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https://www.readbyqxmd.com/read/28644085/pharmacokinetics-of-a-sustained-release-formulation-of-buprenorphine-after-intramuscular-and-subcutaneous-administration-to-american-kestrels-falco-sparverius
#1
David Sanchez-Migallon Guzman, Heather K Knych, Glenn H Olsen, Joanne R Paul-Murphy
Previous studies have validated the clinical use of opioids with μ-receptor affinities for pain management in raptors. Buprenorphine appears to have a longer duration of action and minimal adverse effects when compared to other opioids in American kestrels ( Falco sparverius ). To determine the pharmacokinetics of a sustained release formulation of buprenorphine in kestrels, we administered a commercially available product (Buprenorphine SR-LAB; Wildlife Pharmaceuticals, Windsor, CO, USA) intramuscularly and subcutaneously to adult kestrels in a partial-crossover experimental design study...
June 2017: Journal of Avian Medicine and Surgery
https://www.readbyqxmd.com/read/28623508/clinical-pharmacokinetic-characteristics-of-cebranopadol-a-novel-first-in-class-analgesic
#2
Elke Kleideiter, Chiara Piana, Shaonan Wang, Robert Nemeth, Michael Gautrois
BACKGROUND AND OBJECTIVES: Cebranopadol is a novel first-in-class analgesic acting as a nociceptin/orphanin FQ peptide and opioid peptide receptor agonist with central analgesic activity. It is currently in clinical development for the treatment of chronic pain conditions. This trial focuses on the clinical pharmacokinetic (PK) properties of cebranopadol after oral single- and multiple-dose administration. METHODS: The basic PK properties of cebranopadol were assessed by means of noncompartmental methods in six phase I clinical trials in healthy subjects and patients...
June 16, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28603935/the-effects-of-ketoconazole-and-cimetidine-on-the-pharmacokinetics-of-oral-tramadol-in-greyhound-dogs
#3
B KuKanich, K KuKanich, J Black
Tramadol is administered to dogs for analgesia but has variability in its extent of absorption, which may hinder its efficacy. Additionally, the active opioid metabolite (M1) occurs in low concentrations. The purpose of this study was to determine if administration of oral tramadol with suspected metabolism inhibitors (ketoconazole, cimetidine) would lead to improved bioavailability of tramadol and M1. Six healthy Greyhounds were included. They were administered tramadol orally and intravenously, M1 intravenously, oral tramadol with oral ketoconazole and oral tramadol with oral cimetidine...
June 11, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28589874/effects-of-time-and-storage-conditions-on-the-chemical-and-microbiologic-stability-of-diluted-buprenorphine-for-injection
#4
Johnathan M DenHerder, Ralph L Reed, Jennifer L Sargent, Gerd Bobe, Jan F Stevens, Helen E Diggs
Buprenorphine is a partial μ-opioid agonist used for analgesia. Due to the small size of laboratory rodents, buprenorphineHCl is typically diluted 10- or 20-fold with a sterile diluent, such as saline, for accurate dosing. Protocols for preparing andstoring diluted buprenorphine vary by institution, and little published information is available regarding stability andbeyond-use dating of specific buprenorphine preparations. The purpose of this study was to determine the chemical andmicrobiologic stability of diluted buprenorphine stored for a maximum of 180 d...
June 6, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28578919/opioid-consumption-and-pain-in-gynecological-cancer-patients-treated-with-interstitial-brachytherapy
#5
Lucas C Mendez, Stephen Choi, Laura D'Alimonte, Elizabeth Barnes, Lisa Barbera, Eric Leung
PURPOSE: Interstitial brachytherapy (ISBT) has advantages over the intracavitary techniques in the treatment of gynecological malignancies. The insertion of catheters into tumor enables higher dose conformality and normal tissue sparing. However ISBT can be associated with pain due its invasiveness. The goal of this study is to assess pain and opioid consumption of patients implanted with a perineal ISBT applicator. METHODS AND MATERIALS: Forty-eight patients were treated with ISBT from September 2014 to April 2016...
