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https://www.readbyqxmd.com/read/27909835/breakthrough-chemotherapy-induced-nausea-and-vomiting-report-of-a-nationwide-survey-by-the-cinv-study-group-of-japan
#1
Kazuo Tamura, Keisuke Aiba, Toshiaki Saeki, Yoichi Nakanishi, Toshiharu Kamura, Hideo Baba, Kazuhiro Yoshida, Nobuyuki Yamamoto, Yuko Kitagawa, Yoshihiko Maehara, Mototsugu Shimokawa, Koichi Hirata, Masaki Kitajima
BACKGROUND: We conducted a nationwide survey on chemotherapy-induced nausea and vomiting (CINV) in Japan and demonstrated good compliance with Japanese CINV guidelines, resulting in good control of vomiting. However, almost half the patients experienced breakthrough CINV. We analyzed the survey results in relationship to the management of patients with breakthrough CINV. METHODS: This multicenter, prospective, observational study analyzed data for 1910 patients in Japan scheduled for moderately or highly emetogenic chemotherapy (MEC and HEC, respectively)...
December 1, 2016: International Journal of Clinical Oncology
https://www.readbyqxmd.com/read/27905561/anti-hu-antibodies-activate-enteric-and-sensory-neurons
#2
Qin Li, Klaus Michel, Anita Annahazi, Ihsan E Demir, Güralp O Ceyhan, Florian Zeller, Lars Komorowski, Winfried Stöcker, Michael J Beyak, David Grundy, Gianrico Farrugia, Roberto De Giorgio, Michael Schemann
IgG of type 1 anti-neuronal nuclear antibody (ANNA-1, anti-Hu) specificity is a serological marker of paraneoplastic neurological autoimmunity (including enteric/autonomic) usually related to small-cell lung carcinoma. We show here that IgG isolated from such sera and also affinity-purified anti-HuD label enteric neurons and cause an immediate spike discharge in enteric and visceral sensory neurons. Both labelling and activation of enteric neurons was prevented by preincubation with the HuD antigen. Activation of enteric neurons was inhibited by the nicotinic receptor antagonists hexamethonium and dihydro-β-erythroidine and reduced by the P2X antagonist pyridoxal phosphate-6-azo (benzene-2,4-disulfonic acid (PPADS) but not by the 5-HT3 antagonist tropisetron or the N-type Ca-channel blocker ω-Conotoxin GVIA...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27894202/rolapitant-for-the-prevention-of-delayed-nausea-and-vomiting-over-initial-and-repeat-courses-of-emetogenic-chemotherapy
#3
Bernardo Rapoport, Ronwyn van Eeden, Teresa Smit
Introduction Chemotherapy-induced nausea and vomiting (CINV) is a debilitating side effect of many cytotoxic chemotherapy regimens. Although sustained antiemetic control across repeated chemotherapy cycles is important for cancer treatment continuation, few studies have investigated the efficacy of antiemetic prophylaxis over multiple chemotherapy cycles. Areas Covered Here we discuss the use of antiemetic hydroxytryptamine type 3 (5-HT3) receptor and neurokinin (NK)-1 receptor antagonists for prevention of CINV, limiting our review to clinical trials in the context of multiple-cycle chemotherapy, with a focus on the NK-1 receptor antagonist rolapitant...
November 29, 2016: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/27889278/safety-and-efficacy-of-nepa-an-oral-fixed-combination-of-netupitant-and-palonosetron-in-older-patients
#4
Matti Aapro, Karin Jordan, Richard J Gralla, Giada Rizzi, Giorgia Rossi, Marco Palmas, Anna V Alyasova, Alla S Lisyanskaya, Snežana M Bošnjak, Paul J Hesketh
OBJECTIVES: Prevention of chemotherapy-induced nausea and vomiting is critical in older cancer patients. NEPA is an oral fixed combination of netupitant 300mg, a new NK1 receptor antagonist (RA), and palonosetron 0.5mg, a pharmacologically distinct 5-HT3 RA. This retrospective analysis evaluated the efficacy and safety of NEPA in older patients. METHODS: Patients aged ≥65 and ≥70years from one phase II and two phase III trials were considered. Chemotherapy-naive patients with malignant tumors were treated with anthracycline-cyclophosphamide (AC), non-AC-based moderately emetogenic chemotherapy (non-AC MEC), or highly emetogenic chemotherapy (HEC)...
