- Drinking Levels and Profiles of Alcohol Addicted Rats Predict Response to Nalmefene. [Journal Article]
- FPFront Pharmacol 2019; 10:471
- CONCLUSIONS: Our results suggest that nalmefene reduces alcohol intake during a relapse-like situation but effectiveness can differ greatly at the individual level. However, who responds may be informed by examining drinking profiles and rats that show high drinking levels prior to treatment are more likely to respond to nalmefene.
- Evaluation of the Effect of Morphine and Imiquimodon Expression of TLR2 and TLR4 from Lesion RNA Extracted from BALB/c Mice Infected with Leishmania major. [Journal Article]
- AJAvicenna J Med Biotechnol 2019 Apr-Jun; 11(2):202-205
- CONCLUSIONS: However, in this study it was found that despite decreasing the size of lesion in all treated groups, expression of TLR4 in the morphine, nalmefene, morphine plus nalmefene treated groups compared to the control group was decreased. Therefore, morphine may have a different function mechanism in treatment of the Leishmaniasis with the L. major.
- Selecting an appropriate alcohol pharmacotherapy: review of recent findings. [Journal Article]
- COCurr Opin Psychiatry 2019; 32(4):266-274
- CONCLUSIONS: Three new published RCTs focus on baclofen and naltrexone. These results are consistent with old findings demonstrating that naltrexone reduces heavy drinking. Several RCT on baclofen do not support the use of baclofen for treatment of AUD. Encouraging results have been reported for topiramate, gabapentin and also varenicline, which might be useful in patients with comorbid nicotine dependence.
- The More You Take It, the Better It Works: Six-Month Results of a Nalmefene Phase-IV Trial. [Journal Article]
- JCJ Clin Med 2019 Apr 06; 8(4)
- CONCLUSIONS: The data provided by this phase-IV study suggest that nalmefene is an effective, well-tolerated treatment for alcohol-dependence in real world, clinical settings.
- Fighting fire with fire: development of intranasal nalmefene to treat synthetic opioid overdose. [Journal Article]
- JPJ Pharmacol Exp Ther 2019 Apr 02
- The dramatic rise in overdose deaths linked to synthetic opioids (e.g., fentanyl, carfentanil) may require more potent, longer duration opiate antagonists than naloxone. Both the high affinity of nal…
The dramatic rise in overdose deaths linked to synthetic opioids (e.g., fentanyl, carfentanil) may require more potent, longer duration opiate antagonists than naloxone. Both the high affinity of nalmefene at μ opiate receptors and its long half-life led us to examine the feasibility of developing an intranasal (IN) formulation as a rescue medication that could be especially useful in treating synthetic opioid overdose. In this study, the pharmacokinetic properties of IN nalmefene were compared with an intramuscular (IM) injection in a cohort of healthy volunteers. Nalmefene was absorbed slowly following IN administration, with a median Tmax of 2 h. Addition of the absorption enhancer dodecyl maltoside (Intravail®) reduced Tmax to 0.25 h and increased C max by ~2.2-fold. The pharmacokinetic properties of IN nalmefene (3 mg) formulated with dodecyl maltose has characteristics consistent with an effective rescue medication: its onset of action is comparable to an IM injection of nalmefene (1.5 mg) previously approved to treat opioid overdose. Furthermore, the Cmax following IN administration is ~3-fold higher than following IM dosing, comparable to previously reported plasma concentrations of nalmefene observed 5 min. following a 1 mg IV dose. The high affinity, very rapid onset, and long half-life (>7 h) of IN nalmefene present distinct advantages as a rescue medication, particularly against longer-lived synthetic opioids.
- Alcohol-related chronic exocrine pancreatic insufficiency: diagnosis and therapeutic management: a review of the literature and a proposal for treatment by the Italian Association for the Study of the Pancreas and the Italian Society on Alcohol. [Journal Article]
- MMMinerva Med 2019 Apr 01
- Current estimates of the prevalence of chronic pancreatitis, one of the most common causes of exocrine pancreatic insufficiency, are in the range of 3-10 per 100,000 people in many parts of the world…
Current estimates of the prevalence of chronic pancreatitis, one of the most common causes of exocrine pancreatic insufficiency, are in the range of 3-10 per 100,000 people in many parts of the world. Alcohol is a very important risk factor for exocrine pancreatic insufficiency and is involved in nearly half of all cases. The main hypothesis regarding the role of chronic alcohol consumption in pancreatitis is that there must be additional environmental or genetic risk factors involved for ongoing damage to occur. Treatment of patients with alcohol-related exocrine pancreatic insufficiency is complex, as the patient has two concomitant pathologies, alcohol-use disorder (AUD) and exocrine pancreatic insufficiency/chronic pancreatitis. Alcohol abstinence is the starting point for treatment, although even this along with the most advanced therapies allow only a slowdown in progression rather than restoration of function. This position paper of the Italian Association for the Study of the Pancreas and the Italian Society on Alcohol provides an overview of the pathogenesis of alcohol-related pancreatitis and discuss diagnostic issues. Treatment options for both exocrine pancreatic insufficiency/chronic pancreatitis (with a focus on pancreatic enzyme replacement therapy) and AUD (acamprosate, disulfiram, oral naltrexone, long-acting injectable naltrexone, sodium oxybate, nalmefene, baclofen, and psychosocial interventions) are also reviewed.
