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https://www.readbyqxmd.com/read/28501575/the-anti-asthmatic-drug-pranlukast-suppresses-the-delayed-phase-vomiting-and-reverses-intracellular-indices-of-emesis-evoked-by-cisplatin-in-the-least-shrew-cryptotis-parva
#1
Nissar A Darmani, Seetha Chebolu, Weixia Zhong, William D Kim, Matthew Narlesky, Joia Adams, Fanglong Dong
The introduction of second generation serotonin 5-HT3 receptor (5-HT3) antagonist palonosetron combined with long-acting substance P neurokinin NK1 receptor (NK1) antagonists (e.g. netupitant) has substantially improved antiemetic therapy against early- and delayed-phases of emesis caused by highly emetogenic chemotherapeutics such as cisplatin. However, the improved efficacy comes at a cost that many patients cannot afford. We introduce a new class of antiemetic, the antiasthmatic leukotriene CysLT1 receptor antagonist pranlukast for the suppression of cisplatin-evoked vomiting...
May 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28460548/clinical-pharmacology-of-neurokinin-1-receptor-antagonists-for-the-treatment-of-nausea-and-vomiting-associated-with-chemotherapy
#2
Bernardo Rapoport, Teresa Smit
Five NK-1 RA formulations are commercially available to treat the delayed phase of chemotherapy-induced nausea and vomiting (CINV) occurring between days 2-5 post chemotherapy (aprepitant oral capsule and suspension, fosaprepitant intravenous infusion, netupitant/palonosetron capsules and rolapitant tablet) but no direct comparative studies have been conducted to determine their relative clinical utility. Areas covered: Information on pharmacology and safety of the NK-1 RAs derived from PubMed showed that all bind the NK-1 receptor with high affinity and selectivity...
May 2, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28453189/guideline-for-the-prevention-of-acute-chemotherapy-induced-nausea-and-vomiting-in-pediatric-cancer-patients-a-focused-update
#3
Priya Patel, Paula D Robinson, Jennifer Thackray, Jacqueline Flank, Mark T Holdsworth, Paul Gibson, Andrea Orsey, Carol Portwine, Jason Freedman, Jennifer R Madden, Robert Phillips, Lillian Sung, L Lee Dupuis
This update of the 2013 clinical practice guideline provides clinicians with guidance regarding the use of aprepitant and palonosetron for the prevention of acute chemotherapy-induced nausea and vomiting (CINV) in children. The recommendations were based on three systematic reviews. Substantive changes were made to the guideline recommendations including the inclusion of palonosetron to the 5-HT3 antagonists recommended for children receiving highly emetogenic chemotherapy (HEC) and the recommendation of aprepitant for children 6 months of age or older receiving HEC...
April 28, 2017: Pediatric Blood & Cancer
https://www.readbyqxmd.com/read/28414209/polypharmacological-in-silico-bioactivity-profiling-and-experimental-validation-uncovers-sedative-hypnotic-effects-of-approved-and-experimental-drugs-in-rat
#4
Georgios Drakakis, Keith A Wafford, Suzanne C Brewerton, Michael J Bodkin, David A Evans, Andreas Bender
In this work, we describe the computational ("in silico") mode-of-action analysis of CNS-active drugs, which is taking both multiple simultaneous hypotheses as well as sets of protein targets for each mode-of-action into account, and which was followed by successful prospective in vitro and in vivo validation. Using sleep-related phenotypic readouts describing both efficacy and side effects for 491 compounds tested in rat, we defined an "optimal" (desirable) sleeping pattern. Compounds were subjected to in silico target prediction (which was experimentally confirmed for 21 out of 28 cases), followed by the utilization of decision trees for deriving polypharmacological bioactivity profiles...
May 1, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28396308/new-options-and-controversies-in-the-management-of-chemotherapy-induced-nausea-and-vomiting
#5
Sara M Koth, Jill Kolesar
PURPOSE: An expanding array of options for prevention and treatment of chemotherapy-induced nausea and vomiting (CINV), including regimens containing olanzapine or recently approved neurokinin 1 (NK1) receptor antagonists, are reviewed. SUMMARY: Up to 80% of patients receiving chemotherapy have CINV. Current practice guidelines recommend that patients treated with highly emetogenic chemotherapy also receive a 3-drug antiemetic regimen initiated on the day of and continued for 3 days after chemotherapy administration, with the most commonly used 3-drug regimen consisting of an NK1 receptor antagonist, a 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist, and dexamethasone...
