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Low dose naltrexon

Samy K Metyas, Karen Yeter, John Solyman, Daniel Arkfeld
Fibromyalgia is a chronic pain disorder characterized by diffuse musculoskeletal pain, fatigue, sleep disturbance and cognitive impairment. A significant number of fibromyalgia patients do not respond adequately to the current drugs (pregabalin, milnacipran, duloxetine) approved for fibromyalgia treatment by the Food and Drug Administration (FDA). Thus, there is still a need for adjunctive therapies. Naltrexone is an opioid receptor antagonist used to treat alcohol and opioid dependence. It is hypothesized that low dose naltrexone causes transient blockade of opioid receptors centrally resulting in a rebound of endorphin function which may attenuate pain in fibromyalgia...
March 21, 2017: Current Rheumatology Reviews
Mariana Alvarado-Bañuelos, Eliana Barrios De Tomasi, Jorge Juárez
INTRODUCTION: Opioid antagonist treatments such as naltrexone (NTX) and naloxone reduce consummatory behavior of palatable food (PF) and other incentives. Meanwhile, a significant increase in alcohol consumption has been observed when it is offered immediately after ending NTX treatment, an effect apparently produced by increased opioidergic activity caused by up-regulation of opioid receptors. OBJECTIVE: On this basis we assessed changes in the consumption of PF after opioid antagonist treatment in rats with different preferences for that food...
March 23, 2016: Nutritional Neuroscience
Linda Gowing, Robert Ali, Jason M White, Dalitso Mbewe
BACKGROUND: Managed withdrawal is a necessary step prior to drug-free treatment or as the endpoint of substitution treatment. OBJECTIVES: To assess the effects of buprenorphine versus tapered doses of methadone, alpha2-adrenergic agonists, symptomatic medications or placebo, or different buprenorphine regimens for managing opioid withdrawal, in terms of the intensity of the withdrawal syndrome experienced, duration and completion of treatment, and adverse effects...
February 21, 2017: Cochrane Database of Systematic Reviews
K Noon, J Sturgeon, M Kao, B Darnall, S Mackey
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
Maria Sullivan, Adam Bisaga, Martina Pavlicova, C Jean Choi, Kaitlyn Mishlen, Kenneth M Carpenter, Frances R Levin, Elias Dakwar, John J Mariani, Edward V Nunes
OBJECTIVE: At present there is no established optimal approach for transitioning opioid-dependent adults to extended-release injection naltrexone (XR-naltrexone) while preventing relapse. The authors conducted a trial examining the efficacy of two methods of outpatient opioid detoxification for induction to XR-naltrexone. METHOD: Participants were 150 opioid-dependent adults randomly assigned 2:1 to one of two outpatient detoxification regimens, naltrexone-assisted detoxification or buprenorphine-assisted detoxification, followed by an injection of XR-naltrexone...
January 10, 2017: American Journal of Psychiatry
Y Zhou, M Rubinstein, M J Low, M J Kreek
Opioid receptor antagonist naltrexone reduces alcohol consumption and relapse in both humans and rodents. This study investigated whether hypothalamic proopiomelanocortin (POMC) neurons (producing beta-endorphin and melanocortins) play a role in alcohol drinking behaviors. Both male and female mice with targeted deletion of two neuronal Pomc enhancers nPE1 and nPE2 (nPE-/-), resulting in hypothalamic-specific POMC deficiency, were studied in short-access (4-h/day) drinking-in-the-dark (DID, alcohol in one bottle, intermittent access (IA, 24-h cycles of alcohol access every other day, alcohol vs...
November 21, 2016: Genes, Brain, and Behavior
Waldemar Siemens, Carola Xander, Joerg J Meerpohl, Sabine Buroh, Gerd Antes, Guido Schwarzer, Gerhild Becker
BACKGROUND: This is an update of the original Cochrane review published in 2013 (Issue 6). Pruritus occurs in patients with disparate underlying diseases and is caused by different pathologic mechanisms. In palliative care patients, pruritus is not the most prevalent but is one of the most puzzling symptoms. It can cause considerable discomfort and affects patients' quality of life. OBJECTIVES: To assess the effects of different pharmacological treatments for preventing or treating pruritus in adult palliative care patients...
