Development of palliative medicine in the United Kingdom and Ireland
Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita in Textbook of Palliative Medicine and Supportive Care, 2015
Aprepitant was the first-in-class agent approved in 2003 by the U.S. Food and Drug Administration. The neurokinin-1 receptor antagonist is used in combination with a serotonin inhibitor and dexamethasone for prevention of high to moderate emetogenic chemotherapies. Aprepitant is generally administered as a 3-day oral regimen of 125mg on day 1 and 80mg on days 2 and 3. Aprepitant is well tolerated with clinical studies reporting diarrhea, fatigue, headache, and hiccups [25,32-34]. sible drug-drug interactions. dosing options include Hydroxyzine 25-50 mg by mouth every 6 hoursMeclizine 25-50 mg by mouth every 6 hours
Drug profiles: generic names A–Z
Jerome Z. Litt, Neil H. Shear in Litt's Drug Eruption & Reaction Manual, 2017
Clinically important, potentially hazardous interactions with: acebutolol, alfuzosin, amiodarone, amitriptyline, amprenavir, aprepitant, atazanavir, atenolol, atorvastatin, avanafil, bisoprolol, bosentan, carbamazepine, celiprolol, cilostazol, cobicistat/elvitegravir/emtricitabine/tenofovir alafenamide, cobicistat/elvitegravir/emtricitabine/tenofovir disoproxil, colchicine, copanlisib, corticosteroids, cyclosporine, deflazacort, delavirdine, dronedarone, dutasteride, efavirenz, epirubicin, erythromycin, fingolimod, flibanserin, lurasidone, midostaurin, mifepristone, moricizine, naldemedine, naloxegol, neratinib, nevirapine, nifedipine, olaparib, oxprenolol, posaconazole, ranolazine, silodosin, simvastatin, sonidegib, sulpiride, telaprevir, venetoclax
Postoperative nausea and vomiting
Hemanshu Prabhakar, Charu Mahajan, Indu Kapoor in Manual of Neuroanesthesia, 2017
Manage the patients with prophylaxis failureand undergoing treatment of PONV: Previous studies observed that patients who received ondansetron prophylaxis and developed PONV within the first 4 postoperative hours(h) did not respond to a second dose of ondansetron or to crossover with granisetron.33,34 If PONV develops 6 h postoperatively, a second dose of a 5-HT3 antagonists or butyrophenones (droperidol or haloperidol) can be effective. Readministration of longer-acting drugs, for example, dexamethasone, TDS, aprepitant, and palonosetron, is not recommended. (Figure 30.2). It is appropriate.
UVR-B-induced NKR-1 Expression in Ocular Tissues is blocked by Substance P Receptor Antagonist Fosaprepitant in the Exposed as well as Unexposed Partner Eye
Published in Ocular Immunology and Inflammation, 2021
Janine Gross, Alfred R. Wegener, Martin Kronschläger, Carl-Ludwig Schönfeld, Frank G. Holz, Linda M. Meyer
Aprepitant has been used not only successfully for the treatment of chemotherapy- and post-operative-induced nausea and vomiting, but also for the therapy in migraine, pain, and emesis.40 It has recently demonstrated that Aprepitant is an antitumor drug with no known side effects.39,56 Consistent with previous studies, indicating no toxic side effects of Aprepitant and Fosaprepitant26,29, in the current study Fosaprepitant was well tolerated by the mice and no externally visible side effect during the days of treatment was observed. These properties of Aprepitant linked to the effective inhibition of inflammation in several animal models,26,36,40 make this drug interesting for many ocular diseases such as corneal neovascularization (CNV) or AMD.
Emerging drugs in the treatment of chronic cough
Published in Expert Opinion on Emerging Drugs, 2023
Danica Brister, Mustafaa Wahab, Moaaz Rashad, Nermin Diab, Martin Kolb, Imran Satia
Neurokinin-1 receptor antagonists are predominantly centrally acting compounds which have been used to treat nausea and are now under investigation for the treatment of chronic cough. Orvepitant reduced awake cough frequency, patient reported cough severity and improved quality of life in an open label study of 13 patients [74]. However, a double-blind RCT of 315 patients failed to show reduction in cough frequency up to its highest dose ranges, despite improvement in severity and quality of life measures [75,76]. Orvepitant is currently being investigated in a sub-group of patients with RCC secondary to IPF, with a novel Idiopathic Pulmonary Fibrosis Cough Severity Scale as the primary outcome [77]. Serlopitant was also studied, but results were similarly negative [78]. While it has only been studied in patients with lung cancer and bothersome cough, aprepitant is a licensed anti-nausea medication which showed positive results with 3 days of treatment in a placebo-controlled cross-over RCT in 20 patients. Aprepitant improved 24-h cough frequency as well as patient reported outcomes in this study [79].
Chronic cough: Investigations, management, current and future treatments
Published in Canadian Journal of Respiratory, Critical Care, and Sleep Medicine, 2021
I. Satia, M. Wahab, E. Kum, H. Kim, P. Lin, A. Kaplan, P. Hernandez, J. Bourbeau, L. P. Boulet, S. K. Field
Current neuromodulator treatments all target sensory suppression transmission in the central nervous system to reduce the urge to cough sensation and cough.89 There has been recent interest in targeting the neurokinin-1 (NK-1) receptor in the brainstem. Aprepitant is a licensed NK-1 antagonist for the treatment of chemotherapy related nausea and vomiting. A small proof of concept in patients with lung cancer and cough demonstrated that 3 days of treatment was associated with a 30% reduction in 24-hr cough frequency.109 This led to phase 2 studies of orvepitant and serlopitant in patients with RCC. An open label study of orvepitant demonstrated reduction in cough frequency by 26% at week 4 which surprisingly continued to be effective at week 8, 4-weeks after the end of the last dose.110 The full published results of the placebo-controlled phase 2 b study are awaited but data in abstract form suggest orvepitant significantly improved patient reported outcomes including the LCQ, cough severity and urge to cough VAS, but did not significantly reduce cough frequency.111 A pre-specified sub-group of patients who had a high cough frequency at baseline showed an almost statistically significant reduction in cough frequency (p = 0.066). Published data on serlopitant are awaited, but the brief study results on clinicaltrials.gov suggest the study results were negative.112
Related Knowledge Centers
- Dexamethasone
- Substance P
- Anaphylaxis
- Pregnancy
- Ondansetron
- Chemotherapy-Induced Nausea & Vomiting
- Postoperative Nausea & Vomiting
- Oral Administration
- Nk1 Receptor Antagonist
- Tachykinin Receptor 1