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Immunosuppressants, rheumatic and gastrointestinal topics
Published in Evelyne Jacqz-Aigrain, Imti Choonara, Paediatric Clinical Pharmacology, 2021
Evelyne Jacqz-Aigrain, Imti Choonara
Racecadotril is a specific inhibitor of enkephalinase, a cell membrane peptidase located in various tissues, notably the epithelium of the small bowel. Studies in animals and humans show that oral racecadotril has an effect on secretory diarrhoea caused by cholera without influencing the intestinal transit time. These effects were anatagonised by the opioid-receptor antagonist naloxone suggesting an involvement of endogenous opioid peptides. In randomised controlled trials in children with acute diarrhoea racecadotril (1.5 mg/kg administered orally 3 times daily) used as adjuvant therapy to oral rehydration was well tolerated and reduced the output of stools by up to 50% [12,13].
Gastrointestinal and liver infections
Published in Michael JG Farthing, Anne B Ballinger, Drug Therapy for Gastrointestinal and Liver Diseases, 2019
A promising new approach has been the development of an enkephalinase inhibitor, racecadotril, which has pro-absorptive activity through its ability to potentiate endogenous enkephalins in the intestine.54, 55 Randomized controlled trials in adults and children confirm that this is an effective agent for reducing stool weight and bowel frequency, without the unwanted effects of rebound constipation, which is commonly reported with anti-motility, anti-diarrhoeal agents.56-58 Studies in children have shown that it is safe and superior in efficacy to loperamide.58
Rotavirus
Published in Dongyou Liu, Handbook of Foodborne Diseases, 2018
Lijuan Yuan, Tammy Bui, Ashwin Ramesh
Since ORS only serves to offset dehydration, adjunctive treatments continue to be proposed and studied with the aim of reducing rotavirus diarrhea. The antisecretory drug racecadotril has been proven to be effective in decreasing intestinal water loss and has been licensed for use in Europe to treat acute, watery diarrhea.234,235
Evaluating the cost utility of racecadotril in addition to oral rehydration solution versus oral rehydration solution alone for children with acute watery diarrhea in four low middle-income countries: Egypt, Morocco, Philippines and Vietnam
Published in Journal of Medical Economics, 2022
Tamlyn Anne Rautenberg, Martin Downes, Pham Huy Tuan Kiet, Nermeen Ashoush, Antonio Rosete Dennis, Kyoo Kim
Racecadotril is an oral enkephalinase inhibitor used for the treatment of acute diarrhoea and authorised by the European Medicines Agency39,40. To date, no study has been done to evaluate the cost utility of racecadotril for the treatment of children with diarrhea in LMIC, although several studies have been published for high-income and upper-middle-income countries41–43. In view of the persistent challenge of diarrhoea, the growing importance of HTA in the countries in focus and the acceptability of leveraging on existing economic evaluations, this study has been undertaken. The objective is to evaluate R + ORS versus ORS alone in children under the age of five with acute watery diarrhoea in Egypt, Morocco, Philippines and Vietnam to support emerging HTA processes and inform public health funding bodies at country level.
Current strategies toward safer mu opioid receptor drugs for pain management
Published in Expert Opinion on Therapeutic Targets, 2019
Aliza T. Ehrlich, Brigitte L. Kieffer, Emmanuel Darcq
Another effort has been made to generate endogenous opioid peptide analogues [79]. This approach is appealing as it will use the naturally produced analgesic properties of endogenous opioids and improve at the same time their stability and bioavailability. Several methods have been used during the last few decades to make peptides druggable such as glycosylation, cyclization, modification of the C- and N-terminal and packaging of opioid peptides and are reviewed in detail in [79]. These strategies are still in their early stages, requiring a significant need of development due to the challenges in stabilizing peptides with short in-vivo half-life, and increasing their bioavailability making them capable of crossing the blood brain barrier. Another interesting approach consists of increasing peptide levels by inhibiting the enzyme(s) responsible for endogenous opioid peptide degradation [80]. The enzymes that degrade endogenous enkephalin opioid peptides are known as enkephalinases. The designed inhibitors of enkephalinases such as aminopeptidase N and neutral endopeptidase neprilysn (NEP), are called racecadotril, ubenimex (bestatin), and RB-101. Remarkably, preclinical observations support that these enkephalinase inhibitors are capable of producing efficient analgesia without respiratory depression, reward, tolerance and constipation [81]. This strategy is very appealing because it circumvents exogenous opioid use thereby avoiding dependency issues and lethal complications like respiratory depression, however until now enkephelinase inhibitors have not made it into the clinic to treat pain.
All-cause gastroenteritis hospitalisations of children decreased after the introduction of rotavirus vaccine in Stockholm
Published in Infectious Diseases, 2022
Selma Olsson-Åkefeldt, Maria Rotzén-Östlund, Berit Hammas, Margareta Eriksson, Rutger Bennet
The fall in outpatients treated for gastroenteritis was less pronounced than for admitted patients which agrees with that rotavirus vaccines have been shown to be better at preventing severe infections [9]. However, a change in our emergency department routines with more frequent oral or intravenous rehydration and increased use of ondansetron and racecadotril may also have contributed to our observed fall in all-cause gastroenteritis and rotavirus gastroenteritis admissions noted already some years prevaccination.