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https://www.readbyqxmd.com/read/29858921/perioperative-antiemetic-efficacy-of-dexamethasone-versus-5-ht3-receptor-antagonists-a-meta-analysis-and-trial-sequential-analysis-of-randomized-controlled-trials
#1
REVIEW
Preet Mohinder Singh, Anuradha Borle, Rajesh Panwar, Jeetinder Kaur Makkar, Ian McGrath, Anjan Trikha, Ashish Sinha
BACKGROUND: Dexamethasone has many desirable pharmacologic properties for perioperative use. Its antiemetic potential has been a focus of many recent trials. METHODS: Trials comparing dexamethasone to 5-HT3-receptor antagonists (5HT3-RA) for 24 h postoperative vomiting incidences published till August 2017 were searched in the medical database. Comparisons for antiemetic efficiency variables (vomiting incidence, nausea incidence, rescue antiemetic need, and patients with complete response) during early (until 6 h) and late postoperative phase were made...
June 1, 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29801770/-consequences-of-the-monoaminergic-systems-cross-talk-in-the-antidepressant-activity
#2
L Tritschler, R Gaillard, A M Gardier, D J David, J-P Guilloux
Selective serotonin reuptake inhibitors (SSRIs) are the most prescribed antidepressant treatment for treat major depressive disorders. Despite their effectiveness, only 30% of SSRI-treated patients reach remission of depressive symptoms. SSRIs by inhibiting the serotonin transporter present some limits with residual symptoms. Increasing not only serotonin but also norepinephrine and dopamine levels in limbic areas seems to improve remission. Anatomical relationships across serotoninergic, dopaminergic and noradrenergic systems suggest tight reciprocal regulations among them...
May 22, 2018: L'Encéphale
https://www.readbyqxmd.com/read/29796708/should-palonosetron-be-a-preferred-5-ht-3-receptor-antagonist-for-chemotherapy-induced-nausea-and-vomiting-an-updated-systematic-review-and-meta-analysis
#3
REVIEW
Ronald Chow, David G Warr, Rudolph M Navari, May Tsao, Marko Popovic, Leonard Chiu, Milica Milakovic, Henry Lam, Carlo DeAngelis
PURPOSE: Chemotherapy-induced nausea and vomiting (CINV) continues to be a common side effect of systemic anticancer therapy, decreasing quality of life and increasing resource utilization. The aim of this meta-analysis was to investigate the comparative efficacy and safety of palonosetron relative to other 5-HT3 RAs. METHODS: A literature search was carried out in Ovid MEDLINE, Embase, and Cochrane Central Register of Controlled Trials. Full-text references were then screened and included in this meta-analysis if they were an RCT and had adequate data regarding one of the five primary endpoints-complete response (CR), complete control (CC), no emesis, no nausea, or no rescue medications...
May 23, 2018: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/29794645/evaluation-of-the-use-of-fosaprepitant-for-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-in-pediatric-patients
#4
Sarah Timaeus, Joshua Elder, Kyle Franco
A neurokinin-1 (NK1) receptor antagonist is recommended with a 5-HT3 receptor antagonist and dexamethasone for prevention of chemotherapy-induced nausea and vomiting (CINV) in adult patients receiving highly emetogenic chemotherapy. Data for fosaprepitant use in pediatric patients is lacking. A retrospective chart review was conducted using an electronic medical record to characterize the use of fosaprepitant in patients aged 10 months to 18 years at a single institution from August 2015 to January 2017. Thirty-nine patients received fosaprepitant 4 mg/kg (maximum, 150 mg) for prevention of CINV, and 35 were included in the analysis...
May 22, 2018: Journal of Pediatric Hematology/oncology
https://www.readbyqxmd.com/read/29793334/the-c-and-e-subunits-of-the-serotonin-5-ht-3-receptor-subtly-modulate-electrical-properties-of-the-receptor
#5
Nor Syafinaz Yaakob, Dan-Thanh Nguyen, Betty Exintaris, Helen Ruth Irving
Serotonin type 3 (5-hydroxytrptamine-3, 5-HT3 ) receptors are ligand-gated cation channels present in both central and peripheral nervous systems. In humans there are five different subunits (A, B, C, D and E) of 5-HT3 receptors which can form homomeric or heteromeric receptors that may account for discrepancies in patient responses to treatments. The present study commences characterisation of the profiles of human 5-HT3 receptors containing C and/or E subunits. Recombinant 5-HT3 receptors were expressed transiently in HEK293T cells and expression was checked via immunocytochemistry staining against each epitope-tagged subunits...
