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Naloxegol

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https://www.readbyqxmd.com/read/29765749/naloxegol-hydrogen-oxalate-displaying-a-hydrogen-bonded-layer-structure
#1
Thomas Gelbrich, Christoph Langes, Marijan Stefinovic, Ulrich J Griesser
In the salt (5α,6α)-6-[(2,5,8,11,14,17,20-hepta-oxadocosan-22-yl)-oxy]-3,14-dihy-droxy-17-(prop-2-en-1-yl)-4,5-ep-oxy-morphinan-17-ium hydrogen oxalate, C34 H54 NO11 + ·C2 HO4 - the polyether unit of the naloxegol cation adopts the shape of a squashed open letter 'O'. In the crystal, the hydrogen oxalate anions are linked into a chain by O-H⋯O hydrogen bonds. Each naloxegol unit is hydrogen bonded to three hydrogen oxalate ions via two O-H⋯O and one N-H⋯O inter-actions. The resulting hydrogen-bonded two-dimensional layer structure is 3,5-connected and has the 3,5 L50 topology...
April 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/29572333/risk-of-clinically-relevant-pharmacokinetic-based-drug-drug-interactions-with-drugs-approved-by-the-u-s-food-and-drug-administration-between-2013-and-2016
#2
Jingjing Yu, Zhu Zhou, Jessica Tay-Sontheimer, Rene H Levy, Isabelle Ragueneau-Majlessi
A total of 103 drugs (including 14 combination drugs) were approved by the U.S. Food and Drug Administration from 2013 to 2016. Pharmacokinetic-based drug interaction profiles were analyzed using the University of Washington Drug Interaction Database and the clinical relevance of these observations was characterized based on information from New Drug Application reviews. CYP3A was identified as a major contributor to clinical drug-drug interactions (DDIs), involved in approximately 2/3 of all interactions. Transporters (alone or with enzymes) were found to participate in about half of all interactions, although most of these were weak-to-moderate interactions...
March 23, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29504415/cardiovascular-safety-of-the-selective-%C3%AE-opioid-receptor-antagonist-naloxegol-a-novel-therapy-for-opioid-induced-constipation
#3
William B White, Peter Kowey, Ulysses Diva, Mark Sostek, Raj Tummala
BACKGROUND: Naloxegol is a novel selective, peripherally acting μ-opioid receptor antagonist for treating opioid-induced constipation (OIC) in patients with chronic pain syndromes. We analyzed the cardiovascular (CV) safety of naloxegol based on data from its development program prior to approval by the US Food and Drug Administration in 2015. METHODS: Comprehensive CV safety analyses were performed in 4 clinical studies of naloxegol (12.5 and/or 25 mg) in patients with noncancer pain and OIC: two 12-week, double-blind, randomized studies; a 12-week, double-blind, extension study; and a 52-week, randomized, open-label study versus usual care...
January 1, 2018: Journal of Cardiovascular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29432808/the-impact-of-naloxegol-on-anal-sphincter-function-using-a-human-experimental-model-of-opioid-induced-bowel-dysfunction
#4
Debbie Grønlund, Jakob L Poulsen, Klaus Krogh, Christina Brock, Donghua Liao, Hans Gregersen, Asbjørn M Drewes, Anne E Olesen
BACKGROUND AND AIMS: Opioid treatment interferes with anal sphincter function and its regulation during defecation. This may result in straining, incomplete evacuation, and contribute to opioid-induced bowel dysfunction (OIBD). Employing an experimental model of oxycodone-induced OIBD, we hypothesized that co-administration of the peripherally acting μ-opioid antagonist naloxegol would improve anal sphincter function in comparison to placebo. METHODS: In a double-blind randomized crossover trial, 24 healthy males were assigned to a six-day treatment of oral oxycodone 15 mg twice daily in combination with either oral naloxegol 25 mg once daily or placebo...
