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https://www.readbyqxmd.com/read/29337220/botaf-a-new-buthus-occitanus-tunetanus-scorpion-toxin-produces-potent-analgesia-in-rodents
#1
Riadh Maatoug, Jed Jebali, Régis Guieu, Michel De Waard, Riadh Kharrat
This work reports the purification of new potent scorpion neuropeptide, named BotAF, by an activity-guided screening approach. BotAF is a 64-residue long-chain peptide that shares very high similarity with the original β-like scorpion toxin group, in which several peptides have been characterized to be anti-nociceptive in rodents. BotAF administration to rodents does not produce any toxicity or motor impairment, including at high doses. In all models investigated, BotAF turned out to be an efficient peptide in abolishing acute and inflammatory (both somatic and visceral) pain in rodents...
January 11, 2018: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/29325337/-the-application-of-combining-low-dose-naloxone-with-ropivacaine-in-supraclavicular-brachial-plexus-block
#2
J Tang, S Y Zhang, F J Lu, W H Qin, Y S Shi
Objective: To observe the effect of low dose naloxone combinewith ropivacaine for supraclavicular brachial plexus block. Methods: Seventy patients undergoing elective upper limb surgery were randomly divided into two groups, ropivacaine group (Group R, n=35) and naloxone group (Group N, n=35). An ultrasound guided technique was used in both two groups.The onset and duration time of sensory and motor blockade, visual analog score(VAS)of 3, 6, 12, 18, 24 h postoperatively, time of first request fordezocine, total amount of dezocine needed, incidence of nausea and vomiting postoperatively(PONV) and patients' satisfaction score for analgesia in 24 h after surgery were measured...
December 26, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/29298517/histamine-h1-receptor-antagonists-facilitate-electroacupuncture-analgesia
#3
Jaung-Geng Lin, Yu-Chen Lee, Cheng-Hao Tu, Iona MacDonald, Hsin-Yi Chung, Sih-Ting Luo, Shih-Ya Hung, Yi-Hung Chen
This study investigated the influence of the histamine H1 receptor antagonists, chlorpheniramine (CHL) and pyrilamine, on the analgesic effects of acupuncture in mice. Nociceptive response was evaluated by the acetic acid-induced abdominal writhe test. Electroacupuncture (EA) at bilateral ST36 reduced the manifestations of acetic acid-induced abdominal writhing, whereas needle insertion without electrostimulation had no such effect. Notably, EA treatment was not associated with any analgesic effects in mice pretreated with naloxone...
January 3, 2018: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29284510/the-napressim-trial-the-use-of-low-dose-prophylactic-naloxone-infusion-to-prevent-respiratory-depression-with-intrathecally-administered-morphine-in-elective-hepatobiliary-surgery-a-study-protocol-and-statistical-analysis-plan-for-a-randomised-controlled-trial
#4
David Cosgrave, Marie Galligan, Era Soukhin, Victoria McMullan, Siobhan McGuinness, Anand Puttappa, Niamh Conlon, John Boylan, Rabia Hussain, Peter Doran, Alistair Nichol
BACKGROUND: Intrathecally administered morphine is effective as part of a postoperative analgesia regimen following major hepatopancreaticobiliary surgery. However, the potential for postoperative respiratory depression at the doses required for effective analgesia currently limits its clinical use. The use of a low-dose, prophylactic naloxone infusion following intrathecally administered morphine may significantly reduce postoperative respiratory depression. The NAPRESSIM trial aims to answer this question...
December 29, 2017: Trials
https://www.readbyqxmd.com/read/29194445/safety-and-efficacy-of-an-oxycodone-vaccine-addressing-some-of-the-unique-considerations-posed-by-opioid-abuse
#5
M D Raleigh, S J Peterson, M Laudenbach, F Baruffaldi, F I Carroll, S D Comer, H A Navarro, T L Langston, S P Runyon, S Winston, M Pravetoni, P R Pentel
Among vaccines aimed at treating substance use disorders, those targeting opioids present several unique medication development challenges. 1) Opioid overdose is a common complication of abuse, so it is desirable for an opioid vaccine to block the toxic as well as the addictive effects of opioids. 2) It is important that an opioid vaccine not interfere with the action of opioid antagonists used to reverse opioid overdose or treat addiction. 3) Some opioids are immunosuppressive and chronic ongoing opioid use could interfere with vaccine immunogenicity...
