Naltrexone and problems in pain management

Vickers, Andrew; Jolly, Ann

doi:10.1136/bmj.332.7534.132

Cited by 35 publications

(18 citation statements)

References 4 publications

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“…The most effective and commonly used drugs to relieve acute pain are opioids, which act at the same receptors that naltrexone blocks. Despite over two decades of clinical experience managing acute pain states in the presence of oral naltrexone, there are only a limited number of published clinical studies regarding the feasibility of overriding naltrexone-induced opioid receptor blockade with high doses of opioid analgesics for pain management (43)(44)(45). Adverse effects of opioids are multiple in number, are usually receptor mediated, difficult to separate from the desired analgesic effect and progressively increase as the opioid dose increases (46,47).…”

Section: Suppression Of Morphine Antinociception By Xr-ntx: Extent Ofmentioning

confidence: 98%

Nonclinical Pharmacology of VIVITROL®: A Monthly Injectable Naltrexone for the Treatment of Alcohol Dependence

Dean

2009

Opiate Receptors and Antagonists

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Oral naltrexone is a nonselective opioid antagonist. It is approved for the pharmacological treatment of alcohol and opioid dependence, but the efficacy of oral naltrexone is limited by poor patient compliance. To address this limitation, numerous attempts have been made by many groups to develop an injectable extendedrelease formulation of naltrexone including. At Alkermes, different formulations of naltrexone, encapsulated into biodegradable polymer microspheres [e.g., Alkermes' Medisorb® extended-release naltrexone (XR-NTX); VIVITROL®], were tested using in vitro assays and in vivo models to select a lead formulation. Pharmacokinetic studies in rats confirmed that the principle formulation produced stable, pharmacologically relevant plasma levels of naltrexone for ~1 month following a single injection. The pharmacodynamic effects (antagonism of morphine antinociception) of XR-NTX corresponded well with the pharmacokinetic profile from the same animals. While brain mu-opioid receptor density was found to increase over time in these rats, it did not appear to affect the ability of naltrexone to suppress morphine antinociception. Additional results in rats suggested that it may be feasible to manage acute pain in XR-NTX-treated patients by titrating typical opioid analgesics upwards to patient comfort under medical observation without causing further sedation or additional respiratory depression. Finally, the pharmacokinetic profile of XR-NTX in monkeys confirmed the long duration of elevated plasma concentrations of naltrexone. Both naltrexone and the poly(d,Llactide-co-glycolide) (PLG) polymer matrix in which it is encapsulated are welltolerated. VIVITROL was approved by the Food and Drug Administration (FDA) in 2006 for once-monthly administration for the pharmacological treatment of alcohol dependence.

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Section: Suppression Of Morphine Antinociception By Xr-ntx: Extent Ofmentioning

confidence: 98%

Nonclinical Pharmacology of VIVITROL®: A Monthly Injectable Naltrexone for the Treatment of Alcohol Dependence

Dean

2009

Opiate Receptors and Antagonists

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“…Naltrexone will render even large doses of opioids ineffectual. 12 It is important that its use is recognized before elective procedures so that pain management can be planned. In the emergency situation, altern ative methods of analgesia will be necessary.…”

Section: Managing Severe Pain In the Recovery Wardmentioning

confidence: 99%

Control of acute pain in postoperative and post-traumatic situations and the role of the acute pain service

Vickers

2008

Anaesthesia & Intensive Care Medicine

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“…There is experimental evidence of µ-opioid receptor upregulation following antagonist withdrawal (Millan et al, 1988) and abrupt discontinuation of naltrexone may therefore lead to a period of increased opioid sensitivity (Vickers & Jolly, 2006). As the effect of naltrexone diminishes after it has been ceased, the amount of opioid required to maintain analgesia may also need to be decreased in order to avoid signs of excessive opioid dose (in particular, respiratory depression).…”

Section: Chapter 11mentioning

confidence: 99%

“…It has been recommended that, where possible, naltrexone be stopped for at least 24 hours before surgery (Mitra & Sinatra, 2004;Vickers & Jolly, 2006). In these patients and in patients requiring surgery within this 24-hour period, multimodal analgesic regimens (eg NSAIDs, paracetamol, ketamine, tramadol and regional analgesia) should also be employed.…”

Section: Naltrexonementioning

confidence: 99%

“…The usual oral maintenance dose is up to 25 to 50 mg daily; long acting implantable pellets are also available in some countries Vickers & Jolly, 2006). Orally administered, naltrexone has an apparent half-life of about 14 hours and binds to opioid receptors for over 24 hours following a single dose (Vickers & Jolly, 2006), which can create difficulties in the acute pain setting.…”

Section: Naltrexonementioning

confidence: 99%

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Safety of opioid patch initiation in Australian residential aged care

Gadzhanova

Roughead

Pont

2015

Medical Journal of Australia

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Objective: To explore opioid use by aged care facility residents before and after initiation of transdermal opioid patches. Design: A cross‐sectional cohort study, analysing pharmacy data on individual patient supply between 1 July 2008 and 30 September 2013. Setting: Sixty residential aged care facilities in New South Wales. Participants: Residents receiving an initial opioid patch during the study period. Main outcome measure: The proportion of residents who were opioid‐naive in the 4 weeks prior to patch initiation was determined. In addition, the patch strength at initiation and the daily dose of transdermal patches and of additional opioids 1 month after initiation were determined. Results: An opioid patch was initiated in 596 of 5297 residents (11.3%: 2.6% fentanyl, 8.7% buprenorphine) in the 60 residential aged care facilities. The mean age at initiation was 87 years, and 74% of the recipients were women. The proportion of recipients who were opioid‐naive before patch initiation was 34% for fentanyl and 49% for buprenorphine. Most were initiated at the lowest available patch strength, and the dose was up‐titrated after initiation. Around 15% of fentanyl users and 10% of buprenorphine users needed additional regular opioids after patch initiation. Conclusions: The results suggest some inappropriate initiation of opioid patches in Australian residential aged care facilities. Contrary to best practice, a third of residents initiated on fentanyl patches were opioid‐naive in the 4 weeks before initiation.

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Naltrexone and problems in pain management

Abstract: How to manage acute pain in people taking an opioid antagonist

Cited by 35 publications

References 4 publications

Nonclinical Pharmacology of VIVITROL®: A Monthly Injectable Naltrexone for the Treatment of Alcohol Dependence

Nonclinical Pharmacology of VIVITROL®: A Monthly Injectable Naltrexone for the Treatment of Alcohol Dependence

Control of acute pain in postoperative and post-traumatic situations and the role of the acute pain service

Safety of opioid patch initiation in Australian residential aged care

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