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Aprepitant

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https://www.readbyqxmd.com/read/28032216/effectiveness-of-aprepitant-in-addition-to-ondansetron-in-the-prevention-of-nausea-and-vomiting-caused-by-fractionated-radiotherapy-to-the-upper-abdomen-avert
#1
Steven Ades, M Halyard, K Wilson, T Ashikaga, R Heimann, S Kumar, W Blackstock
PURPOSE: Despite a lower risk of nausea and vomiting in patients receiving radiotherapy to the upper abdomen (UA-RINV) with prophylactic 5-HT3 antagonist therapy, patients can still experience UA-RINV. The aim of this multicenter phase II study was to assess effectiveness, safety, and tolerability of protracted dual NK1-receptor and 5-HT3 antagonist prophylaxis against UA-RINV. METHODS: Patients receiving fractionated radiotherapy with radiosensitizing chemotherapy received oral ondansetron 8 mg po q12 h and aprepitant 125/80/80 mg on a Monday, Wednesday, Friday schedules throughout radiotherapy...
December 28, 2016: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28018788/efficacy-of-triple-antiemetic-therapy-palonosetron-dexamethasone-aprepitant-for-chemotherapy-induced-nausea-and-vomiting-in-patients-receiving-carboplatin-based-moderately-emetogenic-chemotherapy
#2
Toshimichi Miya, Kunihiko Kobayashi, Mitsunori Hino, Masahiro Ando, Susumu Takeuchi, Masahiro Seike, Kaoru Kubota, Akihiko Gemma
BACKGROUND: Chemotherapy-induced nausea and vomiting (CINV) is a major adverse toxicity of cancer chemotherapy. Recommended treatments for prevention of CINV vary among published guidelines, and optimal care for CINV caused by moderately emetogenic chemotherapy has not been established. This study assessed the efficacy and safety of triple antiemetic therapy comprising palonosetron, dexamethasone and aprepitant for carboplatin-based chemotherapy. Chemotherapy-naïve patients with lung cancer scheduled for a first course of a carboplatin-containing regimen formed the study cohort...
2016: SpringerPlus
https://www.readbyqxmd.com/read/28013351/differential-effects-of-aprepitant-a-clinically-used-neurokinin-1-receptor-antagonist-on-the-expression-of-conditioned-psychostimulant-versus-opioid-reward
#3
Padmanabhan Mannangatti, Santhanalakshmi Sundaramurthy, Sammanda Ramamoorthy, Lankupalle D Jayanthi
RATIONALE: Neurokinin-1 receptor (NK1R) signaling modulates behaviors associated with psychostimulants and opioids. Psychostimulants, such as amphetamine (AMPH) and cocaine, bind to monoamine transporters and alter their functions. Both dopamine and norepinephrine transporters are regulated by NK1R activation suggesting a role for NK1R mediated catecholamine transporter regulation in psychostimulant-mediated behaviors. OBJECTIVES: The effect of in vivo administration of aprepitant (10 mg/kg) on the expression of AMPH (0...
December 24, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27986268/-incidence-and-risk-factors-for-ifosfamide-related-encephalopathy-in-sarcoma-patients
#4
Natacha Stern, Ilyes Sakji, Anne-Sophie Defachelles, Cyril Lervat, Thomas Ryckewaert, Guillaume Marliot, Charlotte Peugniez, Dominique Deplanque, Nicolas Penel
CONTEXT: Ifosfamide remains one of the major cytotoxic drugs for sarcoma management. Ifosfamid-related encephalopathy (IRE) is a rare but severe adverse event, without clearly identified risk factors. METHOD: We have carried out a single-center, retrospective study to assess the occurrence and the risk factors for IRE after the two first cycles of chemotherapy. We have collected the data-describing patients, biological data, tumors characteristics (histology, leptomeningeal metastasis) and ifosfamide administration modalities...