April 10, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28392826/nepa-a-new-fixed-combination-of-netupitant-and-palonosetron-is-a-cost-effective-intervention-for-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-in-the-uk
#6
REVIEW
Helene Cawston, Francois Bourhis, Jennifer Eriksson, Pierfrancesco Ruffo, Paolo D'Agostino, Marco Turini, Lee Schwartzberg, Alistair McGuire
BACKGROUND: The objective was to evaluate the cost-effectiveness of NEPA, an oral fixed combination netupitant (NETU, 300 mg) and palonosetron (PA, 0.5 mg) compared with aprepitant and palonosetron (APPA) or palonosetron (PA) alone, to prevent chemotherapy-induced nausea and vomiting (CINV) in patients undergoing treatment with highly or moderately emetogenic chemotherapy (HEC or MEC) in the UK. SCOPE: A systematic literature review and meta-analysis were undertaken to compare NEPA with currently recommended anti-emetics...
2017: Drugs in Context
https://www.readbyqxmd.com/read/28376213/neurokinin-1-receptor-antagonist-based-triple-regimens-in-preventing-chemotherapy-induced-nausea-and-vomiting-a-network-meta-analysis
#7
Yaxiong Zhang, Yunpeng Yang, Zhonghan Zhang, Wenfeng Fang, Shiyang Kang, Youli Luo, Jin Sheng, Jianhua Zhan, Shaodong Hong, Yan Huang, Ningning Zhou, Hongyun Zhao, Li Zhang
Background: Neurokinin-1 receptor antagonists (NK-1RAs) are widely used for chemotherapy-induced nausea and vomiting (CINV) control in patients with highly emetogenic chemotherapy (HEC) and/or moderately emetogenic chemotherapy (MEC). Whether the efficacy and toxicity of antiemesis are different among various NK-1RA-based triple regimens is unknown. Methods: Data of complete responses (CRs) in the acute, delayed, and overall phases and treatment-related adverse events (TRAEs) were extracted from electronic databases...
February 1, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/28365889/antiemetic-therapy-for-non-anthracycline-and-cyclophosphamide-moderately-emetogenic-chemotherapy
#8
REVIEW
Naoki Inui
Although antiemetic management in cancer therapy has improved, chemotherapy-induced nausea and vomiting remain common and troubling adverse events. Chemotherapeutic agents are classified based on their emetogenic effects, and appropriate antiemetics are recommended according to this categorization. Chemotherapy categorized as moderately emetogenic is associated with a wide spectrum of emetic risks. Combined anthracycline and cyclophosphamide regimens have been recently reclassified as highly emetogenic chemotherapy regimen...
May 2017: Medical Oncology
https://www.readbyqxmd.com/read/28363413/action-of-bacopa-monnieri-to-antagonize-cisplatin-induced-emesis-in-suncus-murinus-house-musk-shrew
#9
Ihsan Ullah, Fazal Subhan, Zengbing Lu, Sze Wa Chan, John A Rudd
Bacopa monnieri (BM, family Scrophulariaceae) is used in several traditional systems of medicine for the management of epilepsy, depression, neuropathic pain, sleep disorders and memory deficits. The present study investigated the potential of BM methanol (BM-MetFr) and BM n-butanol fractions (BM-ButFr) to reduce chemotherapy-induced emesis in Suncus murinus (house musk shrew). Cisplatin (30 mg/kg, i.p.) reliably induced retching and/or vomiting over a 2 day period. BM-MetFr (10-40 mg/kg, s.c.) and BM-ButFr (5-20 mg/kg, s...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28357406/comparison-of-ramosetron-with-palonosetron-for-prevention-of-postoperative-nausea-and-vomiting-in-patients-receiving-opioid-based-intravenous-patient-controlled-analgesia-after-gynecological-laparoscopy
#10
Eun Jin Ahn, Geun Joo Choi, Hyun Kang, Chong Wha Baek, Yong Hun Jung, Young Cheol Woo
We aimed to compare the effects of ramosetron and palonosetron in the prevention of postoperative nausea and vomiting (PONV) in patients that received opioid-based intravenous patient-controlled analgesia (IV-PCA) after gynecological laparoscopy. We reviewed the electronic medical records of 755 adults. Patients were classified into two groups, ramosetron (group R, n = 589) versus palonosetron (group P, n = 166). Based on their confounding factors, 152 subjects in each group were selected after the implementation of propensity score matching...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28346200/compatibility-and-stability-of-rolapitant-injectable-emulsion-admixed-with-intravenous-palonosetron-hydrochloride
#11
George Wu, Stanley Yeung, Frank Chen
Neurokinin-1 receptor antagonist, 5-hydroxytryptamine-3 RA, and dexamethasone combination therapy is standard of care for the prevention of chemotherapy-induced nausea and vomiting. Herein we describe the physical and chemical stability of rolapitant injectable emulsion 166.5 mg in 92.5 mL (185 mg hydrochloride salt) admixed with palonosetron injection 0.25 mg in 5 mL (0.28 mg hydrochloride salt). Admixtures were prepared and stored in two types of container closures (110-mL Crystal Zenith plastic and glass bottles) and four types of intravenous administration sets (or intravenous tubing sets)...
