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

Delayed gastric emptying, gastroparesis, is one of the sequelae of diabetes mellitus. Symptoms may include postprandial nausea, epigastric pain, bloating, vomiting, early satiety and unpredictable blood sugar fluctuations. Nowadays diagnosis is made by the measurement of gastric emptying with a radionuclide test meal. Using this technique some 50% of diabetic patients show signs of disordered gastric emptying. Relief is best delivered by agents promoting gastric emptying. In phase II single-dose studies metoclopramide, domperidone, cisapride, erythromycin and renzapride were all able to enhance gastric evacuation of solid and liquid meals in patients with diabetic gastroparesis. A few short term studies support the efficacy of domperidone and renzapride, but long term trials are lacking. Erythromycin, mimicking the potent gastrokinetic effect of motilin, may hold considerable promise for the future. Experience with erythromycin in diabetic gastroparesis is nonetheless very limited. To some extent the therapeutic effectiveness of metoclopramide and cisapride has been established in placebo-controlled trials. In trials with a placebo-controlled crossover design, however, only metoclopramide showed a sustained positive effect. Metoclopramide, which combines gastrokinetic and antiemetic properties seems, so far, the best therapeutic option in diabetic gastroparesis. Cisapride may be considered as a good alternative in cases where limited efficacy or side effects preclude the use of metoclopramide.
 ...
PMID:Diabetic gastroparesis. A critical reappraisal of new treatment strategies. 128 Oct 70

In 16 patients with symptomatic gastroesophageal reflux disease (GERD) 24-h intraesophageal pH monitoring (Medilog 1010, Oxford) was carried out after placebo, cisapride (4 x 5 mg) and cimetidine (3 x 200 mg plus 400 mg at bedtime). The per cent time at which intraesophageal pH < 4.0 (refluxive time) was analysed. Cisapride shortened daytime and postprandial refluxive time from 16.1 +/- 14.5% and 12.6 +/- 9.2% to 5.1 +/- 4.4% and 7.5 +/- 6.5%, respectively (p < 0.01, p < 0.05). Whereas, cimetidine shortened particularly night refluxive time from 24.7 +/- 14.1% to 8.8 +/- 6.9% (p < 0.01) and total time from 20.4 +/- 12.8% to 12.0 +/- 6.4% (p < 0.05).
 ...
PMID:Effect of cisapride and cimetidine on 24-hour intraesophageal pH monitoring in patients with gastroesophageal reflux disease. 130 54

1. In hen colon 5-HT induces a tetrodotoxin-resistant, bumetanide-sensitive, chloride secretion, positively coupled with adenylate cyclase activity. 2. The 5-HT receptor mediating this response seems non-classical since it cannot be blocked by 5-HT1-like, 5-HT2 or 5-HT3 antagonists. 3. Effects are presented of new putative 5-HT agonists and antagonists on short circuit current and cord conductance in the hen colon, using the Ussing chamber technique. 4. The substituted benzamides, cisapride and BRL 24924, induced a dose-dependent short circuit currents but both with less potency than 5-HT. 5. Cisapride mediated this dose-dependent bumetanide sensitive response mainly by release of acetylcholine, since atropine reduced cisapride response by 70%. 6. Neither BRL 24924, 5-HTP-DP, ketanserin, ICS 205-930, prazosin, yohimbine, atropine nor piroxicam, covering the 5-HT1P, 5-HT2P, 5-HT2, 5-HT3, 5-HT4, adrenergic and muscarinic receptor types and the prostaglandin synthesis, altered 5-HT induced increases in short circuit current and cord conductance. 7. Results suggest (a) cisapride mediates it's response mainly by releasing acetylcholine, which then stimulates muscarinic receptors to release 5-HT. (b) Involvement of a non-classical 5-HT receptor subtype in 5-HT induced chloride secretion in hen colon.
 ...
PMID:Involvement of non-classical 5-HT receptor in serotonin and cisapride induced secretion in hen colon. 135 3

The present investigation was undertaken with the aim of evaluating the clinical efficacy on dyspeptic symptoms associated with duodenogastric reflux gastritis of two drugs belonging to two different groups: a prokinetic (cisapride) and a cytoprotective agent (sucralfate). A total of 18 patients with duodenogastric reflux gastritis diagnosed on the basis of symptoms, endoscopy and histology were studied. Nine were given 30 mg of cisapride/daily and 9 4 g of sucralfate/daily for two months according to a randomization list. Pyrosis, epigastric pain, sense of epigastric repletion and foul-tasting mouth were considered on a scale from 0 to 4 attributed by the patient. The total score of dyspeptic symptoms significantly decreased only after cisapride (p less than 0.05). Considering each symptom alone, neither cisapride or sucralfate were able to significantly improve them. Cisapride seems to the better than sucralfate in improving dyspeptic symptoms associated with duodeno-gastric reflux gastritis.
 ...
PMID:[Cisapride and sucralfate in dyspepsia associated with duodenogastric reflux gastritis]. 139 Nov 44

