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Aprepitant

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https://www.readbyqxmd.com/read/28790262/-determination-of-the-effect-of-aprepitant-and-fosaprepitant-for-nausea-in-patients-with-oral-cancer-receiving-combination-chemotherapy-with-tpf
#1
Kimio Uchiyama, Manabu Yamada, Yuusuke Shiiba, Shingo Kasazaki, Kenichirou Suga, Hiroshi Iwabuchi, Seiji Asoda, Keita Uehara
The objective of this study was to determine the effect of aprepitant(from days 1 to 3, po)and fosaprepitant(day 1, iv) for nausea in patients with oral cancer receiving combination chemotherapy with docetaxel, nedaplatin, or cisplatin(divided doses for 5 days), and 5-fluorouracil(TPF).The incidence rate of nausea in the aprepitant group was 60%(6/10), and that in the fosaprepitant group was 90%(9/10).The incidence rate of continuous nausea for more than 2 days was significantly lower in the aprepitant group than in the fosaprepitant group(40%[4/10]vs 90%[9/10], p=0...
July 2017: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28765126/cost-utility-and-budget-impact-analyses-of-the-use-of-nepa-for-chemotherapy-induced-nausea-and-vomiting-prophylaxis-in-italy
#2
Umberto Restelli, Gabriella Saibene, Patrizia Nardulli, Roberta Di Turi, Erminio Bonizzoni, Francesca Scolari, Tania Perrone, Davide Croce, Luigi Celio
OBJECTIVE: To evaluate the efficiency of resources allocation and sustainability of the use of netupitant+palonosetron (NEPA) for chemotherapy-induced nausea and vomiting (CINV) prophylaxis assuming the Italian National Health Service (NHS) perspective. A published Markov model was adapted to assess the incremental cost-utility ratio of NEPA compared with aprepitant (APR) + palonosetron (PALO), fosaprepitant (fAPR) + PALO, APR + ondansetron (ONDA), fAPR + ONDA in patients receiving a highly emetogenic chemotherapy (HEC) and with APR + PALO and fAPR + PALO in patients receiving a moderately emetogenic chemotherapy (MEC)...
August 1, 2017: BMJ Open
https://www.readbyqxmd.com/read/28753469/nk1-receptor-antagonists-for-depression-why-a-validated-concept-was-abandoned
#3
REVIEW
Nadia M J Rupniak, Mark S Kramer
BACKGROUND: NK1 receptor antagonists were abandoned despite antidepressant efficacy in five randomized clinical trials. The loss of confidence may be attributed to the failure of a Phase III clinical program with the NK1 receptor antagonist aprepitant in Major Depression. This review examines how PET receptor occupancy was used to select doses for aprepitant and that these may not have achieved adequate exposure. METHODS: PubMed, Google Scholar, and FDA databases were searched for articles concerning NK1 receptor antagonists, human PET receptor occupancy and clinical trials in Major Depression...
July 20, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28749696/the-influence-of-physiological-gastrointestinal-surfactant-ratio-on-the-equilibrium-solubility-of-bcs-class-ii-drugs-investigated-using-a-four-component-mixture-design
#4
Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin W Halbert
The absorption of poorly water-soluble drugs is influenced by the luminal gastrointestinal fluid content and composition which controls solubility. Simulated intestinal fluids have been introduced into dissolution testing including endogenous amphiphiles and digested lipids at physiological levels; however, in vivo individual variation exists in the concentrations of these components, which will alter drug absorption through an effect on solubility. The use of a factorial design of experiment and varying media by introducing different levels of bile, lecithin and digested lipids has been previously reported, but here we investigate the solubility variation of poorly-soluble drugs through more complex biorelevant amphiphile interactions...
July 27, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737398/in-vivo-mechanisms-of-intestinal-drug-absorption-from-aprepitant-nanoformulations
#5
Carl Roos, David Dahlgren, Staffan Berg, Jan Westergren, Bertil Abrahamsson, Christer Tannergren, Erik Sjögren, Hans Lennernäs
Over recent decades there has been an increase in the proportion of BCS class II and IV drug candidates in industrial drug development. To overcome the biopharmaceutical challenges associated with the less favorable properties of solubility and/or intestinal permeation of these substances, the development of formulations containing nanosuspensions of the drugs has been suggested. The intestinal absorption of aprepitant from two nanosuspensions (20 μM and 200 μM total concentrations) in phosphate buffer, one nanosuspension (200 μM) in fasted-state simulated intestinal fluid (FaSSIF), and one solution (20 μM) in FaSSIF was investigated in the rat single-pass intestinal perfusion model...
