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https://www.readbyqxmd.com/read/27915445/granisetron-extended-release-injection-a-review-in-chemotherapy-induced-nausea-and-vomiting
#1
Emma D Deeks
An extended-release (ER) subcutaneously injectable formulation of the first-generation 5-HT3 receptor antagonist granisetron is now available in the USA (Sustol(®)), where it is indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) following moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide combination chemotherapy regimens in adults. Granisetron ER is administered as a single subcutaneous injection and uses an erosion-controlled drug-delivery system to allow prolonged granisetron release...
December 3, 2016: Drugs
https://www.readbyqxmd.com/read/27895421/carbon-monoxide-contributes-to-the-constipating-effects-of-granisetron-in-rat-colon
#2
Carmela Nacci, Margherita Fanelli, Maria Assunta Potenza, Valentina Leo, Monica Montagnani, Maria Antonietta De Salvia
AIM: To investigate the mechanisms underlying the potential contribution of the heme oxygenase/carbon monoxide (HO/CO) pathway in the constipating effects of granisetron. METHODS: For in vivo studies, gastrointestinal motility was evaluated in male rats acutely treated with granisetron [25, 50, 75 μg/kg/subcutaneous (sc)], zinc protoporphyrin IX [ZnPPIX, 50 μg/kg/intraperitoneal (ip)] and hemin (50 μmol/L/kg/ip), alone or in combination. For in vitro studies, the contractile neurogenic response to electrical field stimulation (EFS, 3, 5, 10 Hz, 14 V, 1 ms, pulse trains lasting 10 s), as well as the contractile myogenic response to acetylcholine (ACh, 0...
November 14, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/27826967/palonosetron-induced-anaphylaxis-during-general-anesthesia-a-case-report
#3
Hyungjun Park, Kyunghwan Oh, Hoonhee Lee, Ji Hyang Lee, Sun Myoung Kang, So Young Park, Hyouk Soo Kwon, You Sook Cho, Hee Bom Moon, Tae Bum Kim
Palonosetron is a 5-hydroxytryptamine-3 (5-HT-3) receptor antagonist used for preventing postoperative nausea and vomiting. Compared with ondansetron and granisetron, it is a better drug because of prolonged action and minimal side effects. Some adverse effects of palonosetron have been reported. In this report, we describe a 37-year-old male who developed severe hypersensitivity reactions to palonosetron during surgery for kidney donation. His medical history was unremarkable, except for inguinal hernia with herniorrhaphy 8 years ago...
January 2017: Allergy, Asthma & Immunology Research
https://www.readbyqxmd.com/read/27821979/comparison-of-efficacy-of-granisetron-and-promethazine-in-control-of-hyperemesis-gravidarum
#4
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/27809336/polymorphisms-in-cyp1a1-and-cyp3a5-genes-contribute-to-the-variability-in-granisetron-clearance-and-exposure-in-pregnant-women-with-nausea-and-vomiting
#5
Martha L Bustos, Yang Zhao, Huijun Chen, Steve N Caritis, Raman Venkataramanan
BACKGROUND: Nausea and vomiting affect up to 90% of pregnant women. Granisetron is a potent and highly selective serotonin receptor antagonist and is an effective antiemetic. Findings from a prior study in pregnant women demonstrated a large interindividual variability in granisetron exposure. Granisetron is primarily metabolized by the cytochrome P450 (CYP) enzymes CYP1A1 and CYP3A and is likely a substrate of the ABCB1 transporter. Single-nucleotide polymorphisms (SNPs) in CYP3A, CYP1A1, and ABCB1 can alter drug metabolism...
