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Results for “GASTROINTESTINAL MOTILITY”

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PubMed1991

[The potentials of erythromycin derivatives in the treatment of gastrointestinal motility disorders].

In low dosages erythromycin imitates the effect of motilin on the gastrointestinal motility. In vitro experiments show that erythromycin is a motilin agonist: it displaces motilin which is bound to its receptor; it directly acts on smooth musculature and it possesses the same animal and tissue specificity. Structural changes cause adequate changes in the binding affinity and in the contractile activity. Several motilides such as erythromycin derivatives with prokinetic properties have no antibiotic activity, but they cause a distinct increase of the prokinetic activity. Motilides may be defined as a new group of prokinetic substances: the motilinomimetics. Erythromycin normalises the delayed evacuation of the stomach of solid and fluid food in diabetic, idiopathic and postvagotomy gastroparesis. For the treatment of gastrooesophageal reflux disease, gastritis, pathological overgrowth of the small intestine, hypokinesia of the gallbladder and the chronic obstipation erythromycin appears as a promising medicament. The substances with a stronger effect may become even still more useful medicaments. A better understanding of the relation between motilin and motilides may lead to new knowledge about the regulation of the gastrointestinal motility.

Biliary Tract↗

PubMed1991

Effects of famotidine on upper gastrointestinal motility in patients with progressive systemic sclerosis.

The effects of famotidine on human upper gastrointestinal motility were investigated, together with the relationship of gastric alkalinization and serum gastrin levels to changes produced by famotidine. Intravenous famotidine (20 mg), at a dose level in which an inhibitory effect on acetylcholinesterase activity is not recognized, was given to 13 patients with progressive systemic sclerosis but no other disorders. Gastric phasic motor activity was not changed significantly, but the lower esophageal sphincter pressure was elevated significantly in comparison with 15 controls given physiological saline, even when gastric phasic motor activity was taken into consideration. Gastric alkalinization with 7% sodium bicarbonate did not significantly increase the sphincter pressure in all 7 subjects so treated. No significant correlation was recognized between the serum gastrin level, the lower esophageal sphincter pressure, and the gastric motility index in any of the 3 groups. It was, therefore, concluded that intravenous administration of famotidine affected upper gastrointestinal motility, especially the lower esophageal sphincter pressure, through an as yet unknown mechanism other than inhibition of acetylcholinesterase activity, gastric alkalinization, or elevation of serum gastrin levels.

Adult↗

PubMed2006

Gastrointestinal motility during cardiopulmonary bypass: a sonomicrometric study.

Cardiopulmonary bypass (CPB) is known to impair the integrity of the gastrointestinal tract. However, little is known about the movement behavior of the gastrointestinal tract during CPB. This study was aimed to assess the gastrointestinal motility with sonomicrometry, a distance measurement using ultrasound, in a porcine model of CPB. Twelve pigs weighing 70-112 kg were having a standard hypothermic CPB for 120 min either with the nonpulsatile flow (n = 6) or the pulsatile flow (n = 6). Before CPB, piezoelectric echo crystals were placed either along the longitudinal or the circular axis of the pylorus. Patterns of gut movement and the total sonomicrometric activity (TSA) were recorded at several time intervals during experiments as qualitative and quantitative parameters of gut motility. Results showed that the intact regular rhythmic pattern of gut movement was detected before CPB. This pattern changed little when CPB started, but it disappeared at 60 min when the body temperature lowered down to 32 degrees Celsius. During the same period, the TSA reduced significantly along the longitudinal as well as the circular directions of the pylorus. There was no significant difference between the nonpulsatile and pulsatile groups. Gut blood flow reduced significantly in both groups, but it was not associated with the reduced sonomicrometric activity. In conclusion, gastrointestinal motility during CPB can be measured qualitatively and quantitatively by sonomicrometry in a large animal model. Suppression of gut motility during CPB does not seem to be associated with the mode of perfusion but with the reduced body temperature during the hypothermic phase of CPB.

Animals↗

PubMed1991

[Medicamentous modification of gastrointestinal motility and secretion].