August 10, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28735677/genetic-risk-factors-associated-with-antiemetic-efficacy-of-palonosetron-aprepitant-and-dexamethasone-in-japanese-breast-cancer-patients-treated-with-anthracycline-based-chemotherapy
#6
Satoshi Yokoyama, Satoshi Tamaru, Shinya Tamaki, Daisuke Nakanishi, Akiya Mori, Tomokazu Yamakawa, Takaaki Ao, Yasuhiko Sakata, Toshiro Mizuno, Takuya Iwamoto, Kenichi Watanabe, Makoto Simomura, Keiki Kawakami, Naomi Konishi, Shinichi Kageyama, Shoichiro Ohtani, Tomomi Yamada, Susumu Ban, Kazuya Ooi
INTRODUCTION: Breast cancer patients often receive anthracycline-based chemotherapy, and chemotherapy-induced nausea and vomiting (CINV) remains one of the most uncomfortable and distressing adverse reactions. Poor control of CINV reduces the relative dose intensity of chemotherapy agents, which has been associated with poor clinical outcomes and shorter survival. The aim of the present study was to identify genetic risk factors associated with anthracycline-based CINV. PATIENTS AND METHODS: We evaluated CINV attributable to anthracycline-based chemotherapy in Japanese breast cancer patients treated with an antiemetic regimen that included palonosetron, aprepitant, and dexamethasone...
June 29, 2017: Clinical Breast Cancer
https://www.readbyqxmd.com/read/28733700/feasibility-of-olanzapine-multi-acting-receptor-targeted-antipsychotic-agent-for-the-prevention-of-emesis-caused-by-continuous-cisplatin-or-ifosfamide-based-chemotherapy
#7
Seiko Bun, Kan Yonemori, Toru Akagi, Emi Noguchi, Tatsunori Shimoi, Akihiko Shimomura, Mayu Yunokawa, Chikako Shimizu, Yasuhiro Fujiwara, Yoshinori Makino, Yoshikazu Hayashi, Kenji Tamura
Background To determine the feasibility and efficacy of olanzapine, which is approved by the Pharmaceuticals and Medical Devices Agency as multi acting receptor targeted antipsychotic agent of the thienobenzodiazepine class, for prevention of chemotherapy-induced nausea and vomiting (CINV) in patients undergoing continuous five-day chemotherapy. Patients and methods This study was a prospective dose escalation study at a single center (UMIN ID: UMIN000015386). Patients received a combination of adriamycin and ifosfamide (AI) or a combination of bleomycin, etoposide, and cisplatin (BEP)...
July 21, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28694084/olanzapine-reduces-chemotherapy-induced-nausea-and-vomiting-compared-with-aprepitant-in-myeloma-patients-receiving-high-dose-melphalan-before-stem-cell-transplantation-a-retrospective-study
#8
Steven Trifilio, Colleen Welles, Kristin Seeger, Shivani Mehta, MaryAnne Fishman, Katherine McGowan, Kathryn Strejcek, Emily Eiten, Carolyn Pirotte, Elizabeth Lucier, Sean DeFrates, Jayesh Mehta
INTRODUCTION: Acute and delayed chemotherapy-induced nausea and vomiting (CINV) occurs in most patients who receive high-dose melphalan and significantly affects patients' quality of life during autologous stem cell transplantation. Faced with unsatisfactory results using an aprepitant-based regimen, an olanzapine-based regimen was initiated, with the hope of improving the incidence of acute and delayed CINV. A retrospective study was conducted to compare the effectiveness of olanzapine- versus aprepitant-based regimens for CINV prevention in adult hematopoietic stem cell recipients who received high-dose melphalan...