2017: PloS One
https://www.readbyqxmd.com/read/29181532/management-of-suspected-opioid-overdose-with-naloxone-in-out-of-hospital-settings-a-systematic-review
#6
Roger Chou, P Todd Korthuis, Dennis McCarty, Phillip O Coffin, Jessica C Griffin, Cynthia Davis-O'Reilly, Sara Grusing, Mohamud Daya
Background: Naloxone is effective for reversing opioid overdose, but optimal strategies for out-of-hospital use are uncertain. Purpose: To synthesize evidence on 1) the effects of naloxone route of administration and dosing for suspected opioid overdose in out-of-hospital settings on mortality, reversal of overdose, and harms, and 2) the need for transport to a health care facility after reversal of overdose with naloxone. Data Sources: Ovid MEDLINE (1946 through September 2017), PsycINFO, Cochrane Central Register of Controlled Trials, CINAHL, U...
November 28, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/29051703/buprenorphine-naloxone-maintenance-therapy-an-observational-retrospective-report-on-the-effect-of-dose-on-18%C3%A2-months-retention-in-an-office-based-treatment-program
#7
Theodore V Parran, A G Mace, Yael J Dahan, Christopher A Adelman, Mykola Kolganov
CONTEXT AND OBJECTIVE: Buprenorphine has been available with few reports of the dose range necessary to adequately maintain patients. We report on the effect of 8 mg/d versus 16 mg/d of buprenorphine on long-term patient retention in office-based opioid maintenance (OBOMT). DESIGN SETTING AND PARTICIPANTS: Case series, at an urban hospital-based primary care clinic providing OBOMT to 157 opiate-dependent, low socioeconomic status, uninsured, nonhomeless patients...
2017: Substance Abuse: Research and Treatment
https://www.readbyqxmd.com/read/29029049/intraoperative-naloxone-reduces-remifentanil-induced-postoperative-hyperalgesia-but-not-pain-a-randomized-controlled-trial
#8
C-H Koo, S Yoon, B-R Kim, Y J Cho, T K Kim, Y Jeon, J-H Seo
Background: Intraoperative use of a high-dose remifentanil may induce postoperative hyperalgesia. Low-dose naloxone can selectively reverse some adverse effects of opioids without compromising analgesia. We thus hypothesized that the intraoperative use of a high-dose remifentanil combined with a low-dose naloxone infusion reduces postoperative hyperalgesia compared with the use of remifentanil alone. Methods: Patients undergoing elective thyroid surgery were randomly assigned into one of three groups, depending on the intraoperative effect-site concentration of remifentanil, with or without a continuous infusion of naloxone: 4 ng ml-1 remifentanil with 0...
December 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28944983/oral-prolonged-release-oxycodone-naloxone-for-managing-pain-and-opioid-induced-constipation-a-review-of-the-evidence
#9
REVIEW
Bart J Morlion, Stefan A Mueller-Lissner, Renato Vellucci, Wojciech Leppert, Benoît C Coffin, Sara L Dickerson, Tony O'Brien
BACKGROUND: Opioids provide effective relief from moderate-to-severe pain and should be prescribed as part of a multifaceted approach to pain management when other treatments have failed. Fixed-dose oxycodone/naloxone prolonged-release tablets (OXN PR) were designed to address the opioid class effect of opioid-induced constipation (OIC) by combining the analgesic efficacy of oxycodone with the opioid receptor antagonist, naloxone, which has negligible systemic availability when administered orally...
September 25, 2017: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/28944554/limited-potential-of-cebranopadol-to-produce-opioid-type-physical-dependence-in-rodents
#10
Thomas M Tzschentke, Babette Y Kögel, Stefanie Frosch, Klaus Linz
Cebranopadol is a novel potent analgesic agonist at the nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors. As NOP receptor activation has been shown to reduce side effects related to the activation of μ-opioid peptide (MOP) receptors, the present study evaluated opioid-type physical dependence produced by cebranopadol in mice and rats. In a naloxone-precipitated withdrawal assay in mice, a regimen of seven escalating doses of cebranopadol over 2 days produced only very limited physical dependence as evidenced by very little withdrawal symptoms (jumping) even at cebranopadol doses clearly exceeding the analgesic dose range...
