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Palliative Care of Gastroparesis
Published in Victor R. Preedy, Handbook of Nutrition and Diet in Palliative Care, 2019
New prokinetic drugs are in the pipeline with the promise of being as effective as approved drugs, but with less adverse effects (Chedid and Camilleri 2017; Sanger and Pasricha 2017) (Table 29.5). Potential novel drugs include ghrelin agonists with prokinetic activity in GP. Relamorelin has been shown to improve symptoms and gastric emptying in diabetic GP patients. An additional benefit of ghrelin agonists is appetite stimulation. Alternative therapeutic options are available and should be tailored according to symptoms as well as underlying pathophysiology.
Management of Diabetic Gastroparesis
Published in Emmanuel C. Opara, Sam Dagogo-Jack, Nutrition and Diabetes, 2019
Kenneth L. Koch, Khalil N. Bitar
Unfortunately, many drugs designed to improve the rate of gastric emptying have not improved the symptoms associated with GP. Studies of prokinetic drugs and gastric stimulation have shown that the rate of gastric emptying does not correlate with the symptoms associated with GP [50]. Domperidone is a dopamine2 antagonist that does not cross the blood-brain barrier, improves nausea and gastric dysrhythmias, and improves the rates of gastric emptying in some patients with diabetic GP [51]. Domperidone is not available in the United States, except through a special US Food and Drug Administration (FDA) program. The ghrelin-agonist relamorelin (Allergan) is in phase III trials for patients with vomiting and T1DM or T2DM and GP [52]. The stimulation of ghrelin appears to increase the rate of gastric emptying and reduce vomiting.
Pharmacotherapeutic advances for chronic idiopathic constipation in adults
Published in Expert Opinion on Pharmacotherapy, 2022
Gabrio Bassotti, Paolo Usai Satta, Ginevra Berti, Mariantonia Lai, Vincenzo Villanacci, Massimo Bellini
However, it is likely that in the near future more drugs will be available for the treatment of CIC, some with new interesting mechanisms of action and, hopefully, with good long-term results and a limited amount of adverse events. Whether these drugs will be cost-effective or affordable by the majority of CIC patients is still unknown. Among these, 5-HT4 receptor agonists (in particular, tegaserod and velusetrag) will hopefully be soon available and, due to the apparent favorable safety profile (especially evident for tegaserod), could obtain a place among the therapeutic options. Relamorelin, although seemingly less powerful on stimulating colonic propulsive activity, could be effectively used in association to other drugs, due to its different mechanism of action. Of course, other drugs such as mizagliflozin are extremely interesting and, due to a completely different action compared to other drugs, could represent a further weapon to treat CIC patients, even though the cost of such a treatment is still unknown.
Current and future treatment management strategies for gastroparesis
Published in Expert Opinion on Orphan Drugs, 2019
Priyadarshini Loganathan, Mahesh Gajendran, Richard McCallum
Ghrelin also referred to as ‘hunger hormone’ is a peptide produced by ghrelinergic cells in the gastrointestinal tract which functions as a neuropeptide in the central nervous system [47]. When the stomach is empty, ghrelin is secreted and when the stomach is stretched, secretion stops. Ghrelin acts on hypothalamic brain cells both to increase hunger, and to increase gastric acid secretion and gastrointestinal motility to prepare the body for food intake [48]. The receptor for ghrelin is found on the same cells in the brain as the receptor for leptin, the satiety hormone that has opposite effects from ghrelin [49]. Ghrelin receptor agonists are the newer class of medications that stimulate gastric motility in both animal models and in humans to improve GE [50]. One of the ghrelin receptor agonist with promising outcomes is Relamorelin (RM-131), which is a selective pentapeptide ghrelin receptor agonist with potent prokinetic properties [51]. In a Phase 2a study on patients with diabetic GP, relamorelin dosed at 10 µg (mcg) twice daily, subcutaneously for 4 weeks, improved the symptoms of diabetic GP, especially in patients with vomiting at baseline [52]. In a Phase 2B randomized controlled trial, patients were randomized to 10 mcg twice daily, 30 mcg twice daily, 100 mcg twice daily, or placebo. Patients treated with relamorelin had clinically significant reductions in core diabetic GP symptoms (nausea, abdominal pain, postprandial fullness/bloating, and vomiting) and overall composite score, and was well tolerated [53]. The current plan is to initiate Phase 3 clinical trials now with the 10 mcg dose to achieve FDA approval status.
State-of-the-art pharmacotherapy for autonomic dysfunction in Parkinson’s disease
Published in Expert Opinion on Pharmacotherapy, 2020
Cecilia Quarracino, Matilde Otero-Losada, Francisco Capani, Santiago Pérez-Lloret
Relamorelin is a subcutaneously administered ghrelin analog that binds to the growth hormone secretagogue receptor-1a (GHS-1a), also known as ghrelin receptor, with at least three times the affinity of its natural ligand, ghrelin. Ghrelin receptor activation induces gastric motility, colonic movements, and improves constipation symptoms in the general population [113]. A multicenter, randomized, double-blind, placebo-controlled trial was set to study the effects of relamorelin treatment in PD patients, but the recruitment goals were not met, and no significant conclusions could be drawn [114].