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Opioid dosing

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https://www.readbyqxmd.com/read/27922029/safety-of-eluxadoline-in-patients-with-irritable-bowel-syndrome-with-diarrhea
#1
Brooks D Cash, Brian E Lacy, Philip S Schoenfeld, Leonard S Dove, Paul S Covington
OBJECTIVES: Eluxadoline is a mixed μ-opioid receptor (OR) and κ-OR agonist and δ-OR antagonist, approved for the treatment of irritable bowel syndrome with diarrhea (IBS-D). This analysis evaluated the safety and tolerability of eluxadoline 75 and 100 mg twice daily (BID) in one Phase 2 (IBS-2001) and two Phase 3 (IBS-3001 and IBS-3002) studies. METHODS: Adults with IBS-D (Rome III criteria) were randomized to placebo or eluxadoline (75 or 100 mg) BID for 12 (IBS-2001), 26 (IBS-3002), or 52 (IBS-3001) weeks...
December 6, 2016: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/27918873/loperamide-the-poor-man-s-methadone-brief-review
#2
Cornel N Stanciu, Samantha A Gnanasegaram
Loperamide is widely available as an inexpensive, over-the-counter remedy commonly used for management of diarrhea. Although an opioid, at therapeutic doses it acts primarily on the gastrointestinal tissues; however, larger than recommended amounts facilitate central nervous system (CNS) penetration. Such high doses of loperamide have recently gained popularity among users of opioids to manage withdrawal symptomatology and, less frequently, to achieve psychoactive effects. Chronic loperamide use can result in development of tolerance and, upon abrupt cessation of use, withdrawal...
December 5, 2016: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/27916366/rubus-occidentalis-analgesic-effect-in-a-rat-model-of-incisional-pain
#3
Geun Joo Choi, Hyun Kang, Won Joong Kim, Ji Wung Kwon, Beom Gyu Kim, Yoo Shin Choi, Young Joo Cha, Jin Soo Ko
BACKGROUND: The purpose of this study was to evaluate the analgesic effect of Rubus occidentalis extract (ROE) in a rat model of incisional pain. The involved mechanisms and proinflammatory cytokine response were also examined. MATERIALS AND METHODS: To investigate the analgesic effect, rats were intraperitoneally administered with normal saline or various doses of ROE before or after a plantar incision. To evaluate the involved mechanism, rats were intraperitoneally administered yohimbine, dexmedetomidine, prazosin, naloxone, atropine, or mecamylamine after a plantar incision; ROE was then administered intraperitoneally...
November 2016: Journal of Surgical Research
https://www.readbyqxmd.com/read/27909965/correction-of-negative-effect-of-antenatal-hypoxia-on-liver-tissue-homeostasis-in-newborn-albino-rats-with-opioid-peptides
#4
O G Pinaeva, E N Sazonova, O A Lebed'ko, S S Timoshin
We studied the possibility of correction of the negative effects of antenatal hypoxia on the liver tissue homeostasis in 7-day-old albino rats by administration of opioid peptides in a dose of 100 μg/kg on postnatal days 2-6. Administration of mixed μ/δ-opioid receptor agonist Dalargin neutralized deviations of gravimetric indicators, parameters of proliferative activity, and activity of the nucleolar apparatus of hepatocytes. Administration of the non-opiate Leu-enkephalin analogue did not normalize gravimetric parameters and nucleolar apparatus parameters, however, it significantly increased the pool of proliferating hepatocytes...
December 2, 2016: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/27908840/prescription-opioid-taper-support-for-outpatients-with-chronic-pain-a-randomized-controlled-trial
#5
Mark D Sullivan, Judith A Turner, Cory DiLodovico, Angela D'Appolonio, Kari Stephens, Ya-Fen Chan
Patients receiving long-term opioid therapy for chronic pain and interested in tapering their opioid dose were randomly assigned to a 22-week taper support intervention (psychiatric consultation, opioid dose tapering, and 18 weekly meetings with a physician assistant to explore motivation for tapering and learn pain self-management skills) or usual care (N=35). Assessments were conducted at baseline and 22 and 34 weeks after randomization. Using an intention-to-treat approach, we constructed linear regression models to compare groups at each follow-up...
