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      Transdermal buprenorphine in the management of persistent pain – safety aspects

      Therapeutics and Clinical Risk Management

      Dove Medical Press

      opioids, chronic pain, buprenorphine, transdermal buprenorphine, safety

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          Abstract

          By virtue of their efficacy, opioid analgesics have long been used for the treatment of both acute and chronic pain. Concerns regarding their safety and tolerability have frequently prevented this class of drugs achieving their full therapeutic potential, and their reported association with drug abuse and dependence has led to a reduced acceptance by many patients. Indeed, there is a variety of opioid-like side effects which are common to all members of the class, but some opioids have a more favourable safety profile than others. Buprenorphine is a semisynthestic opioid with a μ-agonistic and κ-antagonistic receptor-binding profile. Studies over the past two decades have shown buprenorphine to have a complex and unique pharmacological profile, which results in enhanced therapeutic benefits combined with a favourable safety profile. Having been underused before, the development of a new transdermal drug delivery system for buprenorphine has revived interest in this substance. Transdermal buprenorphine (Gruenenthal GmbH, Aachen, Germany) provides a noninvasive method of rate-controlled drug release ensuring constant and predictable serum buprenorphine levels over a prolonged period. This preparation has been shown to be advantageous for long-term treatment of chronic pain patients providing reliable pain control, few adverse events, and good patient acceptance.

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          Most cited references 70

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          Validation of World Health Organization Guidelines for cancer pain relief: a 10-year prospective study.

          This paper reports on the experience gained using World Health Organization Guidelines for cancer pain relief over a 10-year period in an anaesthesiology-based pain service associated with a palliative care programme. The course of treatment of 2118 patients was assessed prospectively over a period of 140,478 treatment days. Non-opioid analgesics (WHO step I) were used on 11%, weak opioids (WHO step II) on 31% and strong opioids (WHO step III) on 49% of treatment days. Administration was via the enteral route on 82% and parenterally on 9% of treatment days. On the remaining days, either spinally applied opioids (2%) or other treatments (6%) were utilised. Fifty-six percent of the patients were treated with morphine. Morphine dose escalation was observed in about one-half of the patients being cared for until death, whereas the other half had stable or decreasing doses over the course of treatment. Co-analgesics were administered on 37% of days, most often antidepressants (15%), anticonvulsants (13%) and corticosteroids (13%). Adjuvants to treat symptoms other than pain were prescribed on 79% of days, most commonly laxatives (42%), histamine-2-receptor antagonists (39%) and antiemetics (35%). In addition, palliative antineoplastic treatment was performed in 42%, nerve blocks in 8%, physiotherapy in 5%, psychotherapy in 3% and TENS in 3% of patients. A highly significant pain reduction was achieved within the 1st week of treatment (P < 0.001). Over the whole treatment period, good pain relief was reported in 76%, satisfactory efficacy in 12% and inadequate efficacy in 12% of patients. In the final days of life, 84% rated their pain as moderate or less, while 10% were unable to give a rating. Analgesics remained constantly effective in all 3 steps of the WHO ladder. Other clinical symptoms were likewise significantly reduced at 1 week after initial assessment, with the exception of neuropsychiatric symptoms. During the course of treatment, the latter were the major symptoms on 23% of days, followed by nausea (23%), constipation (23%) and anorexia (20%). Our results emphasise once again the marked efficacy and low rate of complications associated with oral and parenteral analgesic therapy as the mainstay of pain treatment in the palliative care of patients with advanced cancer. Wide dissemination of WHO guidelines among doctors and healthcare workers is thus necessary to effect a clear improvement in the treatment of the many patients suffering from cancer pain in the clinical and home setting.
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            The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.

            Three different syndromes produced by congeners of morphine have been identified in the nondependent chronic spinal dog. These syndromes have been attributed to interaction of agonists with three distinguishable receptors (mu, kappa and sigma). Morphine is the prototype agonist for the mu receptor, ketocyclazocine for the kappa receptor and SKF-10,047 for the sigma receptor. The morphine syndrome (mu) in the dog is characterized by miosis, bradycardia, hypothermia, a general depression of the nociceptive responses and indifference to environmental stimuli. Ketocyclazocine (kappa) constricts pupils, depresses the flexor reflex and produces sedation but does not markedly alter pulse rate or the skin twitch reflex. SKF-10,047 (sigma), in contrast to morphine and ketocyclazocine, causes mydriasis, tachypnea, tachycardia and mania. The effects of these three drugs can be antagonized by the pure antagonist naltrexone, indicating that they are agonists. Further, chronic administration of morphine, ketocyclazocine and SKF-10,047 induces tolerance to their agonistic effects. Morphine suppresses abstinence in morphine-dependent dogs while ketocyclazocine does not. Ketocyclazocine at best precipitated only a liminal abstinence syndrome in the morphine-dependent dog, indicating that it had little affinity for the morphine receptor. Ketocyclazocine thus appears to be a selective agonist at the kappa receptor. Further, it has been shown that buprenorphine is a partial agonist of the mu type which both suppressed and precipitated abstinence in the morphine-dependent dog while morphine and propoxyphene are stronger agonists. Apomorphine and SKF-10,047 produce similar pharmacologic effects suggesting that sigma activity may involve a dopaminergic mechanism.
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              Clinical pharmacology of buprenorphine: ceiling effects at high doses.

              The purpose of this study was to characterize the acute effects of buprenorphine, an opioid partial mu-agonist, across a wide range of doses in comparison to methadone. Healthy adult male volunteers, who had experience with but were not physically dependent on opioids, participated while residing on a closed research unit. Four subjects received buprenorphine (0, 1, 2, 4, 8, 16, and 32 mg sublingually and five subjects received methadone (0, 15, 30, 45, and 60 mg orally) in ascending order at 1-week intervals. Physiologic, subjective, and behavioral measures were monitored for 96 hours after drug administration. Both drugs produced typical opioid agonist effects (positive mood, sedation, respiratory depression, and miosis), some of which persisted for 24 to 48 hours. A plateau was observed for the dose effects of buprenorphine on subjective measures and respiratory depression. Pharmacokinetic data revealed that plasma concentrations of buprenorphine were linearly related to dose, indicating no limits on sublingual absorption in this dose range. This study shows a plateau on buprenorphine effects, consistent with its partial agonist classification, and that single doses of buprenorphine up to 70 times the recommended analgesic dose are well tolerated by nondependent humans.
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                Author and article information

                Journal
                Ther Clin Risk Manag
                Therapeutics and Clinical Risk Management
                Therapeutics and Clinical Risk Management
                Dove Medical Press
                1176-6336
                1178-203X
                March 2006
                March 2006
                : 2
                : 1
                : 115-125
                Affiliations
                Pain Clinic, General Hospital Klagenfurt Klagenfurt, Austria
                Author notes
                Correspondence: Rudolf Likar General Hospital Klagenfurt, St. Veither Strasse 47, 9026 Klagenfurt, Austria Tel +43 463 5382 6120 Fax +43 463 5382 3070 Email r.likar@ 123456aon.at
                Article
                1661652
                18360586
                © 2006 Dove Medical Press Limited. All rights reserved
                Categories
                Review

                Medicine

                buprenorphine, chronic pain, safety, opioids, transdermal buprenorphine

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