November 23, 2016: Journal of Geriatric Oncology
https://www.readbyqxmd.com/read/27885469/nepa-a-fixed-oral-combination-of-netupitant-and-palonosetron-improves-control-of-chemotherapy-induced-nausea-and-vomiting-cinv-over-multiple-cycles-of-chemotherapy-results-of-a-randomized-double-blind-phase-3-trial-versus-oral-palonosetron
#5
Matti Aapro, Meinolf Karthaus, Lee Schwartzberg, Igor Bondarenko, Tomasz Sarosiek, Cristina Oprean, Servando Cardona-Huerta, Vincent Hansen, Giorgia Rossi, Giada Rizzi, Maria Elisa Borroni, Hope Rugo
PURPOSE: Antiemetic guidelines recommend co-administration of targeted prophylactic medications inhibiting molecular pathways involved in emesis. NEPA is a fixed oral combination of a new NK1 receptor antagonist (RA), netupitant (NETU 300 mg), and palonosetron (PALO 0.50 mg), a pharmacologically distinct 5-HT3 RA. NEPA showed superior prevention of chemotherapy-induced nausea and vomiting (CINV) compared with oral PALO in a single chemotherapy cycle; maintenance of efficacy/safety over continuing cycles is the objective of this study...
November 24, 2016: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/27870735/combination-of-5-ht3-antagonist-and-dexamethasone-is-superior-to-5-ht3-antagonist-alone-for-ponv-prophylaxis-after-laparoscopic-surgeries-a-meta-analysis
#6
Anirban Som, Sulagna Bhattacharjee, Souvik Maitra, Mahesh K Arora, Dalim Kumar Baidya
INTRODUCTION: 5-Hydroxytryptamine type 3 (5-HT3) receptor antagonists are the most commonly used drugs for postoperative nausea vomiting (PONV) prophylaxis. Dexamethasone is another antiemetic with proven efficacy in reducing PONV. The aim of this study was to conduct a systematic review and meta-analysis of randomized controlled trials (RCTs) to compare the combination of dexamethasone and 5-HT3 antagonist versus a 5-HT3 antagonist alone as prophylaxis of PONV in laparoscopic surgical patients...
December 2016: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/27856931/5-ht3-receptor-antagonists-for-the-prevention-of-postoperative-shivering-a-meta-analysis
#7
Chengmao Zhou, Yu Zhu, Zhen Liu, Lin Ruan
OBJECTIVE: We evaluated the efficacy of 5-HT3 receptor antagonists for the prevention of postoperative shivering. METHODS: We searched PubMed, the Cochrane Library, EMBASE and Web of Knowledge to find randomized controlled trials (RCT) of 5-HT3 receptor antagonists for the prevention of postoperative shivering. Two researchers independently screened studies, extracted data, and assessed quality in accordance with the inclusion and exclusion criteria, and then conducted a meta-analysis using RevMan 5...
November 17, 2016: Journal of International Medical Research
https://www.readbyqxmd.com/read/27824106/peripheral-and-spinal-5-ht-receptors-participate-in-cholestatic-itch-and-antinociception-induced-by-bile-duct-ligation-in-rats
#8
Bin Tian, Xue-Long Wang, Ya Huang, Li-Hua Chen, Ruo-Xiao Cheng, Feng-Ming Zhou, Ran Guo, Jun-Cheng Li, Tong Liu
Although 5-HT has been implicated in cholestatic itch and antinociception, two common phenomena in patients with cholestatic disease, the roles of 5-HT receptor subtypes are unclear. Herein, we investigated the roles of 5-HT receptors in itch and antinociception associated with cholestasis, which was induced by common bile duct ligation (BDL) in rats. 5-HT-induced enhanced scratching and antinociception to mechanical and heat stimuli were demonstrated in BDL rats. 5-HT level in the skin and spinal cord was significantly increased in BDL rats...
November 8, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27821979/comparison-of-efficacy-of-granisetron-and-promethazine-in-control-of-hyperemesis-gravidarum
#9
Ashraf Aleyasin, Elham Saffarieh, Hassan Torkamandi, Somayeh Hanafi, Fariborz Sadeghi, Atossa Mahdavi, Fatemeh Bahmaei, Mohammadreza Javadi
PURPOSE: Hyperemesis gravidarum is the third leading cause of hospitalization during pregnancy. 5-HT3-receptor antagonists are the most effective against chemotherapy-induced nausea and vomiting and radiation. This randomized study aimed to compare and evaluate the efficacies of granisetron and promethazine for controlling nausea and vomiting of pregnancy. METHODS: The included patients were administered (oral and intravenous) granisetron and promethazine randomly...
December 2016: Journal of Obstetrics and Gynaecology of India
https://www.readbyqxmd.com/read/27816366/comparison-of-ramosetron-with-ondansetron-for-prevention-of-intrathecal-morphine-induced-nausea-and-vomiting-after-primary-total-knee-arthroplasty-a-randomized-control-trial
#10
Piya Pinsornsak, Mungkorn Teeyaphudit, Chaivet Ruetiwarangkoon, Adisai Chaiwuttisak
BACKGROUND: Spinal anesthesia with intrathecal morphine is a reliable, easy to apply, and cost effective method for controlling pain after total knee arthroplasty (TKA). However, postoperative nausea and vomiting (PONV) is a major concern. 5-Hydroxytryptamine receptor 3 (5-HT3) antagonists like ondansetron and ramosetron are commonly used for preventing PONV, but the optimal choice remains unclear. We conducted a study to assess the effectiveness of ramosetron and ondansetron, hypothesizing that the longer acting ramosetron may be better than ondansetron in the first 48 hours after TKA, performed with spinal anesthesia and intrathecal morphine...