December 13, 2016: Bulletin du Cancer
https://www.readbyqxmd.com/read/27980320/substance-p-inhibits-the-collagen-synthesis-of-rat-myocardial-fibroblasts-induced-by-ang-ii
#5
Zhiyong Yang, Xinzhong Zhang, Naipeng Guo, Bin Li, Sheng Zhao
BACKGROUND The aim of this study was to explore the regulating effects of Substance P (SP) on the collagen synthesis of rat myocardial fibroblasts (CFBs) induced by angiotensin II (Ang II) and its potential mechanism. MATERIAL AND METHODS The CFBs of a neonatal SD rat were separately cultured and divided into the control group, Ang II treatment group, and treatment groups with different concentrations of SP, Ang II +; each group was given corresponding treatment respectively. RESULTS Ang II successfully induced the collagen synthesis of CFBs...
December 16, 2016: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/27940083/statistical-investigation-of-simulated-fed-intestinal-media-composition-on-the-equilibrium-solubility-of-oral-drugs
#6
Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin W Halbert
Gastrointestinal fluid is a complex milieu and it is recognised that gut drug solubility is different to that observed in simple aqueous buffers. Simulated gastrointestinal media have been developed covering fasted and fed states to facilitate in vitro prediction of gut solubility and product dissolution. However, the combination of bile salts, phospholipids, fatty acids and proteins in an aqueous buffered system creates multiple phases and drug solubility is therefore a complex interaction between these components, which may create unique environments for each API...
December 7, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27930525/efficacy-analysis-of-the-aprepitant-combined-antiemetic-prophylaxis-for-non-round-cell-soft-tissue-sarcoma-patients-received-adriamycin-and-ifosfamide-therapy
#7
Hitoshi Kusaba, Hozumi Kumagai, Kyoko Inadomi, Tomoya Matsunobu, Katsumi Harimaya, Kotoe Takayoshi, Shuji Arita, Hiroshi Ariyama, Koichi Akashi, Eishi Baba
Appropriate antiemetic prophylaxis for moderately emetogenic chemotherapy in patients with non-round cell soft-tissue sarcomas (NRC-STS) remains unclear. We retrospectively investigated efficacy and safety of aprepitant-combined antiemetic prophylaxis in patients with NRC-STS receiving adriamycin plus ifosfamide (AI) therapy. Forty NRC-STS patients were enrolled, their median age was 50 years (range 18-74), and 13 (32.5%) were female. Median cycle number of AI therapy was 4. Twenty patients received the doublet antiemetic prophylaxis (5-hydroxytryptamine-3 receptor antagonist and dexamethasone), and 20 received triplet (5-hydroxytryptamine-3 receptor antagonist, dexamethasone, and aprepitant)...
December 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27888795/targeting-tachykinin-receptors-in-neuroblastoma
#8
Anton G Henssen, Andrea Odersky, Annabell Szymansky, Marleen Seiler, Kristina Althoff, Anneleen Beckers, Frank Speleman, Simon Schäfers, Katleen De Preter, Kathy Astrahanseff, Joachim Struck, Alexander Schramm, Angelika Eggert, Andreas Bergmann, Johannes H Schulte
Neuroblastoma is the most common extracranial tumor in children. Despite aggressive multimodal treatment, high-risk neuroblastoma remains a clinical challenge with survival rates below 50%. Adding targeted drugs to first-line therapy regimens is a promising approach to improve survival in these patients. TACR1 activation by substance P has been reported to be mitogenic in cancer cell lines. Tachykinin receptor (TACR1) antagonists are approved for clinical use as an antiemetic remedy since 2003. Tachykinin receptor inhibition has recently been shown to effectively reduce growth of several tumor types...
November 18, 2016: Oncotarget
https://www.readbyqxmd.com/read/27873176/palonosetron-aprepitant-and-dexamethasone-for-prevention-of-nausea-and-vomiting-after-high-dose-melphalan-in-autologous-transplantation-for-multiple-myeloma-a-phase-ii-study
#9
Atsushi Isoda, Rie Saito, Fuminori Komatsu, Yuki Negishi, Noriyasu Oosawa, Tetsuya Ishikawa, Yuri Miyazawa, Morio Matsumoto, Morio Sawamura, Akihiro Manaka
Chemotherapy-induced nausea and vomiting (CINV) is a significant side effect in multiple myeloma (MM) patients receiving high-dose melphalan treatment followed by autologous stem cell transplantation (ASCT). We evaluated the efficacy and safety of a triple antiemetic combination of palonosetron, aprepitant, and low-dose dexamethasone in 24 MM patients who received melphalan conditioning (100 mg/m(2) on days 1-2) before ASCT (on day 4). Intravenous palonosetron (0.75 mg on day 1), oral aprepitant (125 mg on day 1; 80 mg on days 2-4), and intravenous dexamethasone (6...