January 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775777/antidepressant-potential-of-novel-flavonoids-derivatives-from-sweet-violet-viola-odorata-l-pharmacological-biochemical-and-computational-evidences-for-possible-involvement-of-serotonergic-mechanism
#6
Nasiara Karim, Imran Khan, Abeer Abdelhalim, Ajmal Khan, Sobia Ahsan Halim
Plant-derived natural constituents are of great interest in modern drug discovery due to their natural diversity. Viola odorata L has been traditionally used for the treatment of neuropsychiatric disorders. The present study was undertaken to isolate phytoconstituents including three flavonoids 5,7-Dihydroxy-3,6-dimethoxyflavone[1] 5,7,4'-trihydroxy-3',5'dimethoxyflavone [2] and 5,7,4'-trihydroxy-3'-methoxyflavone [3] from the whole plant of Viola odorata L and to investigate the antidepressant-like effects of these compounds and their possible mechanism of action using antagonists of the serotonergic, dopaminergic and adrenergic system...
May 15, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29759144/tropisetron-attenuates-lipopolysaccharide-induced-neuroinflammation-by-inhibiting-nf-%C3%AE%C2%BAb-and-sp-nk1r-signaling-pathway
#7
Yan Yu, Wanhu Zhu, Qing Liang, Jing Liu, Xu Yang, Guangchun Sun
Tropisetron, an antagonist of serotonin type 3 receptors (5-HT3 Rs), has been investigated in colonic inflammatory process. Since substance P/neurokinin 1 receptor (SP/NK1R) signaling pathway plays a key role in several sensory neuronal inflammatory. We evaluated the anti-inflammatory activity of tropisetron in mice cerebral cortex, and discovered that it was a potential inhibitor in LPS-mediated neuron inflammation through SP/NK1R signaling pathway. We found that tropisetron significantly reduced the increased number of iba-1 positive microglia, down-regulated the gene transcription and protein expression of IL-1β,IL-6 and TNF-α in LPS stimulated cerebral cortex...
July 15, 2018: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/29747744/yokukansan-contains-compounds-that-antagonize-the-5-ht-3-receptor
#8
Yukiko Nakamura, Yusuke Ishida, Makoto Kondo, Shoichi Shimada
BACKGROUND: We recently focused on alkaloids in Uncaria hook (a constituent of the Kampo medicine, yokukansan) and identified the pharmacological action of geissoschizine methyl ether on several G protein-coupled receptors. However, the functions of other identified alkaloids in Uncaria hook, including hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine, are not clear. PURPOSE: To evaluate the effect of seven alkaloids in Uncaria hook (hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine and geissoschizine methyl ether) on the hydroxytryptamine type-3 (5-HT3 ) receptor ion channel...
April 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29702501/the-latest-consensus-on-antiemetics
#9
Jørn Herrstedt
PURPOSE OF REVIEW: The present review summarizes and discuss the most recent updated antiemetic consensus. RECENT FINDINGS: Two new neurokinin (NK)1-receptor antagonists, netupitant and rolapitant, have been approved by the Food and Drug Administration and the European Medicines Agency and incorporated in the latest versions of the MASCC/ESMO, ASCO, and NCCN guidelines. Guidelines all recommend a combination of a serotonin (5-HT)3-receptor antagonist, dexamethasone, and a NK1-receptor antagonist in patients receiving highly emetogenic chemotherapy (HEC) with the addition of the multireceptor targeting agent, olanzapine, as an option in cisplatin or anthracycline-cyclophosphamide chemotherapy...
July 2018: Current Opinion in Oncology
https://www.readbyqxmd.com/read/29682620/a-prospective-cohort-study-of-patient-reported-vomiting-retching-nausea-and-antiemetic-use-during-neoadjuvant-long-course-radiation-therapy-and-concurrent-5-fluorouracil-based-chemotherapy-for-rectal-adenocarcinoma
#10
Kristopher Dennis, Liang Zeng, Carlo De Angelis, Hans Chung, Natalie Coburn, Edward Chow, C Shun Wong
Background and purpose: Antiemetic guidelines suggest daily prophylaxis with a serotonin3 receptor antagonist (5-HT3 RA) as an option for patients receiving long-course neoadjuvant radiation therapy and concurrent 5-fluorouracil-based chemotherapy for rectal cancer, despite the risks that 5-HT3 RA-induced constipation may pose. We explored the incidence of patient-reported vomiting, retching, nausea and antiemetic intake among patients in this setting to determine if these risks are justified...
