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)

Chronic intestinal pseudo-obstruction is defined as a syndrome related to any process which affects intestinal regulation and propulsion. Its origin may be muscular, neurogenic or hormonal, excluding Hirschsprung's disease or any known mechanical obstruction. Between 1989 and 1991, 11 patients with intestinal pseudo-obstruction were studied at our centre, and included nine hyperganglionisms B, and two hypoganglionisms) and two visceral myopathies (Berdon's syndrome). Diagnosis was established in all cases by histologic study. The techniques of haematoxylin-eosin, acetylcholinesterase, enolase, protein S-100 and Smith were used in neuropathies and haematoxylin-eosin and Masson's trichromic in myopathies. Intestinal motility was studied by ano-rectal and gastrointestinal manometry in seven and three cases respectively. Gastrointestinal manometry and radiology permitted differentiation of localized and diffuse forms of involvement. Medical treatment consisted of total parenteral nutrition when oral feeding was impossible, and in five cases, cisapride was given, with good results in four. Derivative surgery was performed in cases of diffuse involvement, and resection with anastomosis in those of localized forms. We conclude that: 1. Diagnosis is established according to histologic criteria. 2. Complementary examinations should be directed towards distinguishing localized from diffuse involvement. 3. Cisapride was effective in the treatment of neuropathies in the majority of cases.
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PMID:[Intestinal dysmotility-pseudo-obstruction]. 150 66

The effects of Cisapride on gastric outflow/pressure relationships have been examined in conscious dogs. In the digestive state, after inhibition of emptying in the first 10 min, Cisapride accelerated gastric emptying for 110 min by increasing the volume (7.3 +/- 1.2 vs. 2.3 +/- 0.3 ml) rather than by decreasing the interval between flow pulses (4.9 +/- 0.2 vs. 4.5 +/- 0.1s). After non-nutrient gastric loading, Cisapride also first inhibited and then accelerated gastric emptying as the consequence of both a larger stroke volume (8.0 +/- 1.7 vs. 3.2 +/- 0.5 ml) and more frequent pulses (3.9 +/- 0.1 vs. 4.9 +/- 0.1 s). In both situations, Cisapride increased the amplitude of the antral/pyloric pressure waves. Antropyloroduodenal resistance increased substantially in the first 10 min after Cisapride then recovered to its control value. We conclude that stimulation of antropyloroduodenal motility by Cisapride can both impede and increase gastric emptying by changes in antroduodenal resistance.
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PMID:Changes in antroduodenal resistance induced by Cisapride in conscious dogs. 151 31

Cisapride, a prokinetic drug with a novel mechanism of action, was compared with another prokinetic drug, metoclopramide, and an H2-blocker, ranitidine, in the treatment of nonulcer dyspepsia. In a double-blind study, 60 patients with severe dyspeptic symptoms received cisapride 5 mg TID, metoclopramide 10 mg TID, or ranitidine 150 mg BID for 8 weeks. Symptoms were evaluated during treatment and 4 weeks after the end of therapy. All three drugs effectively controlled the symptoms of chronic functional upper gastrointestinal tract disorders. The prokinetic drugs, particularly cisapride, were significantly better than ranitidine in controlling symptoms, especially reflux symptoms. All three drugs were generally well tolerated; cisapride in particular was associated with fewer adverse effects.
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PMID:Cisapride, metoclopramide, and ranitidine in the treatment of severe nonulcer dyspepsia. 152 89

It has been suggested that benzamides, like cisapride, exert their effects on the guinea-pig ileum via activation of a 5-HT receptor (5-HT4 receptor?) mechanism. The aim of this study was to determine whether an how the 5-HT4 receptor (previously described in mouse colliculi neurones) is involved in the cisapride-induced effect. The effects induced by cisapride were compared with those of 5-hydroxytryptamine (5-HT) and 5-methoxytryptamine (5-MeOT) either alone or in the presence of a 5-HT4 antagonist (micromolar concentration of ICS 205-930) or a benzamide antagonist (R 50 595). As a model we used the electrically stimulated longitudinal muscle myenteric plexus preparation from the guinea-pig ileum. Cisapride (3.10(-7) M), 5-HT and a 5-HT4 receptor agonist 5-MeOT (3.10(-10)-10(-6) M) induced similar effects, i.e. enhancement of the twitch responses. After rinsing the organ baths, a second addition of the agonists resulted in a similar response. The studied agonists showed mutual desensitization. Cisapride desensitized the response induced by 5-HT or 5-MeOT, and 5-MeOT or 5-HT desensitized the effect induced by cisapride. In preparations preincubated with a 5-HT4 receptor antagonist, ICS 205-930- (3.10(-6) M) or R 50 595 (3.10(-7) M), a benzamide with a specific antagonistic action on the effect induced by 5-HT and benzamides on the guinea-pig ileum, the effects induced by cisapride, 5-HT and 5-MeOT were abolished. These results indicate that cisapride indeed exerts its effect via an agonistic action on a serotonin receptor, probably the previously described 5-HT4 receptor.
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PMID:Is the action of cisapride on the guinea-pig ileum mediated via 5-HT4 receptors? 155 39

