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Aprepitant

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https://www.readbyqxmd.com/read/29788447/varicella-zoster-virus-induces-nuclear-translocation-of-the-neurokinin-1-receptor-promoting-lamellipodia-formation-and-viral-spread-in-spinal-astrocytes
#1
Andrew N Bubak, Christina N Como, Anna M Blackmon, Seth Frietze, Teresa Mescher, Dallas Jones, Randall J Cohrs, Petr Paucek, Nicholas L Baird, Maria A Nagel
Background: Varicella zoster virus (VZV) can present as a myelopathy with spinal astrocyte infection. Recent studies support a role for the neurokinin-1 receptor (NK-1R) in virus infections, as well as for cytoskeletal alterations that may promote viral spread. Thus, we examined the role of NK-1R in VZV-infected primary human spinal astrocytes (HA-sps) to shed light on the pathogenesis of VZV myelopathy. Methods: Mock- and VZV-infected HA-sps were examined for substance P (subP) production, NK-1R localization, morphological changes and viral spread in the presence or absence of NK-1R antagonists, aprepitant and rolapitant...
May 19, 2018: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/29744791/olanzapine-as-antiemetic-drug-in-oncology-a-retrospective-study-in-non-responders-to-standard-antiemetic-therapy
#2
Florian Slimano, Florence Netzer, Isabelle Borget, François Lemare, Benjamin Besse
Background The role of olanzapine in the treatment of chemotherapy-induced nausea and vomiting (CINV) in addition to the antiemetic therapeutic combination with aprepitant, setrons, and corticosteroids has not been well defined. Objective To investigate the effectiveness of the addition of olanzapine to a standard triplet therapy for the prevention of CINV in patients who experienced CINV during their first chemotherapy course, despite receiving a well-managed prevention protocol. Setting One comprehensive cancer centre in France...
May 9, 2018: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/29724299/comparison-of-antiemetic-effects-of-granisetron-and-palonosetron-in-patients-receiving-bendamustine-based-chemotherapy
#3
M Uchida, T Nakamura, Y Makihara, K Suetsugu, H Ikesue, Y Mori, K Kato, M Shiratsuchi, K Hosohata, T Miyamoto, K Akashi
The antiemetic effects and safety of granisetron and palonosetron against chemotherapy-induced nausea and vomiting (CINV) were retrospectively evaluated in patients with non-Hodgkin lymphoma receiving bendamustine-based chemotherapy. A total of 61 patients were eligible for this study. Before starting the bendamustine-based chemotherapy, granisetron or palonosetron were intravenously administered with or without aprepitant and/or dexamethasone. The proportions of patients with complete control (CC) during the overall (during the 6 days after the start of the chemotherapy), acute (up to 2 days), and delayed (3 to 6 days) phases were assessed...
May 1, 2018: Die Pharmazie
https://www.readbyqxmd.com/read/29721755/human-acute-myeloid-leukemia-cells-express-neurokinin-1-receptor-which-is-involved-in-the-antileukemic-effect-of-neurokinin-1-receptor-antagonists
#4
A Molinos-Quintana, P Trujillo-Hacha, J I Piruat, J A Bejarano-García, E García-Guerrero, J A Pérez-Simón, Miguel Muñoz
The substance P/neurokinin-1 receptor system has been implicated in tumor cell proliferation. Neurokinin-1 receptor has been identified in different solid tumors but not frequently in hematopoietic malignant cells. We investigated the presence of the Neurokinin-1 receptor in acute myeloid leukemia cell lines (KG-1 and HL-60), demonstrating that acute myeloid leukemia cell lines overexpress the truncated Neurokinin-1 receptor isoform compared with lymphocytes from healthy donors. Using the MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) method, we demonstrated that substance P induced cell proliferation in both acute myeloid leukemia cell lines...
