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Low dose naloxone

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https://www.readbyqxmd.com/read/28291086/opioid-type-respiratory-depressant-side-effects-of-cebranopadol-in-rats-are-limited-by-its-nociceptin-orphanin-fq-peptide-receptor-agonist-activity
#1
Klaus Linz, Wolfgang Schröder, Stefanie Frosch, Thomas Christoph
BACKGROUND: Cebranopadol is a first-in-class analgesic with agonist activity at classic opioid peptide receptors and the nociceptin/orphanin FQ peptide receptor. The authors compared the antinociceptive and respiratory depressant effects of cebranopadol and the classic opioid fentanyl and used selective antagonists to provide the first mechanistic evidence of the contributions of the nociceptin/orphanin FQ peptide and μ-opioid peptide receptors to cebranopadol's respiratory side-effect profile...
April 2017: Anesthesiology
https://www.readbyqxmd.com/read/28277185/changes-in-the-incentive-value-of-food-after-naltrexone-treatment-depend-on-a-differential-preference-for-a-palatable-food-in-male-rats
#2
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
https://www.readbyqxmd.com/read/28275232/the-differential-effects-of-low-and-high-doses-of-apelin-through-opioid-receptors-on-the-blood-pressure-of-rats-with-renovascular-hypertension
#3
Mahboobeh Yeganeh-Hajahmadi, Hamid Najafipour, Farzaneh Rostamzadeh
The apelin/APJ system has an important role in the regulation of vascular tone and blood pressure. Opioid receptors (OPRs) are also important cardiovascular regulators and exert many of their effects by modulating the function of other G-protein-coupled receptors. The aim of this study was to analyze the interaction of apelin and the opioid system with respect to vascular responses to apelin in rats with renovascular hypertension (two-kidney, one clip (2K1C)). Homodynamic studies were carried out in 2K1C rats...
March 9, 2017: Hypertension Research: Official Journal of the Japanese Society of Hypertension
https://www.readbyqxmd.com/read/28144724/pharmacokinetics-of-a-new-nasal-formulation-of-naloxone
#4
Ida Tylleskar, Arne Kristian Skulberg, Turid Nilsen, Sissel Skarra, Phatsawee Jansook, Ola Dale
PURPOSE: Nasal naloxone is wanted for bystander administration in opioid overdose and as a needle-free alternative for emergency medical personnel. Epidemiologic studies have indicated a therapeutic effect of bystander administration of low-concentration/high-volume formulations. The objective for this study was to describe the nasal pharmacokinetics of a new high-concentration/low-volume nasal formulation of naloxone. METHODS: This was an open, randomized triple crossover trial in healthy, human volunteers (n = 12) where two doses of nasal naloxone (0...
January 31, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28126501/hyperalgesic-and-hypoalgesic-mechanisms-evoked-by-the-acute-administration-of-ccl5-in-mice
#5
Sara González-Rodríguez, Miguel G Álvarez, Mario García-Domínguez, Ana Lastra, Rafael Cernuda-Cernuda, Alicia R Folgueras, María Teresa Fernández-García, Agustín Hidalgo, Ana Baamonde, Luis Menéndez
We show here that the intraplantar administration of CCL5 in mice produces hyperalgesia at low doses but activates compensatory antinociceptive mechanisms at doses slightly higher. Thus, the injection of 3-10 ng of CCL5 evoked thermal hyperalgesia through the activation of CCR1 and CCR5 receptors, as demonstrated by the inhibitory effect exerted by the selective antagonists J113863 (0.01-0.1 μg) and DAPTA (0.3-3 μg), respectively. The prevention of this hyperalgesia by diclofenac (1-10 μg), the inhibitors of COX-1 SC-560 (0...
January 23, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28078167/a-novel-strategy-for-attenuating-opioid-withdrawal-in-neonates
#6
Giovanni C Santoro, Samarth Shukla, Krishna Patel, Jakub Kaczmarzyk, Stergiani Agorastos, Sandra Scherrer, Yoon Young Choi, Christina Veith, Joseph Carrion, Rebecca Silverman, Danielle Mullin, Mohamed Ahmed, Wynne K Schiffer, Jonathan D Brodie, Stephen L Dewey
The rate of Neonatal Abstinence Syndrome (NAS) has drastically increased over the past decade. The average hospital expense per NAS patient has tripled, while the number of babies born to opioid-dependent mothers has increased to 5 in 1000 births. Current treatment options are limited to opioid replacement and tapering. Consequently, we examined the efficacy of prenatal, low-dose and short-term vigabatrin (γ-vinyl GABA, GVG) exposure for attenuating these symptoms as well as the metabolic changes observed in the brains of these animals upon reaching adolescence...
August 2016: Journal of Addiction Research & Therapy
https://www.readbyqxmd.com/read/28059581/hot-and-cold-drugs-national-park-service-medication-stability-at-the-extremes-of-temperature
#7
Patil Armenian, Danielle Campagne, Geoff Stroh, Crystal Ives Tallman, William Z D Zeng, Thomas Lin, Roy R Gerona
STUDY OBJECTIVE: National Park Service (NPS) Parkmedics provide medical care in austere environments. The objective of this study was to evaluate the stability of specific medications used by Parkmedics at extremes of temperatures likely to be faced in the field. METHODS: This is a bench research study conducted in the laboratory setting over a 4-week period. Parenteral medications were separated into 4 temperature exposure groups: A) 45°C (hot); B) -20°C (cold); C) hot then cold temperatures alternating weekly; and D) cold then hot temperatures alternating weekly...
