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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
Neuropharmacology Of Respiration
Published in Alan D. Miller, Armand L. Bianchi, Beverly P. Bishop, Neural Control of the Respiratory Muscles, 2019
Monique Denavit-Saubié, Arthur S. Foutz
In most cases, opioids, when applied locally on respiratory neurons, reduce their discharge frequency.20,62,63,80 However, this reduction of firing is not homogeneous throughout the duration of the respiratory cycle (as occurs with noradrenalin). In tonically discharging neurons, the higher frequency which gives its respiratory modulation to the pattern of discharge is more depressed than the basal frequency in the remaining part of the respiratory cycle.20,63 Consequently, the respiratory modulation of the neuron is reduced and even suppressed, since there is no longer any difference of firing frequency in relation to the respiratory cycle. This smoothing of the modulation of respiratory neurons, which has also been observed after local application of a mu receptor agonist levorphanol, is reversed by administration of naloxone.20 This is probably at the origin of the depression of the motor respiratory output observed under opiate intoxication. Moreover, this mechanism may occur under physiological conditions because an iontophoretic application of naloxone without a preceding administration of opioid slightly increases the modulation of respiratory neurons.63 This neuronal modulation is decreased after local administration of the enkephalinase inhibitor, kelatorphan, which induces a local accumulation of enkephalins.57
Drug Targeting to the Lung: Chemical and Biochemical Considerations
Published in Anthony J. Hickey, Sandro R.P. da Rocha, Pharmaceutical Inhalation Aerosol Technology, 2019
Peter A. Crooks, Narsimha R. Penthala, Abeer M. Al-Ghananeem
Human pulmonary carcinomas have been shown to contain high levels of opioid peptides and their corresponding membrane-bound receptors (Rigaudy et al. 1989). Rigaudy et al. (1989) targeted drugs to these receptors using modified metabolically stable enkephalins linked to cytotoxic drugs. These conjugates were expected to specifically internalize within opiate receptor-baring cells. Cell culture studies with NG 108-15 mouse tumor cells indicated that the peptide-ellipticinium conjugates 53a and 53b were internalized and were intracellularly stable, but showed much lower cytotoxicity than their parent drug towards the opioid receptor-bearing cells. Nevertheless, the study did indicate that enkephalin-derived peptides could be used as specific carriers to target cytotoxic agents towards opioid receptor-rich cells. A similar approach for targeting pulmonary epithelial membrane-bound enkephalinase (Table 3.1) may also be valid, using enkephalin drug or enkephalinase inhibitor-drug conjugates. One potential problem with the drug-targeting strategy is the likelihood that in disease states, membrane receptor populations may not be maintained. In this respect, an approach that uses a carrier capable of binding to multiple types of receptors may be more successful.
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.