The article is a short review of older and more recent drugs aimed to modify the gastrointestinal motility. Cisapride the newer one is considered with particular attention.
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PMID:[Drugs affecting upper respiratory tract motility: cisapride]. 158 33

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.
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PMID:[Medicamentous modification of gastrointestinal motility and secretion]. 164 90

The effects of cisapride on guinea pig gastric smooth muscle were characterized. Cisapride induced concentration-dependent contraction of isolated myocytes with an EC50 of 10(-11) M, which was antagonized in concentration-dependent fashion by atropine. 4-Diphenylacetoxy-N-methylpiperidine-methiodide (4-DAMP) (10(-6) M), a selective M2 glandular receptor antagonist, inhibited contraction to cisapride (10(-10) M), whereas pirenzepine, an M1 receptor antagonist, had no effect. For comparison, carbachol induced contraction with an EC50 of 5 x 10(-11) M, which was also atropine-sensitive. Cisapride-induced contraction was not blocked by methysergide (10(-6) M), a nonselective serotonin antagonist. Cisapride displaced specific binding of [3H]N-methylscopolamine at a single receptor population with a Ki of 6.51 x 10(-5) M and a Bmax of 351.0 fmol/mg protein. Cisapride (10(-6) M) evoked a 73.8 +/- 7.6% increase in inositol 1,4,5-trisphosphate at 30 sec and a maximal increase of greater than 130% at 2 min, which was significantly reduced by atropine (10(-6) M). In contrast, cisapride did not enhance or inhibit basal levels of cyclic AMP. Thus, cisapride induces contraction via specific interaction at smooth muscle M2 glandular muscarinic receptors, which is associated with inositol trisphosphate generation, but not adenylyl cyclase activation.
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PMID:Cisapride acts on muscarinic (glandular M2) receptors to induce contraction of isolated gastric myocytes: mediation via a calcium-phosphoinositide pathway. 166 75

Cisapride (Ci) stimulates lower esophageal sphincter pressure (LESP). This study aims to test whether the effect of Ci on LES in vivo is still present if LES is relaxed by atropine (Atr) and nifedipine (Nife) prior to the administration of Ci. LESP was continuously recorded by manometry in 6 mongrel dogs with esophageal fistulae. Ci was given as an intravenous bolus following either Atr (40 micrograms/kg i.v.) or Nife (20 mg subl.) at the time of maximal LESP decrease (5/15 min later). Basal LES values ranged between 24.5 +/- 2.5 mm Hg (Atr group) and 23.8 +/- 3.9 mm Hg (Nife group). Following Atr, LESP decreased to a minimal value of 7.0 +/- 0.5 mm Hg; after Nife LESP decreased to a minimal value of 12.3 +/- 2.0 mm Hg. Additional administration of Ci was not able to reincrease LESP. We conclude that the action of Ci on LES cannot take place if (1) muscarinergic receptors are blocked by Atr and (2) the Ca2+ activation system is blocked by Nife. Our results suggest that the action of cisapride on LES, as its action on gastrointestinal smooth muscle cells, is mediated by postsynaptic enhancement of acetylcholine release.
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PMID:Cisapride effects on canine lower esophageal sphincter under various pharmacological pretreatments. 166 43

The placental transfer of cisapride, a new prokinetic agent, was studied in a sheep model. The pharmacokinetics of cisapride were studied in the lamb, the pregnant ewe, and the fetus by obtaining blood samples from chronically implanted arterial catheters. Comparable pharmacokinetic parameters were found in the lamb and the adult sheep: half-life, 1.39-1.83 hr; total plasma clearance, 1998-2160 ml/kg/hr; AUC, 92.6-100.1 ng.hr/ml. Cisapride plasma concentrations after continuous infusion were predicted correctly based on the parameters obtained after iv bolus. There was a materno-fetal transfer of cisapride following a single iv bolus administered to the mother. Cisapride crossed the placenta within 5 min and equilibrated with maternal plasma within 20 to 30 min after dosing. The average fetal-to-maternal plasma concentration ratio was 0.71. The amniotic fluid also contained measurable amounts of cisapride. The protein binding of cisapride in maternal and fetal plasma is 89.0% and 88.4%, respectively; the free fraction is 4 times larger than in humans. Cisapride crosses the ovine placental barrier. The sheep placenta is less permeable than the human placenta, but the higher free fraction of cisapride facilitates placental transfer.
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PMID:Study of the placental transfer of cisapride in sheep. Plasma levels in the pregnant ewe, the fetus, and the lamb. 167 93

We investigated the effect of cisapride 20 mg given orally with MST 20 mg on the absorption of morphine in a double-blind, placebo-controlled study. Cisapride increased significantly both plasma concentrations of morphine after 1 h and peak concentrations. There was no significant change in time to peak concentrations, sedation scores or percentage decrease in pupil diameters. Plasma concentrations of amylase were increased in three patients in the MST-placebo group and three in the MST-cisapride group. One patient in the MST-cisapride group developed acute pancreatitis.
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PMID:Effect of cisapride on morphine absorption after oral administration of sustained-release morphine. 171 64


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