piperidines and clebopride

Prokinetic agents are drugs that increase contractile force and accelerate intraluminal transit. They are often used in treating disorders of gastrointestinal motility including gastro-oesophageal reflux disease (GERD). The most widely studied agents include bethanechol, metoclopramide, domperidone and cisapride. These drugs act either by enhancing the effect of acetylcholine or by blocking the effect of an inhibitory neurotransmitter such as dopamine. With the exception of cisapride, the clinical efficacy of the various prokinetic agents in treating GERD has not been confirmed consistently. These agents have variable effects on oesophageal and gastric motor function and are fraught with side-effects. They are effective in relieving mild reflux symptoms but do not predictably heal oesophagitis. On the other hand, cisapride is thus far the most effective prokinetic agent studied for the treatment of GERD. It relieves reflux symptoms and promotes healing of grade I-II oesophagitis, with few side-effects or tachyphylaxis. Its most important role may be in the maintenance treatment of GERD either as a single agent or in combination therapy with an H2-antagonist after oesophagitis healing.

Topics: Adult; Benzamides; Bethanechol; Bethanechol Compounds; Child; Cisapride; Erythromycin; Gastroesophageal Reflux; Gastrointestinal Motility; Humans; Infant; Metoclopramide; Piperidines; Receptors, Cholecystokinin; Serotonin Antagonists

The authors describe the gastro-kinetic drugs that act on functional dyspepsia including metoclopramide, domperidone, clebopride cisapride. Moreover, in some forms of non-ulcer dyspepsia it is useful to give sulglicotide, a cytoprotective drug that has been shown to induce marked improvement of clinical symptoms and endoscopic findings.

Topics: Animals; Anti-Ulcer Agents; Antiemetics; Benzamides; Cisapride; Domperidone; Dyspepsia; Humans; Metoclopramide; Piperidines; Serotonin Antagonists; Sialoglycoproteins

The clinical efficacy and the safety of chronic oral administration of cisapride, a new gastrointestinal prokinetic agent, (10 mg tid) and clebopride (0.5 mg tid) was assayed in 48 outpatients affected with functional dyspepsia, in a randomized double-blind study. Each of the drugs induced a significant reduction in dyspeptic symptoms after 2 and 4 weeks (p less than 0.001). Two patients, given clebopride, dropped out of the study because of severe side effects during the first week of treatment. Mild adverse reactions were reported in 6 out of 23 cisapride-treated patients and in 10 out of 20 clebopride-treated patients who completed the study. The most common side effect of cisapride was diarrhoea and that of clebopride was drowsiness. Cisapride appears to be as effective as clebopride in reducing dyspeptic symptoms and seems to induce less severe side effects.

Topics: Administration, Oral; Adolescent; Adult; Aged; Antiemetics; Benzamides; Chronic Disease; Cisapride; Double-Blind Method; Dyspepsia; Female; Humans; Male; Middle Aged; Piperidines; Serotonin Antagonists

A retrospective study is reported carried out on a group of 166 patients affected by dyspeptic syndrome who presented at least 3 of the 9 symptoms which characterise this pathology. One hundred and twenty-eight patients underwent prokinetic drug therapy and 38 received placebo. Clinical parameters were evaluated following one month of therapy all patients in order to compare them to basal values. The results obtained confirm a satisfactory efficacy of the prokinetic treatment in improving dyspeptic symptoms. Although administered to a smaller number of patients, placebo was also found to play an important role in the multifactorial etiopathogenesis of the dyspeptic syndrome on a functional basis.

Topics: Adult; Antiemetics; Benzamides; Cisapride; Domperidone; Dyspepsia; Female; Humans; Male; Metoclopramide; Middle Aged; Piperidines; Retrospective Studies; Serotonin Antagonists

Gastro-esophageal reflux (GER) in infants was studied using 24-hour esophageal pH monitoring. Gastro-esophageal reflux was detected in 32/41 subjects. In our patients the main symptoms were vomiting, regurgitation, failure-to-thrive, chronic respiratory problems such as asthma, apnea, recurrent pneumonia. All patients with GER were treated appropriately with prone positioning and medical therapy (prokinetic agent and, eventually, ranitidine). Successful treatment of the reflux was obtained in all patients. In our opinion the 24-hour intraesophageal pH monitoring is a highly diagnostic test to identify the presence of GER and evaluate its gravity.

Topics: Antiemetics; Benzamides; Child; Child, Preschool; Cisapride; Esophagus; Female; Gastroesophageal Reflux; Humans; Hydrogen-Ion Concentration; Infant; Infant, Newborn; Male; Monitoring, Physiologic; Piperidines; Posture; Serotonin Antagonists; Time Factors

Topics: Animals; Apomorphine; Benzamides; Dopamine Antagonists; Drug Interactions; Metoclopramide; Mice; Piperidines; Sulpiride; Synapses

Metoclopramide and its newly developed analogue clebopride, together with some of their metabolic products are quantitated, following extraction from biological tissues and fluids, and subsequent separation on silica gel thin-layer chromatographic plates. Diazotisation, followed by coupling with N-(1-naphthyl)ethylenediammonium dichloride, carried out on the thin-layer plate, is utilised for visualisation. The intensity of the spots is measured by photodensitometric analysis. The effect of variation of various experimental conditions is studied. The method has proven to be satisfactory for the measurement of 20 ng/ml of these compounds in biological material; the results are well within the accepted limits of deviation.

Topics: Animals; Antiemetics; Benzamides; Chromatography, Thin Layer; Densitometry; Liver; Male; Metoclopramide; Photochemistry; Piperidines; Rabbits