May 2, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29719604/influence-of-aprepitant-and-localization-of-the-patch-on-fentanyl-exposure-in-patients-with-cancer-using-transdermal-fentanyl
#5
Evelien J M Kuip, Wendy H Oldenmenger, Martine F Visser-Thijs, Peter de Bruijn, Esther Oomen-de Hoop, Ron H J Mathijssen, Carin C D Van der Rijt, Stijn W Koolen
Background and Objectives: The cutaneous fentanyl patch is widely used to treat continuous pain in patients with cancer. Its use is hampered by a high inter- and intrapatient pharmacokinetic variability. Factors that influence this pharmacokinetic variability are largely unclear. The aim of these studies was to test if common patient variables, i) the use of the moderate CYP3A4 inhibitor aprepitant and ii) the localization of the fentanyl patch (upper arm versus thorax) influence systemic exposure to fentanyl in patients with cancer using a transdermal fentanyl patch...
April 6, 2018: Oncotarget
https://www.readbyqxmd.com/read/29674800/olanzapine-versus-aprepitant-for-the-prophylaxis-of-chemotherapy-induced-nausea-and-vomiting-in-breast-cancer-patients-receiving-doxorubicin-cyclophosphamide-regimen-a-prospective-nonrandomized-open-label-study
#6
G Shivaprakash, Karthik S Udupa, V Sarayu, Joseph Thomas, Vishal Gupta, L C Pallavi, Sudhakar Pemminati
OBJECTIVE: Despite the guideline-directed therapy, complete absence of nausea was noted only in 33% of breast cancer patients on anthracycline-cyclophosphamide regimen. Hence, we sought to compare the efficacy of aprepitant (APT) versus olanzapine (OLP) in preventing chemotherapy-induced nausea and vomiting (CINV) in breast cancer patients on doxorubicin-cyclophosphamide regimen. PATIENTS AND METHODS: A prospective, open-label, nonrandomized study was conducted at the Department of Oncology...
November 2017: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/29667586/drug-drug-interactions-with-aprepitant-in-antiemetic-prophylaxis-for-chemotherapy
#7
R Schoffelen, A G Lankheet, C M L van Herpen, J J M van der Hoeven, I M E Desar, C Kramers
In the current guidelines to prevent hemotherapyinduced nausea and vomiting, multiple antiemetic drugs are administered simultaneously. In patients who receive highly emetogenic chemotherapy, aprepitant, an NK1-receptor antagonist, is combined with ondansetron and dexamethasone. Aprepitant can influence the pharmacokinetics of other drugs, as it is an inhibitor and inducer of CYP3A4. Some anticancer drugs and other co-medication frequently used in cancer patients are CYP3A4 or CYP29C substrates. We give an overview of the metabolism and current data on clinically relevant drug-drug interactions with aprepitant during chemotherapy...
April 2018: Netherlands Journal of Medicine
https://www.readbyqxmd.com/read/29577093/evaluation-of-a-neurokinin-1-antagonist-in-preventing-multiple-day-cisplatin-induced-nausea-and-vomiting
#8
Quanfu Li, Wenjuan Wang, Gang Chen, Shuqin Deng, Caihong Jiang, Feng Chen, Jun Zhao, Hui Li, Xiaojun Bai, Yuliang Hu, Lenggaowa Da, Yungaowa Wu, Gaowa Jin
Objective: To perform a prospective non-randomized comparison of the effectiveness and safety of combined neurokinin-1 antagonist aprepitant treatment with the standard multiple-day cisplatin regimen for the prevention of cisplatin-induced nausea and vomiting (CINV). Methods: Patients being administered 3-day cisplatin-based chemotherapy (25 mg/m2 /d) who had never received aprepitant were given either the standard regimen (tropisetron and dexamethasone) or the aprepitant regimen (aprepitant plus tropisetron and dexamethasone)...
