A prominent representative of the prokinetics group is emetrol (domperidone)

emetrol

The search for remedies that normalize the motor and evacuatory activity of the digestive tract has been attracting the attention of medical researchers for several centuries, and they have succeeded, for example Emetrol. Probably one of the first representatives of this group is ginger, which has been used in traditional Chinese medicine as a remedy for abdominal heaviness and nausea since ancient times and has weak antagonistic activity against 5-HT3 receptors. To date, remedies that affect the motor activity of the digestive tract and prevent antiperistalsis contractions of smooth muscles are grouped into a group of prokinetics.

First of all, it is necessary to outline the range of indications for which there is evidence of effectiveness of prokinetics.

A prominent representative of the prokinetics group is emetrol (domperidone)
  • Firstly, it is diseases of the digestive tract in development of which disorders of digestive tract motor activity play an essential role (gastroesophageal reflux disease, postprandial distress syndrome as a variant of functional dyspepsia, ulcer disease with violation of antroduodenal coordination, idiopathic gastroparesis, functional nausea, functional constipation, and irritable bowel syndrome – variant with constipation).
  • Second, the use of prokinetics as antiemetics (e.g., for nausea and vomiting associated with cytostatics intake).
  • Third, diabetic gastroparesis, in which delayed gastric emptying affects the variability of glucose absorption, which causes difficulties in glycemic control and can lead to chronicity of gastroparesis symptoms and low glycemic control. This should also include the prescription of prokinetics in gastroparesis of other etiology.

Emetrol (domperidone) by its chemical structure also belongs to benzimidazole derivatives, is a highly selective blocker of peripheral dopamine receptors (D) type 2 and unlike metoclopramide is free of many side effects due to absence of drug penetration through the blood-brain barrier. Suppressing the effect of dopamine, emetrol (domperidone) increases spontaneous gastric activity, increases lower esophageal sphincter pressure and activates peristalsis of the esophagus and antral stomach. The drug also increases frequency, amplitude and duration of duodenal contractions and decreases time of passage of food masses through the small intestine.

A prominent representative of the prokinetics group is emetrol (domperidone)

Researchers continue to actively study new agents with directional selective prokinetic activity, among which physostigmine and neostigmine are muscarinic receptor agonists that stimulate intestinal activity and only slightly improve gastric emptying; gastric transit-accelerating cholecystokinin receptor antagonists loxyglumide and dexloxyglumide, and the phosphodiesterase-5 inhibitor sildenafil; an alpha-2 agonist (adrenomodulator) clonidine, which normalizes evacuation of gastric contents in functional dyspepsia (postprandial distress syndrome), slowing intestinal transit with decreased visceral colonic hypersensitivity.

A wide range of indications in which the prescription of prokinetics is effective, as well as the features of each of the subgroups of prokinetics (different mechanisms of prokinetic effect, safety profile, preferential activity in relation to the upper or lower floor of the digestive tract) allow the doctor in each clinical case to choose the most effective and safe prokinetics.

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