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Melissa Yéléhé-Okouma, Hervé Martini, Jérémie Lemarié, Pierre Labroca, Nadine Petitpain, Valérie Gibaja, François Paille, Pierre Gillet
Opioid antagonists such as naltrexone and nalmefene are used in drug therapy for alcoholism. Nalmefene, approved in Europe in February 2013 for the reduction of alcohol consumption is used in patients with alcohol dependence. We report 11 cases of opioid withdrawal syndrome after a single dose of nalmefene in patients usually treated with methadone, buprenorphine, but also with fentanyl or loperamide. Nalmefene is both a partial agonist and an antagonist of opioid receptors. Regarding to its opioid antagonist activity, nalmefene is contraindicated in patients with an opioid treatment...
March 21, 2017: Fundamental & Clinical Pharmacology
Darren R Quelch, Inge Mick, John McGonigle, Anna C Ramos, Remy S A Flechais, Mark Bolstridge, Eugenii Rabiner, Matthew B Wall, Rexford D Newbould, Björn Steiniger-Brach, Franz van den Berg, Malcolm Boyce, Dorrit Østergaard Nilausen, Lasse Breuning Sluth, Didier Meulien, Christoph von der Goltz, David Nutt, Anne Lingford-Hughes
BACKGROUND: Nalmefene is a µ- and δ-opioid receptor antagonist, κ-opioid receptor partial agonist that has recently been approved in Europe for treating alcohol dependence. It offers a treatment approach for alcohol-dependent individuals with "high-risk drinking levels" to reduce their alcohol consumption. However, the neurobiological mechanism underpinning its effects on alcohol consumption remains to be determined. Using a randomized, double-blind, placebo-controlled, within-subject crossover design we aimed to determine the effect of a single dose of nalmefene on striatal blood oxygen level-dependent (BOLD) signal change during anticipation of monetary reward using the monetary incentive delay task following alcohol challenge...
January 10, 2017: Biological Psychiatry
Benjamin Rolland, Mickaël Naassila
The concept of binge drinking (BD) refers to patterns of heavy episodic alcohol consumption, with BD primarily occurring among adolescents and young adults. Several official definitions of BD have been proposed, in particular by the World Health Organization, the National Institute on Alcoholism and Alcohol Abuse, and the Substance Abuse and Mental Health Services Administration. Nevertheless, none of these definitions address the psychosocial and medical consequences of the type of alcohol use seen in BD. In practice, BD can thus correspond to either hazardous or harmful use of alcohol (HUA), while the episodic nature of heavy drinking in BD means that it does not meet the criteria for 'alcohol dependence'...
February 15, 2017: CNS Drugs
Ana Martín-Blanco, Barbara Patrizi, Joaquim Soler, Xero Gasol, Matilde Elices, Miquel Gasol, Cristina Carmona, Juan C Pascual
Comorbidity between borderline personality disorder (BPD) and alcohol use disorder (AUD) is high and relevant as alcohol consumption seems to worsen BPD symptomatology. One of the newest treatments for AUD, nalmefene, may be useful to improve BPD symptoms not only indirectly by reducing alcohol consumption but also directly by acting on the opioid system as this system has been related to specific BPD symptoms. This open-label study aimed at evaluating the efficacy of an 8-week nalmefene treatment in reducing alcohol consumption in individuals with BPD and comorbid AUD...
February 8, 2017: International Clinical Psychopharmacology
Katie Witkiewitz, Kevin A Hallgren, Henry R Kranzler, Karl F Mann, Deborah S Hasin, Daniel E Falk, Raye Z Litten, Stephanie S O'Malley, Raymond F Anton
BACKGROUND: Alcohol use disorder (AUD) is a highly prevalent public health problem associated with considerable individual and societal costs. Abstinence from alcohol is the most widely accepted target of treatment for AUD, but it severely limits treatment options and could deter individuals who prefer to reduce their drinking from seeking treatment. Clinical validation of reduced alcohol consumption as the primary outcome of alcohol clinical trials is critical for expanding treatment options...