November 16, 2016: Cochrane Database of Systematic Reviews
Gregory N Ruegsegger, Jacob D Brown, M Cathleen Kovarik, Dennis K Miller, Frank W Booth
The mesolimbic dopamine and opioid systems are postulated to influence the central control of physical activity motivation. We utilized selectively bred rats for high (HVR) or low (LVR) voluntary running behavior to examine (1) inherent differences in mu-opioid receptor (Oprm1) expression and function in the nucleus accumbens (NAc), (2) if dopamine-related mRNAs, wheel-running, and food intake are differently influenced by intraperitoneal (i.p.) naltrexone injection in HVR and LVR rats, and (3) if dopamine is required for naltrexone-induced changes in running and feeding behavior in HVR rats...
December 17, 2016: Neuroscience
David Mischoulon, Lindsay Hylek, Albert S Yeung, Alisabet J Clain, Lee Baer, Cristina Cusin, Dawn Flosnik Ionescu, Jonathan E Alpert, David P Soskin, Maurizio Fava
BACKGROUND: Given the proposed dopaminergic mechanism of low-dose naltrexone (LDN), we examined its efficacy as augmentation for depressive breakthrough on pro-dopaminergic antidepressant regimens. METHODS: 12 adults (67% female, mean age = 45±12) with recurrent DSM-IV major depressive disorder (MDD) on dopaminergic antidepressant regimens (stimulants, dopamine agonists, bupropion [≥300mg/day], aripiprazole [≤2.5mg/day], or sertraline [≥150mg/day]) were randomized to naltrexone 1mg b...
January 15, 2017: Journal of Affective Disorders
Guttorm Raknes, Lars Småbrekke
PURPOSE: Following a TV documentary in 2013, there was a tremendous increase in low dose naltrexone (LDN) use in a wide range of unapproved indications in Norway. We aim to describe the extent of this sudden and unprecedented increase in LDN prescribing, to characterize patients and LDN prescribers, and to estimate LDN dose sizes. METHODS: LDN prescriptions recorded in the Norwegian Prescription Database (NorPD) in 2013 and 2014, and sales data not recorded in NorPD from the only Norwegian LDN manufacturer were included in the study...
February 2017: Pharmacoepidemiology and Drug Safety
Zhe Yi, Shengnan Guo, Xu Hu, Xiaonan Wang, Xiaoqing Zhang, Noreen Griffin, Fengping Shan
Previously it was confirmed that naltrexone, a non-peptide δ-opioid receptor selective antagonist is mainly used for alcoholic dependence and opioid addiction treatment. However, there is increasing data on immune regulation of low dose naltrexone (LDN). The aim of this work was to explore the effect of LDN on the phenotype and function of macrophage. The changes of macrophage after treatment with LDN were examined using flow cytometry (FCM); FITC-dextran phagocytosis and enzyme-linked immunosorbent assay (ELISA)...
October 2016: International Immunopharmacology
Amanda Ellis, Peter M Grace, Julie Wieseler, Jacob Favret, Kendra Springer, Bryce Skarda, Monica Ayala, Mark R Hutchinson, Scott Falci, Kenner C Rice, Steven F Maier, Linda R Watkins
Central neuropathic pain (CNP) is a pervasive, debilitating problem that impacts thousands of people living with central nervous system disorders, including spinal cord injury (SCI). Current therapies for treating this type of pain are ineffective and often have dose-limiting side effects. Although opioids are one of the most commonly used CNP treatments, recent animal literature has indicated that administering opioids shortly after a traumatic injury can actually have deleterious effects on long-term health and recovery...
November 2016: Brain, Behavior, and Immunity
Janice C Froehlich, Stephen M Fischer, Julian E Dilley, Emily R Nicholson, Teal N Smith, Nick J Filosa, Logan C Rademacher
BACKGROUND: This study examined whether varenicline (VAR), or naltrexone (NTX), alone or in combination, reduces alcohol drinking in alcohol-preferring (P) rats with a genetic predisposition toward high voluntary alcohol intake. METHODS: Alcohol-experienced P rats that had been drinking alcohol (15% v/v) for 2 h/d for 4 weeks were fed either vehicle (VEH), VAR alone (0.5, 1.0, or 2.0 mg/kg body weight [BW]), NTX alone (10.0, 15.0, or 20.0 mg/kg BW), or VAR + NTX in 1 of 4 dose combinations (0...
September 2016: Alcoholism, Clinical and Experimental Research
Dina Ibrahim Tawfik, Afaf Sayed Osman, Hedayat Mahmoud Tolba, Aida Khattab, Lubna O Abdel-Salam, Mahmoud M Kamel
BACKGROUND AND AIM: Crohn's disease is a relapsing inflammatory condition afflicting the digestive tract. Drugs used for treatment of Crohn's disease may be associated with serious side effects. Endogenous opioid peptides modulate inflammatory cytokine production. Opioid antagonists have been shown to play a role in healing and repair of tissues. This work was designed to detect the possible beneficial effects of opioid antagonist naltrexone in indomethacin-induced Crohn's disease in rats...
