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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
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
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
Poe-Hirr Hsyu, Daniela Soriano Pignataro, Kyle Matschke
PURPOSE: Bosutinib is an oral, dual Src and Abl tyrosine kinase inhibitor (TKI) approved for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia resistant or intolerant to prior TKI therapy. Bosutinib is primarily metabolized by cytochrome P450 (CYP) 3A4, suggesting drug interaction potential with other CYP3A4 modulators. This open-label, randomized, 2-sequence, 2-period crossover study assessed the effect of single-dose aprepitant, a moderate CYP3A4 inhibitor, on the single-dose pharmacokinetic profile of oral bosutinib 500 mg...
October 7, 2016: European Journal of Clinical Pharmacology
Deepti Ahuja, Sachidanand J Bharati, Nishkarsh Gupta, Ritesh Kumar, Sushma Bhatnagar
Radiation-induced nausea and vomiting (RINV) is one of the most distressing symptoms that adversely affects quality of life (QOL) as well as the ongoing management plan of cancer patients. Although there are protocols for management of chemotherapy induced nausea and vomiting (CINV) but such guidelines are still lacking for RINV. Various agents like 5-hydroxy tryptophan 3 (5-HT3) antagonist, dexamethasone, metoclopramide and haloperidol are used in clinical practice for RINV but the results are not very encouraging...
August 23, 2016: Annals of Palliative Medicine
Wendy Pritchett, Karen Kinsley
Fosaprepitant dimeglumine (Emend IV®) is an IV antiemetic that may be beneficial to patients receiving highly emetogenic regimens. Aprepitant (Emend®) is an oral medication that is administered for three consecutive days, whereas fosaprepitant is a single-dose IV medication that is administered on the day of chemotherapy for 20-30 minutes (depending on the IV access type). Fosaprepitant may be useful, yet it can also present a risk for hypersensitivity reactions and phlebitis. Oncology nurses must be aware of the signs and symptoms of these potential adverse events to properly care for their patients...
October 1, 2016: Clinical Journal of Oncology Nursing
Masahide Matsuda, Tetsuya Yamamoto, Eiichi Ishikawa, Hiroyoshi Akutsu, Shingo Takano, Akira Matsumura
Concomitant use of temozolomide (TMZ) and radiotherapy, which is the standard therapy for patients with high-grade glioma, involves a unique regimen with multiple-day, long-term administration. In a previous study, we showed not only higher incidence rates of chemotherapy-induced nausea and vomiting (CINV) during the overall study period, but also substantially higher incidence rates of moderate/severe nausea and particularly severe appetite suppression during the late phase of the treatment. Here, we prospectively evaluated the efficacy of a combination of palonosetron, aprepitant, and dexamethasone for CINV in patients treated with concomitant TMZ and radiotherapy...
September 23, 2016: Neurologia Medico-chirurgica
Gerhard G Grabenbauer, Göbel Holger
Possible toxic effects following radiation and chemotherapy of gastrointestinal tumours may cause a depletion of the mucosal barrier within the radiation volumes with severe mucositis. Diarrhoea, nausea, emesis and severe malabsorption followed by infections with dehydration and electrolyte disorders have to be encountered. For prevention and treatment of oropharyngeal mucositis an oral care protocol, oral cryotherapy together with benzydamine mouthwash may be recommended. Lower gastrointestinal diarrhoea is best treated by Octreotide (>100 μg s...