November 28, 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/27905916/study-protocol-a-dose-escalating-phase-2-study-of-oral-lisdexamfetamine-in-adults-with-methamphetamine-dependence
#6
Nadine Ezard, Adrian Dunlop, Brendan Clifford, Raimondo Bruno, Andrew Carr, Alexandra Bissaker, Nicholas Lintzeris
BACKGROUND: The treatment of methamphetamine dependence is a continuing global health problem. Agonist type pharmacotherapies have been used successfully to treat opioid and nicotine dependence and are being studied for the treatment of methamphetamine dependence. One potential candidate is lisdexamfetamine, a pro-drug for dexamphetamine, which has a longer lasting therapeutic action with a lowered abuse potential. The purpose of this study is to determine the safety of lisdexamfetamine in this population at doses higher than those currently approved for attention deficit hyperactivity disorder or binge eating disorder...
December 1, 2016: BMC Psychiatry
https://www.readbyqxmd.com/read/27903642/behavioral-characterization-of-kappa-opioid-receptor-agonist-spiradoline-and-cannabinoid-receptor-agonist-cp55940-mixtures-in-rats
#7
Vanessa Minervini, Sujata S Dahal, Charles France
Pain is a significant clinical problem and there is a need for more effective treatments with reduced adverse effects that currently limit the use of mu opioid receptor agonists. Synthetic kappa opioid receptor agonists have no abuse liability and well-documented antinociceptive effects; however, adverse effects (diuresis, dysphoria) preclude their use in the clinic. Combining kappa opioids with non-opioid drugs (cannabinoid receptor agonists) allows for smaller doses of each drug to produce antinociception...
November 30, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27902670/ketamine-infusion-for-pain-control-in-acute-pediatric-sickle-cell-painful-crises
#8
Jonathan M Hagedorn, Evelyn C Monico
OBJECTIVES: Sickle cell disease is the most common hemoglobin variant in the world and can present with recurrent vaso-occlusive painful crises. Pain control in these patients is often difficult and requires a multimodal approach. In patients with uncontrolled pain after traditional pain control methods, ketamine infusions have proven beneficial. Unfortunately, no source alone had described ketamine infusions for pediatric sickle cell patients. Our objective was to provide a thorough definitive reference for health care providers regarding the use of ketamine infusion for pain control in pediatric sickle cell painful crises...
November 29, 2016: Pediatric Emergency Care
https://www.readbyqxmd.com/read/27901359/buprenorphine-transdermal-system-utilization
#9
Laura Wallace, Aditi Kadakia
OBJECTIVES: To evaluate utilization patterns in patients initiating buprenorphine transdermal system (BTDS), CIII, and estimate the proportion decreasing their total opioid dose over time. METHODS: This retrospective cohort study used data from the Truven Health Analytics MarketScan® Commercial Claims and Encounters Database from January 1, 2011 through December 31, 2015. Eligible individuals were adults aged 18-64 years newly dispensed BTDS (index prescription) who had at least six months of insurance coverage prior to (baseline period) and following (study period) the index prescription...
November 30, 2016: Postgraduate Medicine
https://www.readbyqxmd.com/read/27899254/thalidomide-attenuates-the-development-and-expression-of-antinociceptive-tolerance-to-%C3%AE-opioid-agonist-morphine-through-l-arginine-inos-and-nitric-oxide-pathway
#10
Muhammad Imran Khan, Sattar Ostadhadi, Faiza Mumtaz, Majid Momeny, Farima Moghaddaskho, Mahsa Hassanipour, Shahram Ejtemaei-Mehr, Ahmad Reza Dehpour
Morphine is a μ-opioid analgesic drug which is used in the treatment and management of chronic pain. However, due to development of antinociceptive tolerance its clinical use is limited. Thalidomide is an old glutamic acid derivative which recently reemerged because of its potential to counteract a number of disorders including neurodegenerative disorders. The potential underlying mechanisms and effects of thalidomide on morphine-induced antinociceptive tolerance is still elusive. Hence, the present study was designed to explore the effect of thalidomide on the development and expression of morphine antinociceptive tolerance targeting l-arginine-nitric oxide (NO) pathway in mice and T98G human glioblastoma cell line...