November 3, 2016: Pharmacotherapy
https://www.readbyqxmd.com/read/27793640/dexamethasone-combined-with-other-antiemetics-versus-single-antiemetics-for-prevention-of-postoperative-nausea-and-vomiting-after-laparoscopic-cholecystectomy-an-updated-systematic-review-and-meta-analysis
#6
REVIEW
Kamal Awad, Hussien Ahmed, Abdelrahman Ibrahim Abushouk, Safwat Al Nahrawi, Mohammed Yasser Elsherbeny, Salma Muhammad Mustafa, Attia Attia
OBJECTIVE: A systematic review and meta-analysis of published randomized controlled trials was performed to update the present evidence about the safety and efficacy of dexamethasone combined with other antiemetics versus single antiemetics for the prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy. METHODS: A computer literature search of PubMed, Scopus, Web of Science and Embase was conducted to identify the relevant randomized controlled trials...
October 25, 2016: International Journal of Surgery
https://www.readbyqxmd.com/read/27765010/dexamethasone-does-not-diminish-sugammadex-reversal-of-neuromuscular-block-clinical-study-in-surgical-patients-undergoing-general-anesthesia
#7
Katja Rezonja, Tomaz Mars, Ales Jerin, Gordana Kozelj, Neva Pozar-Lukanovic, Maja Sostaric
BACKGROUND: Sugammadex reverses neuromuscular block (NMB) through binding aminosteroid neuromuscular blocking agents. Although sugammadex appears to be highly selective, it can interact with other drugs, like corticosteroids. A prospective single-blinded randomized clinical trial was designed to explore the significance of interactions between dexamethasone and sugammadex. METHODS: Sixty-five patients who were anesthetized for elective abdominal or urological surgery were included...
October 21, 2016: BMC Anesthesiology
https://www.readbyqxmd.com/read/27746523/palonosetron-and-granisetron-in-postoperative-nausea-vomiting-a-randomized-double-blind-prospective-study
#8
Amrita A Gugale, Pradnya Milind Bhalerao
BACKGROUND: Postoperative nausea and vomiting (PONV) is a common occurrence after laparoscopic surgeries. A number of pharmacological agents (antihistamines, butyrophenones, dopamine receptor antagonists) have been tried of which the 5-hydroxytryptamine type 3 receptor antagonists are devoid of most side effects and highly effective in prevention and treatment of PONV. Thus, we evaluated the effectiveness of granisetron and palonosetron in prevention of PONV after laparoscopic surgeries under general anesthesia...
September 2016: Anesthesia, Essays and Researches
https://www.readbyqxmd.com/read/27720614/stimulation-of-contractions-in-pregnant-human-myometrium-is-associated-with-5-ht3-receptors
#9
H Li, M Diao, J Ni, P Li, Q Zhu, Y L Wan, Y S Ma, X M Lin
BACKGROUND: Serotonin (5-HT) is known to play an important role in regulating uterine contractions. However, the specific receptors involved have not been well characterized. We evaluated whether 5-HT3 receptors exist in human myometrium, and their effects on myometrial contractility when stimulated by a 5-HT3 agonist. METHODS: Four tissue samples taken from patients undergoing hysterectomy (n=2) and elective cesarean delivery (n=2) were used to detect expression of 5-HT3 receptors on the myometrium using western blotting...
December 2016: International Journal of Obstetric Anesthesia
https://www.readbyqxmd.com/read/27703112/symptomatic-improvement-of-gastroparesis-with-granisetron-transdermal-system
#10
Hye-Kyung Jung
No abstract text is available yet for this article.
October 30, 2016: Journal of Neurogastroenterology and Motility
https://www.readbyqxmd.com/read/27687434/efficacy-of-palonosetron-in-postoperative-nausea-and-vomiting-ponv-a-meta-analysis
#11
REVIEW
Preet Mohinder Singh, Anuradha Borle, Divakara Gouda, Jeetinder Kaur Makkar, Mahesh K Arora, Anjan Trikha, Ashish Sinha, Basavana Goudra
INTRODUCTION: Palonosetron is a second-generation 5-HT3 receptor antagonist with proposed higher efficacy and sustained action for prophylaxis of postoperative nausea and vomiting (PONV). METHODS: Randomized controlled trials involving adult population undergoing elective surgery under general anesthesia comparing palonosetron to placebo, ramosetron, granisetron, and ondansetron were included. Data were extracted for vomiting incidence (VI), complete response (no nausea/vomiting; Complete Response [CR]), and rescue antiemetic need...
