Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Avinza is a once-daily, extended-release oral morphine preparation. It has a pharmacokinetic profile that exhibits less peak-to-trough fluctuations in plasma concentration whilst providing analgesia statistically identical to that produced by MS Contin (controlled-release morphine sulfate), Oxycontin (oxycodone HCl controlled-release) and six doses of oral morphine sulfate administered every 4 h. Avinza improves quality of sleep by several measures but interestingly gives the best sleep improvement when given in the morning rather than at night. It causes the same side effects of other opioids: constipation, nausea, vomiting, somnolence and mood swings. Doses of 30 - 60 mg/day have been shown to be well tolerated by patients with osteoarthritis (even in the elderly), who have failed other medications.
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PMID:Avinza - 24-h sustained-release oral morphine therapy. 1499 42

The transdermal therapeutic system with fentanyl was released in Germany in 1995. Before and after the release several clinical trials were performed in our pain management unit and in other German pain centers, showing good efficacy after initial dose titration with intravenous patient-controlled analgesia or switching from pretreatment with oral morphine or other opioids. A sequential trial showed less use of laxatives with transdermal fentanyl compared to pretreatment with oral morphine. Safety and efficacy of the transdermal system in clinical practice were confirmed in a nationwide survey with 1005 patients, nearly all of them with cancer pain. Most patients had been treated with opioids, though 22% had received no opioids or only as required before initiation of transdermal fentanyl. The mean duration of transdermal treatment was 71 +/- 83 days. Pain relief with transdermal therapy was swift and efficient. Adverse events with the possibility of a causal relationship to transdermal therapy were documented for 26% of the patients, most frequently nausea, vomiting, constipation and drowsiness. Severe neurotoxic or respiratory complications were reported only rarely. Problems with transdermal application were reported by 12% of the patients, with patch detachment and dermatologic symptoms on the site of application being most frequent. Most patients showered regularly with the patches and only three patients reported that patches became loose under the shower or in the bathtub. In a recent prospective trial driving ability was tested in patients with continuous non-cancer pain, who had received stable doses of transdermal fentanyl. Data were available from 90 healthy volunteers matched to 30 patients, of whom 9 were excluded from the analysis because they took additional drugs in violation of the protocol. None of the performance measures for the 21 remaining fentanyl patients was significantly inferior to the controls. In conclusion, experience with the transdermal therapeutic system with fentanyl has been gathered in clinical trials, a large nationwide survey and clinical practice since the release in 1995. The conversion table based on a conversion ratio of 100 : 1 was safe and efficient in trials and clinical practice. Transdermal fentanyl has become a wellknown and frequently used opioid in the treatment of chronic cancer and non-cancer pain in Germany.
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PMID:Clinical experience with transdermal fentanyl for the treatment of cancer pain in Germany. 1509 25

Studies addressing pain management after pediatric spinal fusion surgery have focused on the use of patient-controlled or epidural analgesia during the immediate postoperative period. Controlled-release (CR) analgesics have been found to be safe and effective in adults. The purpose of this study was to describe the use of oxycodone-CR in pediatric patients after the immediate postoperative period. A retrospective chart review of 62 postoperative spinal fusion patients (10-19 years) was conducted. The mean initial oxycodone-CR dose was 1.24 mg/kg/day. The mean ratio of conversion from parenteral morphine equivalents to oxycodone-CR was 1:1. Mean pain scores decreased from 4.2/10 to 3.7/10 with the transition to oxycodone-CR. Common side effects included dizziness, constipation, and nausea. Oxycodone-CR was used for an average of 13.3 days, which included an average wean time of 6 days. Results of this study demonstrate safe and effective use of oxycodone-CR in the pediatric spinal fusion population.
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PMID:Controlled-release oxycodone for the management of pediatric postoperative pain. 1511 83

