episodes and the chronicity of the problem, are shown in Figure 3.


 

How big a problem is incident pain?

Incident pain is a big problem both because it is common and because of the distress it causes the individual. The incidence and prevalence can only be estimated from small surveys. Portenoy and Hagen [14] reported on 90 patients at the Memorial Sloan-Kettering Cancer Center, and their findings are summarised in Figure 4.



Banning et al studied 200 consecutive referrals to the pain clinic at the Finsen Institute in Copenhagen [15]. Of the 184 patients whose pain they evaluated 172 had pain on movement, 144 had pain at rest and 124 had their sleep interrupted by pain.

From the Danish data most patients with cancer pain will have incident pain related to movement. Of the 131 patients with pain on movement who they re-evaluated 1 to 2 weeks after treatment 83 still had pain on movement, 20 with moderate intensity and 36 with considerable intensity. From the American survey (Figure 4) roughly half the patients had breakthrough pain despite an established analgesic regime. Both these reports are from tertiary care institutions, so that generalising to obtain incidence and prevalence data for the general population is invalid, because patients will be referred precisely because they do have pain. Within this selected population, however, it is a reasonable inference that incident pain is a major problem for most patients who have not started an 'adequate' analgesic regime, and that it remains a major problem for half of those who are established on analgesics.

 
How should incident pain be managed?


Restating the problem, it is that the doses of analgesics required to control the incident pain may be so high that toxicity results when the incident pain is absent. Pain relief in this situation is usually relief of symptoms rather than remedying the cause of the pain. Analgesics do not stretch to accommodate increased severity; increased doses are required, with concomitant risk of increased adverse effects. The questions then arise as to what changes (if any) should be made in our 'conventional' management strategies to cope better with incident pain, and what additional remedies should be considered.

The traditional way to manage cancer pain is illustrated by the WHO ladder (Figure 1). Two questions need to be addressed. The first is whether or not each of the three rungs of the ladder is able to control incident pain. The answer required for each rung is whether or not control is feasible, given adequate management of adverse effects. The incidence data suggests that, for a significant proportion of patients, it is not possible. It is also possible that better management of opioid adverse effects would allow higher opioid doses to be used with fewer adverse effects. An open study of methylphenidate suggests that this may be a useful approach [16]. The second issue is whether the incident pain (pain on movement or on coughing in the postoperative context) is simply the same pain at higher intensity or is something different; is it a quantitative or a qualitative difference?

Quantitative increase in pain on movement - evidence from postoperative pain


The evidence from postoperative pain suggests a quantitative difference between pain at rest and pain on movement; more analgesia is required to control the pain on movement, with the increased risk of adverse effects, but the pain can be controlled, at least by regimes which incorporate all three WHO ladder rungs, and particularly with the addition of local anaesthetic and steroids [17]. The studies from this Copenhagen group have shown that none of the individual rungs of the WHO ladder can achieve this degree of incident pain control on their own. It is only by using combinations that they have made progress. The ability to maintain pain intensity scores of zero on coughing for eight days after colonic resection is remarkable [17]. The regime used was methylprednisolone 30 mg/kg iv before surgery, thoracic epidural infusion of a combination of local anaesthetic and morphine, intrathecal (intraoperative) local anaesthetic and indomethacin 100 mg iv 8 hrly with oral indomethacin as required.

For incident pain in cancer the message must be that if the incident pain is a predictable quantitative increase of the pain at rest, then we should think of combinations of the rungs of the ladder, and of the use of local anaesthetic and steroids when that fails, by oral, subcutaneous [18] or epidural [19] routes. At first sight the Copenhagen regime appears to be way beyond what might be practical for cancer pain patients. The reality, however, is that epidural infusion of combinations of local anaesthetic and opioid is already being used outside hospital, and ten years ago few would have thought that practical. RCTs of combinations are notoriously difficult to conduct in any patient group, let alone epidural combinations in cancer pain patients, but they are badly needed. With an epidural catheter in place it is easy for booster doses to be given in response to episodic increase in pain intensity. The issue is not the technical feasibility, but whether it is an effective method and more appropriate than the alternatives.

Incident pain: qualitative increase in pain


The classes of drugs used commonly are antidepressants, anticonvulsants and steroids. The RCTs of these 3 classes have been in chronic non-cancer pain, and have focused on neuropathic pain syndromes, not on incident pain. The importance of these drugs in that incident pain which is qualitatively different from pain at rest is often of the neuropathic type. It is important then to know whether or not the pain responds to these classes of drugs.

