Sustained-Release Naltrexone For Opioid Dependence

Lobmaier, Philipp; Kornør, Hege; Kunøe, Nikolaj; Bjørndal, Arild

doi:10.1002/14651858.cd006140.pub2

Cited by 74 publications

(50 citation statements)

References 94 publications

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“…If true, this hypothesis indicates that DH␤E, by effectively blocking these small-dose effects, may be an effective antagonist of nicotine's reinforcing effects (Watkins et al, 1999) and might, in a long-acting form of a pharmacological equivalent, be able to be developed as a treatment for tobacco abuse. Currently, it is not known whether nicotinic antagonists, especially subtype-selective antagonists, would be useful smoking cessation treatments in humans, but future studies should investigate this possibility, considering that antagonists are useful pharmacotherapies for opioid addiction (Comer et al, 2002Sullivan et al, 2006; for review, see Lobmaier et al, 2008).…”

Section: Antagonism Of Nicotine 199mentioning

confidence: 99%

Patterns of Nicotinic Receptor Antagonism: Nicotine Discrimination Studies

Jutkiewicz¹,

Brooks²,

Kynaston³

et al. 2011

J Pharmacol Exp Ther

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Evaluation of the discriminative stimulus effects of drugs is a useful procedure for identification of receptor mediation of in vivo drug effects. This assay can be enhanced when the stimulus effects of different doses of agonist are evaluated. In the present study, rats were trained to discriminate small or large doses of nicotine from saline, and interactions of these effects with nicotinic receptor antagonists and partial agonists were determined. The insurmountable nicotine antagonist mecamylamine blocked both the discriminative stimulus and response rate-reducing effects of nicotine but was less effective against the large dose of nicotine. The ␣4␤2*-selective, competitive antagonist dihydro-␤-erythrodine (DH␤E) antagonized the discriminative stimulus effects of both doses but was less effective against the larger training dose of nicotine. Schild analyses of DH␤E suggested that different nicotinic receptor populations may be mediating the stimulus effects of large and small doses of nicotine. This suggestion was supported by observations that the discriminative stimulus effects of the partial agonist cytisine were more like those of the large dose than of the small dose of nicotine and that cytisine antagonized the effects of only the small nicotine dose. Varenicline produced nicotine-like effects in both training dose groups but reduced the discriminative stimulus effects of intermediate doses of nicotine in the group trained to the small dose of nicotine. Overall, these results suggest that small doses of nicotine produce their stimulus effects via ␣4␤2* nicotine receptors, whereas larger doses of nicotine recruit additional nicotine receptor subtypes, as revealed by drug discrimination assays in rats.

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Section: Antagonism Of Nicotine 199mentioning

confidence: 99%

Patterns of Nicotinic Receptor Antagonism: Nicotine Discrimination Studies

Jutkiewicz¹,

Brooks²,

Kynaston³

et al. 2011

J Pharmacol Exp Ther

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“…Slow release depot or implant formulations might secure protective levels of antagonist for extended periods [8][9]. No neuroadaptation occurs [10], and the baby would be born without NAS and without intrauterine opioid exposure.…”

mentioning

confidence: 99%

Is sustained release natrexone an option for heroin‐dependent pregnant women?

Waal

2013

Addiction

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“…At 6-months follow-up, more implant than oral patients had NTX levels above 2ng/ml (p<0.001); 17% vs 62% of patients reported regular heroin use; 63% vs 26% reported being abstinent (p<0.003), 49% and 21% respectively being confirmed by urinalysis. Patients on oral NTX started using heroin at an earlier stage (median [SE] 115 [12] vs 158 [9.4] days); NTX levels in implant patients were above 1 and 2ng/ml for 101 (95% CI 83-119) and 56 (39-73) days respectively for men and 124 (88-175) and 43 (16-79) days for women.…”

Section: Clinical Trials Of Ntx Implants and Dismentioning

confidence: 99%

“…In 2008, before any of the above RCTs appeared, Lobmaier et al published a Cochrane Review 12 . At that time, only one RCT of acceptable quality existed, a DI study comparing two active doses with a placebo injection.…”

Section: Systematic Reviewsmentioning

confidence: 99%

Últimos desarrollos en los implantes y las inyecciones depot de naltrexona; el jovencito de la escalera se está haciendo mayor

Brewer¹,

Streel²

2010

Adicciones

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Implants and depot injections (DI) of naltrexone (NTX) have undergone considerable development since the first commercially available implants appeared in the mid-1990s. In particular, long-acting implants that can deliver relapse-preventing serum NTX levels for around six months have now been subjected to classic randomised controlled trials that have given positive and generally significant results when compared with oral NTX and placebo implants, or with standard post-detoxification care. They also provide lower serum levels that can prevent opiate overdose for several additional months and 3-year mortality rates are similar to those of methadone maintenance treatment (MMT). At least 18 months of antagonist-assisted abstinence may be desirable to normalise new, opiatefree cognitive-behavioural habits and extinguish old, maladaptive ones. We discuss ideological antagonisms between protagonists of MMT and of NTX implants, notably in Australia, but we argue that both treatments can and should co-exist. The main obstacle to the expansion of longacting implant treatment is not the lack of an evidential or theoretical base but the lack of a licensed product. NTX appears to block all opiates if serum levels are adequate and we stress its apparent lack of clinically significant hepatotoxicity. Some patients may need above-average serum levels and occasionally, habitual injectors continue to inject opiates despite experiencing no opiate effects. RESUMEN ABSTRACTLos implantes y las inyecciones depot (ID) de naltrexona (NTX) han experimentado un notable desarrollo desde que aparecieron los primeros implantes comerciales a mediados de los noventa. Específicamente los implantes de larga duración, capaces de proporcionar NTX en suero con niveles capaces de prevenir las recaídas durante unos 6 meses, han sido sometidos recientemente a las clásicas pruebas con control, con resultados positivos y, generalmente, significativamente superiores a la NTX oral o implantes de placebo o tratamientos estándar post desintoxicación. Además proporcionan niveles en sangre suficientes durante varios meses más para prevenir sobredosis por opiáceos. Por otro lado los índices de mortalidad a tres años son similares a los que están en programas de mantenimiento con metadona (PMM). Por lo menos serán necesarios 18 meses de abstinencia con el apoyo de antagonistas para normalizar los nuevos hábitos de comportamiento sin opiáceos y extinguir los viejos hábitos perjudiciales. Se discuten los antagonismos ideológicos que se dan, sobre todo en Australia, entre los protagonistas de PMM y los de implantes de NTX, concluyendo que ambos tipos pueden y deben coexistir. El principal obstáculo para la expansión de los tratamientos con implantes de larga duración no sería pues la falta de evidencia o de base teórica, sino la inexistencia de un fármaco con licencia. NTX parece que bloquea todos los opiáceos si sus niveles en suero son los adecuados; por otro lado debemos tener en cuenta su aparente falta de hepatotoxicidad. Algunos pacientes pueden necesita...

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Sustained-Release Naltrexone For Opioid Dependence

Cited by 74 publications

References 94 publications

Patterns of Nicotinic Receptor Antagonism: Nicotine Discrimination Studies

Patterns of Nicotinic Receptor Antagonism: Nicotine Discrimination Studies

Is sustained release natrexone an option for heroin‐dependent pregnant women?

Últimos desarrollos en los implantes y las inyecciones depot de naltrexona; el jovencito de la escalera se está haciendo mayor

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