Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: CAS:81098-60-4 (Cisapride)
 330 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cisapride is a gastrointestinal prokinetic agent reported to be devoid of direct cholinergic effect from the myenteric plexus of the gut. The effect of cisapride (0.125, 0.5, 2mg/kg, i.p.) on the concentration beta-endorphin and substance P in rat gastrointestinal tract was studied. beta-Endorphinlike immunoreactivity contents were significantly increased in both mucosal and muscular layers of the entire gastrointestinal tract (from gastric body to rectum) of the rats treated with 2 mg/kg of cisapride. beta-Endorphinlike immunoreactivity contents were also increased in a part of the gastrointestinal tract of the rats treated with 0.125 or 0.5 mg/kg of cisapride. Substance P like immunoreactivity contents were significantly decreased in muscular layers of the rectosigmoid colon of the rats treated with 2 mg/kg of cisapride. This study suggests that the prokinetic effects of cisapride may relate to the contents of beta-endorphinlike immunoreactivity and substance P like immunoreactivity in gastrointestinal tract.
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PMID:Effect of cisapride on the concentrations of beta-endorphinlike immunoreactivity and substance P-like immunoreactivity in the rat gastrointestinal tract. 244 24

To investigate the effects of cisapride, a motility-inducing agent, on ano-rectal sphincter functions, standard manometry was performed in 10 healthy male volunteers after 5 days on a 20-mg dose of cisapride in a placebo-controlled double-blind randomized crossover fashion. All subjects kept stool diaries during the experiment. Cisapride significantly increased stool frequency by adding soft and liquid stools; in addition, anal resting pressure was reduced with cisapride in seven of the 10 subjects; mean resting pressure decreased by 16%, while all other measurements were not altered. This suggests that cisapride may act directly on the smooth muscle of the internal anal sphincter. It also supports the view that enhanced defaecation in chronic constipation induced by cisapride may not be achieved by propulsive motor activity in the colon but also by a decreased anal sphincter tone.
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PMID:Effects of cisapride on ano-rectal sphincter function. 251 67

The actions of cisapride on electrical behavior of single myenteric neurons and on the propulsive activity of segments of ileum were studied in vitro. Cisapride (10-300 nM) did not affect the membrane potential, resting properties, or active properties of S neurons. The amplitude of fast nicotinic excitatory postsynaptic potentials recorded from S cells was increased by cisapride in the concentration range of 10 nM to 1 microM. Higher cisapride concentrations (3-10 microM) reduced the amplitude of fast excitatory postsynaptic potentials. Potentiation of fast excitatory postsynaptic potentials by cisapride was antagonized by ICS 205-930 (1 microM) but was unaffected by GR 38032F (1 microM), both compounds being 5-HT3-receptor antagonists. Cisapride did not modify the electrical behavior of AH neurons except at the highest concentrations (3-10 microM), which caused hyperpolarization of some neurons. The propulsive efficiency (i.e., number of peristalses and total amount of fluid ejected per unit of time) of isolated segments of ileum was enhanced by cisapride (100 nM to 3 microM). Higher cisapride concentrations (6 or 10 microM) had a depressant action on propulsive activity. The stimulatory effect of cisapride on propulsion was not antagonized by ICS 205-930 (300 nM or 1 microM). These data indicate that cisapride facilitates cholinergic transmission in the myenteric plexus of guinea pig ileum and that this effect may be at least partially responsible for the increased propulsive efficiency observed in ileal segments.
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PMID:Effects of cisapride on cholinergic neurotransmission and propulsive motility in the guinea pig ileum. 253 5

Anti-cholinesterase activity of dopamine D2 receptor antagonist, domperidone was studied by means of chronically implanted force transducers in the gastrointestinal (GI) tract in five conscious dogs. Cisapride was used as a drug to stimulate endogenous release of acetylcholine. In the digestive state, cisapride (0.25 mg/kg) stimulated 18.6 +/- 5.6% increase in the motor index of the gastric antrum alone, however, combined administration with domperidone (1.0 mg/kg-hr) significantly enhanced the motor index in the gastric antrum and duodenum. In the gastric antrum, the increase was 68.1 +/- 7.2%. During the interdigestive state, cisapride did not always induce the interdigestive migrating contractions (IMC)-like contractions in the GI tract, but the background infusion of domperidone significantly increased the incidence of the occurrence of IMC-like contractions by cisapride. In in vitro study, weak but significant anti-cholinesterase activity was found in domperidone, the activity being about 1/1,000 of that of neostigmine. In dog experiment, similar enhancement of motor stimulating activity of cisapride was observed when neostigmine was given at 1.0 micrograms/kg-hr. In conclusion, domperidone has anti-cholinesterase activity and acts to enhance motor stimulating activity of cisapride through inhibition of cholinesterase activity in the upper digestive tract.
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PMID:[Anti-cholinesterase activity of dopamine D2 receptor antagonist: its clinical significance]. 257 86