September 25, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28856406/panicolytic-like-effects-caused-by-substantia-nigra-pars-reticulata-pretreatment-with-low-doses-of-endomorphin-1-and-high-doses-of-ctop-or-the-nop-receptors-antagonist-jtc-801-in-male-rattus-norvegicus
#11
Juliana Almeida da Silva, Audrey Franceschi Biagioni, Rafael Carvalho Almada, Renato Leonardo de Freitas, Norberto Cysne Coimbra
RATIONALE: Gamma-aminobutyric acid (GABA)ergic neurons of the substantia nigra pars reticulata (SNpr) are connected to the deep layers of the superior colliculus (dlSC). The dlSC, in turn, connect with the SNpr through opioid projections. Nociceptin/orphanin FQ peptide (N/OFQ) is a natural ligand of a Gi protein-coupled nociceptin receptor (ORL1; NOP) that is also found in the SNpr. Our hypothesis is that tectonigral opioid pathways and intranigral orphanin-mediated mechanisms modulate GABAergic nigrotectal connections...
October 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28830119/confirmation-of-carfentanil-u-47700-and-other-synthetic-opioids-in-a-human-performance-case-by-lc-ms-ms
#12
Joshua Seither, Lisa Reidy
Recently, it has been documented that there has been a rise in synthetic opioid abuse. Synthetic opioids are compounds that were created to act as agonists for the opioid receptors. Like synthetic cannabinoids, most of these compounds were created by research groups or pharmaceutical companies in an attempt to find compounds that have medicinal use. Synthetic opioids have severe health implications when abused that can include hospitalization and death. Due to the high potency and the low dose required to produce the desired effects for these compounds, it was hypothesized that they may not be detectable in human performance case samples...
July 1, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28758123/peripheral-antinociception-induced-by-aripiprazole-is-mediated-by-the-opioid-system
#13
Renata Cristina Mendes Ferreira, Ana Flávia Almeida-Santos, Igor Dimitri Gama Duarte, Daniele C Aguiar, Fabricio A Moreira, Thiago Roberto Lima Romero
BACKGROUND: Aripiprazole is an antipsychotic drug used to treat schizophrenia and related disorders. Our previous study showed that this compound also induces antinociceptive effects. The present study aimed to assess the participation of the opioid system in this effect. METHODS: Male Swiss mice were submitted to paw pressure test and hyperalgesia was induced by intraplantar injection of prostaglandin E2 (PGE2, 2 μg). Aripiprazole was injected 10 min before the measurement...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28741741/addiction-related-interactions-of-pregabalin-with-morphine-in-mice-and-humans-reinforcing-and-inhibiting-effects
#14
Elena Vashchinkina, Ossi Piippo, Olga Vekovischeva, Evgeny Krupitsky, Ruslan Ilyuk, Nikholay Neznanov, Kirill Kazankov, Igor Zaplatkin, Esa R Korpi
The gabapentinoid pregabalin is a rapid-acting anxiolytic and analgesic, possibly suitable in supervised opioid detoxification. However, clinicians have been cautious in using it because of its unknown addictive risk and rising number of mortalities after pregabalin self-medication in opioid abusers. Here, we studied interactions of pregabalin and morphine on reward functions of the dopamine system in mice and the efficacy of pregabalin on withdrawal in opioid addicts. After the treatment of mice with pregabalin and morphine, we used electrophysiology to study neuroplasticity in midbrain slices, self-administration and conditioned place preference tests to investigate the rewarding potential of pregabalin and naloxone-precipitated morphine withdrawal to evaluate opioid withdrawal symptoms...
July 25, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28641363/a-phase-iii-randomized-controlled-study-on-the-efficacy-and-improved-bowel-function-of-prolonged-release-pr-oxycodone-naloxone-up-to-160-80-mg-daily-vs-oxycodone-pr
#15
D Dupoiron, A Stachowiak, O Loewenstein, A Ellery, W Kremers, B Bosse, M Hopp
BACKGROUND: Oxycodone/naloxone (OXN PR) is a prolonged-release formulation containing oxycodone and naloxone in a 2:1 ratio. This study aimed to evaluate the tolerability and efficacy of doses up to OXN160/80 mg PR compared with oxycodone prolonged-release formulation (OxyPR) in a randomised controlled trial. METHODS: Two hundred and forty-three patients were randomised to treatment with OXN PR (n = 123) or OxyPR (n = 120) during the 5-week double-blind study...
