1993
DOI: 10.1016/0140-6736(93)92228-l
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Methadone in pain uncontrolled by morphine

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Cited by 124 publications
(44 citation statements)
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“…Methadone's NMDA receptor antagonistic activity 17 in addition to the well known clinical phenomenon of incomplete cross-tolerance to the effects of various opioids may explain this marked improvement also observed by other authors when rotating to methadone from opioids other than fentanyl. 4,10,11 Our study confirms that methadone when used via intravenous PCA after appropriate conversion parameters is safe and can be drastically effective for the relief of pain refractory to fentanyl.…”
Section: Discussionsupporting
confidence: 64%
See 1 more Smart Citation
“…Methadone's NMDA receptor antagonistic activity 17 in addition to the well known clinical phenomenon of incomplete cross-tolerance to the effects of various opioids may explain this marked improvement also observed by other authors when rotating to methadone from opioids other than fentanyl. 4,10,11 Our study confirms that methadone when used via intravenous PCA after appropriate conversion parameters is safe and can be drastically effective for the relief of pain refractory to fentanyl.…”
Section: Discussionsupporting
confidence: 64%
“…6 Several reports have underscored the efficacy of methadone in the treatment of cancer pain, especially for pain refractory to high doses of other opioids. 4,[7][8][9][10] The main concern when using methadone for the treatment of pain is its long and unpredictable half-life and associated risk of delayed overdose, 11,12 unless careful and individualized dose titration is undertaken. Methadone is a synthetic opioid that differs from other opioids because of its long half-life, N-methyl-D-aspartate (NMDA) receptor antagonist activity, and lack of known active metabolites.…”
mentioning
confidence: 99%
“…Coadministration of morphine with MK-801, a noncompetitive NMDA receptor antagonist, has been shown to prevent morphine tolerance in several animal models. 10 Methadone, a potent NMDA antagonist, restores opioid responsiveness in patients whose pain ceases to be controlled by morphine or diamorphine. 11 Patients with persistent pain and adverse effects due to opioids (e.g., intravenous morphine and hydromorphone) have achieved excellent pain relief without significant adverse effects at doses of intravenous methadone much lower than those suggested by opioid conversion charts.…”
Section: Opioid Tolerancementioning
confidence: 99%
“…eine Reduktion unerwünschter Nebenwirkungen erzielt werden. Insbesondere Methadon scheint hier aufgrund der höheren Affinität zum µ-Rezeptor und der antagonistischen Wirkung am NMDARezeptor Vorteile aufzuweisen [15,94]. Nach der Umstellung auf ein anderes Opioid sollte mit 50% der errechneten Äquivalenzdosis begonnen und je nach Bedarf rasch hochtitriert werden, da die Äquivalenzdosen aufgrund der Aktivierung pronozizeptiver Systeme individuell stark variieren können [41].…”
Section: Opioidrotationunclassified