The effects of cisapride, given orally at standard therapeutic dosage (10 mg tds), on proximal small bowel interdigestive motility in ten healthy volunteers was assessed by prolonged ambulatory manometry. Cisapride did not alter the duration of the MMC cycle, duration of phase II or the propagation rate of phase III in either the daytime or nighttime periods. However, when compared to studies, in which subjects received no drug, both nighttime and daytime phase II mean contractile amplitude, but not contractile incidence, were significantly increased (P < or = 0.001) by cisapride. Cisapride significantly increased the incidence of distally propagated clustered activity. We conclude that the major effects of cisapride on healthy small bowel motor function is to increase the mean contractile amplitude and incidence of distally propagated clustered activity.
 ...
PMID:Assessment by prolonged ambulatory manometry of the effect of oral cisapride on proximal small bowel inter-digestive motility. 139 5

Serotonin (5-HT) is a potent contractile agonist in canine coronary artery devoid of endothelium; however, in higher concentrations 5-HT produces concentration-dependent relaxation by activating an as yet uncharacterized receptor. This study explored the possibility that 5-HT-induced relaxation was mediated by interaction with a member of the 5-HT1, 5-HT2, 5-HT3, or 5-HT4 receptor family. 5-HT, 5-carboxamidotryptamine and 5-methoxytryptamine produced concentration-dependent relaxation in vitro in tissues precontracted with prostaglandin F2 alpha (10 microM). The agonist rank order potency for relaxation was 5-carboxamidotryptamine > 5-HT > 5-MeOT. 8-hydroxydipropylaminotetralin (8-OH-DPAT), dipropyl-5-CT, 5-methyltryptamine, sumatriptan, alpha-methyl-5-HT and 2-methyl-5-HT did not produce significant relaxation. The 5-HT1/beta adrenergic receptor antagonist propranolol (1 microM) did not antagonize 5-HT-induced relaxation. 5-HT-induced relaxation was not blocked by tetrodotoxin (0.3 microM), suggesting that neuronal depolarization to release mediators from nerves was not responsible for the relaxation. Neither ketanserin (1 microM) nor ritanserin (1 microM) antagonized 5-HT-induced relaxation, suggesting that 5-HT2 and 5-HT1C receptors do not mediate relaxation. ICS 205-930 (10 microM), a 5-HT3/5-HT4 receptor antagonist, shifted the 5-HT concentration-response curve modestly to the right (pKB = 5.1 +/- 0.1). Cisapride, a 5-HT4 receptor agonist, was not effective either as an agonist (up to 10 microM), or as an antagonist (1 microM) of 5-HT-induced relaxation.(ABSTRACT TRUNCATED AT 250 WORDS)
 ...
PMID:Serotonin-induced relaxation in canine coronary artery smooth muscle. 140 77

The aim of the study was to use a novel combination of two methods for the simultaneous evaluation of two effects of oral cisapride in 10 diabetic patients with autonomic neuropathy; gastric empyting time was measured by following radio-opaque markers and orocaecal transit time by the sulphasalazine-sulphapridine method. The study was of double-blind, randomized, placebo-controlled, cross-over design. It was possible to evaluate the effect of a prokinetic drug on gastric emptying and orocaecal transit times using these two noninvasive techniques at the same time. Cisapride significantly reduced both the gastric empyting (1.2 h versus 2.1 h) and orocaecal tansit (5.9 h versus 7.7 h) times.
 ...
PMID:Simultaneous noninvasive evaluation of gastric emptying and orocaecal transit times. Use in studying the actions of cisapride in diabetic patients. 142 66