This article gives an overview on possible new pharmacological tools to modify gastrointestinal motility and/or secretion. The characterization of new subclasses of classical neurotransmitter receptors and of peptidergic receptors offer a new approach for the development of new therapeutic agents. Using molecular biology techniques a variety of receptor subclasses have been demonstrated for muscarinic and alpha 2-adrenergic receptors. Both receptor types are of major importance for the regulation of mucosal secretion in the submucosal plexus and specific ligands for these receptor subtypes could be of clinical interest. In the next paragraphs the possible therapeutic relevance of 5-HT3-receptor antagonists and of opiate agonist and -antagonists is discussed. 5-HT3-antagonists, which can be used as potent antiemetics, also demonstrate quite potent effects on upper gastrointestinal motility such as gastric emptying. Whereas the subclassification of opioids has so far no specific therapeutic consequences there is some evidence that casomorphin, a derivative of the casein of the milk, could be used as a possible antidiarhoic substance. The use of antagonist and agonists on peptidergic receptors with orally active ligands offer a further new therapeutic approach. This is discussed for CCK-antagonists and erythromycin-analogues which are agonists at the motilin receptor. Besides this experimental approach to modify defined receptor subclasses, there are new substances with so far not clearly defined mechanism of action, which, however, have potent therapeutic effects. Cisapride, a new potent prokinetic drug with little side effects, is now available for clinical use for a wide range of motility disorders.

Digestive System↗

PubMed1983

[Effect of stimulation of the tooth pulp on gastrointestinal motility in rabbits].

Effects of electrical stimulation of the inciser tooth pulp on the gastrointestinal motility were investigated in the rabbit anesthetized with urethane and chloralose. Pulpal Stimulation caused an excitatory or an inhibitory effect in the gastric body and antrum and the ducodenum. After bilateral splanchnicotomy the excitatory response to the pulpal stimulation was reinforced or the inhibitory response converted to the excitatory response. An additional cervical vagotomy abolished the excitatory and inhibitory response. Atropine diminished the spontaneous efferent discharges of vagal gastric branch (VGB) and abolished the excitatory and inhibitory response to stimulation of the pulp and the inferior alveolar nerve. This agent also blocked the potentials of the VGB evoked by afferent stimulation of the inferior aveolar nerve. Hexamethonium bromide abolished the excitatory and inhibitory responses to the pulpal stimulation but did not affect spontaneous discharges and increased discharges of the VGB to pulpal stimulation. Morphine produced decreased rate of the spontaneous discharge of the VGB and abolished increased rate of discharges of the VGB as well as the gastrointestinal responses to pulpal stimulation. It is concluded from these results that the afferent impulses caused by pulpal stimulation and the inferior alveolar nerve 'reflex'ly activate the vagal motor nuclei in the medulla oblongata and the sympathetic splanchnic nuclei in the thoracic segments through the trigeminal nerve: The vagus nerves produced the excitatory response in the gastrointestinal motility, while the splanchnic nerves caused the inhibitory response. It was supposed that sites of action of atropine and morphine is not in peripheral site, but in the central nerves site.

Animals↗

PubMed1975

[Spasmolytic effect of mebeverine on the gastrointestinal motility].

Mebeverine, N-ethyl-4'-[1-methyl-2-(4-methoxyphenyl)ethylamino] butyl-3,4-dimetoxybenzoate, was studied for its inhibitory effect on the motility of the gastrointestinal tract in vivo and in vitro. In both cases its activity was more evident on the hypermotility induced by some common physiological spasmogenic agents than on basal motility. In various tests it was ascertained that mebeverine was able to inhibit the stimulant actions of all the drugs employed, both those acting on specific receptor sites such as histamine and acetylcholine, and those acting directly on the smooth muscle such as substance P, physalaemin etc. This backs up the suggestion of a nonspecific miotropic effect of mebeverine. This compound has the same spasmolytic action at different levels of the gastrointestinal tract and is decisively stronger than papaverine. The lack of remarkable side-effects in the tests which were carried out in vivo with decisively active doses on the gastrointestinal motility and the good inhibitory effect on human isolated strips of the gastrointestinal tract suggest that mebeverine may be useful in the treatment of clinical morbid conditions characterized by hypertone or hypermotility of the gastrointestinal tract.

Animals↗

PubMed2002

Effects of evodiamine on gastrointestinal motility in male rats.

