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Low dose naloxone

Abolfazl Firouzian, Afshin Gholipour Baradari, Abbas Alipour, Amir Emami Zeydi, Alieh Zamani Kiasari, Seyed Abdollah Emadi, Behrooz Kheradmand, Kaveh Hadadi
BACKGROUND: Lumbar discectomy is one of the most commonly performed neurosurgical procedures. Many patients experience postoperative pain after lumbar discectomy. This study evaluated the effect of ultra-low-dose naloxone infusion on pain intensity after lumbar discectomy in individuals receiving patient-controlled analgesia (PCA) with morphine. MATERIALS AND METHODS: In a double-blind, randomized, controlled trial, a total of 80 patients scheduled for open discectomy was randomly assigned to receive naloxone (group N) or placebo (group P)...
September 26, 2016: Journal of Neurosurgical Anesthesiology
James B Lucot
Doses of naloxone far below those which elicit emesis increase the sensitivity to motion sickness. In order to evaluate the possible interaction with broad spectrum antiemetics, low doses of naloxone were tested alone and in combination with 8-hydroxy-2-(di-n-propylamine)tetralin (DPAT), fentanyl and the NK1 antagonist CP-99994. A modified autonomic symptom rating scale was unaffected by any drug and thus considered of little value. Fentanyl and NK1 antagonists decreased the duration of the retch/vomit sequence...
August 30, 2016: Autonomic Neuroscience: Basic & Clinical
Atefeh Bakhtazad, Nasim Vousooghi, Behzad Garmabi, Mohammad Reza Zarrindast
It has been shown previously that cocaine- and amphetamine-regulated transcript (CART) peptide has a modulatory role and homeostatic regulatory effect in motivation to and reward of the drugs of abuse specially psychostimulants. Recent data also showed that in addition to psychostimulants, CART is critically involved in the different stages of opioid addiction. Here we have evaluated the fluctuations in the level of CART peptide in plasma and CSF in different phases of opioid addiction to find out whether CART can serve as a suitable marker in opioid addiction studies...
October 2016: Peptides
Nicholas J Connors, Lewis S Nelson
INTRODUCTION: Opioid abuse and opioid overdose deaths have increased significantly over the past decade. Naloxone is a potentially life-saving medication that can reverse opioid-induced respiratory depression, though precipitated opioid withdrawal can pose acute risks to the patient and medical personnel. The optimal naloxone dose is unclear and few studies address this question. METHODS: A convenience sample of commonly available references were queried for the recommended IV naloxone dose...
September 2016: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
Marzia Lazzari, Claudio Marcassa, Silvia Natoli, Roberta Carpenedo, Clarissa Caldarulo, Maria B Silvi, Mario Dauri
PURPOSE: Chronic pain has a high prevalence in the aging population. Strong opioids also should be considered in older people for the treatment of moderate to severe pain or for pain that impairs functioning and the quality of life. This study aimed to assess the efficacy and safety of the direct switch to low-dose strong opioids (World Health Organization-Step III drugs) in elderly, opioid-naive patients. PATIENTS AND METHODS: This was a single-center, retrospective, observational study in opioid-naive patients aged ≥75 years, with moderate to severe chronic pain (>6-month duration) and constipation, who initiated treatment with prolonged-release oxycodone/naloxone (OXN-PR)...
2016: Clinical Interventions in Aging
Philip Krieter, Nora Chiang, Shwe Gyaw, Phil Skolnick, Roger Crystal, Fintan Keegan, Julie Aker, Melissa Beck, Jennifer Harris
Parenteral naloxone has been approved to treat opiate overdose for over 4 decades. Intranasal naloxone, administered "off label" using improvised devices, has been widely used by both first responders and the lay public to treat overdose. However, these improvised devices require training for effective use, and the recommended volumes (2 to 4 mL) exceed those considered optimum for intranasal administration. The present study compared the pharmacokinetic properties of intranasal naloxone (2 to 8 mg) delivered in low volumes (0...