January 6, 2017: Prehospital Emergency Care
https://www.readbyqxmd.com/read/27902584/effect-of-naloxone-on-intravenous-fentanyl-patient-controlled-analgesia-after-laparoscopic-cholecystectomy
#8
RANDOMIZED CONTROLLED TRIAL
Jun Zheng, Wen Han, Xiao-Dong Han, Xiao-Yuan Ma, Pengbo Zhang
This study aims to evaluate the effect of naloxone on intravenous fentanyl patient-controlled analgesia after laparoscopic cholecystectomy under total intravenous anesthesia.A total of 90 patients, who underwent intravenous fentanyl patient-controlled analgesia after laparoscopic cholecystectomy under total intravenous anesthesia, were included into this study. All patients were randomly divided into 3 groups (each group, n=30): naloxone group (naloxone+fentanyl), tropisetron group (tropisetron+fentanyl), and fentanyl group (fentanyl)...
November 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27890601/tramadol-effects-on-sexual-behavior-in-male-rats-are-mainly-caused-by-its-5-ht-reuptake-blocking-effects
#9
Jocelien D A Olivier, Diana C Esquivel Franco, Ronald Oosting, Marcel Waldinger, Zoltan Sarnyai, Berend Olivier
Tramadol is a well-known and effective analgesic. Recently it was shown that tramadol is also effective in human premature ejaculation. The inhibitory effect of tramadol on the ejaculation latency is probably due to its mechanism of action as a μ-opioid receptor agonist and noradrenaline/serotonin (5-HT) reuptake inhibitor. In order to test this speculation, we tested several doses of tramadol in a rat model of male sexual behavior and investigated two types of drugs interfering with the μ-opioid and the 5-HT system...
November 24, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27861362/effects-of-target-controlled-infusion-of-high-dose-naloxone-on-pain-and-hyperalgesia-in-a-human-thermal-injury-model-a-study-protocol-a-randomized-double-blind-placebo-controlled-crossover-trial-with-an-enriched-design
#10
RANDOMIZED CONTROLLED TRIAL
Anders D Springborg, Elisabeth K Jensen, Bradley K Taylor, Mads U Werner
Mu-opioid-receptor antagonists have been extensively studied in experimental research as pharmacological tools uncovering mechanisms of pain modulation by the endogenous opioid system. In rodents, administration of high doses of mu-opioid-receptor antagonists after the resolution of an inflammatory injury has demonstrated reinstatement of nociceptive hypersensitivity indicating unmasking of latent sensitization. In a recent human study, pain hypersensitivity assessed as secondary hyperalgesia area (SHA), was reinstated 7 days after a mild thermal injury, in 4 out of 12 subjects after a naloxone infusion...
November 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27815762/acceptability-of-naloxone-co-prescription-among-primary-care-providers-treating-patients-on-long-term-opioid-therapy-for-pain
#11
Emily Behar, Christopher Rowe, Glenn-Milo Santos, Diana Coffa, Caitlin Turner, Nina C Santos, Phillip O Coffin
BACKGROUND: Naloxone co-prescription is recommended for patients on long-term opioids for pain, yet there are few data on the practice. OBJECTIVE: To explore naloxone co-prescribing acceptability among primary care providers for patients on long-term opioids. DESIGN: We surveyed providers at six safety-net primary care clinics in San Francisco that had initiated naloxone co-prescribing. Providers were encouraged to offer naloxone to patients on long-term opioids or otherwise at risk of witnessing or experiencing an overdose...
March 2017: Journal of General Internal Medicine
https://www.readbyqxmd.com/read/27673505/ultra-low-dose-naloxone-as-an-adjuvant-to-patient-controlled-analgesia-pca-with-morphine-for-postoperative-pain-relief-following-lumber-discectomy-a-double-blind-randomized-placebo-controlled-trial
#12
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
https://www.readbyqxmd.com/read/27615675/effects-of-naloxone-on-motion-sickness-in-cats-alone-and-with-broad-spectrum-antiemetics
#13
REVIEW
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...
January 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/27349817/evaluation-of-cart-peptide-level-in-rat-plasma-and-csf-possible-role-as-a-biomarker-in-opioid-addiction
#14
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
https://www.readbyqxmd.com/read/27271032/the-evolution-of-recommended-naloxone-dosing-for-opioid-overdose-by-medical-specialty
#15
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
https://www.readbyqxmd.com/read/27257377/switching-to-low-dose-oral-prolonged-release-oxycodone-naloxone-from-who-step-i-drugs-in-elderly-patients-with-chronic-pain-at-high-risk-of-early-opioid-discontinuation
#16
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
https://www.readbyqxmd.com/read/27145977/pharmacokinetic-properties-and-human-use-characteristics-of-an-fda-approved-intranasal-naloxone-product-for-the-treatment-of-opioid-overdose
#17
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
https://www.readbyqxmd.com/read/27143857/long-term-efficacy-and-safety-of-oxycodone-naloxone-prolonged-release-in-geriatric-patients-with-moderate-to-severe-chronic-noncancer-pain-a-52-week-open-label-extension-phase-study
#18
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
https://www.readbyqxmd.com/read/27137715/safety-tolerability-pharmacokinetics-and-pharmacodynamic-effects-of-naloxegol-at-peripheral-and-central-nervous-system-receptors-in-healthy-male-subjects-a-single-ascending-dose-study
#19
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
https://www.readbyqxmd.com/read/27068849/factors-associated-with-non-adherence-and-misuse-of-opioid-maintenance-treatment-medications-and-intoxicating-drugs-among-finnish-maintenance-treatment-patients
#20
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
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