May 30, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29405492/effects-of-naloxegol-on-whole-gut-transit-in-opioid-na%C3%A3-ve-healthy-subjects-receiving-codeine-a-randomized-controlled-trial
#5
H Halawi, P Vijayvargiya, I Busciglio, I Oduyebo, D Khemani, M Ryks, D Rhoten, D Burton, L A Szarka, A Acosta, M Camilleri
BACKGROUND: Nausea, vomiting, and constipation (OIC) are common adverse effects of acute or chronic opioid use. Naloxegol (25 mg) is an approved peripherally active mu-opiate opioid receptor antagonist. AIM: To compare the effects on pan-gut transit of treatment with codeine, naloxegol, or combination in healthy volunteers. METHODS: We conducted a randomized, double-blind, placebo-controlled, single-center, parallel-group study in 72 healthy opioid-naïve adults, randomized to: codeine (30 mg q...
May 2018: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/29374616/efficacy-of-treatments-for-opioid-induced-constipation-a-systematic-review-and-meta-analysis
#6
REVIEW
Judy Nee, Mohammed Zakari, Michael A Sugarman, Julia Whelan, William Hirsch, Shahnaz Sultan, Sarah Ballou, Johanna Iturrino, Anthony Lembo
BACKGROUND & AIMS: Opioid induced constipation (OIC) is a common problem in patients on chronic opioid therapy for cancer-related and non-cancer related pain. Approved treatments for OIC are methylnaltrexone, naloxone, naloxegol, alvimopan, naldemedine, and lubiprostone. Since a meta-analysis performed in 2014, 2 new agents have been approved by the Food and Drug Administration (FDA) for treatment of OIC (naloxegol and naldemedine). METHODS: We conducted a search of the medical literature following the protocol outlined in the Cochrane Handbook for systematic review...
January 25, 2018: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/29322659/integrating-dose-estimation-into-a-decision-making-framework-for-model-based-drug-development
#7
James Dunyak, Patrick Mitchell, Bengt Hamrén, Gabriel Helmlinger, James Matcham, Donald Stanski, Nidal Al-Huniti
Model-informed drug discovery and development offers the promise of more efficient clinical development, with increased productivity and reduced cost through scientific decision making and risk management. Go/no-go development decisions in the pharmaceutical industry are often driven by effect size estimates, with the goal of meeting commercially generated target profiles. Sufficient efficacy is critical for eventual success, but the decision to advance development phase is also dependent on adequate knowledge of appropriate dose and dose-response...
March 2018: Pharmaceutical Statistics
https://www.readbyqxmd.com/read/29207909/the-evolving-role-of-long-term-pharmacotherapy-for-opioid-induced-constipation-in-patients-being-treated-for-noncancer-pain
#8
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/29119706/insights-on-efficacious-doses-of-pamoras-for-patients-on-chronic-opioid-therapy-or-opioid-na%C3%A3-ve-patients
#9
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
#10
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...
April 2018: 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
#11
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
#12
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/28919541/drugs-for-treating-opioid-induced-constipation-a-mixed-treatment-comparison-network-meta-analysis-of-randomized-controlled-clinical-trials
#13
REVIEW
Kannan Sridharan, Gowri Sivaramakrishnan
CONTEXT: Opioid-induced constipation is a common problem associated with chronic use of opioid analgesics. OBJECTIVES: The objective of this study was to compare available interventions for the treatment of opioid-induced constipation, using principles of network meta-analysis. METHODS: Electronic databases were searched for randomized controlled clinical trials evaluating drugs used in opioid-induced constipation. Number of patients with rescue-free bowel movements (RFBM) was the primary outcome, and time for achieving RFBM, adverse events, and changes in the analgesic activity of the opioid analgesics were the secondary outcomes...