October 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28631527/buprenorphine-naloxone-versus-methadone-and-lofexidine-in-community-stabilisation-and-detoxification-a-randomised-controlled-trial-of-low-dose-short-term-opiate-dependent-individuals
#16
Fergus D Law, Alison M Diaper, Jan K Melichar, Simon Coulton, David J Nutt, Judy S Myles
Buprenorphine/naloxone, methadone and lofexidine are medications with utility in the treatment of opiate withdrawal. We report the first randomised controlled trial to compare the effects of these two medications on withdrawal symptoms and outcome during opiate induction/stabilisation and detoxification. A double-blind randomised controlled trial was conducted in an outpatient satellite clinic of a specialist drug service. Eighty opiate dependent individuals meeting DSM-IV criteria for opiate dependence, using ⩽ ½ g heroin smoked/chased or ¼ g heroin injected or ⩽ 30mg methadone, with ⩽ 3 years of opioid dependency, underwent a short-term opiate treatment programme involving induction/stabilisation on methadone 30mg or buprenorphine/naloxone 4mg/1mg, followed by detoxification (where the methadone group was assisted by lofexidine)...
June 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28597483/international-patent-applications-for-non-injectable-naloxone-for-opioid-overdose-reversal-exploratory-search-and-retrieve-analysis-of-the-patentscope-database
#17
REVIEW
Rebecca McDonald, Øyvind Danielsson Glende, Ola Dale, John Strang
ISSUES: Non-injectable naloxone formulations are being developed for opioid overdose reversal, but only limited data have been published in the peer-reviewed domain. Through examination of a hitherto-unsearched database, we expand public knowledge of non-injectable formulations, tracing their development and novelty, with the aim to describe and compare their pharmacokinetic properties. APPROACH: (i) The PatentScope database of the World Intellectual Property Organization was searched for relevant English-language patent applications; (ii) Pharmacokinetic data were extracted, collated and analysed; (iii) PubMed was searched using Boolean search query '(nasal OR intranasal OR nose OR buccal OR sublingual) AND naloxone AND pharmacokinetics'...
June 8, 2017: Drug and Alcohol Review
https://www.readbyqxmd.com/read/28594147/casein-kinase-1-epsilon-deletion-increases-mu-opioid-receptor-dependent-behaviors-and-binge-eating1
#18
L R Goldberg, S L Kirkpatrick, N Yazdani, K P Luttik, O A Lacki, R Keith Babbs, D F Jenkins, W Evan Johnson, C D Bryant
Genetic and pharmacological studies indicate that casein kinase 1 epsilon (Csnk1e) contributes to psychostimulant, opioid, and ethanol motivated behaviors. We previously used pharmacological inhibition to demonstrate that Csnk1e negatively regulates the locomotor stimulant properties of opioids and psychostimulants. Here, we tested the hypothesis that Csnk1e negatively regulates opioid and psychostimulant reward using genetic inhibition and the conditioned place preference assay in Csnk1e knockout mice. Similar to pharmacological inhibition, Csnk1e knockout mice showed enhanced opioid-induced locomotor activity with the mu opioid receptor agonist fentanyl (0...
September 2017: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/28559179/opioid-receptors-mediate-the-acquisition-but-not-the-expression-of-mitragynine-induced-conditioned-place-preference-in-rats
#19
Nurul H M Yusoff, Sharif M Mansor, Christian P Müller, Zurina Hassan
Mitragynine is the main psychoactive ingredient of the herbal drug preparation Kratom (Ketum), derived from the plant Mitragyna speciosa. Kratom is a widely abused drug in Southeast Asian and has a psychostimulant profile at low-medium doses, while high doses have opioidergic effects. Mitragynine was shown to possess opiate receptor affinity. However, its role in the behavioural effects of mitragynine is unclear. Here we asked whether the reinforcing effects of mitragynine are mediated by opiate receptors using a conditioned place preference (CPP) paradigm in rats...
August 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28553701/opioid-antagonists-with-minimal-sedation-for-opioid-withdrawal
#20
REVIEW
Linda Gowing, Robert Ali, Jason M White
BACKGROUND: Managed withdrawal is a necessary step prior to drug-free treatment or as the endpoint of long-term substitution treatment. OBJECTIVES: To assess the effects of opioid antagonists plus minimal sedation for opioid withdrawal. Comparators were placebo as well as more established approaches to detoxification, such as tapered doses of methadone, adrenergic agonists, buprenorphine and symptomatic medications. SEARCH METHODS: We updated our searches of the following databases to December 2016: CENTRAL, MEDLINE, Embase, PsycINFO and Web of Science...
May 29, 2017: Cochrane Database of Systematic Reviews
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