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Methylnaltrexone

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https://www.readbyqxmd.com/read/28580486/the-role-of-endogenous-opioid-system-in-the-regulation-of-heart-tolerance-to-stress-induced-damage
#1
Yu B Lishmanov, S Yu Tsibul'nikov, N V Naryzhnaya, M V Korobov, L N Maslov
In Wistar rats, stress was modeled by 24-h immobilization in a supine posture and stress-induced damage to the heart was assessed by accumulation of (99m)Tc-pyrophosphate in the myocardium. The intensity of stress reaction was measured by serum levels of cortisol and insulin. Both stressinduced damage to the heart and intensity of stress reaction were examined under control conditions and in rats treated with opioid receptor antagonists naltrexone, methylnaltrexone bromide, MR2266, and ICI174.864. Activation of central μ-opioid receptors with endogenous opioids aggravated stress-induced cardiomyopathy, while stimulation of peripheral μ-opioid receptors produced a cardioprotective effect...
June 3, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28554659/naloxegol-an-opioid-antagonist-with-reduced-cns-penetration-mode-of-action-and-human-relevance-for-rat-testicular-tumours
#2
Håkan Andersson, Terri Mitchard, Nakpangi Johnson, Eike Floettmann
Naloxegol is an opioid antagonist which has been developed for the treatment of patients with opioid induced constipation. In the nonclinical safety program naloxegol was shown to have a very benign toxicity profile. In the rat, but not the mouse, 2-year carcinogenicity study a change in tumour pattern with an increase in testicular Leydig cell tumours (LCT) was observed after dosing at high (supra-pharmacological) concentrations. To establish the basis of the increase in LCT and to assess its potential relevance to humans, studies to exclude and potentially identify mode-of-action (MoA) were performed...
May 26, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28554003/opioids-and-opioid-receptors-orchestrate-wound-repair
#3
Ying Wang, Mihir Gupta, Tasneem Poonawala, Mariya Farooqui, Yunfang Li, Fei Peng, Sheldon Rao, Michael Ansonoff, John E Pintar, Kalpna Gupta
We have previously shown that topical opioids including morphine and its congeners promote healing of full thickness ischemic wounds in rats. We examined the contribution of mu opioid receptor (MOPr)-mediated healing of full thickness ischemic wounds using MOPr and delta or kappa opioid receptor knockout (KO) mice. Wound closure in the early (day 5) as well as later phases was delayed in topical morphine or PBS-treated MOPr-KO mice compared with reciprocal treatments of wounds in wild-type (WT) mice. MOPr expression was significantly upregulated at 30 min in the wound margins and colocalized with wound margins and vasculature in the epidermal and dermal layers of the skin...
May 18, 2017: Translational Research: the Journal of Laboratory and Clinical Medicine
https://www.readbyqxmd.com/read/28502630/new-opioid-receptor-antagonist-naltrexone-14-o-sulfate-synthesis-and-pharmacology
#4
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/28423917/management-of-opioid-induced-constipation-in-hospice-patients
#5
Leah Sera, Mary Lynn McPherson
BACKGROUND: Constipation is a common symptom in patients with advanced disease taking opioids. Opioid-induced constipation (OIC) is commonly treated with laxatives and stool softeners. Recently, newer agents have come to market which broaden options for patients in whom first-line therapies are not effective. OBJECTIVE: To determine what pharmacologic regimens are currently used in hospice programs to prevent and treat OIC, whether those regimens have changed with the introduction of newer agents and evidence discouraging the use of docusate, and whether hospice programs are standardizing the management of OIC...
January 1, 2017: American Journal of Hospice & Palliative Care
https://www.readbyqxmd.com/read/28363231/-management-of-adverse-effects-of-opioid-therapy
#6
Stefan Wirz
More than 6 million people in Germany suffer from chronic pain which greatly impairs their wellbeing. Often the only therapeutic option is to use class 2 or 3 analgesic opioids in the WHO classification, as class 1 analgesics may be toxic or of limited efficacy. However, the high incidence of opioid side effects leads to high discontinuation rates. Thus, the success of opioid treatment is also highly dependent on the management of the safety and tolerability of the treatment. Most opioid side effects, such as nausea and sedation, predominantly occur in the initial phase of therapy...
April 2017: Zeitschrift Für Gastroenterologie
https://www.readbyqxmd.com/read/28315644/effects-of-buprenorphine-methylnaltrexone-and-their-combination-on-gastrointestinal-transit-in-healthy-new-zealand-white-rabbits
#7
Manuel Martin-Flores, Bhupinder Singh, Courtney A Walsh, Elizabeth P Brooks, Lacic Taylor, Lisa M Mitchell
Among the many analgesic agents available, buprenorphine appears to be the analgesic used most often in rabbits. Unfortunately, deleterious side effects of opioids, such as gastrointestinal stasis and anorexia, may discourage the use of these agents. Methylnaltrexone is a peripheral opioid antagonist that ameliorates opioid-induced gastrointestinal stasis in others species yet preserves the analgesic effects of buprenorphine. We evaluated whether methylnaltrexone reversed buprenorphine-induced gastrointestinal stasis in 8 healthy male New Zealand White rabbits...