October 8, 2016: Journal of Arthroplasty
https://www.readbyqxmd.com/read/27816008/in-silico-investigation-into-the-interactions-between-murine-5-ht3-receptor-and-the-principle-active-compounds-of-ginger-zingiber-officinale
#11
Anna E Lohning, Wolfgang Marx, Liz Isenring
Gingerols and shogaols are the primary non-volatile actives within ginger (Zingiber officinale). These compounds have demonstrated in vitro to exert 5-HT3 receptor antagonism which could benefit chemotherapy-induced nausea and vomiting (CINV). The site and mechanism of action by which these compounds interact with the 5-HT3 receptor is not fully understood although research indicates they may bind to a currently unidentified allosteric binding site. Using in silico techniques, such as molecular docking and GRID analysis, we have characterized the recently available murine 5-HT3 receptor by identifying sites of strong interaction with particular functional groups at both the orthogonal (serotonin) site and a proposed allosteric binding site situated at the interface between the transmembrane region and the extracellular domain...
October 26, 2016: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27815710/2016-updated-mascc-esmo-consensus-recommendations-prevention-of-nausea-and-vomiting-following-multiple-day-chemotherapy-high-dose-chemotherapy-and-breakthrough-nausea-and-vomiting
#12
Lawrence H Einhorn, Bernardo Rapoport, Rudolph M Navari, Jørn Herrstedt, Mary J Brames
PURPOSE: This review summarizes the recommendations for the prophylaxis of acute and delayed nausea and vomiting induced by multiple-day chemotherapy, high-dose chemotherapy, and breakthrough nausea and vomiting as agreed at the MASCC/ESMO Antiemetic Guidelines update meeting in Copenhagen in June 2015. METHODS: A systematic literature search using PubMed from January 01, 2009 through January 06, 2015 with a restriction to papers in English was conducted. RESULTS: There were three phase III randomized trials in patients undergoing high-dose chemotherapy and stem cell transplant and eight single arm non-randomized clinical studies (single in patients undergoing transplantation and one in patients receiving multiple-day chemotherapy treatment)...
January 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/27810704/selective-corticotropin-releasing-factor-1-receptor-antagonist-e2508-reduces-restraint-stress-induced-defecation-and-visceral-pain-in-rat-models
#13
Ryota Taguchi, Kodo Shikata, Yoshiaki Furuya, Tetsuya Hirakawa, Mitsuhiro Ino, Kogyoku Shin, Hisashi Shibata
N-Cyclopropylmethyl-7-(2,6-dimethoxy-4-methoxymethylphenyl)-2-ethyl-N-(tetrahydro-2H-pyran-4-ylmethyl)pyrazolo[1,5-a]pyridin-3-amine tosylate (E2508) is a newly discovered selective corticotropin-releasing factor 1 receptor antagonist. Here, we investigated the effects of E2508 on wrap restraint stress-induced defecation and visceral pain in rats. Oral pretreatment with E2508 dose-dependently decreased stool weights after 20min wrap restraint stress and significant effects were observed at doses of 30 and 100mg/kg...
January 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/27763704/the-human-serotonin-type-3-receptor-gene-htr3a-e-allelic-variant-database
#14
Jacopo Celli, Gudrun Rappold, Beate Niesler
Serotonin type 3 (5-HT3 ) receptors are ligand-gated ion channels formed by five subunits (5-HT3A-E), which are encoded by the HTR3A, HTR3B, HTR3C, HTR3D, and HTR3E genes. Functional receptors are pentameric complexes of diverse composition. Different receptor subtypes confer a predisposition to nausea and vomiting during chemotherapy, pregnancy, and following surgery. In addition, different subtypes contribute to neurogastroenterologic disorders such irritable bowel syndrome (IBS) and eating disorders as well as comorbid psychiatric conditions...