October 2016: Journal of Clinical Pharmacology
Fabio Guerriero, Anna Roberto, Maria Teresa Greco, Carmelo Sgarlata, Marco Rollone, Oscar Corli
BACKGROUND: Two-thirds of older people suffer from chronic pain and finding valid treatment options is essential. In this 1-yearlong investigation, we evaluated the efficacy and safety of prolonged-release oxycodone-naloxone (OXN-PR) in patients aged ≥70 (mean 81.7) years. METHODS: In this open-label prospective study, patients with moderate-to-severe noncancer chronic pain were prescribed OXN-PR for 1 year. The primary endpoint was the proportion of patients who achieved ≥30% reduction in pain intensity after 52 weeks of treatment, without worsening bowel function...
2016: Drug Design, Development and Therapy
Michael A Eldon, Alan R Kugler, Robert A Medve, Khanh Bui, Kathleen Butler, Mark Sostek
This randomized, double-blind, placebo-controlled, ascending-dose, crossover study evaluated single oral doses of naloxegol (NKTR-118; 8, 15, 30, 60, 125, 250, 500, and 1000 mg), a PEGylated derivative of naloxone, for safety and tolerability, antagonism of peripheral and central nervous system (CNS) effects of intravenous morphine, and pharmacokinetics. Healthy men were randomized 1:1 to naloxegol or naloxegol-matching placebo administered with morphine and lactulose in a 2-period crossover design. Periods were separated by a 5- to 7-day washout...
November 2015: Clinical Pharmacology in Drug Development
Essiina Launonen, Isla Wallace, Elina Kotovirta, Hannu Alho, Kaarlo Simojoki
BACKGROUND: The intravenous (IV) use of opioid maintenance treatment (OMT) medications and other intoxicating drugs among OMT patients is a challenge for many OMT units and affects treatment outcomes. The aim of this study is to examine factors associated with IV use of OMT medications and other intoxicating drugs among Finnish OMT patients. METHODS: A cross-sectional study was conducted among all Finnish OMT patients of whom 60% (n=1508) participated. The data were collected by anonymous questionnaire...
May 1, 2016: Drug and Alcohol Dependence
Emiliano Petrò, Elena Ruffini, Melania Cappuccio, Valeria Guerini, Gloria Belotti, Sara Fascendini, Cristina Licini, Claudio Marcassa
OBJECTIVE: This pilot study evaluated the efficacy and safety of prolonged-release oxycodone/naloxone (OXN-PR) in older subjects with chronic pain and mild-to-moderate cognitive impairment. METHODS: This was a prospective, observational, open-label study of 45-day duration. Patients with moderate-to-severe chronic pain and naïve to strong opioids were recruited from nursing homes and Alzheimer's disease centers. OXN-PR was initiated at low doses (5 mg od or bid) and increased to a maximum of 20 mg bid...
2016: Neuropsychiatric Disease and Treatment
Boris Gourévitch, Jun Cai, Nicholas Mellen
Neonatal abstinence syndrome (NAS) occurs in babies chronically exposed to opioids during pregnancy. NAS shares features with opioid withdrawal symptoms seen in adults, including autonomic dysregulation. Here, the effect of low-dose in utero methadone (MTD) exposure on respiration-modulated networks along the ventral respiratory column (VRC) in ventrolateral medulla was investigated in the neonate Sprague-Dawley rat. MTD was administered via drinking water (3mg/kg/day in drinking water of the mother E7-E21)...
March 20, 2016: Experimental Neurology
L Rombolà, D Amantea, R Russo, A Adornetto, L Berliocchi, L Tridico, M T Corasaniti, S Sakurada, T Sakurada, G Bagetta, L A Morrone
In complementary medicine, aromatherapy uses essential oils to improve agitation and aggression observed in dementia, mood, depression, anxiety and chronic pain. Preclinical research studies have reported that the essential oil obtained from bergamot (BEO) fruit (Citrus bergamia, Risso) modifies normal and pathological synaptic plasticity implicated, for instance, in nociceptive and neuropathic pain. Interestingly, recent results indicated that BEO modulates sensitive perception of pain in different models of nociceptive, inflammatory and neuropathic pain modulating endogenous systems...
2016: Mini Reviews in Medicinal Chemistry
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
A Bakhtazad, N Vousooghi, B Garmabi, M R Zarrindast
Previous studies have shown the prominence of cocaine- and amphetamine-regulated transcript (CART) peptide in rewarding and reinforcing effects of drugs of abuse specially psychostimulants. The data regarding the effects of different stages of opioid addiction on CART expression and the interconnection between CART and opioids are not much available. Here we have studied the changes in the expression level of CART mRNA and protein in various parts of the brain reward pathway in different stages of opioid addiction...