March 2018: Clinical and Translational Radiation Oncology
https://www.readbyqxmd.com/read/29677462/ondansetron-blocks-wildtype-and-p-f503l-variant-small-conductance-calcium-activated-potassium-channels
#11
Jum-Suk Ko, Shuai Guo, Jonathan Hassel, Patricia Celestino-Soper, Ty C Lynnes, James E Tisdale, James J Zheng, Stanley E Taylor, Tatiana Foroud, Michael D Murray, Richard J Kovacs, Xiaochun Li, Shien-Fong Lin, Zhenhui Chen, Matteo Vatta, Peng-Sheng Chen, Michael Rubart
The apamin-sensitive, small conductance, calcium-activated potassium (SK) current ( IKAS ) is encoded by KCNN genes. IKAS importantly contributes to cardiac repolarization in conditions associated with reduced repolarization reserve. To test the hypothesis that IKAS inhibition contributes to drug-induced long QT (diLQT) syndrome, we (1) screened for KCNN variants among patients with diLQT, (2) determined the properties of heterologously expressed wildtype and variant KCNN channels, and (3) determined if the 5-HT3 receptor antagonist ondansetron blocks IKAS ...
April 20, 2018: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29658099/identification-of-serotoninergic-system-components-in-stallion-sperm
#12
F Jiménez-Trejo, I Coronado-Mares, M Boeta, I González-Santoyo, R Vigueras-Villaseñor, C Arriaga-Canon, L A Herrera, M Tapia-Rodríguez
Assisted reproductive techniques have been used on several domestic animals to preserve desirable traits in strains of high genetic and commercial value; however in equines its efficiency rate is relatively low. To increase the conception ratio in stallions, some research groups have used pharmacological treatments which promote sperm hyperactivation in order to increase male's fertility rates. In this way, our previous work suggests that serotonin (5-HT) could be a good pharmacological candidate that facilitates conception rate in domestic horses...
April 16, 2018: Histology and Histopathology
https://www.readbyqxmd.com/read/29655943/effects-of-a-histamine-h-4-receptor-antagonist-on-cisplatin-induced-anorexia-in-mice
#13
Kouichi Yamamoto, Rikuya Okui, Atsushi Yamatodani
Cancer chemotherapy often induces gastrointestinal symptoms such as anorexia, nausea, and vomiting. Antiemetic agents are effective in inhibiting nausea and vomiting, but patients still experience anorexia. We previously reported that chemotherapeutic agent-induced anorexia is associated with an increase of inflammatory cytokines. Other studies also reported that antagonism of the histamine H4 receptor is anti-inflammatory. In this study, we investigated the involvement of the H4 receptor in the development of chemotherapy-induced anorexia in mice...
May 29, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29649465/therapeutic-time-window-and-regulation-of-autophagy-by-mild-hypothermia-after-intracerebral-hemorrhage-in-rats
#14
Feifei Song, Cen Guo, Yang Geng, Xuqing Wu, Wei Fan
Although recent studies have shown that mild hypothermia has neuroprotective effects on intracerebral hemorrhage (ICH), the therapeutic time window of the therapy and the role of autophagy as a potential neuroprotective mechanism remain unclear. This study was aimed to investigate the appropriate time window of mild hypothermia and the regulation of autophagy during the treatment in a rat model of autologous blood-injected ICH injury. The rats were divided into Sham, normothermic (NT) and hypothermic (HT) groups...
July 1, 2018: Brain Research
https://www.readbyqxmd.com/read/29587564/mirtazapine-attenuates-nicotine-seeking-behavior-in-rats
#15
Susana Barbosa-Méndez, Alberto Salazar-Juárez
BACKGROUND: Nicotine is the major psychoactive component of tobacco. A number of pharmacological therapies have been evaluated, with poor results. Given the lack of success of these therapies, several authors have proposed alternative therapeutic strategies. One of these is the use of antidepressant drugs that may have a specific effect on the neural pathways or receptors underlying nicotine addiction. Mirtazapine is an antagonist of α2 NE receptors (noradrenergic receptor), 5-HT2A/C and 5-HT3 receptors and has demonstrated efficacy in reducing behavioral effects induced by drugs of abuse in human and animal models...