October 20, 2016: Human Mutation
https://www.readbyqxmd.com/read/27757785/2-3-o-substituted-atp-derivatives-as-potent-antagonists-of-purinergic-p2x3-receptors-and-potential-analgesic-agents
#15
Diego Dal Ben, Anna Marchenkova, Ajiroghene Thomas, Catia Lambertucci, Andrea Spinaci, Gabriella Marucci, Andrea Nistri, Rosaria Volpini
Blocking membrane currents evoked by the activation of purinergic P2X3 receptors localized on nociceptive neurons represents a promising strategy for the development of agents useful for the treatment of chronic pain conditions. Among compounds endowed with such antagonistic action, 2',3'-O-(2,4,6-trinitrophenyl)-ATP (TNP-ATP) is an ATP analogue, whose inhibitory activity on P2X receptors has been previously reported. Based on the results of molecular modelling studies performed with homology models of the P2X3 receptor, novel adenosine nucleotide analogues bearing cycloalkyl or arylalkyl substituents replacing the trinitrophenyl moiety of TNP-ATP were designed and synthesized...
October 18, 2016: Purinergic Signalling
https://www.readbyqxmd.com/read/27746348/chronic-5-ht3-receptor-antagonism-ameliorates-seizures-and-associated-memory-deficit-in-pentylenetetrazole-kindled-mice
#16
Awanish Mishra, Rajesh Kumar Goel
Our previous studies have suggested a strong involvement of serotonergic innervations in epileptogenesis and associated memory impairment. Several studies have suggested that the modulation of 5-HT3 receptors could serve as a promising tool for the management of epilepsy and memory deficit. The present study was envisaged to confirm this hypothesis. In this study, kindling was induced in male Swiss Albino mice using a subconvulsive dose of pentylenetetrazole (PTZ) (35mg/kg at 48±2h). Once the animals were kindled, they were treated with a vehicle, ondansetron (0...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27743549/serotonergic-agents-act-on-5-ht3-receptors-in-the-brain-to-block-seizure-induced-respiratory-arrest-in-the-dba-1-mouse-model-of-sudep
#17
Carl L Faingold, Marcus Randall, Chang Zeng, Shifang Peng, Xiaoyan Long, Hua-Jun Feng
Drugs that enhance the action of serotonin (5-hydroxytrypamine, 5-HT), including several selective serotonin reuptake inhibitors (SSRIs), reduce susceptibility to seizure-induced respiratory arrest (S-IRA) that leads to death in the DBA/1 mouse model of sudden unexpected death in epilepsy (SUDEP). However, it is not clear if specific 5-HT receptors are important in the action of these drugs and whether the brain is the major site of action of these agents in this SUDEP model. The current study examined the actions of agents that affect the 5-HT3 receptor subtype on S-IRA and whether intracerebroventricular (ICV) microinjection of an SSRI would reduce S-IRA susceptibility in DBA/1 mice...
November 2016: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/27729680/bradycardia-after-intravenous-ondansetron-with-asystole-on-rechallenge-a-case-report
#18
EDITORIAL
Jonathan H Rapp, Meggie Yuen, Teena Abraham
PURPOSE: There have been 3 published reports (4 cases) of symptomatic sinus bradycardia occurring after intravenous (IV) administration of the selective 5-hydroxytryptamine 3 (5-HT3) receptor antagonist ondansetron. We report a fifth case in which the patient developed asystole after rechallenge with ondansetron. SUMMARY: A 36-year-old pregnant patient with no cardiac history, status post cerclage for cervical insufficiency, experienced nausea in the post ambulatory care unit after administration of morphine and indomethacin for pain...
November 2015: Hospital Pharmacy
https://www.readbyqxmd.com/read/27725889/shuyu-capsules-relieve-premenstrual-syndrome-depression-by-reducing-5-ht3ar-and-5-ht3br-expression-in-the-rat-brain
#19
Fang Li, Jizhen Feng, Dongmei Gao, Jieqiong Wang, Chunhong Song, Sheng Wei, Mingqi Qiao
The effects of the Shuyu capsule on 5-HT3AR and 5-HT3BR expression in a rat model of premenstrual syndrome (PMS) depression and on 5-HT3AR and 5-HT3BR expression and hippocampal neuron 5-HT3 channel current were investigated, to elucidate its mechanism of action against PMS depression. PMS depression model rats were divided into depression and Shuyu- and fluoxetine-treated groups, which were compared to control rats for frontal lobe and hippocampal 5-HT3AR and 5-HT3BR expression and behavior. The depressed model rats displayed symptoms of depression, which were reduced in treated and normal control rats...
2016: Neural Plasticity
https://www.readbyqxmd.com/read/27722211/rolapitant-hydrochloride-prophylactic-treatment-for-chemotherapy-induced-nausea-and-vomiting
#20
R Navari
Chemotherapy-induced nausea and vomiting (CINV) is a significant clinical issue which affects patients' quality of life as well as treatment decisions. Significant improvements in the control of CINV have occurred in the past 15 years with the introduction of new antiemetic agents: 5-HT3 receptor antagonists, tachykinin NK1 receptor antagonists and olanzapine. Aprepitant was the first NK1 receptor antagonist introduced (2003) for the prevention of CINV in combination with a 5-HT3 receptor antagonist and dexamethasone...
August 2016: Drugs of Today
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