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Development of palliative medicine in the United Kingdom and Ireland
Published in Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita, Textbook of Palliative Medicine and Supportive Care, 2015
These substances inhibit the effects of substance P on the nucleus tractus solitarius. In early clinical trials, the neurokinin-1 receptor antagonist aprepitant was effective in the prevention of acute and delayed chemotherapy-induced nausea and vomiting associated with single or multiple cycles of highly emetogenic chemotherapy, when combined with best available therapy, including a 5-HT3 receptor antagonist and dexamethasone. Aprepitant is used in doses of 125mg on day one and then 80mg once daily on days 2 and 3 and is generally well tolerated [29]. Fosaprepitant and casopitant represent the new generation of neurokinin-1 receptor antagonists [6].
A pharmacological overview of aprepitant for the prevention of postoperative nausea and vomiting
Published in Expert Review of Clinical Pharmacology, 2023
Andrew Padilla, Ashraf S Habib
A recent network meta-analysis included data from 585 studies and 97,516 patients. The primary outcome of this analysis was postoperative vomiting. In this review, there was high certainty evidence for the clinical efficacy of aprepitant in reducing post-operative vomiting, alongside with other four antiemetics (ramosetron, granisetron, dexamethasone and ondansetron). When ranking the antivomiting efficacy compared with placebo, fosaprepitant ranked first and aprepitant third, while another NK1 antagonist (casopitant) ranked second. Of note, casopitant is not currently approved or available for the management of PONV. The review identified that combination of drugs was generally more effective than monotherapy in the prevention of vomiting. The review also suggested that, in comparison to combinations of dexamethasone-ondansetron, dexamethasone-granisetron, and droperidol-ondansetron, aprepitant alone had comparable efficacy for reducing post-operative vomiting. There was no apparent dose response for the antivomiting efficacy of aprepitant. However, the review identified aprepitant’s anti-nausea effects as modest with uncertainty. Other agents in the D2 antagonist and 5-HT3 antagonist class demonstrated better anti-nausea efficacy compared with the NK1 antagonists [12].
Antagonism of NK-1R using aprepitant suppresses inflammatory response in rheumatoid arthritis fibroblast-like synoviocytes
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Xiaoping Liu, Yuelan Zhu, Wei Zheng, Tangliang Qian, Haiyu Wang, Xiujuan Hou
The neurokinin-1 receptor (NK-1R), an important member of three receptor subtypes for tachykinins, mediates intracellular signalling of the neuropeptide substance P (SP) [7]. NK-1R is mainly located in the central nervous system (CNS). Previous studies have reported that NK-1R is found in brain regions that regulate affective behaviours and addiction [8]. NK-1R activation plays a key role in regulating alcohol and drug abuse. Also, NK-1R can mediate stress- and anxiety-related effects by modulating monoaminergic neurotransmission and neuroendocrine responses [9]. Interestingly, it has been recently demonstrated that NK-1R is expressed in the periphery and SP has attracted increasing attention for its physiologic actions via NK-1R in the periphery [10]. Inhibition of NK-1R using its specific antagonists has been used for the treatment of addiction. Numerous NK-1R antagonists, including netupitant rolapitant, aprepitant, and casopitant, have been developed [11]. However, the expression patterns of NK-1R and its biological functions in FLSs and the pathogenesis of RA have not been reported before. In the current study, we aimed to investigate the expression patterns and physiological roles of NK-1R in RA-FLSs and the TNF-α-induced inflammatory response in FLSs.