The gut is a neurological organ, which implies that many neuroactive drugs such as opioid analgesics can seriously disturb gastrointestinal function, because many of the transmitters and transmitter receptors present in the brain are also found in the enteric nervous system. One of the most common manifestations of opioid-induced bowel dysfunction is constipation which results from blockade of peristalsis and intestinal fluid secretion. The discovery of opioid receptor antagonists with a peripherally restricted site of action, such as N-methylnaltrexone and alvimopan, makes it possible to normalize bowel function in opiate-treated patients without compromising central opioid analgesia. There is emerging evidence that opioid receptor antagonists may also have prokinetic actions, reversing pathological states of gastrointestinal hypomotility that are due to overactivity of the enteric opioid system.
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PMID:Opioids and opioid receptors in the enteric nervous system: from a problem in opioid analgesia to a possible new prokinetic therapy in humans. 1513 26

Patients with moderate or severe pain following knee arthroplasty and washout from standard patient-controlled analgesia (PCA) were randomized to receive 20 mg of an extended-release (ER) oxymorphone formulation (n = 65) or placebo (n = 61) q12h for 1 day. Oxymorphone PCA was used as rescue analgesic. Oxymorphone ER provided significant improvements over placebo for most standard single-dose analgesic parameters, including mean total pain relief (TOTPAR) over 0 to 12 hours (19.30 vs. 13.72; p = 0.0056), as well as for all multiple-dose (24-h) efficacy assessments. Oxymorphone-treated patients used significantly less rescue PCA than those who received placebo (p < 0.02). Adverse events such as nausea and constipation were typical of opioids, and laboratory and physical findings were similar between groups. Oxymorphone ER was effective and generally well tolerated. A single dose was active from 2 hours until > or = 12 hours after administration. Comparisons with other oral opioids are warranted, especially in the setting of outpatient and day surgery.
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PMID:Efficacy of oxymorphone extended release in postsurgical pain: a randomized clinical trial in knee arthroplasty. 1519 81

The authors evaluated prospectively the efficacy and safety of continuous subcutaneous morphine administration for postoperative analgesia after posterior spinal fusion and instrumentation for idiopathic scoliosis. Thirty patients were given the subcutaneous morphine infusion (20 mg/day), and 20 patients were not given morphine (control group). Postoperative pain control was assessed using a verbal response score (VRS) and a visual analog pain scale (VAS). The number of times the patient requested supplemental analgesics was also evaluated. VRS and VAS measurements were significantly lower in the continuous subcutaneous morphine group compared with the control group. Also, analgesic consumption in the continuous subcutaneous morphine group was lower than that of the control group. There was no respiratory depression or constipation. Preemptive analgesia using continuous subcutaneous infusion of morphine is a simple, safe, and effective method to control postoperative pain after posterior instrumentation and spinal fusion for idiopathic scoliosis.
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PMID:Effects of preemptive analgesia using continuous subcutaneous morphine for postoperative pain in scoliosis surgery: a randomized study. 1530 11

Opioids are associated with a number of adverse effects, constipation being the most common long-term adverse effect in patients with advanced cancer. Significant progress has been made over the past several decades in understanding the mechanisms of action of opioid compounds; however, these advances have yielded few new treatments for the bowel dysfunction caused by opioids. Methylnaltrexone, the first peripheral opioid receptor antagonist and currently under clinical investigation, has the potential to prevent or treat opioid-induced peripherally mediated side effects, such as constipation, without interfering with analgesia. This article reviews existing clinical data on methylnaltrexone, focusing on the antagonism of opioid-induced adverse effects in the gut.
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PMID:Clinical status of methylnaltrexone, a new agent to prevent and manage opioid-induced side effects. 1532 15