November 21, 2016: International Journal of Hematology
https://www.readbyqxmd.com/read/27868231/aprepitant-in-pediatric-patients-using-moderate-and-highly-emetogenic-protocols-a-systematic-review-and-meta-analyses-of-randomized-controlled-trials
#10
Lucas Miyake Okumura, Fernanda D' Athayde Rodrigues, Maria Angelica Pires Ferreira, Leila Beltrami Moreira
AIMS: To review the efficacy and safety of aprepitant in combination with ondansetron and dexamethasone (triple therapy) in children and adolescents on moderate to highly emetogenic chemotherapy. METHODS: Medline, Embase, Scielo, Lilacs, Cochrane and congress abstracts published until September 2016 were used as data sources. Two reviewers independently selected manuscripts and extracted data. A third reviewer solved discrepancies in study's selection and data extraction...
November 20, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27835967/carbonyl-reductase-identification-and-development-of-whole-cell-biotransformation-for-highly-efficient-synthesis-of-r-3-5-bis-trifluoromethyl-phenyl-ethanol
#11
Kangling Chen, Kefei Li, Jian Deng, Baoqi Zhang, Jinping Lin, Dongzhi Wei
BACKGROUND: (R)-[3,5-bis(trifluoromethyl)phenyl] ethanol [(R)-3,5-BTPE] is a valuable chiral intermediate for Aprepitant (Emend) and Fosaprepitant (Ivemend). Biocatalyzed asymmetric reduction is a preferred approach to synthesize highly optically active (R)-3,5-BTPE. However, the product concentration and productivity of reported (R)-3,5-BTPE synthetic processes remain unsatisfied. RESULTS: A NADPH-dependent carbonyl reductase from Lactobacillus kefir (LkCR) was discovered by genome mining for reduction of 3,5-bis(trifluoromethyl) acetophenone (3,5-BTAP) into (R)-3,5-BTPE with excellent enantioselectivity...
November 11, 2016: Microbial Cell Factories
https://www.readbyqxmd.com/read/27826874/efficacy-and-safety-of-aprepitant-for-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-during-the-first-cycle-of-moderately-emetogenic-chemotherapy-in-korean-patients-with-a-broad-range-of-tumor-types
#12
Jeong Eun Kim, Joung-Soon Jang, Jae-Weon Kim, Yong Lee Sung, Chi-Heum Cho, Myung-Ah Lee, Do-Jin Kim, Myung-Ju Ahn, Kil Yeon Lee, Sun Jin Sym, Myong Choel Lim, Hun Jung, Eun Kim Cho, Kyung Wan Min
PURPOSE: This study evaluated the efficacy and safety of a 3-day aprepitant regimen for the prevention of chemotherapy-induced nausea and vomiting (CINV) during the first cycle of non-anthracycline plus cyclophosphamide (AC)-based moderately emetogenic chemotherapy (MEC) based on government guidelines in Korean patients. METHODS: This multicenter, randomized, double-blind, phase IV trial (NCT01636947) enrolled adult South Korean patients with a broad range of tumor types who were scheduled to receive a single dose of ≥1 MEC agent...
November 8, 2016: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/27826027/evaluation-of-pentravan-%C3%A2-pentravan-%C3%A2-plus-phytobase-%C3%A2-lipovan-%C3%A2-and-pluronic-lecithin-organogel-for-the-transdermal-administration-of-antiemetic-drugs-to-treat-chemotherapy-induced-nausea-and-vomiting-at-the-hospital
#13
F Bourdon, M Lecoeur, L Leconte, V Ultré, M Kouach, P Odou, C Vaccher, C Foulon
The objective of this study was to evaluate five commercial ready-to-use transdermal vehicles (Phytobase(®), Lipovan(®), Pentravan(®), Pentravan(®) Plus and Pluronic Lecithin Organogel (PLO)), for the compounding of three antiemetic drugs (ondansetron, dexamethasone and aprepitant) and their administration in combination to treat chemotherapy-induced nausea and vomiting (CINV) at the hospital. Drugs were individually formulated in these vehicles and in mixture in Pentravan(®) Plus using different penetration enhancers...