March 1, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28176913/peripherally-acting-%C3%AE-opioid-receptor-antagonists-as-treatment-options-for-constipation-in-noncancer-pain-patients-on-chronic-opioid-therapy
#8
REVIEW
Joseph V Pergolizzi, Robert B Raffa, Marco Pappagallo, Charles Fleischer, Joseph Pergolizzi, Gianpietro Zampogna, Elizabeth Duval, Janan Hishmeh, Jo Ann LeQuang, Robert Taylor
Opioid-induced constipation (OIC), a prevalent and distressing side effect of opioid therapy, does not reliably respond to treatment with conventional laxatives. OIC can be a treatment-limiting adverse event. Recent advances in medications with peripherally acting μ-opioid receptor antagonists, such as methylnaltrexone, naloxegol, and alvimopan, hold promise for treating OIC and thus extending the benefits of opioid analgesia to more chronic pain patients. Peripherally acting μ-opioid receptor antagonists have been clinically tested to improve bowel symptoms without compromise to pain relief, although there are associated side effects, including abdominal pain...
2017: Patient Preference and Adherence
https://www.readbyqxmd.com/read/28168885/methylnaltrexone-versus-naloxone-for-opioid-induced-constipation-in-the-medical-intensive-care-unit
#9
Cristian Merchan, Diana Altshuler, John Papadopoulos
BACKGROUND: Opioid-induced constipation (OIC) is common in critically ill patients; it leads to complications that can increase hospital stay and, rarely, bowel perforation. Opioid antagonists are considered a logical approach to treat OIC; however, the agent of choice has yet to be determined. OBJECTIVE: To assess the effectiveness and safety of enteral naloxone (NTX) versus subcutaneous methylnaltrexone (MNTX) for the treatment of OIC in the medical intensive care unit...
March 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28162731/-480-oral-methylnaltrexone-does-not-negatively-impact-analgesia-in-patients-with-opioid-induced-constipation-and-chronic-noncancer-pain
#10
L Webster, J Peppin, J Harper, R Israel
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28155805/effects-of-buprenorphine-methylnaltrexone-and-their-combination-on-gastrointestinal-transit-in-healthy-new-zealand-white-rabbits
#11
Manuel Martin-Flores Bhupinder Singh Courtney A Walsh Elizabeth P Brooks Laci C Taylor And Lisa M Mitchell
Among the many analgesic agents available, buprenorphine appears to be the analgesic used most often in rabbits. Unfortunately,deleterious side effects of opioids, such as gastrointestinal stasis and anorexia, may discourage the use of these agents.Methylnaltrexone is a peripheral opioid antagonist that ameliorates opioid-induced gastrointestinal stasis in others species yet preserves the analgesic effects of buprenorphine. We evaluated whether methylnaltrexone reversed buprenorphine-inducedgastrointestinal stasis in 8 healthy male New Zealand White rabbits...
February 2, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28110513/effect-of-methylnaltrexone-and-naloxone-on-esophageal-motor-function-in-man
#12
E Scarpellini, A Pauwels, R Vos, N Rommel, J Tack
BACKGROUND: Endogenous opioids (EO) acting on μ-opiod receptors in central and enteric nervous system (ENS) control gastrointestinal motility but it is still unclear whether EO in ENS may control esophageal function in man, thus we will study the effects of methylnaltrexone (MNTX), a peripherally selective, and naloxone (NA), a non-selective μ-opiod receptor antagonist, on esophageal motility in healthy subjects. METHODS: Fifteen HV (6 M; 34.1 ± 0.6 years; BMI: 22...
March 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28092666/loss-of-%C3%AE-opioid-receptor-signaling-in-nociceptors-but-not-microglia-abrogates-morphine-tolerance-without-disrupting-analgesia
#13
Gregory Corder, Vivianne L Tawfik, Dong Wang, Elizabeth I Sypek, Sarah A Low, Jasmine R Dickinson, Chaudy Sotoudeh, J David Clark, Ben A Barres, Christopher J Bohlen, Grégory Scherrer
Opioid pain medications have detrimental side effects including analgesic tolerance and opioid-induced hyperalgesia (OIH). Tolerance and OIH counteract opioid analgesia and drive dose escalation. The cell types and receptors on which opioids act to initiate these maladaptive processes remain disputed, which has prevented the development of therapies to maximize and sustain opioid analgesic efficacy. We found that μ opioid receptors (MORs) expressed by primary afferent nociceptors initiate tolerance and OIH development...