March 1, 2018: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/29582424/antinociceptive-and-anti-inflammatory-effects-of-1-2-bis-4-methoxyphenylselanyl-styrene-in-mice-involvement-of-the-serotonergic-system
#16
Roberta Gonçalves Anversa, Fernanda Severo Sabedra Sousa, Paloma Taborda Birmann, David Borba Lima, Eder João Lenardão, César Augusto Bruning, Lucielli Savegnago
BACKGROUND: Pain is one of the most prevalent, costly and disabling conditions that reduces quality of life. Although there are many analgesics available, there is some concern regarding their efficacy, safety and side effects. Organic selenium compounds are attractive targets of various research groups due to their pharmacological properties. OBJECTIVES: The aim of this study was to evaluate the antinociceptive and anti-inflammatory activity of 1,2-bis-(4-methoxyphenylselanyl) styrene (BMOSE) in mice, as well as to investigate the mechanism involved in the antinociceptive effect...
March 27, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29566578/aminobenzisoxazole-compounds-as-agonists-of-%C3%AE-7-nicotinic-acetylcholine-receptors-a-patent-evaluation-wo-2017027600
#17
Yang He, Jingshan Shen
alpha 7 subtype nicotinic acetylcholine receptor (α7 nAChR) ligands, that is, ligands that interact with the orthosteric or allosteric binding sites of α7 nAChR, hold great potential for several therapeutic applications. Numerous compounds have been designed targeting α7 nAChR but most of them cannot be used therapeutically for various reasons. Areas covered: The patent application describes a series of germinal substituted aminobenzisoxazole compounds as α7 nAChR ligands. These compounds were claimed as potential therapeutics for treating and/or improving cognitive function...
May 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29559911/vortioxetine-treatment-reverses-subchronic-pcp-treatment-induced-cognitive-impairments-a-potential-role-for-serotonin-receptor-mediated-regulation-of-gaba-neurotransmission
#18
Alan L Pehrson, Christian S Pedersen, Kirstine Sloth Tølbøl, Connie Sanchez
Major depressive disorder (MDD) is associated with cognitive impairments that may contribute to poor functional outcomes. Clinical data suggests that the multimodal antidepressant vortioxetine attenuates some cognitive impairments in MDD patients, but the mechanistic basis for these improvements is unclear. One theory suggests that vortioxetine improves cognition by suppressing γ-amino butyric acid (GABA)ergic neurotransmission, thereby increasing glutamatergic activation. Vortioxetine's effects on cognition, GABA and glutamate neurotransmission have been supported in separate experiments, but no empirical work has directly connected vortioxetine's cognitive effects to those on GABA and glutamate neurotransmission...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29556812/getting-it-right-the-first-time-recent-progress-in-optimizing-antiemetic-usage
#19
Lee Schwartzberg
Recent years have witnessed significant improvements in the prevention and management of chemotherapy-induced nausea and vomiting (CINV), allowing patients to complete their prescribed chemotherapy regimens without compromising quality of life. This reduction in the incidence of CINV can be primarily attributed to the emergence of effective, well-tolerated antiemetic therapies, including serotonin (5-hydroxytryptamine or 5-HT3) receptor antagonists, neurokinin-1 (NK-1) receptor antagonists, and the atypical antipsychotic olanzapine...
March 2018: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/29548482/efficacy-of-neurokinin-1-receptor-antagonists-in-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-in-patients-receiving-carboplatin-based-chemotherapy-a-systematic-review-and-meta-analysis
#20
REVIEW
Massimo Di Maio, Chiara Baratelli, Paolo Bironzo, Francesca Vignani, Emilio Bria, Elisa Sperti, Maddalena Marcato, Fausto Roila
According to current ESMO - MASCC guidelines, a combination of a neurokinin-1 receptor antagonist (NK1RA), dexamethasone and a 5-HT3 receptor antagonist (5-HT3RA) is recommended to prevent carboplatin-induced emesis, albeit with moderate level of confidence and not unanimous consensus. We performed a meta-analysis of randomized trials (RCTs) comparing NK1RA + dexamethasone + 5-HT3RA vs. dexamethasone + 5-HT3RA in patients receiving the first cycle of carboplatin-based chemotherapy. Primary outcome was complete response (CR), defined as no emesis and no use of rescue medication...
April 2018: Critical Reviews in Oncology/hematology
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