Inefficacy of high‐dose transdermal fentanyl in a patient with neuropathic pain a case report

Bleeker, Chris P.; Bremer, Robbert C.; Dongelmans, Dave A.; Dongen, R.T.M. van; Crul, B.J.P.

doi:10.1053/eujp.2000.0220

Cited by 30 publications

(18 citation statements)

References 14 publications

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“…In clinic, neuropathic pain caused by peripheral nerve injury is often reported to be less sensitive to morphine (Arnér and Meyerson 1988;Kupers et al, 1991;Bleeker et al, 2001). Similar results were also observed with experimental animal models of neuropathic pain (Ossipov et al, 1995;IdanpaanHeikkila et al, 1997).…”

Section: Discussionsupporting

confidence: 74%

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Loss of Peripheral Morphine Analgesia Contributes to the Reduced Effectiveness of Systemic Morphine in Neuropathic Pain

Rashid

Inoue

Toda

et al. 2004

J Pharmacol Exp Ther

111

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It is well known that the analgesic potency of morphine is reduced in neuropathic pain. In this study, we demonstrate that the decreased effectiveness of systemic morphine in neuropathic pain might be caused by the loss of morphine analgesia at the periphery. When given s.c. or i.t., the dose-response curves for morphine analgesia in Hargreaves thermal test were shifted rightward in partial sciatic nerve-injured mice compared with control sham-operated mice. The dose-response curves for i.c.v. morphine analgesia, however, were unchanged in nerve-injured mice, indicating no decrease in morphine potency at the supraspinal level. On the other hand, the dosedependent analgesia produced by intraplantar (i.pl.) morphine in sham-operated mice almost completely disappeared in nerve-injured mice. With the more sensitive algogenic-induced nociceptive flexion test, significant reduction in the analgesic potency of systemic morphine was observed for bradykinin (BK) nociception in nerve-injured mice, and the analgesic effect of i.pl. morphine against BK nociception in sham-operated mice disappeared in nerve-injured mice. In immunohistochemical experiments, we found that, under normal state, -opioid receptors (MOPs) were mainly expressed in small-diameter unmyelinated dorsal root ganglion (DRG) neurons and colocalized with bradykinin B2 receptors. When we examined MOP expression in the DRG of nerve-injured mice, we observed a drastic decrease in MOP expression. Altogether, these data suggest that the lower potency of systemic morphine in neuropathic pain could be at least partly caused by the decreased MOP expression in DRG and subsequent loss of peripheral morphine analgesia in such a condition.

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Section: Discussionsupporting

confidence: 74%

“…However, they are reported to have suboptimal therapeutic efficacy against neuropathic pain (Arnér and Meyerson 1988;Kupers et al, 1991;Bleeker et al, 2001). Analgesic potency of both systemic and intrathecal morphine is greatly reduced in animal models of neuropathic pain (Ossipov et al, 1995;Idanpaan-Heikkila et al, 1997).…”

mentioning

confidence: 99%

Loss of Peripheral Morphine Analgesia Contributes to the Reduced Effectiveness of Systemic Morphine in Neuropathic Pain

Rashid

Inoue

Toda

et al. 2004

J Pharmacol Exp Ther

111

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“…Most of the available conventional and unconventional therapeutic approaches to treat neuropathic pain are subjected to various limitations. The opiates are reported to have suboptimal therapeutic efficacies in neuropathic pain (Ossipov et al, 1995;Bleeker et al, 2001). They are also well known to induce tolerance and dependence in addition to the other side effects such as gastrointestinal distress and respiratory depression.…”

Section: Discussionmentioning

confidence: 99%

“…Although the opioids have been used for centuries to cure many extremely painful conditions, there have been continuous debates over their efficacy in neuropathic pain (Ossipov et al, 1995;Bleeker et al, 2001). Moreover, the other unconventional therapeutic approaches such as use of certain antidepressants or anticonvulsants and use of topical capsaicin are associated with suboptimal efficacies and/or side effects (Bridges et al, 2001).…”

mentioning

confidence: 99%

Nonopioid and Neuropathy-Specific Analgesic Action of the Nootropic Drug Nefiracetam in Mice

Rashid¹,

Ueda²

2002

J Pharmacol Exp Ther

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Nootropic drug nefiracetam and related compounds are used in diseases with learning and memory deficits. Recent studies have implicated relationships between learning, memory, and chronic pain. Thus, in the present report, we have studied the effects of nootropic drug nefiracetam on the thermal and mechanical hyperalgesia induced by partial sciatic nerve ligation or streptozotocin treatment in mice. In the thermal paw withdrawal test, p.o., s.c., i.t., and i.c.v. administration of nefiracetam dose dependently reversed the thermal hyperalgesia observed in nerve-injured mice. Nefiracetam (p.o. and i.t.) also significantly reversed the thermal hyperalgesia observed in streptozotocin-induced diabetic mice. In the paw pressure test, p.o. and i.t. administration of nefiracetam dose dependently reversed the mechanical hyperalgesia observed in both nerveinjured and diabetic mice. In contrast, nefiracetam had no effect in sham-operated or control nondiabetic mice in all paradigms. Among other pyrrolidine nootropics (p.o.), aniracetam produced significant analgesic effects. Other analogs also had some, but not significant, analgesic effects. Finally, nefiracetam (p.o.)-induced analgesia in injured mice was not affected by opioid antagonist naloxone (s.c., i.t., and i.c.v.) but was dose dependently inhibited by nicotinic antagonist mecamylamine (i.t. and i.c.v.). The analgesic effect of i.t. nefiracetam was also blocked by i.t. mecamylamine pretreatment. Together, these findings suggest that nefiracetam, a new member of the piracetam group of cognition enhancers, could be a good therapeutic tool against neuropathic pain. We also demonstrate that nefiracetam-induced analgesic action was nonopioid in nature and was due to stimulation of nicotinic cholinergic system at spinal and supraspinal levels.

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“…Opioids are among the most effective analgesics for many types of pain (Rashid et al, 2004). However, opioids are reported to have suboptimal therapeutic efficacy against neuropathic pain (Bleeker et al, 2001;Cherny et al, 1994). There have been reports that chronic morphine treatment leading to 'morphine tolerance' may indeed induce the death of neurons (Hameed et al, 2010;Mao et al, 2002).…”

Section: Opioid Tolerance In Neuropathic Painmentioning

confidence: 99%

Neural - Glial Interaction in Neuropathic Pain

Manaheji¹

2012

Basic Principles of Peripheral Nerve Disorders

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Inefficacy of high‐dose transdermal fentanyl in a patient with neuropathic pain a case report

Cited by 30 publications

References 14 publications

Loss of Peripheral Morphine Analgesia Contributes to the Reduced Effectiveness of Systemic Morphine in Neuropathic Pain

Loss of Peripheral Morphine Analgesia Contributes to the Reduced Effectiveness of Systemic Morphine in Neuropathic Pain

Nonopioid and Neuropathy-Specific Analgesic Action of the Nootropic Drug Nefiracetam in Mice

Neural - Glial Interaction in Neuropathic Pain

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