The recent randomised controlled studies of antidepressants have reinforced the messages that first generation tricyclic antidepressants are more effective as analgesics in this context than the more selective antidepressants, that the relief and its duration do not depend on the quality of the pain (burning, shooting etc.), and that the relief can be obtained well within the first week [20, 21, 22, 23]. It is possible therefore to increase dose quickly to achieve an adequate trial of antidepressants without wasting time which is precious to the patient. Systematic review of anticonvulsants [24] showed similar benefit and risk levels to antidepressants [25]. There is little evidence on which to recommend one anticonvulsant rather than another. The oral (and intravenous) use of the local anaesthetics is based on good animal studies, but again we do not have adequate RCT evidence to recommend their use in man [26]. The use of steroids remains an enigma. In postoperative pain the analgesic effect of steroids has been shown. Widespread use of steroids in palliative care to control pains resistant to other therapy has not been subjected to the customary trials in non-cancer pain, because of concern about adverse effects. The use of steroids is therefore based on experience. The most recent development is the idea that ketamine, as a clinically available antagonist at the N-methyl-D-aspartate receptor complex, may be useful in this type of pain. Three recent studies support this idea, and we hope that full-scale RCTs will show whether or not this is a useful ploy [27, 28, 29].

The place of opioids in the treatment of this qualitatively different pain remains problematic. Doses of oral opioid adequate to control the incident pain may be excessive when the incident pain stops. This begs the question as to whether opioids can control this type of pain. The evidence suggests that, for some patients at least, they can [13], and that all patients should have an adequate trial of opioids. The problem remains that adverse effects may be overwhelming in the absence of the incident pain. If opioids could be given rapidly in response to the presence of the incident pain, were effective, and did not remain active when the incident pain had gone, then they would be appropriate.

Giving opioids as rapid 'boosters' in this context requires the use of routes of administration other than oral, because speed of onset of effect is too slow orally. Subcutaneous, intramuscular and intravenous routes can all provide faster speed of onset of effect than oral opioids, but with an inevitable increase in the logistic complexity. Bolus, infusion or patient-controlled analgesia (PCA) techniques are all possible [30], but being possible as alternatives to the oral route for cancer pain management in general does not necessarily mean more effective or more appropriate for incident pain. With new opioids such as remifentanil [31] which have a faster offset of effect than those available currently, it should be possible to test whether or not fast onset/fast offset opioids by injectable routes can improve incident pain management.


The Future

It is striking that there is so little data from controlled trials to guide our practice when the two incidence studies emphasise the importance of incident pain. Some thoughts for these studies are that the pain must be characterised well. Pain assessments need to be made at maximal pain, if predictable, and / or with the movement(s) which provoke maximal pain. We would suggest that the number of painful episodes should also be an outcome measure, with an indication of the severity of the episodes. A measure of typical pain intensity and typical pain relief [32] may be particularly valuable if the pain is unpredictable. Just as important are the design requirements of the studies [33]. Given that it is very difficult for any of us to do studies on substantial numbers of patients in this group, it surely is time that we combined forces to produce valid answers to worthwhile questions. 


Red Herrings
Tolerance


Clinicians argue that tolerance to opioids, if it occurs, is driven by disease rather than by pharmacological tolerance. The first problem is that tolerance is used by some to mean any increase in dose, whereas others use it in the more technical sense of an increased dose required to produce the same effect.

It is ingenuous to argue that opioid tolerance does not occur in man - fleeting glimpses have been seen which echo the solid findings of both acute and chronic opioid tolerance in animal models [34]. The classic Houde experiments showed chronic tolerance when patients' analgesic response to a test dose was measured before and after chronic dosing [35, 36]. The pragmatic issues are whether the dose escalation required by some patients and producing difficult adverse effects could be avoided (safely) by blocking a tolerance-induced need for dose escalation, or (more simply) by changing opioid or indeed route of administration. 


Addiction

Clinical pain management has emphasised a difference between the clinical and the laboratory pharmacology of opiates. It is as though there is one opiate pharmacology when the opiate is used to counteract pain, and another when it is not.