The effects of evodiamine on gastric emptying, gastrointestinal transit, and plasma levels of cholecystokinin (CCK) were studied in male rats. Evodiamine, isolated from the dry unripened fruit of Evodia rutaecarpa Bentham (a Chinese medicine named Wu-chu-yu), has been recommended for abdominal pain, acid regurgitation, nausea, diarrhea, and dysmenorrhea. Gastrointestinal motility was assessed in rats 15 min after intragastric instillation of a test meal containing charcoal and Na(2)51CrO(4). Gastric emptying was determined by measuring the amount of radiolabeled chromium contained in the small intestine as a percentage of the initial amount received. Gastrointestinal transit was evaluated by calculating the geometric center of distribution of the radiolabeled marker. Blood samples were collected for CCK radioimmunoassay (RIA). After administration of evodiamine (0.67-6.00 mg/kg), both gastric emptying and gastrointestinal transit were inhibited, whereas the plasma concentration of CCK was increased in a dose-dependent manner. The selective CCK(1) receptor antagonists, devazepide and lorglumide, effectively attenuated the evodiamine-induced inhibition of gastric emptying and gastrointestinal transit. L-365,260 (3R-(+)-N-(2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-yl)-N'-(3-methylphenyl)-urea), a selective CCK(2) receptor antagonist, did not alter the evodiamine-induced inhibition of gastric emptying and gastrointestinal transit. These results suggest that evodiamine inhibits both gastric emptying and gastrointestinal transit in male rats via a mechanism involving CCK release and CCK(1) receptor activation.

Animals↗

PubMed1988

Comparative study on effects of 14- and 16-membered macrolides on gastrointestinal motility in unanaesthetized dogs.

Comparative studies on the effects of 14-membered and 16-membered macrolides on gastrointestinal motility were conducted in unanaesthetized dogs. Midecamycin acetate, a new 16-membered macrolide, and leucomycin, another 16-membered macrolide, did not disturb the gastrointestinal motility and no dogs showed any adverse effects. In contrast, erythromycin stearate, erythromycin ethylsuccinate and triacetyloleandomycin, 14-membered macrolides, caused adverse effects such as strong contractile motility, nausea, vomiting and diarrhoea. The adverse effects of macrolides on the gastrointestinal tract are related to their chemical structure.

Administration, Oral↗

PubMed2002

Changes in gastrointestinal motility after subtotal colectomy in dogs.

PURPOSE: This study was conducted to examine recovery from diarrhea after subtotal colectomy by observing changes in gastrointestinal motility, neuropeptides, and autonomic nerves in the enteric nervous system in dogs. METHODS: The moisture volume of intestinal matter recovered from the ileal side of the anastomosis was defined as the diarrhea index. Gastrointestinal motility was measured using strain gauge force transducers (SG) for 24 weeks after subtotal colectomy. Immunohistochemical changes in neuropeptides in the residual intestine, acetylcholinesterase activation of cholinergic fibers, and fluorohistochemical changes of adrenergic fibers in the myenteric plexuses were evaluated. RESULTS: The digestive tract transit time returned to normal in the early postoperative period, but decreased moisture volume was seen in the intestinal matter after 8 postoperative weeks. Migrating contraction waves propagating beyond the site of anastomosis, signaling recovery of intestinal motility, were noted after 8 postoperative weeks, corresponding to reconstruction of cholinergic fibers in the anastomotic section. Transient activation of vasoactive intestinal polypeptide was seen in the residual intestine, but this had normalized by the eighth postoperative week. Lengthened villi in the residual intestine were also seen after 8 postoperative weeks. CONCLUSION: The decreased moisture volume in the intestinal matter is due to the improvements we observed in the eighth postoperative week.

Acetylcholinesterase↗

PubMed1989

Inhibitory effect of galanin on postprandial gastrointestinal motility and gut hormone release in humans.

Galanin was infused intravenously in 8 healthy volunteers at a dose of 40 pmol/kg.min for 1 h to investigate the pharmacologic effects of this peptide on postprandial gastrointestinal motility and gut peptide release in humans. Galanin strongly inhibited gastrointestinal motility. Gastric emptying was significantly delayed, with the time taken to empty 50% of the gastric contents increasing from 59.0 +/- 4.8 min (control infusion) to 99.3 +/- 4.7 min (galanin infusion). Mouth-to-cecum transit time increased from 67.5 +/- 6.9 to 126.3 +/- 18.5 min. Galanin potently suppressed the initial postprandial rise in plasma concentrations of glucose, insulin, peptide tyrosine tyrosine, neurotensin, enteroglucagon, pancreatic glucagon, somatostatin, and pancreatic polypeptide, but did not change gastric inhibitory polypeptide, motilin, peptide histidine methionine, and gastrin concentrations compared with control. The results indicate that an infusion of galanin has potent effects on the gastrointestinal tract in humans. The changes in motor activity in particular suggest that the local galaninergic innervation could have an important physiologic role in the control of human gastrointestinal propulsive motor activity.