August 2016: Best Practice & Research. Clinical Gastroenterology
Fateme Sanaati, Safa Najafi, Zahra Kashaninia, Masoud Sadeghi
BACKGROUND: Chemotherapy-induced nausea and vomiting (CINV) places a significant burden on the patient. Herbal agents are the most commonly complementary therapies used among the public. This study was done to determine the effect of ginger and chamomile capsules on nausea and vomiting in cases undergoing chemotherapy for breast cancer (BC). MATERIALS AND METHODS: In a randomized, double-blind and clinical trial study, 65 women with BC undergoing chemotherapy were referred to Breast Cancer Research Center, Tehran, Iran, between May 2013 to June 2014...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
Eun Kyung Choi, Dong Gyeong Kim, Younghoon Jeon
We compared the antiemetic efficacy of aprepitant plus palonosetron versus aprepitant plus ramosetron in patients after laparoscopic cholecystectomy. A total of 88, nonsmoking, female patients undergoing laparoscopic cholecystectomy were randomly allocated to 2 groups of 44 each who received palonosetron 0.075 mg (aprepitant plus palonosetron group) and ramosetron 0.3 mg (aprepitant plus ramosetron group) after induction of anesthesia. All patients received aprepitant 80 mg 2 hours before surgery. The incidence of postoperative nausea and vomiting (PONV), use of rescue antiemetic, pain severity, and any side effects were assessed for 24 hours after surgery...
October 2016: Surgical Laparoscopy, Endoscopy & Percutaneous Techniques
John A Rudd, Man P Ngan, Zengbing Lu, Guy A Higgins, Claudio Giuliano, Emanuela Lovati, Claudio Pietra
BACKGROUND AND AIMS: Chemotherapy-induced acute and delayed emesis involves the activation of multiple pathways, with 5-hydroxytryptamine (5-HT; serotonin) playing a major role in the initial response. Substance P tachykinin NK1 receptor antagonists can reduce emesis induced by disparate emetic challenges and therefore have a clinical utility as broad inhibitory anti-emetic drugs. In the present studies, we investigate the broad inhibitory anti-emetic profile of a relatively new NK1 receptor antagonist, netupitant, alone or in combination with the long acting 5-HT3 receptor antagonist, palonosetron, for a potential to reduce emesis in ferrets and shrews...
2016: Frontiers in Pharmacology
Denise E Chou, Amy R Tso, Peter J Goadsby
OBJECTIVE: To assess the efficacy and tolerability of oral aprepitant, a substance P/neurokinin A receptor antagonist, in controlling nausea associated with IV dihydroergotamine (DHE) administered for medically refractory migrainous headache in patients not responding to standard antiemetics or with a history of uncontrolled nausea with DHE. METHODS: This was a retrospective chart review of prospectively collected hourly diary data and clinical notes of patients hospitalized between 2011 and 2015 for inpatient treatment with DHE...
October 11, 2016: Neurology
Samaneh Bayati, Davood Bashash, Shahin Ahmadian, Ava Safaroghli-Azar, Kamran Alimoghaddam, Ardeshir Ghavamzadeh, Seyed H Ghaffari
Increasing number of genetic and cancer biology studies indicated a prominent role for tachykinin NK1 receptor (NK1R) in cancer cell growth and survival. Considering the fact that neoplastic lymphoid precursors in acute lymphoblastic leukemia (ALL) carry a three- to four-fold NK1R expression as compared to normal lymphocytes, using NK1R antagonist seems to be noteworthy in the treatment of ALL patients. In this study, we found that inhibition of NK1R with aprepitant, a selective high-affinity antagonist of the human NK1R, exerts cytotoxic and anti-proliferative effects against pre-B ALL-derived Nalm-6 cells either as single drug or in combination with doxorubicin...
September 6, 2016: European Journal of Pharmacology
Omar Abdel-Rahman
A network meta-analysis of the comparative effectiveness of neurokinin 1 (NK-1) inhibitors in the prophylaxis of highly emetogenic chemotherapy induced nausea and vomiting has been conducted. Eligible studies included randomized trials evaluating aprepitant, fosaprepitant, netupitant (NEPA), casopitant and rolapitant containing regimens in the setting of highly emetogenic chemotherapy. Primary outcomes of interest include complete response (CR) and rate of no significant nausea. After preclusion of ineligible studies, 19 studies were included in the final analysis...