June 14, 2016: Neuroscience
Edward C Emery, Ana Paula Luiz, John N Wood
INTRODUCTION: Chronic pain is a massive clinical problem. We discuss the potential of subtype selective sodium channel blockers that may provide analgesia with limited side effects. AREAS COVERED: Sodium channel subtypes have been linked to human pain syndromes through genetic studies. Gain of function mutations in Nav1.7, 1.8 and 1.9 can cause pain, whilst loss of function Nav1.7 mutations lead to loss of pain in otherwise normal people. Intriguingly, both human and mouse Nav1...
August 2016: Expert Opinion on Therapeutic Targets
Nicholas A Buckley, Andrew H Dawson, David N Juurlink, Geoffrey K Isbister
An understanding of mechanisms, potential benefits and risks of antidotes is essential for clinicians who manage poisoned patients. Of the dozens of antidotes currently available, only a few are regularly used. These include activated charcoal, acetylcysteine, naloxone, sodium bicarbonate, atropine, flumazenil, therapeutic antibodies and various vitamins. Even then, most are used in a minority of poisonings. There is little randomized trial evidence to support the use of most antidotes. Consequently, decisions about when to use them are often based on a mechanistic understanding of the poisoning and the expected influence of the antidote on the patient's clinical course...
March 2016: British Journal of Clinical Pharmacology
Yongzhen Liu, Xiaohua Li, Allan Xu, Azmi F Nasser, Christian Heidbreder
A simple, sensitive and rapid liquid chromatography/electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) method was developed and validated for simultaneous quantification of naloxone, buprenorphine and its metabolite norbuprenorphine in human plasma. Human plasma samples were extracted using a single step liquid-liquid extraction, and then separated on an Imtakt Unison UK-C18 column (2.1×50mm, 3μm) using alkaline mobile phases with gradient elution. All of the analytes were detected in positive ion mode using multiple reaction monitoring (MRM)...
February 20, 2016: Journal of Pharmaceutical and Biomedical Analysis
Rose G Jannuzzi
OBJECTIVES: Opioid-induced pruritus is a common side effect of opioid treatment in patients with acute pain associated with surgery or childbirth. There are several options available to treat opioid-induced pruritus, including nalbuphine. However, it is not known whether nalbuphine offers greater efficacy in treating pruritus without attenuation of analgesia and an increase in the incidence of adverse outcomes. METHODS: A systematic search of studies assessing treatment efficacy of nalbuphine was conducted through Medline, PubMed, Cochrane Library, CINAHL, and ProQuest databases...
January 2016: Clinical Journal of Pain
Lynn R Webster, Michael D Smith, Cemal Unal, Andrew Finn
In developmental research, plasma buprenorphine concentrations comparable to a 2 mg buprenorphine-naloxone (BN) sublingual tablet have been achieved with a 0.75 mg dose of BN buccal film, a small, bioerodible polymer film for application to mucosal membranes. This was a randomized, double-blind, placebo-controlled, single-dose, four-period crossover study in opioid-dependent subjects with chronic pain receiving >100 mg oral morphine equivalents daily who experienced withdrawal following a naloxone challenge dose...
2015: Journal of Pain Research
Ralf Baron, Jan-Peter Jansen, Andreas Binder, Manuel Pombo-Suarez, Lieven Kennes, Matthias Müller, Dietmar Falke, Ilona Steigerwald
OBJECTIVE: To evaluate tolerability, safety, and quality-of-life outcomes in non-opioid-pretreated patients with severe chronic low back pain with a neuropathic component receiving tapentadol PR vs. oxycodone/naloxone PR. METHODS: Eligible patients (average pain intensity [numerical rating scale] ≥ 6; painDETECT positive/unclear ratings) were randomized to twice-daily tapentadol PR 50 mg or oxycodone/naloxone PR 10 mg/5 mg. After a 21-day titration (maximum twice-daily doses: tapentadol PR 250 mg, or oxycodone/naloxone PR 40 mg/20 mg plus oxycodone PR 10 mg), target doses were continued for 9 weeks...
June 2016: Pain Practice: the Official Journal of World Institute of Pain
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