2018: Open Medicine (Warsaw, Poland)
https://www.readbyqxmd.com/read/29558695/transcription-factor-specificity-protein-1-modulates-tgf%C3%AE-1-smad-signaling-to-negatively-regulate-sigirr-expression-by-human-m1-macrophages-stimulated-with-substance-p
#9
Rui Yamaguchi, Arisa Sakamoto, Reona Yamaguchi, Misa Haraguchi, Shinji Narahara, Hiroyuki Sugiuchi, Yasuo Yamaguchi
The stimuli inducing expression of single immunoglobulin IL-1-related receptor (SIGIRR) and the relevant regulatory mechanisms are not well defined. Transforming growth factor β1 (TGFβ1) delays internalization of neurokinin-1 receptor (NK1R) and subsequently enhances cellular signaling. This study investigated the effect of TGFβ1 on SIGIRR protein production by human M1 macrophages in response to stimulation with substance P (SP). SP caused upregulation of SIGIRR expression in a concentration-dependent manner, whereas aprepitant (an NK1R inhibitor) blunted this response...
August 2018: Cytokine
https://www.readbyqxmd.com/read/29535504/bioequivalence-of-htx-019-aprepitant-iv-and-fosaprepitant-in-healthy-subjects-a-phase-i-open-label-randomized-two-way-crossover-evaluation
#10
Tom Ottoboni, Mary Rose Keller, Matt Cravets, Neil Clendeninn, Barry Quart
Introduction: Fosaprepitant, an intravenous (IV) aprepitant prodrug for chemotherapy-induced nausea and vomiting prophylaxis, is associated with systemic and infusion-site reactions attributed in part to its surfactant, polysorbate 80. HTX-019 is an IV aprepitant formulation free of polysorbate 80 and other synthetic surfactants. Materials and methods: This open-label, single-dose, randomized, two-way crossover bioequivalence study compared pharmacokinetics and safety of HTX-019 and fosaprepitant...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29523668/ten-year-trends-in-antiemetic-prescribing-in-patients-receiving-highly-emetogenic-chemotherapy
#11
Ciara C O'Sullivan, Holly K Van Houten, Lindsey R Sangaralingham, Alexis D Leal, Shivani Shinde, Hongfang Liu, David Ettinger, Charles L Loprinzi, Kathryn J Ruddy
Purpose: Prevention of chemotherapy-induced nausea and vomiting is essential to preserve quality of life in patients with cancer receiving highly emetogenic chemotherapy (HEC). Recently, new drugs (eg, fosaprepitant, and the newer neurokinin-1 receptor antagonists [NK1RAs] rolapitant and netupitant) and updated antiemetic guidelines have emerged. However, trends in real-world antiemetic use are understudied. Methods: We identified patients treated with an initial dose of HEC (either cisplatin or doxorubicin/cyclophosphamide) from January 2006 to June 2016 using administrative claims data from a US commercial insurance database (OptumLabs)...
March 2018: Journal of the National Comprehensive Cancer Network: JNCCN
https://www.readbyqxmd.com/read/29503734/oral-rehydration-solution-os-1-as-a-substitute-of-intravenous-hydration-after-cisplatin-administration-in-patients-with-lung-cancer-a-prospective-multicenter-trial
#12
Hidehito Horinouchi, Kaoru Kubota, Akihiko Miyanaga, Shinji Nakamichi, Masahiro Seike, Akihiko Gemma, Yuki Yamane, Futoshi Kurimoto, Hiroshi Sakai, Shintaro Kanda, Yutaka Fujiwara, Hiroshi Nokihara, Noboru Yamamoto, Tomohide Tamura, Yuichiro Ohe
Background: The aim of this trial was to evaluate the safety and efficacy of oral hydration as a substitute for intravenous hydration after cisplatin (CDDP) administration. Methods: The major eligibility criteria included patients with lung cancer, indications for a CDDP-based regimen at a dose of 60 mg/m2 or higher, an age of between 20 and 74 years and adequate renal function. Antiemetic prophylaxis consisted of an appropriate dose of palonosetron, aprepitant, dexamethasone and magnesium sulfate (8 mEq)...