- Impact of Substance Use Disorder Pharmacotherapy on Executive Function: A Narrative Review. [Review]
- FPFront Psychiatry 2019; 10:98
- Substance use disorders are chronic, relapsing, and harmful conditions characterized by executive dysfunction. While there are currently no approved pharmacotherapy options for stimulant and cannabis…
Substance use disorders are chronic, relapsing, and harmful conditions characterized by executive dysfunction. While there are currently no approved pharmacotherapy options for stimulant and cannabis use disorders, there are several evidence-based options available to help reduce symptoms during detoxification and aid long-term cessation for those with tobacco, alcohol and opioid use disorders. While these medication options have shown clinical efficacy, less is known regarding their potential to enhance executive function. This narrative review aims to provide a brief overview of research that has investigated whether commonly used pharmacotherapies for these substance use disorders (nicotine, bupropion, varenicline, disulfiram, acamprosate, nalmefene, naltrexone, methadone, buprenorphine, and lofexidine) effect three core executive function components (working memory, inhibitory control and cognitive flexibility). While pharmacotherapy-induced enhancement of executive function may improve cessation outcomes in dependent populations, there are limited and inconsistent findings regarding the effects of these medications on executive function. We discuss possible reasons for the mixed findings and suggest some future avenues of work that may enhance the understanding of addiction pharmacotherapy and cognitive training interventions and lead to improved patient outcomes.
- Psychotic Decompensation During Nalmefene Treatment in a Patient With Schizoaffective Disorder: A Case Report. [Journal Article]
- JDJ Dual Diagn 2019 Apr-Jun; 15(2):118-121
- CONCLUSIONS: This case indicates that the AEs of nalmefene should be specifically investigated in patients with psychiatric disorders.
- Simultaneous extraction of acidic and basic drugs via on-chip electromembrane extraction using a single-compartment microfluidic device. [Journal Article]
- AAnalyst 2019 Feb 11; 144(4):1159-1166
- In this study, a new chip was designed for simultaneous extraction of acidic and basic drugs by a single chamber on-chip electromembrane extraction (CEME) followed by high performance liquid chromato…
In this study, a new chip was designed for simultaneous extraction of acidic and basic drugs by a single chamber on-chip electromembrane extraction (CEME) followed by high performance liquid chromatography. Diclofenac (DIC) and nalmefene (NAL) were selected as acidic and basic model analytes, respectively. In this device, simultaneous extraction of the analytes was carried out using a single compartment. The chip was composed of three PMMA (polymethyl methacrylate) parts with sandwiched structures and carved spiral microfluidic channels in each part. The middle part was cut and an "M" pattern provided interfaces for contact between the sample solution flow and two porous polypropylene sheets on both sides. Two other parts had the same spiral channels dedicated to the corresponding acceptor phases of the acidic and basic analytes and were located at both sides. Each polypropylene sheet was impregnated with the appropriate organic solvent for the acidic and basic analytes. Two platinum electrodes connected to a power supply were mounted at the bottom of the acceptor channels. These electrodes provided the electrical fields across SLMs to extract the analytes from a single sample flow. When the extraction was completed, the acceptor solutions were collected, mixed, and then injected into the chromatographic system. The effective parameters on the extraction efficiency were investigated and optimized. Under the optimal conditions, the calibration curves were linear in the range of 9.0-500 μg L-1 for NAL and 11.0-500 μg L-1 for DIC with the coefficient of determination (R2) higher than 0.9913. The relative standard deviations (RSD%) based on five replicate measurements were less than 6.3%. LOD values were 4.0 and 3.0 μg L-1 for DIC and NAL, respectively. Finally, the method was successfully applied to determine DIC and NAL in the human urine samples and satisfactory results were obtained (recovery ≥90).
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- Nalmefene, Given as Needed, in the Routine Treatment of Patients with Alcohol Dependence: An Interventional, Open-Label Study in Primary Care. [Clinical Trial]
- EAEur Addict Res 2018; 24(6):293-303
- CONCLUSIONS: Patients with alcohol dependence treated in primary care with nalmefene, taken as needed, in conjunction with simple psychosocial support, significantly reduced their alcohol consumption. Treatment was well tolerated.