Adult↗

PubMed1982

[Effects of trimebutine maleate on the gastrointestinal motility in conscious dogs].

Trimebutine maleate is known to have beneficial effect in the treatment of gastrointestinal disorders. In conscious dogs with implanted force transducers, effects of trimebutine maleate on the gastrointestinal motility were investigated by intravenous injection, and the results were compared to those with metoclopramide and hyoscine-N-butylbromide. When trimebutine maleate was administered during the motor quiescence in the interdigestive state, contractions were evoked or the quiescent time was shortened in the gastrointestinal tract. In the digestive state, the gastric antral contractile activity was reduced, and duodenal activity was somehow suppressed by trimebutine maleate; but in the jejunum, ileum or colon, the activity was augmented. Injection of metoclopramide evoked a continuous contraction in the gastric antrum and duodenum during the period of motor quiescence in the interdigestive state. In the digestive state, metoclopramide caused a slight enhancement in the contractile activity of the gastric antrum. On the other hand, hyoscine-N-butyl-bromide produced no effect during the period of motor quiescence in the interdigestive state and suppressed the activity of the gastrointestinal tract during the digestive state. Thus, the pattern of action of trimebutine maleate was different from metoclopramide and hyoscine-N-butylbromide. It was concluded that trimebutine maleate produces dual actions, suppression and acceleration, on the gastrointestinal motility in conscious dogs.

Animals↗

PubMed2000

Prokinetic effect of black tea on gastrointestinal motility.

The gastrokinetic effects of hot water extract of black tea [Camellia sinensis, (L) O. Kuntze (Theaceae)] on gastrointestinal motility were studied both in vivo and in vitro. The extract significantly accelerated the gastrointestinal transit (GIT) in vivo in mice. These facilitatory effect was reduced after pretreatment with atropine, hemicholinium-3, morphine, indomethacin, McN-A-343 and L-arginine. In guinea pig ileum, the extract facilitated the peristaltic reflex in response to pressures in normal preparation. The black tea extract and L-NMMA (nitric oxide synthase inhibitor) significantly reduced the electrical field stimulated nonadrenergic, noncholinergic (NANC) relaxation of isolated rat fundal strips. The extract markedly enhanced the tonic ('hump') responses to transmural stimulation in longitudinal muscle of guinea pig ileum which was unaltered in the presence of atropine. These findings suggest a cholinergic involvement and a partial role of prostaglandin and nitric oxide in the mechanism of action of black tea extract on gastrointestinal motility. To determine the effective constituents in black tea responsible for this activity, the effect of black tea polyphenols on GIT were also studied. Thearubigin fraction (but not theaflavin) accelerated GIT significantly which suggests its involvement in the prokinetic effect of black tea.

Animals↗

PubMed1989

The current status of opioid research on gastrointestinal motility.

Apparently conflicting data on opioid effects on gastrointestinal motility have been reported in the literature. The current status is reviewed and an attempt is made to find a common denominator to discrepant results by suggesting functionally contrasting opioid systems modulating the same physiological functions. Upon superimposition, these contrasting systems might result in opposite opioid effects dependent on the actual functional balance between the systems at the time of drug administration. Inhibitory neuromodulation at multiple sites leading to either inhibition or disinhibition by opioids may serve as a common basis of their contrasting effects. This interpretation, though consistent with most of the currently available data, is still a working hypothesis.

Animals↗

PubMed1997

Pharmacological stimulation of gastrointestinal motility: where we are and where are we going?

Drugs affecting gastrointestinal motility have become valuable in the management of a number of diseases. Medications that enhance the transit of material through the gastrointestinal tract are called prokinetics. Although symptom improvement can be seen in a variety of motility disorders, these medications have not shown a selective benefit for a particular motility disturbance or symptom complex. This class of drugs includes several subclasses, each with a distinct mechanism of action. Amongst the existing prokinetic compounds, dopamine antagonists, on the one hand, and cholinomimetic drugs, on the other hand, should be distinguished. Since compounds endowed with dopamine antagonism have the disadvantage of causing neuroendocrine side effects and/or extrapyramidal dyskinetic reactions (seen especially after metoclopramide), the recently developed non-cholinergic non-antidopaminergic compound, cisapride, seems to be the most effective one. Its main mechanism of action is considered to be the stimulation of myenteric cholinergic nerves with consequent increase of acetylcholine release. Recent evidence suggests that blockade of CCK receptors and stimulation of motilin receptors are also promising avenues to increase gastrointestinal motility. Since drugs acting on 5-HT receptors are presently the best available motor-stimulating compounds, new derivatives are being developed as gastrokinetic drugs. Although the long-acting somatostatin analog, octreotide, and the GnRH agonist, leuprolide, have shown prokinetic properties in particular clinical conditions, their widespread use cannot be recommended at present. Further work is needed to determine the predictive value of objective abnormalities for the efficacy of a drug in the individual patient. This is the crucial point to define a rational strategy in clinical practice, especially to establish if functional investigation is needed before a prokinetic drug be given.