November 2016: Journal of Clinical Anesthesia
https://www.readbyqxmd.com/read/27677804/novel-mechanism-of-modulation-at-a-ligand-gated-ion-channel-action-of-5-cl-indole-at-the-5-ht3-a-receptor
#12
Andrew D Powell, Gillian Grafton, Alexander Roberts, Shannon Larkin, Nathanael O'Neill, Josephine Palandri, Reka Otvos, Alison J Cooper, Chris Ulens, Nicholas M Barnes
BACKGROUND AND PURPOSE: The 5-HT3 receptor is a prototypical member of the Cys-loop ligand-gated ion channel (LGIC) superfamily and an established therapeutic target. In addition to activation via the orthosteric site, receptor function can be modulated by allosteric ligands. We have investigated the pharmacological action of Cl-indole upon the 5-HT3 A receptor and identified that this positive allosteric modulator possesses a novel mechanism of action for LGICs. EXPERIMENTAL APPROACH: The impact of Cl-indole upon the 5-HT3 receptor was assessed using single cell electrophysiological recordings and [(3) H]-granisetron binding in HEK293 cells stably expressing the 5-HT3 receptor...
December 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27677233/-5-ht3-antagonists-as-a-substitute-for-metoclopramide-and-domperidone-a-literature-review
#13
I Mouch, J R B J Brouwers, E van 't Riet, P Nieboer, M H Otten, F G A Jansman
OBJECTIVE: To investigate whether the anti-emetics metoclopramide and domperidone can be replaced by 5-HT3-antagonists, as side effects restrict use of these dopamine antagonists. DESIGN: Systematic review. METHOD: We searched the Embase and PubMed databases for articles published in the period 1995-October 2015, in which the efficacy or side effects of metoclopramide or domperidone were compared with at least one of the 5-HT3-antagonists ondansetron, granisetron, tropisetron or palonosetron...
2016: Nederlands Tijdschrift Voor Geneeskunde
https://www.readbyqxmd.com/read/27650869/expression-of-concern-prevention-of-nausea-and-vomiting-after-middle-ear-surgery-granisetron-versus-ramosetron-prevention-of-vomiting-after-tonsillectomy-in-children-granisetron-versus-ramosetron-and-granisetron-droperidol-and-metoclopramide-for-preventing
#14
COMMENT
https://www.readbyqxmd.com/read/27583032/neurokinin-1-inhibitors-in-the-prevention-of-nausea-and-vomiting-from-highly-emetogenic-chemotherapy-a-network-meta-analysis
#15
REVIEW
Omar Abdel-Rahman
A network meta-analysis of the comparative effectiveness of neurokinin 1 (NK-1) inhibitors in the prophylaxis of highly emetogenic chemotherapy induced nausea and vomiting has been conducted. Eligible studies included randomized trials evaluating aprepitant, fosaprepitant, netupitant (NEPA), casopitant and rolapitant containing regimens in the setting of highly emetogenic chemotherapy. Primary outcomes of interest include complete response (CR) and rate of no significant nausea. After preclusion of ineligible studies, 19 studies were included in the final analysis...
September 2016: Therapeutic Advances in Medical Oncology
https://www.readbyqxmd.com/read/27571447/synthesis-and-pharmacological-evaluation-of-11-c-granisetron-and-18-f-fluoropalonosetron-as-pet-probes-for-5-ht3-receptor-imaging
#16
Linjing Mu, Adrienne Müller Herde, Pascal M Rüefli, Filippo Sladojevich, Selena Milicevic Sephton, Stefanie D Krämer, Andrew J Thompson, Roger Schibli, Simon M Ametamey, Martin Lochner
Serotonin-gated ionotropic 5-HT3 receptors are the major pharmacological targets for antiemetic compounds. Furthermore, they have become a focus for the treatment of irritable bowel syndrome (IBS) and there is some evidence that pharmacological modulation of 5-HT3 receptors might alleviate symptoms of other neurological disorders. Highly selective, high-affinity antagonists, such as granisetron (Kytril®) and palonosetron (Aloxi®), belong to a family of drugs (the 'setrons') that are well established for clinical use...