September 2016: Therapeutic Advances in Medical Oncology
Brandon Rowe, Gil Yosipovitch
Paraneoplastic itch occurs as the result of a systemic reaction to an underlying malignancy. Paraneoplastic itch is most commonly associated with lymphoproliferative malignancies and solid tumors that result in cholestasis. Paraneoplastic itch may occur in the absence of a primary rash or in association with dermatologic conditions such as erythroderma, acanthosis nigricans, dermatomyositis, Grover's disease, and eruptive seborrheic keratosis. Treatment of paraneoplastic itch is centered on targeting the underlying malignancy responsible for the systemic reaction...
2016: Current Problems in Dermatology
Yayoi Kamata, Mitsutoshi Tominaga, Kenji Takamori
Patients with atopic dermatitis (AD) suffer from chronic inflammatory dermatitis and antihistamine-resistant itch. The management of intractable pruritus in AD is important, requiring the development of new therapeutic approaches. At present, the standard treatments for AD include topical anti-inflammatory drugs such as calcineurin inhibitors and corticosteroids. Topical emollient treatment is recommended to moisten the skin and to restore and maintain barrier function. Phototherapy is also effective in reducing the number of epidermal nerve fibers, normalizing imbalances in the levels of expression of axon guidance molecules, and inhibiting pruritus...
2016: Current Problems in Dermatology
Kateřina Punčochová, Andrew V Ewing, Michaela Gajdošová, Tomáš Pekárek, Josef Beránek, Sergei G Kazarian, František Štěpánek
PURPOSE: Imaging methods were used as tools to provide an understanding of phenomena that occur during dissolution experiments, and ultimately to select the best ratio of two polymers in a matrix in terms of enhancement of the dissolution rate and prevention of crystallization during dissolution. METHODS: Magnetic resonance imaging, ATR-FTIR spectroscopic imaging and Raman mapping have been used to study the release mechanism of a poorly water soluble drug, aprepitant, from multicomponent amorphous solid dispersions...
August 29, 2016: Pharmaceutical Research
L Lee Dupuis, Lillian Sung, Alexander Molassiotis, Andrea D Orsey, Wim Tissing, Marianne van de Wetering
PURPOSE: To update the 2009 recommendations for the prevention of acute chemotherapy-induced emesis in children. METHODS: We updated the original systematic literature search. Randomized studies were included in the evidence to support this guideline if they were primary studies fully published in full text in English or French; included only children less than 18 years old or, for mixed studies of adults and children, reported the pediatric results separately or the median or mean age was no more than 13 years; evaluated acute chemotherapy-induced nausea and vomiting (CINV) prophylaxis; provided sufficient information to permit determination of the emetogenicity of the antineoplastic therapy administered or the study investigators stated the emetogenicity of the chemotherapy administered; included an implicit or explicit definition of complete acute CINV response; described the antiemetic regimen in full; and reported the complete acute CINV response rate as a proportion...
August 26, 2016: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
Zheng Song, Huaqing Wang, Huilai Zhang, Kuo Zhao, Man Zhang, Fang Yang
We performed a prospective study to investigate the efficacy and safety of triple therapy with aprepitant, ondansetron, and prednisone in non-Hodgkin lymphoma patients receiving R-CEOP or CEOP chemotherapy regimen. All patients were randomly assigned to either an aprepitant regimen (aprepitant plus ondansetron and prednisone), or a control regimen (ondansetron and prednisone) treatment group. For the complete response, the aprepitant group was statistically superior to the control group in the overall study period (76...
August 22, 2016: Leukemia & Lymphoma
Karly P Garnock-Jones
Intravenous fosaprepitant dimeglumine (Emend(®) for injection, IVEmend(®); henceforth referred to as fosaprepitant) is a prodrug of and is rapidly converted to the antiemetic aprepitant, and is approved in several countries worldwide (as part of an antiemetic regimen) for the prevention of nausea and vomiting associated with highly and moderately emetogenic chemotherapy (HEC and MEC). This narrative review discusses the pharmacological properties of intravenous fosaprepitant and its clinical efficacy and tolerability in the prevention of nausea and vomiting associated with HEC and MEC...
September 2016: Drugs
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