Gastric emptying was studied in 10 insulin-treated, long-standing, diabetic out-patients with upper gastrointestinal, dyspeptic symptoms. Autonomic neuropathy, mucosal lesions and chloropeptic hyposecretion were excluded. Gastric emptying of a labelled solid meal (99mTc-sulphur colloid-infiltrated chicken liver) was clearly delayed by comparison with normal subjects: the mean gastric emptying half-time was almost 5-times longer (245.6 vs 52.5 min), and the gastric emptying rate at 120 min was 75% slower. Cisapride 10 mg i.v. significantly accelerated both parameters, and placebo had no effect upon them. In conclusion, gastroparesis may be present in diabetics without autonomic neuropathy, and cisapride may improve gastric emptying in such patients.
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PMID:Cisapride and gastric emptying of a solid meal in dyspeptic diabetics without autonomic neuropathy and in healthy volunteers. 259 76

Cisapride (Prepulsid) is a new prokinetic drug of the gastrointestinal tract. It has indirect muscarinic parasympathicomimetic effects on the neuromuscular junction of smooth muscle that we also observed on the vesical function by four of the six patients presented in this study.
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PMID:[[The effect of cisapride on the neurogenic bladder]. 260 97

Following abdominal radiation a 16-year-old male patient developed nausea and vomiting secondary to gastric stasis, dilatation and impairment of antral motility. Symptoms improved after 2 months of treatment with a cholinergic agonist. Now, 7 years later, symptoms recurred. Cisapride, a newly developed agent which stimulates gastrointestinal motility probably evoked a prompt increase of antral motility and gastric emptying. We conclude that abdominal irradiation may cause gastrointestinal motility disturbances which may respond to medical therapy.
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PMID:[Recurrent gastroparesis following abdominal irradiation. Therapy with cisapride]. 262 54

We have investigated the effect of oral cisapride (10 mg t.i.d.) in a double-blind, placebo-controlled trial in 26 patients with upper gut dysmotility: 11 with gastroparesis (8 diabetic, 3 idiopathic) and 15 with chronic idiopathic intestinal pseudoobstruction. Patients were evaluated at entry and at the end of the 6-wk study by upper gastrointestinal manometry, scintigraphic evaluation of gastric emptying of solids and liquids, measurement of body weight, and scoring of the following symptoms: abdominal pain, nausea, vomiting, early satiety, bloating, and distention. Cisapride and placebo groups were strictly comparable for all parameters assessed. Cisapride resulted in a significant increase in the gastric emptying of solids (p less than 0.05) compared with placebo; cisapride also tended to increase the postcibal antral motility and normalize the abnormal manometric features in the patients with intestinal dysmotility, particularly the characteristics of fasting interdigestive motor complexes and the fed motor pattern. Both cisapride and placebo groups showed an improvement in total symptom scores and there was no significant difference in overall symptom response between the two groups. However, the change in abdominal pain was greater with cisapride (p = 0.07). Cisapride facilitates gastric emptying in patients with upper gut dysmotility. The overall symptomatic benefit during a 6-wk trial of cisapride, 10 mg t.i.d., was not greater than that of placebo, and dose-response as well as longer term trials are necessary to determine the clinical efficacy of this medication.
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PMID:Effect of six weeks of treatment with cisapride in gastroparesis and intestinal pseudoobstruction. 264 50

Twenty-eight patients with chronic idiopathic dyspepsia defined by the presence of chronic unexplained symptoms suggestive of gastric stasis and directly related to food ingestion were included in this prospective study. Gastric emptying of the liquid and solid phases of a meal was quantified by a dual-isotope method, and symptoms were evaluated by a diary and a visual analog scale. Delay in gastric emptying was evidenced in 59% of the dyspeptic patients; it occurred with liquids in more cases than solids. Quantitative and qualitative evaluation of symptoms was of no practical value in predicting the presence of objective stasis. The dyspeptic patients were included in a double-blind randomized controlled trial of cisapride, a new gastrokinetic drug devoid of central antiemetic effects. After six weeks of cisapride treatment, all patients with initially abnormal gastric emptying rates for liquids, and all but one for solids returned to normal ranges, and significant differences between cisapride and placebo groups were observed for half emptying times of both solids (136 +/- 16 min vs 227 +/- 32 min; P less than 0.02) and liquids (61 +/- 4 min vs 132 +/- 37 min; P less than 0.01). Cisapride also significantly improved dyspeptic symptom scores at weeks 3 and 6 of treatment as compared to those measured before treatment. Nevertheless, the decrease in global diary score was significantly higher than that seen with placebo at week 3 (-16 +/- 6 vs -1 +/- 9; P less than 0.05), but not at week 6 (-18 +/- 5 vs -10 +/- 8).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Symptomatic, radionuclide and therapeutic assessment of chronic idiopathic dyspepsia. A double-blind placebo-controlled evaluation of cisapride. 265 42

In a randomized, double-blind, placebo-controlled study, 32 patients with nonulcer dyspepsia received 5 mg of cisapride or placebo three times daily for four weeks after a two-week run-in phase on placebo. Limited antacid use was allowed. Cisapride was superior to placebo in reducing the intensity of epigastric pain at two weeks (P = 0.03) and four weeks (P = 0.01). At the end of treatment, 82% of the cisapride-treated patients and 43% of the controls had no or only mild pain. Minor, gastrointestinal side effects were observed in two cisapride-treated patients and in one control.
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PMID:Relief of epigastric pain in nonulcer dyspepsia: controlled trial of the promotility drug cisapride. 265 6


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