2018: ESMO Open
https://www.readbyqxmd.com/read/29459665/a-randomized-placebo-controlled-pilot-trial-of-aprepitant-combined-with-standard-antiemetic-therapy-for-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-in-patients-undergoing-cyclophosphamide-based-conditioning-regimens-prior-to-hematopoietic-stem
#13
Joseph Bubalo, Kelsey Mulverhill, Gabrielle Meyers, Brandon Hayes-Lattin, Richard Maziarz
The aim of this study was to evaluate the safety and efficacy of aprepitant when used prophylactically to prevent nausea and vomiting during cyclophosphamide-based conditioning regimens. The primary objective of this study was to determine if there was a difference in the number of emesis-free days in patients who received aprepitant as compared to those who received placebo. This prospective, randomized, double blind, placebo-controlled study was performed in 40 adult patients who received a cyclophosphamide-containing HSCT conditioning regimen...
February 20, 2018: Bone Marrow Transplantation
https://www.readbyqxmd.com/read/29416232/the-role-of-neurokinin-1-substance-p-antagonists-in-the-prevention-of-postoperative-nausea-and-vomiting
#14
Dionne Okafor, Alan David Kaye, Rachel J Kaye, Richard D Urman
Postoperative nausea and vomiting (PONV) can be very debilitating for surgical patients, and effective management reduces potential morbidity, aiding in patient satisfaction, and minimizing the need for unintended hospital stays. Risk factors include female sex, nonsmoker, and having a previous history of motion sickness or PONV. Anesthetic risk factors include receiving opioids, not receiving a total intravenous anesthetic (TIVA), exposure to nitrous oxide, and extended length of anesthetic. Many treatments, including serotonin antagonists, dopamine antagonists, corticosteroids, inhaled isopropyl alcohol, and anticholinergics, as well as techniques such as TIVA, have been utilized over recent decades in an attempt to reduce PONV incidence...
October 2017: Journal of Anaesthesiology, Clinical Pharmacology
https://www.readbyqxmd.com/read/29409391/adverse-events-associated-with-aprepitant-pediatric-bone-cancer-patients
#15
Lucas M Okumura, Sacha A da Silva Ries, Clarice F Meneses, Mariana B Michalowski, Maria Angelica P Ferreira, Leila B Moreira
An eight-year long case series follow-up study with pediatric bone cancer patients was conducted to compare the occurrence of adverse events associated with aprepitant with official sources of drug information (manufacturer's leaflet, clinical trials, and European Medicines Agency leaflet). All patients admitted were analyzed, representing 192 aprepitant cycles. Anorexia, febrile neutropenia, and headache were observed in frequencies over 43.8 per 100 patients, which was higher than previous estimates. Adverse events were classified as probable or possible, by using Naranjo score...
January 1, 2018: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/29389803/antileukemic-effects-of-neurokinin-1-receptor-inhibition-on-hematologic-malignant-cells-a-novel-therapeutic-potential-for-aprepitant
#16
Samaneh Bayati, Elham Razani, Davood Bashash, Ava Safaroghli-Azar, Majid Safa, Seyed H Ghaffari
Genetic and laboratory studies have remodeled the conventional understanding of cancer pathogenesis by identifying different molecular alterations. Intrigued by the contribution of neurokinin-1 receptor (NK1R) network in cancer pathogenesis, we investigated the antileukemic effects of aprepitant, a nonpeptide antagonist of NK1R, in a panel of hematological cell lines. In this study, we found that aprepitant decreased the survival of all the tested cells; however, as compared with NB4, viability of the other cell lines was inhibited at higher concentrations...
March 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29345696/antiemetic-efficacy-and-safety-of-granisetron-or-palonosetron-alone-and-in-combination-with-a-corticosteroid-for-abvd-therapy-induced-nausea-and-vomiting
#17
Mayako Uchida, Tsutomu Nakamura, Kojiro Hata, Hiroyuki Watanabe, Yasuo Mori, Koji Kato, Kenjiro Kamezaki, Katsuto Takenaka, Motoaki Shiratsuchi, Keiko Hosohata, Toshihiro Miyamoto, Koichi Akashi
Background: Antiemetic effects and safety of granisetron or palonosetron alone and in combination with a corticosteroid against chemotherapy-induced nausea and vomiting (CINV) were retrospectively evaluated in patients with Hodgkin lymphoma receiving adriamycin, bleomycin, vinblastine, and dacarbazine (ABVD) therapy. Methods: A total of 39 patients were eligible for this study. Before ABVD therapy, granisetron or palonosetron was intravenously administered with or without a corticosteroid (dexamethasone or hydrocortisone) and aprepitant...