June 20, 2017: Clinical Lymphoma, Myeloma & Leukemia
https://www.readbyqxmd.com/read/28691209/efficacy-of-the-oral-neurokinin-1-receptor-antagonist-aprepitant-for-nausea-and-vomiting-induced-by-cisplatin-and-carboplatin-in-japanese-patients-with-gynecological-cancer
#9
Masae Ikeda, Masako Shida, Takeshi Hirasawa, Toshinari Muramatsu, Mikio Mikami
AIM: This study was conducted to evaluate the efficacy and the difference in effects of the oral neurokinin-1(NK-1) receptor antagonist aprepitant for chemotherapy-induced nausea/vomiting (CINV) in Japanese patients with gynecological cancer receiving highly emetogenic (cisplatin) and moderately emetogenic (carboplatin) chemotherapy. METHODS: Aprepitant was added during the second course of chemotherapy in Japanese patients with grade ≥ 2 (Common Terminology Criteria for Adverse Events, version 3...
July 10, 2017: Journal of Obstetrics and Gynaecology Research
https://www.readbyqxmd.com/read/28674839/the-role-of-aprepitant-in-prevention-of-postoperative-nausea-and-vomiting-after-bariatric-surgery
#10
Isaac W Therneau, Erin E Martin, Juraj Sprung, Todd A Kellogg, Darrell R Schroeder, Toby N Weingarten
BACKGROUND: Postoperative nausea and vomiting (PONV) is common with bariatric surgery. We examined the PONV rate in bariatric surgical patients who received triple antiemetic prophylaxis (dexamethasone, droperidol, and ondansetron) with and without antiemetic aprepitant. METHODS: Medical records of female patients undergoing laparoscopic bariatric surgery from January 1, 2014, to July 28, 2016, were reviewed for PONV episodes during 48 postoperative hours. RESULTS: In total, 338 patients received triple antiemetic, of whom 172 (51%) also received aprepitant...
July 3, 2017: Obesity Surgery
https://www.readbyqxmd.com/read/28638451/antiemetic-effectiveness-and-cost-saving-of-aprepitant-plus-granisetron-is-superior-to-palonosetron-in-gastrointestinal-cancer-patients-who-received-moderately-emetogenic-chemotherapy
#11
Haruka Toda, Hitoshi Kawazoe, Akiko Yano, Yuji Yamamoto, Yuji Watanabe, Yasunori Yamamoto, Yoichi Hiasa, Yoshihiro Yakushijin, Akihiro Tanaka, Hiroaki Araki
Purpose The therapeutic benefit of a three-drug combination of antiemetics has not been established in moderately emetogenic chemotherapy (MEC). The aim of this study was to compare the antiemetic effectiveness and cost-saving of palonosetron plus dexamethasone (control group) with aprepitant, granisetron, and dexamethasone (study group) in cancer patients who received MEC. Methods We switched the standard antiemetic treatment from the control group to the study group in gastrointestinal cancer patients who received MEC after October 2015...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28636760/successful-management-of-refractory-diabetic-gastroparesis-with-long-term-aprepitant-treatment
#12
N Fountoulakis, J Dunn, S Thomas, J Karalliedde
BACKGROUND: People with gastroparesis who develop treatment-resistant (refractory) disease pose a difficult challenge, especially in the setting of end-stage renal disease (ESRD) or post pancreas transplant. Aprepitant (a neurokinin-receptor antagonist) is licensed for the short-term treatment of chemotherapy-induced nausea. There is lack of information on its long-term efficacy and safety in people with diabetic gastroparesis. CASE REPORT: Case 1 was 73-year-old man with Type 2 diabetes of 25 years' duration and ESRD requiring dialysis...
June 21, 2017: Diabetic Medicine: a Journal of the British Diabetic Association
https://www.readbyqxmd.com/read/28633504/a-phase-ii-study-of-palonosetron-aprepitant-dexamethasone-and-olanzapine-for-the-prevention-of-cisplatin-based-chemotherapy-induced-nausea-and-vomiting-in-patients-with-thoracic-malignancy
#13
Kazuhisa Nakashima, Haruyasu Murakami, Kouichi Yokoyama, Shota Omori, Kazushige Wakuda, Akira Ono, Hirotsugu Kenmotsu, Tateaki Naito, Fumie Nishiyama, Mami Kikugawa, Masayo Kaneko, Yumiko Iwamoto, Satomi Koizumi, Keita Mori, Takeshi Isobe, Toshiaki Takahashi
Background: The three-drug combination of a 5-hydroxytryptamine type 3 receptor antagonist, a neurokinin 1 receptor antagonist and dexamethasone is recommended for patients receiving highly emetogenic chemotherapy. However, standard antiemetic therapy is not completely effective in all patients. Methods: We conducted an open-label, single-center, single-arm Phase II study to evaluate the efficacy of olanzapine in combination with standard antiemetic therapy in preventing chemotherapy-induced nausea and vomiting in patients with thoracic malignancy receiving their first cycle of cisplatin-based chemotherapy...