February 2018: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/28898536/treatment-with-naloxegol-versus-placebo-pain-assessment-in-patients-with-noncancer-pain-and-opioid-induced-constipation
#14
Lynn Webster, Ulysses Diva, Raj Tummala, Mark Sostek
OBJECTIVE: To summarize results from pain and opioid use assessments with naloxegol in adults with opioid-induced constipation (OIC) and chronic noncancer pain. METHODS: Two phase 3 randomized, double-blind, 12-week studies evaluated the efficacy and safety of oral naloxegol (12.5 or 25 mg daily) in adults (18 to < 85 years) with confirmed OIC and chronic noncancer pain: KODIAC-04 (NCT01309841) and KODIAC-05 (NCT01323790). Pain level was assessed daily (11-point numeric rating scale [NRS]; 0 = no pain, 10 = worst imaginable pain)...
September 12, 2017: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/28858018/naloxegol-for-managing-opioid-induced-constipation
#15
Krystal N Shelton, Jennifer N Clements
Naloxegol is a peripherally acting mu-opioid receptor antagonist for opioid-induced constipation in adults with chronic noncancer pain. This drug's once-daily oral formulation can be used as monotherapy and helps to decrease the constipating effects of opioid therapy; however, it has been associated with abdominal pain.
September 2017: JAAPA: Official Journal of the American Academy of Physician Assistants
https://www.readbyqxmd.com/read/28782266/population-exposure-response-modeling-supported-selection-of-naloxegol-doses-in-phase-iii-studies-in-patients-with-opioid-induced-constipation
#16
Nidal Al-Huniti, Hongmei Xu, Diansong Zhou, Sergey Aksenov, Robert Fox, Khanh H Bui
Naloxegol is approved for the treatment of opioid-induced constipation (OIC) in adults with chronic noncancer pain. Population exposure-response models were developed using data from a phase II study comprising 185 adults with OIC. The weekly probability of response defined as having ≥3/week spontaneous bowel movements (SBMs) and ≥1 SBM/week increase over baseline was characterized by a longitudinal mixed-effects logistic regression dose-response model, and the probability of time to discontinuation was modeled with a Weibull distribution function...
October 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28769555/naloxegol-in-opioid-induced-constipation-a-new-paradigm-in-the-treatment-of-a-common-problem
#17
REVIEW
Stephanie C Yoon, Heather C Bruner
Opioid-induced constipation (OIC) imposes a significant burden for patients taking pain medications, often resulting in decreased quality of life. Treatment of OIC with traditional medications for functional constipation can be incompletely effective, leading to nonadherence with opioid treatment and undertreated pain. An emerging class of medications that counteract the adverse effects of opioids in the gastrointestinal tract while preserving central nervous system-based pain relief may represent a paradigm shift in the prevention and treatment of OIC...
2017: Patient Preference and Adherence
https://www.readbyqxmd.com/read/28554659/naloxegol-an-opioid-antagonist-with-reduced-cns-penetration-mode-of-action-and-human-relevance-for-rat-testicular-tumours
#18
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/28548207/pharmacometric-modeling-of-naloxegol-efficacy-and-safety-impact-on-dose-and-label
#19
REVIEW
N Al-Huniti, D Zhou, H Xu, S Aksenov, K H Bui, R Fox, G Helmlinger, D Stanski
Naloxegol is a peripherally acting μ-opioid receptor antagonist that was developed for the treatment of opioid-induced constipation. Modeling and simulation of naloxegol efficacy and tolerability informed selection of doses for phase III studies and provided comprehensive dosage recommendations for the naloxegol US package insert.
November 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28504549/determination-of-naloxegol-in-human-biological-matrices
#20
Yan Li, Mark Hoffmann, Paul Severin
AIM: Naloxegol is an oral peripherally acting μ-opioid receptor antagonist approved for the treatment of opioid-induced constipation. Sensitive, robust, bioanalytical methods were required to quantitate naloxegol in human biological matrices as part of the clinical development program. METHODOLOGY/RESULTS: Analytical plasma samples were prepared using Solid Phase Extraction (SPE) coupled with concentration. The method's linearity was established at 0.1-50 ng/ml with up to 100-fold dilution...
April 2017: Bioanalysis
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