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https://www.readbyqxmd.com/read/29207909/the-evolving-role-of-long-term-pharmacotherapy-for-opioid-induced-constipation-in-patients-being-treated-for-noncancer-pain
#1
Brandi L Bowers, Andrew J Crannage
Nationally, the prescription of opioids for acute and chronic pain is increasing. As opioid use continues to expand and become of increased concern for health-care practitioners, so do the adverse effects and long-term management of those effects. Opioid-induced constipation (OIC) presents a unique challenge because tolerance does not develop to this particular adverse effect, making chronic pain management a delicate balance between relieving pain and preventing long-term adverse effects such as constipation and dependence...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/29134730/role-of-central-versus-peripheral-opioid-system-in-antinociceptive-and-anti-inflammatory-effect-of-botulinum-toxin-type-a-in-trigeminal-region
#2
V Drinovac Vlah, B Filipović, L Bach-Rojecky, Z Lacković
BACKGROUND: Although botulinum toxin type A (BT-A) is approved for chronic migraine treatment, its site and mechanism of action are still elusive. Recently our group discovered that suppression of CGRP release from dural nerve endings might account for antimigraine action of pericranially injected BT-A. We demonstrated that central antinociceptive effect of BT-A in sciatic region involves endogenous opioid system as well. Here we investigated possible interaction of BT-A with endogenous opioid system within the trigeminal region...
November 13, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/29119706/insights-on-efficacious-doses-of-pamoras-for-patients-on-chronic-opioid-therapy-or-opioid-na%C3%A3-ve-patients
#3
K van Malderen, H Halawi, M Camilleri
BACKGROUND: Opioid-induced constipation (OIC) is a major side effect of opioid use. Centrally acting antagonists result in opioid withdrawal or worsening of pain and lead to use of peripherally acting mu-opioid receptor antagonists (PAMORAs). The required doses of the PAMORAs, methylnaltrexone and naloxegol, in the treatment of OIC are well established in chronic opioid users. OIC may occur after short duration of opioid treatment; the required doses of naloxone, naltrexone, and PAMORAs in opioid-naïve subjects (with no opioid use for at least 3 months) are unclear...
November 9, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/29092627/evidence-based-review-of-pharmacotherapy-for-opioid-induced-constipation-in-noncancer-pain
#4
Julie A Murphy, Erica A Sheridan
OBJECTIVE: To summarize and evaluate the existing literature regarding medications to treat opioid-induced constipation (OIC) in patients with chronic noncancer pain (CNCP). DATA SOURCES: PubMed, EMBASE, and Web of Science were searched using the following terms: constipation, opioid, chronic, pain, noncancer, nonmalignant, methylnaltrexone, alvimopan, lubiprostone, naloxegol, and naldemedine. STUDY SELECTION AND DATA EXTRACTION: The search was limited to randomized controlled trials reporting human outcomes...
October 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29016552/the-efficacy-of-peripheral-opioid-antagonists-in-opioid-induced-constipation-and-postoperative-ileus-a-systematic-review-of-the-literature
#5
Eric S Schwenk, Alexander E Grant, Marc C Torjman, Stephen E McNulty, Jaime L Baratta, Eugene R Viscusi
Opioid-induced constipation has a negative impact on quality of life for patients with chronic pain and can affect more than a third of patients. A related but separate entity is postoperative ileus, which is an abnormal pattern of gastrointestinal motility after surgery. Nonselective μ-opioid receptor antagonists reverse constipation and opioid-induced ileus but cross the blood-brain barrier and may reverse analgesia. Peripherally acting μ-opioid receptor antagonists target the μ-opioid receptor without reversing analgesia...
November 2017: Regional Anesthesia and Pain Medicine
https://www.readbyqxmd.com/read/28946783/peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonists-for-the-treatment-of-opioid-related-side-effects-mechanism-of-action-and-clinical-implications
#6
John M Streicher, Edward J Bilsky
Opioid receptors are distributed throughout the central and peripheral nervous systems and on many nonneuronal cells. Therefore, opioid administration induces effects beyond analgesia. In the enteric nervous system (ENS), stimulation of µ-opioid receptors triggers several inhibitory responses that can culminate in opioid-induced bowel dysfunction (OBD) and its most common side effect, opioid-induced constipation (OIC). OIC negatively affects patients' quality of life (QOL), ability to work, and pain management...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/28810695/long-term-safety-and-efficacy-of-subcutaneous-methylnaltrexone-in-patients-with-opioid-induced-constipation-and-chronic-noncancer-pain-a-phase-3-open-label-trial
#7
Lynn R Webster, Edward Michna, Arif Khan, Robert J Israel, Joseph R Harper
Objective: Methylnaltrexone, a peripherally acting µ-opioid receptor antagonist, alleviates opioid-induced constipation. Understanding its long-term safety and efficacy profile in patients with chronic noncancer pain is warranted given the persistence of opioid-induced constipation. Methods. : In this phase 3, multicenter, open-label trial, adults with chronic noncancer pain (N = 1034) received subcutaneous methylnaltrexone 12 mg once daily for 48 weeks...
August 1, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28776489/pharmacokinetic-study-of-methylnaltrexone-after-single-and-multiple-subcutaneous-administrations-in-healthy-chinese-subjects
#8
Dan Zhang, Jing-Yi Ma, Man Yang, Ming Deng, Huichen Liu
1. Pharmacokinetics of methylnaltrexone (MNTX) were evaluated after subcutaneous administrations (s.c.) in healthy Chinese subjects. 2. In a cross-over single dose study, 12 subjects were given 0.075, 0.15, and 0.3 mg/kg of MNTX bromide injection. In a multiple doses study, another 12 subjects subcutaneously received 0.15 mg/kg of MNTX bromide injection every 48 hours, in total 5 administrations. The concentrations of MNTX in plasma were quantified by LC-MS/MS. 3. After single s.c. administrations of 0...
August 4, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28580486/the-role-of-endogenous-opioid-system-in-the-regulation-of-heart-tolerance-to-stress-induced-damage
#9
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
#10
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...
August 15, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28554003/opioids-and-opioid-receptors-orchestrate-wound-repair
#11
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...
July 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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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