May 31, 2017: Brachytherapy
https://www.readbyqxmd.com/read/28560952/effects-of-time-and-storage-conditions-on-the-chemical-and-microbiologic-stability-of-diluted-buprenorphine-for-injection
#6
Ralph L Reed, Johnathan M DenHerder, Jennifer L Sargent, Gerd Bobe, J Fred Stevens, Helen E Diggs
Buprenorphine is a partial μ-opioid agonist used for analgesia. Due to the small size of laboratory rodents, buprenorphineHCl is typically diluted 10- or 20-fold with a sterile diluent, such as saline, for accurate dosing. Protocols for preparing andstoring diluted buprenorphine vary by institution, and little published information is available regarding stability and beyond-use dating of specific buprenorphine preparations. The purpose of this study was to determine the chemical and microbiologic stability of diluted buprenorphine stored for a maximum of 180 d...
May 30, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28542675/analgesic-effects-of-intravenous-acetaminophen-vs-placebo-for-endoscopic-sinus-surgery-and-postoperative-pain-a-randomized-clinical-trial
#7
Matthew A Tyler, Kent Lam, Faramarz Ashoori, Chunyan Cai, Joshua J Kain, Samer Fakhri, Martin J Citardi, Davide Cattano, Amber Luong
Importance: Intravenous acetaminophen is a commonly prescribed analgesic for the prevention and treatment of postsurgical pain. Its efficacy in the context of endoscopic sinus surgery (ESS) has yielded mixed results. Objective: To compare the efficacy of perioperative intravenous acetaminophen (IVAPAP) with that of placebo in improving early postoperative pain after endoscopic sinus surgery (ESS). Design, Setting, and Participants: A prospective, randomized clinical trial including 62 patients undergoing ESS for chronic rhinosinusitis in a single tertiary referral hospital...
May 25, 2017: JAMA Otolaryngology—Head & Neck Surgery
https://www.readbyqxmd.com/read/28530786/morphine-for-chronic-neuropathic-pain-in-adults
#8
REVIEW
Tess E Cooper, Junqiao Chen, Philip J Wiffen, Sheena Derry, Daniel B Carr, Dominic Aldington, Peter Cole, R Andrew Moore
BACKGROUND: Neuropathic pain, which is caused by a lesion or disease affecting the somatosensory system, may be central or peripheral in origin. Neuropathic pain often includes symptoms such as burning or shooting sensations, abnormal sensitivity to normally painless stimuli, or an increased sensitivity to normally painful stimuli. Neuropathic pain is a common symptom in many diseases of the nervous system. Opioid drugs, including morphine, are commonly used to treat neuropathic pain...
May 22, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28516342/pharmacokinetic-bioequivalence-studies-of-an-extended-release-oxycodone-hydrochloride-tablet-in-healthy-japanese-subjects-under-fasting-and-fed-conditions-without-an-opioid-antagonist
#9
Kaoru Toyama, Hidetoshi Furuie, Kana Kuroda, Hitoshi Ishizuka
Oxycodone is a semisynthetic opioid used for the treatment of moderate to severe pain. Two separate studies were conducted to assess the pharmacokinetic bioequivalence of a newly formulated oxycodone hydrochloride extended-release tablet to a marketed oxycodone product in Japan under fasting and fed conditions. Each study was a randomized, open-label, single-dose, single-center, two-period, two-way crossover study. Healthy male Japanese subjects received the oxycodone 10-mg products under fasting and fed conditions...
May 17, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28514508/methadone-for-neuropathic-pain-in-adults
#10
REVIEW
Ewan D McNicol, McKenzie C Ferguson, Roman Schumann
BACKGROUND: This review replaces an earlier review, "Methadone for chronic non-cancer pain in adults". This review serves to update the original and includes only studies of neuropathic pain. Methadone belongs to a class of analgesics known as opioids, that are considered the cornerstone of therapy for moderate-to-severe postsurgical pain and pain due to life-threatening illnesses; however, their use in neuropathic pain is controversial. Methadone has many characteristics that differentiate it from other opioids, which suggests that it may have a different efficacy and safety profile...