June 17, 2017: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28605064/characterization-of-the-chloroquine-induced-mouse-model-of-pruritus-using-an-automated-behavioural-system
#14
Gema Tarrasón, Carla Carcasona, Peter Eichhorn, Bibiana Pérez, Amadeu Gavaldà, Núria Godessart
Pruritus is a major symptom of several dermatological diseases but has limited therapeutic options available. Animal models replicating the pathophysiology of pruritus are needed to support the development of new drugs. Induction of pruritus by chloroquine (CQ) in mice is widely used, although, as with similar models, it has low throughput and does not distinguish between anti-pruritic effects and confounding factors such as sedation. To overcome these issues, we incorporated into the model an automated system that measures both scratching and locomotor behaviour simultaneously...
June 12, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28577951/aprepitant-for-refractory-nivolumab-induced-pruritus
#15
Jiro Ito, Daichi Fujimoto, Ayaka Nakamura, Tohru Nagano, Keiichiro Uehara, Yukihiro Imai, Keisuke Tomii
Although substantial progress has been made in the treatment of non-small-cell lung cancer (NSCLC) patients with immune checkpoint inhibitors (ICIs), severe immune-related adverse events (irAEs) sometimes occur. Here, we report a case of severe refractory pruritus after Stevens-Johnson syndrome (SJS) in a patient with NSCLC treated with nivolumab. The patient was a 76-year-old Japanese woman with advanced NSCLC treated with nivolumab. After the second dose, she experienced severe rash with mucous involvement...
July 2017: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/28550801/the-nk-1-receptor-antagonist-l-732-138-induces-apoptosis-in-human-gastrointestinal-cancer-cell-lines
#16
Miguel Muñoz, Marisa Rosso, Rafael Coveñas
BACKGROUND: Gastric and colon cancer cells express the neurokinin-1 receptor (NK-1R) and the peptide substance P (SP), after binding to this receptor, elicits the proliferation of gastrointestinal cancer cells and an antiapoptotic effect. In these cells, NK-1R antagonists (L-733,060: a piperidine derivative; aprepitant: a morpholine derivative) block, after binding to the NK-1R, the action of SP and exert an antiproliferative action, both antagonists promote apoptosis and the death of cancer cells...
February 12, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28470980/aprepitant-and-fosaprepitant-drug-interactions-a-systematic-review
#17
Priya Patel, J Steven Leeder, Micheline Piquette-Miller, L Lee Dupuis
AIMS: Aprepitant and fosaprepitant, commonly used for the prevention of chemotherapy-induced nausea and vomiting, alter cytochrome P450 activity. This systematic review evaluates clinically significant pharmacokinetic drug interactions with aprepitant and fosaprepitant and describes adverse events ascribed to drug interactions with aprepitant or fosaprepitant. METHODS: We systematically reviewed the literature to September 11, 2016 to identify articles evaluating drug interactions involving aprepitant/fosaprepitant...
May 4, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28460548/clinical-pharmacology-of-neurokinin-1-receptor-antagonists-for-the-treatment-of-nausea-and-vomiting-associated-with-chemotherapy
#18
REVIEW
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...
June 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
#19
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/28447301/management-of-chemotherapy-induced-nausea-and-vomiting-in-pediatric-patients
#20
REVIEW
Rudolph M Navari
Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life and is perceived by patients as a major adverse effect of the treatment. This review summarizes the safety and efficacy of current antiemetic agents for the prevention of CINV in children. Information on antiemetic prophylaxis for CINV in children was obtained from a literature review of current peer-reviewed articles and recent international guidelines. The literature review and the international antiemetic guidelines provide recommendations for use of specific antiemetics in children based on the emetogenicity of the chemotherapy...
June 2017: Paediatric Drugs
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