January 2017: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28285236/efficacy-of-nepa-netupitant-palonosetron-across-multiple-cycles-of-chemotherapy-in-breast-cancer-patients-a-subanalysis-from-two-phase-iii-trials
#12
Hope S Rugo, Giorgia Rossi, Giada Rizzi, Matti Aapro
OBJECTIVES: Breast cancer (BC) patients represent a high-risk population for experiencing chemotherapy-induced nausea and vomiting (CINV), since they frequently receive highly emetogenic anthracycline-cyclophosphamide-based (AC) chemotherapy, and are often female and young, two predisposing risk factors for CINV. Guidelines recommend the combination of a neurokinin-1 receptor antagonist (NK1RA), 5-hydroxytryptamine-3 RA (5-HT3RA), and dexamethasone (DEX) for CINV prophylaxis in AC-treated patients...
March 9, 2017: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/28250483/intravenous-palonosetron-compared-with-a-combination-of-ramosetron-and-dexamethasone-in-preventing-post-operative-nausea-and-vomiting-in-patients-undergoing-gynaecological-surgeries-under-spinal-anaesthesia-a-randomised-study
#13
Archana B Narayanappa, Shivakumar Gurulingaswamy, Umesh N Prabhakaraiah, Somsundar R Gurushanth, Vinay Sapare, Nagaraj Goud
BACKGROUND AND AIMS: Post-operative nausea and vomiting (PONV) is one of the most common complications in patients undergoing gynaecological surgeries under spinal anaesthesia (SA). Palonosetron has the unique property of controlling 'delayed chemotherapy-induced nausea and vomiting' when compared to older serotonin antagonists. This study compared the effectiveness of palonosetron with a combination of ramosetron and dexamethasone in preventing PONV. METHODS: Sixty patients undergoing gynaecological surgeries under SA were randomly allocated into two groups of thirty each, to receive either a combination of 0...
February 2017: Indian Journal of Anaesthesia
https://www.readbyqxmd.com/read/28191518/corticosteroids-the-oldest-agent-in-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-what-about-the-guidelines
#14
Florence Van Ryckeghem
Chemotherapy-induced nausea and vomiting (CINV) remains one of the most disturbing side effects of cancer treatment. Research in antiemetic therapy has progressed gradually since the early eighties, and the development of antiemetic agents continues. This review focuses on the current management of CINV based on the most recent guidelines, and adherence to the latter is examined more carefully. Setrons (5HT3 receptor antagonists), corticosteroids, and NK-1 receptor antagonists are the cornerstones of antiemetic therapy...
April 1, 2016: Journal of Translational Internal Medicine
https://www.readbyqxmd.com/read/28160077/effectiveness-of-antiemetic-triplet-therapy-with-aprepitant-palonosetron-and-dexamethasone-for-gynecologic-cancer-patients-receiving-carboplatin-and-paclitaxel-a-prospective-single-arm-study
#15
Fuminori Ito, Naoto Furukawa
PURPOSE: There is no positive evidence for the efficacy of antiemetic triplet therapy with aprepitant (APR), palonosetron (PALO), and dexamethasone (DEX) for moderate emetogenic chemotherapy, especially for gynecologic malignancies. Thus, the present study evaluated the efficacy of this triplet therapy in patients receiving carboplatin and paclitaxel (CP) for gynecologic malignancy. METHODS: Seventy patients with gynecologic cancer receiving CP were enrolled into a prospective single-arm study with APR (125 mg on day 1, 80 mg on days 2-3), PALO (0...