The respiratory depression which haunts prescribers in acute pain management is seen readily in studies of volunteers who are not in pain. For patients with opiate-sensitive pain, given appropriate doses of opiate, respiratory depression is minimal [37, 38]. The balance between pain and opiate respiratory effects is seen clearly in chronic pain. Patients maintained on oral morphine, with no clinical respiratory depression, and who then receive successful nerve blocks, must have their morphine dose reduced. Failure to reduce the dose will result in respiratory depression [39, 40]. One explanation is that the respiratory centre receives nociceptive input [41]. Presence of this input counterbalances any respiratory depressant effect of the opiate. Absence of this input, because of the successful nerve block, leaves the respiratory depressant effect of the opiate unopposed.

The clinical message is that opiates need to be titrated against pain. Doses higher than necessary for the relief of pain run the risk of respiratory depression. Prophylactic use of opiates, infusion without regard to pain experienced, doses greater than those required for analgesia (as in deliberate ITU use to facilitate ventilation of a patient), use for purposes other than analgesia (e.g. sedation), or use in non-nociceptive pain, thus all carry potential risk. Concern about respiratory depression should not inhibit the appropriate use of opioids, and that is to provide analgesia when the pain may reasonably be thought to be opiate sensitive. A postoperative patient still complaining of pain when the previous dose can be assumed to have been absorbed needs more drug.

Similarly the drug-seeking behaviour synonymous with street addiction is not found in patients after pain relief with opiates, either in childbirth, or after operations or after myocardial infarction [42]. Street addicts are not in pain. The political message is that medical use of opiates does not create street addicts. Medical use may indirectly increase availability to those who are already addicts, but restricting medical use hurts patients. 


Adverse Effects
Specific adverse effects; metabolism


If an opiate has no specific advantage over morphine and has a specific disadvantage, such as a troublesome adverse effect not found with morphine, then there is little logic in choosing that drug in preference to morphine. Any drug which produced fewer side-effects than morphine, at a dose which provided the same degree of analgesia, would be an improvement. High dose fentanyl in cardiac anaesthesia causes less haemodynamic disruption than high dose morphine. For most clinically important side-effects there is no comparative evidence at equivalent analgesic doses to recommend any of the alternatives. Single-dose postoperative studies showed a higher incidence of nausea and vomiting with pethidine [43], and dysphoria (see below) with those mixed agonist-antagonists which have a relatively high affinity for kappa and sigma receptors [44]. As with non-steroidal anti-inflammatory drugs, the risk:benefit ratio may be different at equianalgesic dosing within the same patient [45], but we cannot predict these individual responses.


DYSPHORIA

Dysphoria occurs with all opiates, but the incidence varies widely between drugs. Pentazocine, butorphanol and nalbuphine have this potential [46]. The greater than 20% incidence with pentazocine and butorphanol contrasts sharply with the 3% incidence seen with other opiates. There is little sense in using an opiate which produces a higher incidence of dysphoria than morphine without any compensating advantage. 


TOXIC METABOLITES

Pethidine is metabolised to norpethidine which is toxic [47]. It causes tremor, twitching, agitation and convulsions, and the incidence of these problems increases with multiple dosing and in the presence of impaired renal function [47, 48]. Morphine-3-glucuronide (M3G) may be a toxic metabolite. When this becomes problematic is still unclear. 


ACTIVE METABOLITE

Whereas diamorphine [49] and M3G [50] do not bind to opiate receptors, 6-monoacetylmorphine, morphine, morphine-6-glucuronide (M6G) and normorphine do. Recent work on the metabolites of morphine has important clinical implications [51, 52]. Quantitatively the most important active metabolite is M6G, because M3G and M6G are the major metabolites of morphine in man [53, 54] and because of the greater potency of M6G compared with morphine. In rats, M6G is 45 times more potent than morphine intracerebrally and nearly 4 times more potent subcutaneously [55]; intrathecal injection gave potency ratios been 10 and 20 [56]. M6G may contribute substantially to the analgesic effect of morphine, in both single and repeated doses [57, 58, 59].
 

Diamorphine is a classical pro-drug. Without analgesic activity itself, it initiates the "cascade" into the active 6-monoacetylmorphine, morphine and M6G. Because of the speed of these reactions, there is no clinical advantage over morphine by oral or intramuscular routes, either in terms of greater analgesic efficacy or of improved mood [60, 49]. This does not exclude advantage from intravenous, spinal or other routes. 