January 2017: Alcoholism, Clinical and Experimental Research
Karl Mann, Lars Torup, Per Sørensen, Antoni Gual, Robert Swift, Brendan Walker, Wim van den Brink
Nalmefene, a mu- and delta-opioid receptor (MOR, DOR) antagonist and a partial kappa-opioid receptor (KOR) agonist, is approved in the European Union and other countries for the reduction of alcohol consumption in alcohol dependent patients with a high drinking risk level according to WHO ("target population"). This review presents an overview of nalmefene׳s pharmacology, its mechanisms of action and a meta-analysis on its efficacy in reducing alcohol consumption. The review was based on a systematic search of the literature...
December 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
(no author information available yet)
No abstract text is available yet for this article.
September 2016: Drug and Therapeutics Bulletin
Florian Naudet, Clément Palpacuer, Rémy Boussageon, Bruno Laviolle
Nalmefene was the first treatment approved by the European Medicines Agency for reducing alcohol consumption in adult patients with alcohol dependence. It is often presented as a paradigm shift in therapeutics, but major issues limit the interpretation of the evidence supporting its use. The randomised trials submitted provided no evidence of harm reduction, the differences on consumption outcomes were of questionable clinical relevance, the target population was defined a posteriori and the drug was compared to a placebo although naltrexone was already used off-label...
August 18, 2016: BMC Medicine
Jamie H Rose, Anushree N Karkhanis, Björn Steiniger-Brach, Sara R Jones
The development of pharmacotherapeutics that reduce relapse to alcohol drinking in patients with alcohol dependence is of considerable research interest. Preclinical data support a role for nucleus accumbens (NAc) κ opioid receptors (KOR) in chronic intermittent ethanol (CIE) exposure-induced increases in ethanol intake. Nalmefene, a high-affinity KOR partial agonist, reduces drinking in at-risk patients and relapse drinking in rodents, potentially due to its effects on NAc KORs. However, the effects of nalmefene on accumbal dopamine transmission and KOR function are poorly understood...
July 27, 2016: International Journal of Molecular Sciences
Philippe Laramée, Aurélie Millier, Thor-Henrik Brodtkorb, Nora Rahhali, Olivier Cristeau, Samuel Aballéa, Stephen Montgomery, Sara Steeves, Mondher Toumi, Jürgen Rehm
BACKGROUND AND OBJECTIVE: When modelling the pathophysiology of a disease, it is important to select a modelling approach that can adequately replicate its course. The objective of this paper was to compare the outcomes obtained by the Markov and discrete-time microsimulation modelling approaches using nalmefene clinical trial data. METHODS: Markov and microsimulation modelling approaches assessing alcohol dependence treatment with psychosocial support with or without nalmefene were compared in terms of the modelled evolution of patients' alcohol consumption and the resulting occurrence of alcohol-attributable harmful events over 1 year...
November 2016: Clinical Drug Investigation
Jørgen G Bramness, Karl Mann, Friedrich M Wurst
BACKGROUND: Acamprosate, disulfiram (DIS), naltrexone and nalmefene can be used in treating alcohol use disorders. The drugs are, however, underutilized. METHODS: In this survey of marketing status and perceived efficacy, member societies of the European federation for addiction societies were asked to report on the status of these drugs in their country. Results were obtained from 20 European countries showing that the drugs were registered in most countries. RESULTS AND CONCLUSION: The drugs were mentioned in guidelines in approximately half and were partially or fully reimbursed in half to two-thirds countries...
2016: European Addiction Research
M Soyka, M Friede, J Schnitker
No abstract text is available yet for this article.
November 2016: Pharmacopsychiatry
F Naudet
No abstract text is available yet for this article.
November 2016: Pharmacopsychiatry
Philippe Laramée, Aurélie Millier, Nora Rahhali, Olivier Cristeau, Samuel Aballéa, Clément François, Ylana Chalem, Mondher Toumi, Jürgen Rehm
BACKGROUND: Alcohol dependence causes considerable harm to patients. Treatment with nalmefene, aiming to reduce consumption rather than maintain complete abstinence, has been licensed based on trials demonstrating a reduction in total alcohol consumption and heavy drinking days. Relating these trial outcomes to harmful events avoided is important to demonstrate the clinical relevance of nalmefene treatment. METHODS: A predictive microsimulation model was developed to compare nalmefene plus brief psychosocial intervention (BRENDA) versus placebo plus BRENDA for the treatment of patients with alcohol dependence and a high or very high drinking risk level based on three pooled clinical trials...