Gastrointestinal Diseases↗

PubMed1984

Elevated ANA titers in patients with severely abnormal gastrointestinal motility.

We studied a group of six patients with clinical, radiological, and/or manometric features of severely abnormal gastrointestinal motility. Symptoms suggestive of esophageal, small bowel, or colonic involvement were present from 1 1/2 to 40 years. All patients had elevated antinuclear antibody (ANA) titers. None had clinical or radiographic features suggestive of progressive systemic sclerosis or other connective tissue diseases. Two patients had pathologic examinations of intestinal specimens, and these did not show changes suggestive of progressive systemic sclerosis. We conclude that patients with severe gastrointestinal motility disorders can have elevated ANA titers without features of progressive systemic sclerosis or other connective tissue diseases.

Aged↗

PubMed1984

[Effects of trimebutine maleate (TM-906) on the gastrointestinal motility in anesthetized dogs].

Effects of trimebutine maleate (TM-906) on the spontaneous motility of the gastrointestinal tracts were investigated in anesthetized dogs by means of force transducers. TM-906, administrated intravenously or intraduodenally, produced an inhibition followed by a potentiation of the spontaneous motility in the stomach, and caused a potentiation of the spontaneous motility in the duodenum, jejunum, ileum and colon. These effects of TM-906 were observed also in the vagotomized dogs as in the intact dogs. From these results, it is suggested that TM-906 modulates the spontaneous motility of the gastrointestinal tracts primarily through the peripheral mechanism.

Anesthesia↗

PubMed1986

Comparison of the side effects and gastrointestinal motility observed after administration of erythromycin and josamycin to dogs.

The effects of intravenous erythromycin and josamycin on gastrointestinal motility in dogs have been compared. Erythromycin interrupted the basal motility pattern in the fasted state and induced irregular bursts of spikes in both the fasted and fed states. Emesis occurred in all the dogs in the fasted state experiments and in four out of six dogs in the fed state experiments. Josamycin did not disturb gastrointestinal motility and no dog showed signs of discomfort. The difference in the chemical structure of erythromycin and josamycin is the main reason for their differential effect on the gastrointestinal tract.

Animals↗

PubMed1993

Effect of a new colonic prokinetic compound, T-1815, on gastrointestinal motility in anesthetized and conscious fasted dogs.

Effect of T-1815, a new colonic prokinetic compound, on gastrointestinal motility was studied in anesthetized and conscious dogs fasted for 24 hr before experiment. In anesthetized dogs, intravenous injection of T-1815 in doses of 0.3-3.0 mg/kg caused a biphasic effect on the gastric motility, a slight decrease followed by a slight increase. While the compound elicited only an increase in motility of the duodenum, jejunum and colon. In the colon, high-amplitude contractions were observed in 2 out of 5 animals at 1 mg/kg, i.v. of T-1815 and 4 out of 5 animals at 3 mg/kg. Bethanechol at 0.01 mg/kg, i.v. produced only a potentiation of the motility in all of the sites, but never induced high-amplitude contractions in the colon. During the interdigestive state in conscious dogs, intravenous T-1815 at 1 and 3 mg/kg caused contractions similar to the interdigestive phase III contractions at the stomach and duodenum in only 2 out of 7 experiments, and colonic motility was slightly depressed at 3 mg/kg. Oral administration of T-1815 at 30 and 50 mg/kg did not elicit the phase III-like contractions but produced persistent contractions at the stomach and duodenum in 2 out of 4 conscious animals during the interdigestive state. In the proximal and middle colon, high-amplitude contractions were observed in 5 out of 7 animals by 10-50 mg/kg, p.o. of T-1815. From the above results, it is concluded that the pharmacological effect of T-1815 on gastrointestinal motility is different from that of the cholinergic agonist. In addition, T-1815 seems to have a characteristic to induce high-amplitude contractions which are known to be closely related to defecation.

Administration, Oral↗