Morphine is a potent analgesic, yet, like most opioid narcotics, it exerts unwanted side effects such as constipation and respiratory suppression, thereby limiting its clinical utility. Pharmacological approaches taken to preserve the analgesic properties, while eliminating the unwanted side effects, have met with very limited success. Here, we provide evidence that altering mu opioid receptor regulation may provide a novel approach to discriminate morphine's beneficial and deleterious effects in vivo. We have previously reported that mice lacking the G protein-coupled receptor regulatory protein, beta-arrestin 2, display profoundly altered morphine responses. beta-Arrestin 2 knockout mice have enhanced and prolonged morphine analgesia with very little morphine tolerance. In this report, we examine whether the side effects of morphine treatment are also augmented in this animal model. Surprisingly, the genetic disruption of opioid receptor regulation, while enhancing and prolonging analgesia, dramatically attenuates the respiratory suppression and acute constipation caused by morphine.
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PMID:Morphine side effects in beta-arrestin 2 knockout mice. 1591

The transdermal matrix patch formulation of buprenorphine has been shown to be effective in managing moderate-to-severe cancer pain and severe pain unresponsive to nonopioid analgesics. Clinical trials have revealed that it is possible to switch from weak opioids or low doses of step III opioids to transdermal buprenorphine without any problems. With buprenorphine patches, the sublingual buprenorphine intake was dose-dependently reduced and was superior to placebo in this respect. The proportion of responders increased with the buprenorphine dose, and a higher proportion of patients receiving buprenorphine patches reported uninterrupted sleep for longer than 6 h compared with those receiving placebo. In a long-term, open, follow-up study in which the mean duration of treatment was 7.5 months, analgesia was rated as at least satisfactory by 90% of patients. Almost 60% of patients could manage their pain with one patch alone or with one additional sublingual tablet a day during the whole period of treatment, indicating a low incidence of tolerance development. The buprenorphine transdermal patch was assessed as user friendly by 94.6% of patients. In a postmarketing surveillance study, pain relief with transdermal buprenorphine was rated as good or very good by 70% of the responders. Postmarketing surveillance studies have shown that transdermal buprenorphine is also effective in the management of nociceptive and neuropathic pain, which some studies have shown to be relatively insensitive to mu-opioid analgesics, such as morphine. Transdermal buprenorphine was well tolerated. Most adverse events were either local reactions to the patch that generally subsided within 24 h or systemic events typical of treatment with opioid analgesics, such as nausea, vomiting and constipation.
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PMID:Transdermal buprenorphine in the treatment of chronic pain. 1593 64

Contemporary standard pharmacological care for the treatment of noncancer pain includes the use of opioid medications. The responsiveness of neuropathic pain to opioids has long been an area of controversy. Evidence from multiple randomized controlled trials indicates that opioids can relieve pain in a variety of neuropathic pain syndromes. Opioids are typically reserved for moderate to severe pain that cannot be relieved by the nonsteroidal anti-inflammatory drugs (NSAIDs). Opioids are often used in combination with other adjuvants or other analgesic agents. The advantage of opioids is the lack of a ceiling effect of the pure mu opioid agonists. The disadvantages of these drugs are a series of mechanism-based opioids-related side effects (e.g., nausea, drowsiness, constipation) and the potential issue of their abuse and misuse. Each patient needs to undergo a comprehensive evaluation and receive education on the treatment. The physician must be well conversant with the differential diagnosis and definitions of physical dependence, tolerance, pseudotolerance, aberrant behaviors, addiction, and pseudoaddiction. No specific opioid drug is intrinsically ''better'' than the others. Opioid rotation refers to the switch from one opioid to another when the degree of analgesia obtained is limited by the persistence of adverse effects or the occurrence of clinically relevant tolerance. This approach is based on the observation that a patient's response varies from opioid to opioid. At present, after 1) appropriate selection of patients and 2) longitudinal patient care with routine assessment of degree of analgesia, functional daily activities, adverse events and aberrant behaviors is carried out, opioid therapy can be the safest and most effective treatment measure for quality of life improvement in the chronic pain patient.
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PMID:Opioid therapy for chronic noncancer pain: practice guidelines for initiation and maintenance of therapy. 1601 15


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