Identification of the human cytochrome P450 (P450) enzymes involved in the metabolism of cisapride and racemic norcisapride [(+/-)-norcisapride] was investigated at 0.1 and 1 microM, concentrations that span the mean plasma C(max) for cisapride. Formation of norcisapride (Nor), 3-fluoro-4-hydroxycisapride (3F), and 4-fluoro-2-hydroxycisapride (4F) from cisapride and an uncharacterized metabolit...

BACKGROUND Lengthening of the QT interval and torsades de pointes resulting in cardiac arrests and deaths have been noticed during treatment with cisapride, a newly developed gastrointestinal prokinetic agent. The rapid (I[Kr]) and slow (I[Ks]) components of the delayed rectifier current (I[K]) are candidate ionic currents to explain cisapride-related toxicity because of their role in repolariz...

BACKGROUND Cisapride, a gastrointestinal prokinetic agent, was recently withdrawn from the market because of its propensity to induce torsade de pointes (TdP) arrhythmias. The present study examines the electrophysiological actions of cisapride in the isolated arterially perfused canine left ventricular wedge preparation. METHODS AND RESULTS Transmembrane action potentials from epicardial and...

Background—Cisapride, a gastrointestinal prokinetic agent, was recently withdrawn from the market because of its propensity to induce torsade de pointes (TdP) arrhythmias. The present study examines the electrophysiological actions of cisapride in the isolated arterially perfused canine left ventricular wedge preparation. Methods and Results—Transmembrane action potentials from epicardial and M...

OBJECTIVE To evaluate the comparative efficacy of enteral cisapride, metoclopramide, erythromycin, and placebo for promoting gastric emptying in critically ill patients with intolerance to gastric enteral nutrition (EN). DESIGN A randomized, crossover study. SETTING Adult medical intensive care unit at a university-affiliated private hospital and trauma intensive care unit at a university t...

Aim—To determine the eVect of cisapride on gastrointestinal motility in preterm infants. Methods—Cisapride (0.2 mg/kg, 8 hourly ) or placebo was given first for seven days in a double blind randomised crossover study of 10 preterm infants. Gastrointestinal motility was assessed on day 3 of each treatment. The half gastric emptying time (GET1⁄2) was determined by using ultrasonography to measure...

The goals of the present study were to identify the enzyme responsible for metabolism of itopride hydrochloride (itopride) and to evaluate the likelihood of drug interaction involving itopride. In human liver microsomes, the involvement of flavin-containing monooxygenase in N-oxygenation, the major metabolic pathway of itopride, was indicated by the following results: inhibition by methimazole ...

OBJECTIVE We prospectively studied the effect of cisapride per se on QT interval in young infants (3-6 months) with gastroesophageal reflux (GER) in a controlled setting. STUDY DESIGN The infants diagnosed with GER and deemed to require therapy with cisapride were divided into 2 groups. Group A comprised infants with GER who underwent an electrocardiogram (ECG) before initiation of therapy wi...

drug-containing suspension and/or solution. They are useful in preparing pellets with a uniform drug content as well as for producing a modified release solid oral dosage form. Even though a variety of polymeric coating techniques have been developed, one popular method relies on the use of a fluidized bed coater. Several studies have focused on the critical process variables as well as their e...

Some patients with gastro-oesophageal reflux disease have delayed gastric emptying. This study investigates the effect of cisapride on gastric emptying in 34 patients with proved reflux and delayed gastric emptying of solids. They were enrolled in a double blind controlled crossover study. Placebo or cisapride (10 mg) tablets were given three times a day for three days followed by further asses...