November 26, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27898458/smoking-status-and-opioid-related-problems-and-concerns-among-men-and-women-on-chronic-opioid-therapy
#11
Kelly C Young-Wolff, Daniella Klebaner, Constance Weisner, Michael Von Korff, Cynthia I Campbell
OBJECTIVES: Smokers on chronic opioid therapy for non-cancer pain use prescription opioids at higher dosages and are at increased risk for opioid misuse and dependence relative to non-smokers. The current study aims to assess whether smoking is associated with problems and concerns with chronic opioid therapy from the perspective of the patient. METHODS: In a large sample (N=972) of adult patients prescribed opioids for chronic noncancer pain, we examined sex-specific associations between smoking status and patient perceptions of problems and concerns with chronic opioid therapy using regression analyses, adjusting for covariates...
November 28, 2016: Clinical Journal of Pain
https://www.readbyqxmd.com/read/27896372/opioid-receptor-agonists-may-favorably-affect-bone-mechanical-properties-in-rats-with-estrogen-deficiency-induced-osteoporosis
#12
Aleksandra Janas, Joanna Folwarczna
The results of epidemiological, clinical, and in vivo and in vitro experimental studies on the effect of opioid analgesics on bone are inconsistent. The aim of the present study was to investigate the effect of morphine (an agonist of opioid receptors), buprenorphine (a partial μ opioid receptor agonist and κ opioid receptor antagonist), and naloxone (an antagonist of opioid receptors) on the skeletal system of female rats in vivo. The experiments were carried out on 3-month-old Wistar rats, divided into two groups: nonovariectomized (intact; NOVX) rats and ovariectomized (OVX) rats...
November 28, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27896019/naloxone-and-metabolites-quantification-in-cord-blood-of-prenatally-exposed-newborns-and-correlations-with-maternal-concentrations
#13
Samantha L Wiegand, Madeleine J Swortwood, Marilyn A Huestis, John Thorp, Hendreé E Jones, Neeta L Vora
Objective To quantify naloxone and metabolite concentrations in newborns prenatally exposed to sublingual buprenorphine/naloxone and to correlate neonatal and maternal metabolite concentrations. Methods This is a prospective observational cohort study. Eleven pregnant women treated for opioid use disorder with sublingual buprenorphine/naloxone were enrolled. Maternal and newborn blood was collected and analyzed for naloxone, buprenorphine, and metabolites via liquid chromatography tandem mass spectrometry...
October 2016: American Journal of Perinatology Reports
https://www.readbyqxmd.com/read/27893881/ultra-high-dose-opioids-with-low-efficacy-and-significant-harm-time-to-make-a-change-a-teachable-moment
#14
Paul Guillod, Ellen L Edens, William C Becker
No abstract text is available yet for this article.
November 28, 2016: JAMA Internal Medicine
https://www.readbyqxmd.com/read/27890744/gene-expression-of-pro-opiomelanocortin-and-melanocortin-receptors-is-regulated-in-the-hypothalamus-and-mesocorticolimbic-system-following-nicotine-administration
#15
Damla E Tapinc, Rabia Ilgin, Egemen Kaya, Oguz Gozen, Muzeyyen Ugur, Ersin O Koylu, Lutfiye Kanit, Aysegul Keser, Burcu Balkan
Pro-opiomelanocortin (POMC)-derived peptides and their receptors have been shown to play important roles in natural and drug-induced reward and reinforcement. Reward process may involve the regulation of POMC gene expression and the gene expression of POMC-derived peptide receptors. The present study investigated the alterations observed in the transcript levels of POMC, melanocortin 3 (MC3R), melanocortin 4 (MC4R) and mu-opioid receptors (MOR) in the hypothalamus and mesocorticolimbic system during nicotine exposure...