Gastroparesis is a frequently unrecognized complication of insulin-dependent diabetes mellitus, which subjects these patients to the risk of aspiration at induction of anaesthesia. The effect of oral cisapride on volume and pH of gastric contents was studied in 24 diabetic and 24 non-diabetic uraemic patients undergoing renal transplantation. All patients were allocated randomly in a double-blind fashion to receive either 10 mg of cisapride or placebo orally approximately 100 min before anaesthesia and three times daily for the first 2 postoperative days. After the induction of anaesthesia, gastric contents were aspirated through a nasogastric tube, and the pH and volume were measured. The emptiness of the stomach was verified by gastroscopy. Gastric volumes exceeding 0.4 ml.kg-1 were observed in 12/24 of the diabetic and 4/24 of the non-diabetic uraemic patients (P < 0.01). The pH of the gastric contents did not differ between the groups, ranging from 1-8 in diabetics and 1-7 in non-diabetics. Cisapride lacked effect on gastric contents and postoperative gastrointestinal motility. Diabetic uraemic patients had larger gastric volumes than their non-diabetic controls at induction of anaesthesia. Cisapride had no effect on gastric emptying preoperatively nor on postoperative bowel function.
 ...
PMID:Increased volume of gastric contents in diabetic patients undergoing renal transplantation: lack of effect with cisapride. 144 79

Two models of transsphincteric flow and a model evaluating pumping activity were established in the anesthetized Australian brush-tailed possum to determine whether the sphincter of Oddi (SO) acts as a resistor or as a pump. A simple model of transsphincteric flow (inflow only) demonstrated that at physiological common bile duct (CBD) pressure, 9.5 +/- 0.3 cmH2O (n = 7), transsphincteric flow occurred between SO pressure waves (n = 10). A second more complex transsphincteric flow model was established that permitted simultaneous measurements of inflow, outflow, CBD pressure, SO basal pressure, SO contraction frequency, and amplitude. At physiological CBD pressure, inflow always equaled outflow (157.0 +/- 11.2 and 156.4 +/- 11.4 microliters/min, respectively; n = 7). The SO displayed regular contractions superimposed on a basal pressure of 1.1 +/- 0.4 mmHg. Contraction amplitude was 12.6 +/- 3.0 mmHg and the frequency was 3.6 +/- 0.4 contractions/min (n = 7). Pressure waves recorded in the CBD corresponded to the SO contractions and reflected SO activity. Transsphincteric flow occurred between SO contractions and was obstructed by these contractions. Stimulation of SO activity (basal pressure and contraction frequency) with intra-arterial injections of motilin (200 ng/kg) or erythromycin (200 micrograms/kg) abolished transsphincteric flow. Reduction in SO contraction frequency to 72.7 +/- 7.2% (P < 0.01, paired t test) after administration of Cisapride (2 mg/kg iv) increased transsphincteric flow to 147.6 +/- 12.3% (n = 7, P < 0.05, paired t test). In six possums, possible SO pumping action was evaluated. A manometer was connected to the CBD, and a second manometer was connected to the duodenum surrounding the papilla.(ABSTRACT TRUNCATED AT 250 WORDS)
 ...
PMID:Sphincter of Oddi regulates flow by acting as a variable resistor to flow. 144 42

The effects of cisapride on the gastrointestinal contractile activity and pharmacokinetics of disopyramide were determined in beagle dogs and patients with arrhythmia. In the animal experiments, the gastric motor index was significantly decreased by i.v. administration of disopyramide in a dose-dependent fashion. The peak decrease of the motor index was observed within 5 min after i.v. injection of disopyramide; the motor index then recovered gradually to the level present prior to drug administration. I.v. administration of cisapride (0.5 mg/kg) markedly increased gastrointestinal contractile activity following the decrease induced by disopyramide pretreatment (5 mg/kg, i.v.). In the clinical studies, the gastric emptying test was performed using the acetaminophen method. A significant correlation between plasma concentrations of disopyramide and gastric emptying time has been found (p < 0.001). The combination of disopyramide (100 mg t.i.d.) and cisapride (2.5 mg t.i.d.) significantly increased gastric emptying compared with that induced by disopyramide alone. The peak plasma concentration of disopyramide in association with cisapride oral administration was significantly higher, and the apparent absorption rate constant and lag time of disopyramide were about 2-fold higher and 2-fold shorter, respectively, than for disopyramide alone. Cisapride, acting as a cholinergic agonist, may counteract the anticholinergic effect of disopyramide on gastric motility. As a factor influencing drug absorption, gastric emptying is of importance, as it determines the rate of drug delivery to the small intestine. Therefore, the oral administration of disopyramide with cisapride may be useful for patients with delayed gastric emptying.
 ...
PMID:Effects of cisapride on gastrointestinal motor activity and gastric emptying of disopyramide. 147 39


1 2 3 4 5 6 7 8 9 10 Next >>