May 17, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28499616/effective-analgesic-doses-of-tramadol-or-tapentadol-induce-brain-lung-and-heart-toxicity-in-wistar-rats
#11
Juliana Faria, Joana Barbosa, Sandra Leal, Luís Pedro Afonso, João Lobo, Roxana Moreira, Odília Queirós, Félix Carvalho, Ricardo Jorge Dinis-Oliveira
Tramadol and tapentadol are extensively prescribed for the treatment of moderate to severe pain. Although these drugs are very effective in pain treatment, the number of intoxications and deaths due to both opioids is increasing, and the underlying toxic mechanisms are not fully understood. The present work aimed to study the potential biochemical and histopathological alterations induced by acute effective (analgesic) doses of tramadol and tapentadol, in Wistar rats. Forty-two male Wistar rats were divided into different groups: a control, administered with normal saline solution, and tramadol- or tapentadol-treated groups (10, 25 or 50mg/kg - typical effective analgesic dose, intermediate and maximum recommended doses, respectively)...
June 15, 2017: Toxicology
https://www.readbyqxmd.com/read/28474460/long-term-efficacy-and-safety-of-oxycodone-naloxone-prolonged-release-formulation-up-to-180-90-mg-daily-results-of-the-open-label-extension-phase-of-a-phase-iii-multicenter-multiple-dose-randomized-controlled-study
#12
D Dupoiron, A Stachowiak, O Loewenstein, A Ellery, W Kremers, B Bosse, M Hopp
BACKGROUND: The inclusion of naloxone with oxycodone in a fixed combination prolonged-release formulation (OXN PR) improves bowel function compared with oxycodone (Oxy) alone without compromising analgesic efficacy. In a recent 5-week, randomized, double-blind comparative trial of OXN PR and OxyPR, it could be shown that the beneficial properties of OXN PR extend to doses up to 160/80 mg. METHODS: Bowel function, pain, quality of life (QoL) and safety of OXN PR up to 180/90 mg daily were evaluated in a 24-week open-label extension phase of the 5-week randomized comparative study in patients with non-malignant or malignant pain requiring opioids and suffering from opioid-induced constipation...
May 4, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28469535/association-between-deep-sedation-from-continuous-intravenous-sedatives-and-extubation-failures-in-mechanically-ventilated-patients-in-the-pediatric-intensive-care-unit
#13
Jennifer M Schultheis, Travis S Heath, David A Turner
OBJECTIVE: The primary objective of this study was to determine whether an association exists between deep sedation from continuous infusion sedatives and extubation failures in mechanically ventilated children. Secondary outcomes evaluated risk factors associated with deep sedation. METHODS: This was a retrospective cohort study conducted between January 1, 2009, and October 31, 2012, in the pediatric intensive care unit (PICU) at Duke Children's Hospital. Patients were included in the study if they had been admitted to the PICU, had been mechanically ventilated for ≥48 hours, and had received at least one continuous infusion benzodiazepine and/or opioid infusion for ≥24 hours...
March 2017: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/28468518/buprenorphine-for-the-treatment-of-the-neonatal-abstinence-syndrome
#14
RANDOMIZED CONTROLLED TRIAL
Walter K Kraft, Susan C Adeniyi-Jones, Inna Chervoneva, Jay S Greenspan, Diane Abatemarco, Karol Kaltenbach, Michelle E Ehrlich
BACKGROUND: Current pharmacologic treatment of the neonatal abstinence syndrome with morphine is associated with a lengthy duration of therapy and hospitalization. Buprenorphine may be more effective than morphine for this indication. METHODS: In this single-site, double-blind, double-dummy clinical trial, we randomly assigned 63 term infants (≥37 weeks of gestation) who had been exposed to opioids in utero and who had signs of the neonatal abstinence syndrome to receive either sublingual buprenorphine or oral morphine...