February 4, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28156661/efficacy-of-triple-antiemetic-therapy-palonosetron-dexamethasone-aprepitant-for-chemotherapy-induced-nausea-and-vomiting-in-patients-receiving-carboplatin-based-moderately-emetogenic-chemotherapy
#16
Kunihiko Kobayashi, Mitsunori Hino, Masahiro Ando, Susumu Takeuchi, Masahiro Seike, Kaoru Kubota, Akihiko Gemma
226 Background: Chemotherapy-induced nausea and vomiting (CINV) is a major adverse toxicity of cancer chemotherapy. Recommended treatments for prevention of CINV vary among guidelines, and optimal care for CINV caused by moderately emetogenic chemotherapy has not been established. This study assess efficacy and safety of triple antiemetic therapy consist palonosetron, dexamethasone and aprepitant for carboplatin-based chemotherapy. METHODS: Chemotherapy-naïve patients with lung cancer scheduled for a first course of a carboplatin-containing regimen formed the study cohort...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28156571/disparities-in-the-availability-of-and-access-to-antiemetics-recommended-by-the-international-antiemetic-guidelines-in-serbia-japan-and-nepal
#17
Ana Zilic, Bishal Gyawali
117 Background: Guideline-consistent antiemetic therapy requires 4 classes of antiemetics (AEs) to be available and accessible for the optimal prevention of chemotherapy induced nausea and vomiting (CINV): serotonin3 receptor antagonists (5HT3RAs), neurokinin 1 receptor antagonists (NK1RAs), dopamine receptor antagonists (DOPRAs) and dexamethasone. To evaluate disparities in the availability and accessibility of AEs recommended by the international antiemetic guidelines for the prevention of CINV inpatients treated in governmental hospitals in Nepal (low), Serbia (upper-middle) and Japan (high-income)...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28152932/national-comprehensive-cancer-network-petitions-submissions-and-outcomes
#18
Dinah Faith Huff, William J Hrushesky, Charles Lee Bennett, Kevin Knopf, Michael Baum
248 Background: The National Comprehensive Cancer Network (NCCN) invites petitions to its scientific panels. Most ( > 95%) are from the pharmaceutical industry lobbying to include their products in the NCCN Guidelines. Rarely, physicians request scientific scrutiny of the guidelines. We report the experience of Oncology Analytics (OA) with petition submissions and the possible impact on guidelines. METHODS: From 2011-2015, OA made 7 petitions to NCCN. The content of each was tracked into subsequent NCCN Guidelines to ascertain whether any changes resulted...
March 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28108820/prevention-of-chemotherapy-induced-nausea-the-role-of-neurokinin-1-nk1-receptor-antagonists
#19
Snežana M Bošnjak, Richard J Gralla, Lee Schwartzberg
Chemotherapy-induced nausea (CIN) has a significant negative impact on the quality of life of cancer patients. The use of 5-hydroxytryptamine-3 (5-HT3) receptor antagonists (RAs) has reduced the risk of vomiting, but (except for palonosetron) their effect on nausea, especially delayed nausea, is limited. This article reviews the role of NK1RAs when combined with 5-HT3RA-dexamethasone in CIN prophylaxis. Aprepitant has not shown consistent superiority over a two-drug (ondansetron-dexamethasone) combination in nausea control after cisplatin- or anthracycline-cyclophosphamide (AC)-based highly emetogenic chemotherapy (HEC)...
May 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28096679/a-phase-ii-single-arm-trial-of-palonosetron-for-the-prevention-of-acute-and-delayed-chemotherapy-induced-nausea-and-vomiting-in-malignant-glioma-patients-receiving-multidose-irinotecan-in-combination-with-bevacizumab
#20
Mary Lou Affronti, Sarah Woodring, Katherine B Peters, James E Herndon, Frances McSherry, Patrick N Healy, Annick Desjardins, James J Vredenburgh, Henry S Friedman
PURPOSE: Given that the prognosis of recurrent malignant glioma (MG) remains poor, improving quality of life (QoL) through symptom management is important. Meta-analyses establishing antiemetic guidelines have demonstrated the superiority of palonosetron (PAL) over older 5-hydroxytryptamine 3-receptor antagonists in chemotherapy-induced nausea and vomiting (CINV) prevention, but excluded patients with gliomas. Irinotecan plus bevacizumab is a treatment frequently used in MG, but is associated with low (55%) CINV complete response (CR; no emesis or use of rescue antiemetic) with commonly prescribed ondansetron...
2017: Therapeutics and Clinical Risk Management
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