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Low dose naloxone

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https://www.readbyqxmd.com/read/28529359/the-journey-of-opioid-substitution-therapy-in-india-achievements-and-challenges
#1
Ravindra Rao
Opioids are one of the most problematic illegal substances globally. Opioid abuse is associated with complications in various spheres of the user's life, his/her family, and the society. Injecting drug use (IDU) is also linked to public health problems such as HIV infection and viral hepatitis. Medications form an important cornerstone in the treatment of opioid dependence. Treatment strategies such as "detoxification" alone or long-term treatment with opioid antagonist have limited acceptability and retention rates...
January 2017: Indian Journal of Psychiatry
https://www.readbyqxmd.com/read/28502631/a-brain-targeted-ampakine-compound-protects-against-opioid-induced-respiratory-depression
#2
Wei Dai, Dian Xiao, Xiang Gao, Xin-Bo Zhou, Tong-Yu Fang, Zheng Yong, Rui-Bin Su
The use of opioid drugs for pain relief can induce life-threatening respiratory depression. Although naloxone effectively counteracts opioid-induced respiratory depression, it diminishes the efficacy of analgesia. Our studies indicate that ampakines, in particular, a brain-targeted compound XD-8-17C, are able to reverse respiratory depression without affecting analgesia at relatively low doses. Mice and rats were subcutaneously or intravenously injected with the opioid agonist TH-030418 to induce moderate or severe respiratory depression...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28502630/new-opioid-receptor-antagonist-naltrexone-14-o-sulfate-synthesis-and-pharmacology
#3
Ferenc Zádor, Kornél Király, András Váradi, Mihály Balogh, Ágnes Fehér, Dóra Kocsis, Anna I Erdei, Erzsébet Lackó, Zoltán S Zádori, Sándor Hosztafi, Béla Noszál, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
Opioid antagonists, naloxone and naltrexone have long been used in clinical practice and research. In addition to their low selectivity, they easily pass through the blood-brain barrier. Quaternization of the amine group in these molecules, (e.g. methylnaltrexone) results in negligible CNS penetration. In addition, zwitterionic compounds have been reported to have limited CNS access. The current study, for the first time gives report on the synthesis and the in vitro [competition binding, G-protein activation, isolated mouse vas deferens (MVD) and mouse colon assay] pharmacology of the zwitterionic compound, naltrexone-14-O-sulfate...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28430384/pharmacokinetics-of-concentrated-naloxone-nasal-spray-over-first-30%C3%A2-minutes-post-dosing-analysis-of-suitability-for-opioid-overdose-reversal
#4
Gill Mundin, Rebecca McDonald, Kevin Smith, Stephen Harris, John Strang
BACKGROUND AND AIMS: Lack of non-injectable naloxone formulations has impeded widespread take-home provision for the prevention of heroin/opioid overdose deaths. For non-injectable formulations that are finally being investigated, rapid onset of action and sufficient bioavailability will be vital. We present analysis of data from a study of concentrated naloxone nasal spray formulations. Our aims are: to assess 1) pharmacokinetic properties and 2) suitability for overdose reversal in terms of naloxone absorption within 30 minutes post-dosing...
April 21, 2017: Addiction
https://www.readbyqxmd.com/read/28410920/potential-drug-interaction-with-opioid-agonist-in-the-setting-of-chronic-low-dose-opioid-antagonist-use
#5
James B Leonard, Vidya Nair, Christopher J Diaz, Jonathan B Penoyar, Penelope A Goode
Low dose naltrexone (LDN) has been evaluated in several small studies for the treatment of inflammatory conditions. It is thought to work through modulation of inflammatory mediators and upregulation of endogenous opioid receptors. This may hypersensitize patients to exogenous opioids. Drug-drug interaction screening tools built into electronic health records and other services identify the interaction as risk of opioid withdrawal rather than hypersensitivity. We present a case of a drug-drug interaction in a patient who was receiving LDN treatment of multiple sclerosis...
April 6, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28349575/low-dose-naloxone-for-prophylaxis-of-postoperative-nausea-and-vomiting-a-systematic-review-and-meta-analysis
#6
Robert W Barrons, Joseph Andrew Woods
STUDY OBJECTIVE: To determine whether postoperative administration of low-dose intravenous naloxone decreases the incidence of postoperative nausea and vomiting (PONV) and its impact on postoperative opioid requirements and pain scores. DESIGN: Meta-analysis of nine randomized controlled trials. PATIENTS: A total of 946 adult and pediatric patients who received low-dose intravenous naloxone for 24 hours after various surgeries. MEASUREMENTS AND MAIN RESULTS: Systemic literature searches of the Cochrane Central Register of Controlled Trials, Evidence-Based Medicine Reviews, PubMed, and Ovid MEDLINE databases were conducted...
March 28, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28336575/pharmacologic-profile-of-naloxegol-a-peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonist-for-the-treatment-of-opioid-induced-constipation
#7
Eike Floettmann, Khanh Bui, Mark Sostek, Kemal Payza, Michael Eldon
Opioid-induced constipation (OIC) is a common side effect of opioid pharmacotherapy for the management of pain because opioid agonists bind to µ-opioid receptors in the enteric nervous system (ENS). Naloxegol, a polyethylene glycol derivative of naloxol, which is a derivative of naloxone and a peripherally acting µ-opioid receptor antagonist, targets the physiologic mechanisms that cause OIC. Pharmacologic measures of opioid activity and pharmacokinetic measures of central nervous system (CNS) penetration were employed to characterize the mechanism of action of naloxegol...
May 2017: Journal of Pharmacology and Experimental Therapeutics
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
#8
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
#9
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
#10
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
#11
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
#12
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 3-10ng 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 (0.01-0.1μg) and DAPTA (0.3-3μg), respectively. The prevention of this hyperalgesia by diclofenac (1-10μg), 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
#13
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
#14
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...
May 2017: Prehospital Emergency Care
https://www.readbyqxmd.com/read/27902584/effect-of-naloxone-on-intravenous-fentanyl-patient-controlled-analgesia-after-laparoscopic-cholecystectomy
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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