August 29, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27565788/2016-updated-mascc-esmo-consensus-recommendations-prevention-of-acute-chemotherapy-induced-nausea-and-vomiting-in-children
#17
L Lee Dupuis, Lillian Sung, Alexander Molassiotis, Andrea D Orsey, Wim Tissing, Marianne van de Wetering
PURPOSE: To update the 2009 recommendations for the prevention of acute chemotherapy-induced emesis in children. METHODS: We updated the original systematic literature search. Randomized studies were included in the evidence to support this guideline if they were primary studies fully published in full text in English or French; included only children less than 18 years old or, for mixed studies of adults and children, reported the pediatric results separately or the median or mean age was no more than 13 years; evaluated acute chemotherapy-induced nausea and vomiting (CINV) prophylaxis; provided sufficient information to permit determination of the emetogenicity of the antineoplastic therapy administered or the study investigators stated the emetogenicity of the chemotherapy administered; included an implicit or explicit definition of complete acute CINV response; described the antiemetic regimen in full; and reported the complete acute CINV response rate as a proportion...
January 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/27401036/local-anesthetic-like-inhibition-of-the-cardiac-sodium-channel-nav1-5-%C3%AE-subunit-by-5-ht3-receptor-antagonists
#18
Mariet P Van't Klooster, Nilufar Foadi, Axel Hage, Carsten Stoetzer, Florian Wegner, Mirjam Eberhardt, Andreas Leffler
5-hydroxytryptamine 3 receptor (5-HT3 receptor) antagonists are administered for prevention and therapy of nausea and vomiting. Although regarded as safe therapeutics, they can also provoke arrhythmias by prolonging the QRS interval. However, the mechanisms mediating this cardiotoxicity are poorly understood. Here we investigated effects of 5-HT3 receptor antagonists on the cardiac Na(+) channel Nav1.5. We explored the interaction of dolasetron, tropisetron, granisetron and ondansetron on the human α-subunit Nav1...
October 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27400689/granisetron-transdermal-system-for-treatment-of-symptoms-of-gastroparesis-a-prescription-registry-study
#19
Deena Midani, Henry P Parkman
Background/Aims: Serotonin receptor (eg, 5-HT₃) antagonists are used to treat nausea and vomiting from a variety of causes. Granisetron transdermal system (GTS) is an appealing delivery system for patients with gastroparesis. To assess if GTS improves nausea and vomiting and other gastroparesis symptoms in patients with gastroparesis. Methods: Patients with gastroparesis and symptoms of nausea and vomiting refractory to conventional treatment were treated with GTS...
October 30, 2016: Journal of Neurogastroenterology and Motility
https://www.readbyqxmd.com/read/27392852/high-throughput-screening-for%C3%A2-identification-of-blood-brain-barrier-integrity-enhancers-a-drug-repurposing-opportunity-to-rectify-vascular-amyloid-toxicity
#20
Hisham Qosa, Loqman A Mohamed, Sweilem B Al Rihani, Yazan S Batarseh, Quoc-Viet Duong, Jeffrey N Keller, Amal Kaddoumi
The blood-brain barrier (BBB) is a dynamic interface that maintains brain homeostasis and protects it from free entry of chemicals, toxins, and drugs. The barrier function of the BBB is maintained mainly by capillary endothelial cells that physically separate brain from blood. Several neurological diseases, such as Alzheimer's disease (AD), are known to disrupt BBB integrity. In this study, a high-throughput screening (HTS) was developed to identify drugs that rectify/protect BBB integrity from vascular amyloid toxicity associated with AD progression...
July 6, 2016: Journal of Alzheimer's Disease: JAD
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