PATHOPHYSIOLOGY

Unexpected degree and duration of effect can be obtained with morphine, codeine and dihydrocodeine when they are used in patients with severely impaired renal function [61]. Cumulation of M6G is the probable explanation of this phenomenon. Prolonged respiratory depression has been reported in man in association with negligible plasma concentrations of morphine but with very high concentrations of M3G and M6G [62]. Glucuronidation of morphine is altered little in hepatic failure [63], but in pre-coma kinetics [64] and dynamics [65] are altered.

Problems should arise only if a fixed-dose schedule is used without taking account of renal function, or without adequate titration against pain intensity. Drug doses should be decreased markedly if creatinine clearance is less than 30 ml min-1. With less severe renal dysfunction the potential problem emphasises the need for careful titration, remembering that renal function deteriorates with advancing age.


NAUSEA AND VOMITING AND CONSTIPATION

It has been very difficult to obtain data on adverse effect incidence from randomised studies. The recent paper by Moulin et al [66] showed that a third of the forty patients experienced adverse effects under this heading.
Prescribing Opioids in Chronic Non-cancer Pain

The argument that patients in pain who do not have cancer should not be given opioids is of great concern. If opioids provide pain relief for a patient, and there is no other effective remedy, who is to decide that the patient should be denied pain relief and for what reason? Obviously not all patients with non-cancer pain should be treated with opioids. There are, however, of a small number of patients in whom opioids are the only effective remedy. It is the right of these patients to obtain effective relief, and of their doctors to prescribe such relief for them, which should be upheld.

The reasons given commonly for withholding opioids in non-cancer pain include concern for the patient and concern for the community. The concern for the patient is that opioids may make the patient a drug addict and that opioids may have other adverse effects on the patient's health. The concern for the community is that opioid prescription to this patient group will perforce lead to an increase in street addiction. There is no evidence that patients with chronic non-cancer pain treated with opioids become addicts or that their health is impaired. There is no evidence that such medical availability has any impact on street addiction. Indeed there is evidence to the contrary. When oral opioids began to be used in Sweden to control cancer pain, this increasing medical availability had no impact at all on street addiction [67].

A recent review of the evidence for the treatment of cancer pain [68] is equally valid for opioid prescribing in other pain contexts. The 45 authors, 12 pharmacologists, 10 physicians, 8 pain clinic doctors, 7 psychologists, 3 lawyers, 3 experts from drug addiction and 2 experts in biomedical ethics, could find no medical, psychological, legal or ethical reason to withhold opioids in cancer pain. What then is the difference in pain not due to cancer? The obvious difference is in potential duration of treatment. The longitudinal surveys published to date suggest no difference between the two populations of patients.

The proportion of patients with chronic non-cancer pain for whom opioids might be considered is small, because not all of these patients obtain relief from opioids, some patients are psychologically unsuitable, some patients do not want to take opioids and other doctors involved in the patients' care may oppose opioid use. For those in whom we are considering opioid treatment we use the following guide-lines:

1. all other relevant treatments have failed

2. the pain is shown to be relieved by opioids

3. the patient, after clear explanation and discussion with family and family practitioner, is willing to take opioids

4. other doctors involved in the patient's care agree with opioid prescription

5. appropriate follow-up

Those who oppose opioid prescription should make their motives clear. There is no evidence to support the reasons which they advance. In the absence of such evidence we hope that the rights of that small number of patients for whom opioids are the only effective remedy to obtain relief, and the right of the doctor to prescribe, will be protected.

Clearly it is neither necessary nor desirable to subject patients with terminal disease who are obtaining effective relief from opioids to such a battery of tests. Problems do arise, however, in which this approach may help. The first is the general case when relief is ineffective and it is unclear to the clinician whether or not better relief can be achieved by a higher dose without intolerable or unmanageable adverse effects. This is equivalent to the question 'Can a poor or moderate response be converted to a good response by using a higher concentration?' The second is specific to the vexed question of opioid prescription in chronic non-cancer pain. Such prescribing is viewed as potentially dangerous for both the patient and society [69, 70], although published evidence suggests that neither belief is valid [68]. Opioids should be considered for patients for whom there is no other effective remedy, in whom opioids are effective, and given that both the patient and the patient's doctors agree [71].
 

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