Using human liver microsomes (HLMs) and recombinant cytochrome P450s (CYP450s), we characterized the CYP450 isoforms involved in the primary metabolic pathways of cisapride and documented the ability of cisapride to inhibit the CYP450 system. In HLMs, cisapride was N-dealkylated to norcisapride (NORCIS) and hydroxylated to 3-fluoro-4-hydroxycisapride (3-F-4-OHCIS) and to 4-fluoro-2-hydroxycisap...

We investigated the effect of cisapride, a gastroprokinetic agent, on the obstructed gastric mucosal hemodynamics induced by indomethacin using an organ reflectance spectrophotometry system in rats. Indomethacin (10 mg/kg, i.v.) reduced both the gastric mucosal blood volume and the gastric mucosal blood oxygenation. Pretreatment with cisapride (0.1 mg/kg, i.v.) prevented these deteriorations. T...

Recent reports of torsade de pointes and heart block associated with prolonged QT interval in children receiving cisapride raise questions about its safety. We prospectively examined the effects of cisapride on the QT interval in children. Electrocardiography was performed on 30 children before and after cisapride was administered. An additional 71 children underwent electrocardiography only af...

OBJECTIVE: To determine the effect of the prokinetic agent cisapride in the prevention of aspiration of gastric contents. DESIGN: A prospective randomized two-period crossover study. SETTING: Fourteen-bed polyvalent intensive care unit in a University Hospital. PATIENTS: Eighteen intubated, mechanically ventilated patients who were seated in a semirecumbent position were studied. METHOD: Tc-99 ...

The effect of cisapride (20 mg bid), a new prokinetic drug, on bowel habits and laxative consumption was studied in patients with idiopathic painless constipation and chronic laxative intake. After a four week base line period, spontaneous defection (frequency without laxative intake) and total defecation (total frequency) were measured. Patients with a spontaneous defecation of less than three...

Cisapride is a newly developed substance that stimulates gastrointestinal motility, possibly enhancing acetylcholine release in the gut wall. The aim of our study was to investigate the effect of cisapride on oesophageal motor function in man. In a blind fashion and in random order six healthy volunteers received cisapride (0.5 mg/h intravenously, preceded by a three day oral loading at 10 mg t...

BACKGROUND Cisapride administration for 48 hours has been shown to increase heart rate corrected QT (QTc) interval in preterm neonates. Accumulation of the drug because of liver enzyme immaturity has been suggested to be the reason. If this is correct, a longer survey of QTc interval should disclose an increase even in term neonates. OBJECTIVE A prospective survey of the effects of cisapride ...

The effect of the new prokinetic drug cisapride on the resting lower oesophageal sphincter pressure and on the strength of peristaltic contractions was studied in 10 healthy controls and in 10 reflux patients with abnormally low (less than 10 mm Hg) basal lower oesophageal sphincter pressure. A slow intravenous injection of cisapride 10 mg significantly increased the sphincter pressure in the c...

BACKGROUND Peritoneal ventilation has been shown to be effective in achieving extrapulmonary oxygenation and carbon dioxide elimination in an animal model of severe adult respiratory distress syndrome (ARDS). Cisapride is a "prokinetic" agent (increases gastric emptying), that may increase the splanchnic circulation and thus favourably affect gas exchange in peritoneal ventilation. METHODS Us...

Agonists of the serotonin 5-hydroxytryptamine 4 (5-HT4) receptor are widely used to activate motility in the gastrointestinal tract. Among these, cisapride was recently withdrawn from the U.S. market because of its proarrhythmic effects. Cisapride is a potent blocker of human ether-à-gogo (HERG) K(+) channels and prolongs the cardiac action potential in a reverse use dependence manner. We compa...