October 2016: Neuropeptides
Wai M Liu, Katherine A Scott, Jayne L Dennis, Elwira Kaminska, Alan J Levett, Angus G Dalgleish
It has been reported that lower doses of the opioid antagonist naltrexone are able to reduce tumour growth by interfering with cell signalling as well as by modifying the immune system. We have evaluated the gene expression profile of a cancer cell line after treatment with low-dose naltrexone (LDN), and assessed the effect that adapting treatment schedules with LDN may have on enhancing efficacy. LDN had a selective impact on genes involved with cell cycle regulation and immune modulation. Similarly, the pro-apoptotic genes BAD and BIK1 were increased only after LDN...
August 2016: International Journal of Oncology
Jose L Barboza, Radha Patel, Pooja Patel, Karen Suchanek Hudmon
INTRODUCTION: Cigarette smoking can damage every organ in the body and is the leading known preventable cause of death globally. It is estimated that 70% of patients want to quit, and about 50% report a quit attempt in the past year, yet only 4-7% are successful. These low quit rates represent the importance of appropriate treatment for smoking cessation through behavioral and pharmacotherapeutic means. AREAS COVERED: Pharmacotherapy approximately doubles patients' chances of quitting, and the first-line approved pharmacotherapetuic options include nicotine gum, lozenge, patch, nasal spray, and inhaler, sustained-release bupropion, and varenicline...
August 2016: Expert Opinion on Pharmacotherapy
Kuan Gandelman, Michael Lamson, Joanne Salageanu, Candace Bramson, Kyle Matschke, Bimal Malhotra
WHAT IS KNOWN AND OBJECTIVE: ALO-02 is being developed as an abuse-deterrent formulation of extended-release oxycodone hydrochloride with naltrexone hydrochloride sequestered in the core of pellets contained in capsules. The primary objective of this study was to assess the effects of administration of ALO-02 capsule whole under fed conditions or sprinkling the pellets from ALO-02 capsule on applesauce under fasting conditions on the pharmacokinetics (PK) of oxycodone, naltrexone and 6-ß-naltrexol compared with ALO-02 capsule administered whole under fasting conditions...
September 2015: Clinical Pharmacology in Drug Development
Esa R Korpi, Anni-Maija Linden, Heidi R Hytönen, Nelli Paasikoski, Elena Vashchinkina, Mateusz Dudek, Deron R Herr, Petri Hyytiä
Opioid antagonist treatments reduce alcohol drinking in rodent models and in alcohol-dependent patients, with variable efficacy across different studies. These treatments may suffer from the development of tolerance and opioid receptor supersensitivity, as suggested by preclinical models showing activation of these processes during and after subchronic high-dose administration of the short-acting opioid antagonist naloxone. In the present study, we compared equipotent low and moderate daily doses of naltrexone and nalmefene, two opioid antagonists in the clinical practice for treatment of alcoholism...
March 15, 2016: Addiction Biology
George E Woody, Evgeny Krupitsky, Edwin Zvartau
Naltrexone is an antagonist that binds tightly to μ-opioid receptors and blocks the subjective and analgesic effects of opioids. It does not produce physiologic dependence and precipitates withdrawal if administered to an opioid dependent person, thus starting it must begin with detoxification. It was first available in the mid-1970s as a 50 mg tablet that blocked opioids for 24-36 h if taken daily, or every 2-3 days at higher doses - for example: 100 mg Monday and Wednesday, 150 mg on Friday. From a pharmacological perspective it worked very well and was hoped to be an effective treatment but results were disappointing due to low patient interest and high dropout followed by relapse...
September 2016: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
Sarah Sushchyk, Zheng-Xiong Xi, Jia Bei Wang
Relapse to drug use is often cited as the major obstacle in overcoming a drug addiction. Whereas relapse can occur for a myriad of reasons, it is well established that complex neuroadaptations that occur over the course of addiction are major factors. Cocaine, as a potent dopamine transporter blocker, specifically induces alterations in the dopaminergic as well as other monoaminergic neurotransmissions, which lead to cocaine abuse and dependence. Evidence also suggests that adaptations in the endogenous opioids play important roles in pathophysiology of cocaine addiction...
May 2016: Journal of Pharmacology and Experimental Therapeutics
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