Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Anti-cholinesterase activity of dopamine D2 receptor antagonist, domperidone was studied by means of chronically implanted force transducers in the gastrointestinal (GI) tract in five conscious dogs. Cisapride was used as a drug to stimulate endogenous release of acetylcholine. In the digestive state, cisapride (0.25 mg/kg) stimulated 18.6 +/- 5.6% increase in the motor index of the gastric antrum alone, however, combined administration with domperidone (1.0 mg/kg-hr) significantly enhanced the motor index in the gastric antrum and duodenum. In the gastric antrum, the increase was 68.1 +/- 7.2%. During the interdigestive state, cisapride did not always induce the interdigestive migrating contractions (IMC)-like contractions in the GI tract, but the background infusion of domperidone significantly increased the incidence of the occurrence of IMC-like contractions by cisapride. In in vitro study, weak but significant anti-cholinesterase activity was found in domperidone, the activity being about 1/1,000 of that of neostigmine. In dog experiment, similar enhancement of motor stimulating activity of cisapride was observed when neostigmine was given at 1.0 micrograms/kg-hr. In conclusion, domperidone has anti-cholinesterase activity and acts to enhance motor stimulating activity of cisapride through inhibition of cholinesterase activity in the upper digestive tract.
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PMID:[Anti-cholinesterase activity of dopamine D2 receptor antagonist: its clinical significance]. 257 86

Dyspepsia is a common symptom frequently encountered in general practice. Functional dyspepsia is an exclusion diagnosis after an organic cause has been ruled out, and is a defined entity which can be subdivised in two different subtypes based on the cluster of symptoms, namely epigastric pain and postprandial distress syndromes. The term gastroparesis is used when persistently and severly delayed gastric emptying is found in the absence of mechanical obstruction. Helicobacter pylori infection should be treated, although symptomatic benefice is small. Proton pumps inhibitors offer a clinical benefit in epigastric pain syndrome, whereas prokinetics are probably useful in postprandial distress syndrome. Cisapride has been withdrawn last year due to the risk of potential severe cardiac arrythmies. Domperidone is safer, although caution has to be paid in long-term use because of potential ventricular arrythmies. Dietary advice and psychological therapies might be a useful adjunct. There are difficulties with new treatment development for functional dyspepsia, due to pathophysiological heterogeneity, lack of well-accepted endpoints, a huge placebo effect, and unconfirmed results in large clinical studies after early positive results for promising drugs. Acotiamide, a new cholinesterase inhibitor improving dyspeptic symptoms is not yet available in Europe.
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PMID:[Management of gastroparesis and functional dyspepsia after cisapride withdrawal]. 2309 51