February 2017: Nature Medicine
https://www.readbyqxmd.com/read/27928191/defibrotide
#14
Danial E Baker, Kendra Demaris
Each month, subscribers to The Formulary Monograph Service receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing in-services. A comprehensive target drug utilization evaluation/medication use evaluation (DUE/MUE) is also provided each month. With a subscription, the monographs are are available online to subscribers...
November 2016: Hospital Pharmacy
https://www.readbyqxmd.com/read/27860208/randomized-double-blind-trial-of-oral-methylnaltrexone-for-the-treatment-of-opioid-induced-constipation-in-patients-with-chronic-noncancer-pain
#15
Richard Rauck, Neal E Slatkin, Nancy Stambler, Joseph R Harper, Robert J Israel
BACKGROUND: Subcutaneous methylnaltrexone, a peripherally acting μ-opioid receptor antagonist, improves opioid-induced constipation (OIC) in patients with chronic noncancer pain. An oral methylnaltrexone formulation has been developed. METHODS: In this phase 3, double-blind trial, adults with chronic noncancer pain receiving opioid doses of ≥ 50 mg/day oral morphine equivalents with OIC were randomly assigned to oral methylnaltrexone (150, 300, or 450 mg) or placebo once daily (QD) for 4 weeks followed by as-needed dosing for 8 weeks...
November 17, 2016: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/27730272/effects-of-repeated-morphine-on-ultrasonic-vocalizations-in-adult-rats-increased-50-khz-call-rate-and-altered-subtype-profile
#16
Laura M Best, Leah L Zhao, Tina Scardochio, Paul B S Clarke
RATIONALE: Adult rat 50-kHz vocalizations have been proposed to indicate a positive affective state, putatively revealed by a predominance of trill calls over flat calls. However, short-term exposure to non-sedative doses of the euphorigen morphine suppresses calling, with no discernible shift in trill or flat call prevalence. OBJECTIVES: This study aimed to determine whether morphine acutely increases 50-kHz call rates or alters the relative prevalence of trill or flat calls, after long-term morphine exposure or acute pharmacological pretreatment...
January 2017: Psychopharmacology
https://www.readbyqxmd.com/read/27676559/p2-23-effectiveness-of-methylnaltrexone-bromide-as-a-treatment-for-opioid-induced-constipation-in-nsclc-patients-track-supportive-care-and-others
#17
Ioannis A Dimitroulis, Panagiota Stamou, Adamantia Liapikou, Michail Toumbis
No abstract text is available yet for this article.
October 2016: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/27628064/phase-ii-trial-of-subcutaneous-methylnaltrexone-in-the-treatment-of-severe-opioid-induced-constipation-oic-in-cancer-patients-an-exploratory-study
#18
MULTICENTER STUDY
Masanori Mori, Yongli Ji, Santosh Kumar, Takamaru Ashikaga, Steven Ades
BACKGROUND: Methylnaltrexone is a peripherally acting mu-opioid receptor antagonist that has been shown to relieve severe opioid-induced constipation (OIC) in patients with advanced disease receiving palliative care. Its efficacy remains unknown in cancer patients who are not terminally ill. The primary aim of this study was to evaluate the efficacy of methylnaltrexone over 48 h in cancer patients who were not terminally ill. METHODS: In this single-dose phase II trial, cancer patients with a prognosis of ≥3 months and OIC with <3 laxations during the preceding week were eligible...
April 2017: International Journal of Clinical Oncology
https://www.readbyqxmd.com/read/27592058/local-intramuscular-injection-of-a-plasmid-encoding-human-proenkepahlin-attenuates-incision-pain-in-rats
#19
Chunsheng Hu, Zhenzhen Cai, Yuxin Lu, Xiaochen Cheng, Zuze Wu, Qinglin Zhang
We investigated the antinociceptive effect of local intramuscular injection of a plasmid encoding human proenkephalin (pVAX1-hPPE) on postoperative pain in rats. Male Sprague-Dawley rats with incision-induced pain were intramuscularly injected into injured plantaris muscle with empty vector (pVAX1) or pVAX1-hPPE, respectively. Paw mechanical threshold and thermal latency in the 200μg pVAX1-hPPE treated rats were significantly higher at 6h and on 1day, and lasted until day 7 after intramuscular administration, respectively...
October 6, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27582887/the-role-of-naloxegol-in-the-management-of-opioid-induced-bowel-dysfunction
#20
REVIEW
Wojciech Leppert, Jaroslaw Woron
Opioid-induced constipation (OIC) and other gastrointestinal (GI) symptoms of opioid-induced bowel dysfunction (OIBD) significantly deteriorate patients' quality of life and may lead to noncompliance with opioid schedule and undertreatment of pain. Although traditional oral laxatives are the first-line treatment of OIC, they do not address OIBD pathophysiology, and display numerous adverse effects. OIC treatment includes prokinetics (lubiprostone), opioid switch, and changing route of opioid administration...
September 2016: Therapeutic Advances in Gastroenterology
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