2018: Journal of Pharmaceutical Health Care and Sciences
https://www.readbyqxmd.com/read/29330211/olanzapine-based-triple-regimens-versus-neurokinin-1-receptor-antagonist-based-triple-regimens-in-preventing-chemotherapy-induced-nausea-and-vomiting-associated-with-highly-emetogenic-chemotherapy-a-network-meta-analysis
#18
Zhonghan Zhang, Yaxiong Zhang, Gang Chen, Shaodong Hong, Yunpeng Yang, Wenfeng Fang, Fan Luo, Xi Chen, Yuxiang Ma, Yuanyuan Zhao, Jianhua Zhan, Cong Xue, Xue Hou, Ting Zhou, Shuxiang Ma, Fangfang Gao, Yan Huang, Likun Chen, Ningning Zhou, Hongyun Zhao, Li Zhang
BACKGROUND: The current antiemetic prophylaxis for patients treated with highly emetogenic chemotherapy (HEC) included the olanzapine-based triplet and neurokinin-1 receptor antagonists (NK-1RAs)-based triplet. However, which one shows better antiemetic effect remained unclear. MATERIALS AND METHODS: We systematically reviewed 43 trials, involving 16,609 patients with HEC, which compared the following antiemetics at therapeutic dose range for the treatment of chemotherapy-induced nausea and vomiting: olanzapine, aprepitant, casopitant, fosaprepitant, netupitant, and rolapitant...
January 12, 2018: Oncologist
https://www.readbyqxmd.com/read/29315462/aprepitant-as-a-fourth-antiemetic-prophylactic-strategy-in-high-risk-patients-a-double-blind-randomized-trial
#19
L C de Morais, A M Sousa, G F Flora, T R Grigio, G M N Guimarães, H A Ashmawi
BACKGROUND: Post-operative nausea and vomiting (PONV) is one of the most important causes of patient discomfort after laparoscopic surgeries despite the use of a multimodal pharmacological approach. This study assessed whether the addition of aprepitant to a multimodal regimen would further decrease the incidence of PONV in high-risk patients. METHODS: Apfel-score three or four patients, scheduled for laparoscopic procedures to treat abdominal or pelvic cancer, were randomized to receive oral starch (control group) or 80 mg of oral aprepitant (treatment group) before induction of anaesthesia in a double-blind study...
April 2018: Acta Anaesthesiologica Scandinavica
https://www.readbyqxmd.com/read/29248965/effectiveness-of-olanzapine-in-patients-who-fail-therapy-with-aprepitant-while-receiving-highly-emetogenic-chemotherapy
#20
Nikita Mehra, Prasanth Ganesan, Trivadi S Ganesan, Surendran Veeriah, Abirami Boopathy, Venkatraman Radhakrishnan, Manikandan Dhanushkodi, Swaminathan Rajaraman, Sevaluxmy Ganesharajah, Tenali Gnana Sagar
Chemotherapy-induced nausea-vomiting (CINV) compromises the quality of life of patients with cancer. We present data on the effectiveness of olanzapine after failure of aprepitant in patients receiving highly emetogenic chemotherapy (HEC). A single-center prospective study was conducted, where patients ≥ 18 years who failed aprepitant, palonosetron, dexamethasone (APD) received olanzapine, palonosetron and dexamethasone (OPD) in the subsequent cycle of HEC. Failure of APD was defined as occurrence of ≥ grade 2 acute and/or delayed nausea ± vomiting...
December 16, 2017: Medical Oncology
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