December 30, 2016: International Journal of Pharmaceutics
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
#14
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/27795228/neurokinin-1-receptor-antagonist-based-triple-regimens-in-preventing-chemotherapy-induced-nausea-and-vomiting-a-network-meta-analysis
#15
REVIEW
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 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/27793881/therapeutic-innovations-for-targeting-hepatoblastoma
#16
REVIEW
Agnès Garnier, Matthias Ilmer, Roland Kappler, Michael Berger
Hepatoblastoma is the most common pediatric liver tumor. Despite recent advances in treatment with surgery and chemotherapy, the prognosis in advanced stages remains poor. The neurokinin-1 receptor (NK1R) has recently been described to be pivotal in the development of cancer. Furthermore, overwhelming evidence now exists showing that pharmacological manipulation of NK1R can cause a robust anticancer effect. Consequently, NK1R antagonists, such as the clinical drug aprepitant, are under current investigation as future innovative anticancer agents...
2016: Anticancer Research
https://www.readbyqxmd.com/read/27782122/specific-inhibition-of-icam-1-effectively-reduces-bladder-inflammation-in-a-rat-model-of-severe-non-bacterial-cystitis
#17
Xiang Zhang, Hongchao He, Guoliang Lu, Tianyuan Xu, Liang Qin, Xianjin Wang, Xingwei Jin, Boke Liu, Zhonghua Zhao, Zhoujun Shen, Yuan Shao
The development and progression of bladder pain syndrome/interstitial cystitis (BPS/IC) is closely related to bladder inflammation. Intercellular adhesion molecule 1 (ICAM-1) is associated with bladder inflammation in BPS/IC. We investigated the effect of specific inhibition of ICAM-1 using an anti-ICAM-1 antibody (AIA) on bladder inflammation in a rat model of severe non-bacterial cystitis (NBC) resembling BPS/IC by evaluating the bladder inflammation grade, mast cell infiltration and related cytokines and receptors...
October 26, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27762631/optimization-of-the-ussing-chamber-setup-with-excised-rat-intestinal-segments-for-dissolution-permeation-experiments-of-poorly-soluble-drugs
#18
Kristin Forner, Carl Roos, David Dahlgren, Filippos Kesisoglou, Moritz A Konerding, Johanna Mazur, Hans Lennernäs, Peter Langguth
CONTEXT: Prediction of the in vivo absorption of poorly soluble drugs may require simultaneous dissolution/permeation experiments. In vivo predictive media have been modified for permeation experiments with Caco-2 cells, but not for excised rat intestinal segments. OBJECTIVE: The present study aimed to improve the setup of dissolution/permeation experiments with excised rat intestinal segments by assessing suitable donor and receiver media. METHODS: The regional compatibility of rat intestine in Ussing chambers with modified Fasted and Fed State Simulated Intestinal Fluids (Fa/FeSSIFmod) as donor media was evaluated via several parameters that reflect the viability of the excised intestinal segments...
October 20, 2016: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/27746521/postoperative-nausea-and-vomiting-a-simple-yet-complex-problem
#19
REVIEW
Safiya Imtiaz Shaikh, D Nagarekha, Ganapati Hegade, M Marutheesh
Postoperative nausea and vomiting (PONV) is one of the complex and significant problems in anesthesia practice, with growing trend toward ambulatory and day care surgeries. This review focuses on pathophysiology, pharmacological prophylaxis, and rescue therapy for PONV. We searched the Medline and PubMed database for articles published in English from 1991 to 2014 while writing this review using "postoperative nausea and vomiting, PONV, nausea-vomiting, PONV prophylaxis, and rescue" as keywords. PONV is influenced by multiple factors which are related to the patient, surgery, and pre-, intra-, and post-operative anesthesia factors...
September 2016: Anesthesia, Essays and Researches
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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