August 2016: Applied Health Economics and Health Policy
Niamh Fitzgerald, Kathryn Angus, Andrew Elders, Marisa de Andrade, Duncan Raistrick, Nick Heather, Jim McCambridge
BACKGROUND AND AIMS: Nalmefene has been approved in Europe for the treatment of alcohol dependence and subsequently recommended by the UK National Institute for Health and Care Excellence (NICE). This study examines critically the evidence base underpinning both decisions and the issues arising. METHODS: Published studies of nalmefene were identified through a systematic search, with documents from the European Medicines Agency, the NICE appraisal and public clinical trial registries also examined to identify methodological issues...
August 2016: Addiction
Florian Naudet, Bernard Granger, Alain Braillon
No abstract text is available yet for this article.
September 2016: Alcohol and Alcoholism: International Journal of the Medical Council on Alcoholism
Javier Calleja-Conde, Victor Echeverry-Alzate, Elena Giné, Kora-Mareen Bühler, Roser Nadal, Rafael Maldonado, Fernando Rodríguez de Fonseca, Antoni Gual, Jose Antonio López-Moreno
BACKGROUND AND PURPOSE: The opioid antagonist nalmefene (selincro®) was approved for alcohol-related disorders by the European Medicines Agency in 2013. However, there have been no studies regarding the effectiveness of nalmefene when alcohol is used in combination with cocaine. EXPERIMENTAL APPROACH: Using operant alcohol self-administration in Wistar rats and qRT-PCR, we evaluated (i) the dose-response curve for s.c. and p.o. nalmefene; (ii) the effects of nalmefene with increasing concentrations of alcohol; (iii) the efficacy of nalmefene on cocaine-potentiated alcohol responding; and (iv) the gene expression profiles of histone deacetylases (Hdac1-11) in peripheral blood in vivo and in the prefrontal cortex, heart, liver and kidney post mortem...
August 2016: British Journal of Pharmacology
Tim Gaekens, Michel Guillaume, Herman Borghys, Loeckie L De Zwart, Ronald de Vries, Roger C A Embrechts, An Vermeulen, Anton A H P Megens, Josée E Leysen, Piet Herdewijn, Pieter P Annaert, John R Atack
Nalmefene is an opioid antagonist which as a once-a-day tablet formulation has recently been approved for reducing ethanol intake in alcoholic subjects. In order to address the compliance issue in this patient population, a number of potential nalmefene prodrugs were synthesized with the aim of providing a formulation that could provide plasma drug concentrations in the region of 0.5-1.0ng/mL for a one-month period when dosed intramuscular to dogs or minipigs. In an initial series of studies, three different lipophilic nalmefene derivatives were evaluated: the palmitate (C16), the octadecyl glutarate diester (C18-C5) and the decyl carbamate (CB10)...
June 28, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
Julia M A Sinclair, Sophia E Chambers, Celia J Shiles, David S Baldwin
Alcohol use disorders (AUD) cause significant morbidity and mortality worldwide, but pharmacological treatments for them are underused, despite evidence of efficacy. Acamprosate, naltrexone, nalmefene and disulfiram are all approved in one or more region for the treatment of AUD. Baclofen currently has a temporary indication in France. Safety considerations for using psychopharmacological treatments in this patient group include the impact of concurrent alcohol consumption at high levels; multiple physical comorbidities that may interfere with pharmacological effects, distribution and metabolism; and concomitant medication for the treatment of comorbid physical and psychiatric conditions...
July 2016: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
Agnieszka Michalak, Grazyna Biała
The consequences of alcohol dependence concern serious health care, social and economic problems. The scope of many studies is to better understand mechanisms underlying alcohol addiction in order to work out new, more effective treatment strategies. Alcohol affects many neurotransmission systems within the brain. In general, acute alcohol enhances inhibitory transmission, up-regulating the GABAergic system and impairing glutamatergic function, therefore interfering the balance between excitatory and inhibitory synaptic inputs...
January 2016: Acta Poloniae Pharmaceutica
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