November 24, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27890625/pharmacological-treatment-optimization-for-stable-chronic-obstructive-pulmonary-disease-proposals-from-the-soci%C3%A3-t%C3%A3-de-pneumologie-de-langue-fran%C3%A3-aise
#16
M Zysman, F Chabot, P Devillier, B Housset, C M Panzini, N Roche
The Société de Pneumologie de Langue Française proposes a decision algorithm on long-term pharmacological COPD treatment. A working group reviewed the literature published between January 2009 and May 2016. This document lays out proposals and not guidelines. It only focuses on pharmacological treatments except vaccinations, smoking cessation treatments and oxygen therapy. Any COPD diagnosis, based on pulmonary function tests, should lead to recommend smoking cessation, vaccinations, physical activity, pulmonary rehabilitation in case of activity limitation, and short-acting bronchodilators...
November 24, 2016: Revue des Maladies Respiratoires
https://www.readbyqxmd.com/read/27890602/the-endocannabinoid-hydrolysis-inhibitor-sa-57-intrinsic-antinociceptive-effects-augmented-morphine-induced-antinociception-and-attenuated-heroin-seeking-behavior-in-mice
#17
Jenny L Wilkerson, Sudeshna Ghosh, Mohammed Mustafa, Rehab A Abdullah, Micah J Niphakis, Roberto Cabrera, Rafael L Maldonado, Benjamin F Cravatt, Aron H Lichtman
Although opioids are highly efficacious analgesics, their abuse potential and other untoward side effects diminish their therapeutic utility. The addition of non-opioid analgesics offers a promising strategy to reduce required antinociceptive opioid doses that concomitantly reduce opioid-related side effects. Inhibitors of the primary endocannabinoid catabolic enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) show opioid-sparing effects in preclinical models of pain. As simultaneous inhibition of these enzymes elicits enhanced antinociceptive effects compared with single enzyme inhibition, the present study tested whether the dual FAAH-MAGL inhibitor SA-57 [4-[2-(4-chlorophenyl)ethyl]-1-piperidinecarboxylic acid 2-(methylamino)-2-oxoethyl ester] produces morphine-sparing antinociceptive effects, without major side effects associated with either drug class...
November 24, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27890601/tramadol-effects-on-sexual-behavior-in-male-rats-are-mainly-caused-by-its-5-ht-reuptake-blocking-effects
#18
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/27885425/intrathecal-morphine-versus-intravenous-opioid-administration-to-impact-postoperative-analgesia-in-hepato-pancreatic-surgery-a-randomized-controlled-trial
#19
Sara Dichtwald, Menahem Ben-Haim, Laila Papismedov, Shoshana Hazan, Anat Cattan, Idit Matot
PURPOSE: Inadequate analgesia following abdominal surgery may affect outcome. Data in patients undergoing liver surgery suggested that postoperative coagulopathy might delay epidural catheter removal. Thus, alternative analgesic techniques should be evaluated. METHODS: We compared the analgesic efficacy of intraoperative intrathecal morphine [single injection 4 µg/kg before skin incision (ITM group, n = 23)] to intravenous opioids [iv remifentanil infusion during surgery followed by i...
November 24, 2016: Journal of Anesthesia
https://www.readbyqxmd.com/read/27884758/magnesium-enhances-opioid-induced-analgesia-what-we-have-learnt-in-the-past-decades
#20
REVIEW
Magdalena Bujalska-Zadrożny, Jan Tatarkiewicz, Kamila Kulik, Małgorzata Filip, Marek Naruszewicz
Opioids are increasingly used in alleviating pain, including cancer-related pain and postoperative pain. Unfortunately, the development of tolerance, the resistance of neuropathic pain on opioid analgesia or other undesirable effects may limit their utility. In order to reduce opioid doses, and thereby to avoid the risk of side effects and sudden deaths due to overdosing, attempts have been made to introduce co-analgesics. Due to an increasing amount of data concerning a potential enhance of opioid analgesia by the physiological antagonist of N-methyl-d-aspartate receptors, magnesium ions (Mg(2+)), a concomitant use of such a combination seems to be interesting from a clinical point of view...
November 21, 2016: European Journal of Pharmaceutical Sciences
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