June 15, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28451875/prevalence-of-gabapentin-abuse-comparison-with-agents-with-known-abuse-potential-in-a-commercially-insured-us-population
#15
Alyssa M Peckham, Kathleen A Fairman, David A Sclar
BACKGROUND: Despite international calls to make gabapentin a controlled substance, studies of gabapentin use/abuse patterns are limited to small/high-risk samples and adverse event reports. OBJECTIVE: The aim of this study was to conduct a systematic assessment of the abuse potential/prevalence of gabapentin in a large sample. DATA SOURCE: Truven Health MarketScan(®) Commercial Claims and Encounters database, years 2013-2015. ELIGIBILITY CRITERIA: Patients with two or more claims for one or more abusable drugs and ≥12 months' continuous enrollment were sampled for Lorenz curve analysis...
April 27, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28444856/pharmacokinetics-after-a-single-dose-of-naloxone-administered-as-a-nasal-spray-in-healthy-volunteers
#16
E Vanky, L Hellmundt, U Bondesson, S Eksborg, S Lundeberg
BACKGROUND: There is increasing interest in the use of intranasal naloxone to reverse adverse opioid effects during management of procedural pain in children and in adults after overdose. There are limited data on the pharmacokinetics of intranasal naloxone so in this study we aimed to detail the pharmacokinetic profile of the commercially marketed injectable solution of naloxone 0.4 mg/ml when administered as an intranasal spray. METHODS: Twenty healthy volunteers received naloxone as an intranasal spray at a dose of 10 μg/kg...
July 2017: Acta Anaesthesiologica Scandinavica
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
#17
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/28416993/antinociceptive-effect-of-intrathecal-sec-o-glucosylhamaudol-on-the-formalin-induced-pain-in-rats
#18
Sang Hun Kim, Hwa Song Jong, Myung Ha Yoon, Seon Hee Oh, Ki Tae Jung
BACKGROUND: The root of Peucedanum japonicum Thunb., a perennial herb found in Japan, the Philippines, China, and Korea, is used as an analgesic. In a previous study, sec-O-glucosylhamaudol (SOG) showed an analgesic effect. This study was performed to examine the antinociceptive effect of intrathecal SOG in the formalin test. METHODS: Male Sprague-Dawley rats were implanted with an intrathecal catheter. Rats were randomly treated with a vehicle and SOG (10 µg, 30 µg, 60 µg, and 100 µg) before formalin injection...
April 2017: Korean Journal of Pain
https://www.readbyqxmd.com/read/28412373/mechanistic-evaluation-of-tapentadol-in-reducing-the-pain-perception-using-in-vivo-brain-and-spinal-cord-microdialysis-in-rats
#19
Vijay Benade, Ramakrishna Nirogi, Gopinadh Bhyrapuneni, Saivishal Daripelli, Ganesh Ayyanki, Shantaveer Irappanavar, Ranjithkumar Ponnamaneni, Arunkumar Manoharan
Role of monoamine neurotransmitters in the modulation of emotional and pain processing in spinal cord and brain regions is not well known. Tapentadol, a norepinephrine reuptake inhibitor with µ-opioid receptor agonistic activity has recently been introduced for the treatment of moderate to severe pain. The objective of the present study was to examine the effects of tapentadol on modulation of monoamines in the prefrontal cortex and dorsal horn using brain microdialysis. Tapentadol was administered intraperitoneally at 4...
April 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28361412/study-of-%C3%AE-and-%C3%AE-opioid-activities-in-agents-with-various-%C3%AE%C2%BA-receptor-selectivity
#20
O Yu Grechko, R A Litvinov, A A Spasov, A I Rashchenko, D M Shtareva, V A Anisimova, V I Minkin
A putative opioid agonist RU-1205 was ineffective within in vitro model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC50=2.6×10(-7) M. In vivo experiments revealed no significant effects of RU-1205 on respiration and gastrointestinal tract contractile activity. In contrast, butorphanol decreased respiration rate by 25% (25-100 mg/kg) and slowed down the transit of labeled particles along the small intestine by 77...
March 30, 2017: Bulletin of Experimental Biology and Medicine
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