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Chemical Compound Review

Rel-Cisapride     4-amino-5-chloro-N-[(3R,4S)- 1-[3-(4...

Synonyms: CHEMBL74656, AC1NSJW8, SureCN1759279, BSPBio_000420, BPBio1_000462, ...
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Disease relevance of cisapride


Psychiatry related information on cisapride


High impact information on cisapride

  • Generalized sympathetic and vagal dysfunctions influence the response of patients with neuropathic chronic intestinal motility disorder to two doses of cisapride [11].
  • Cisapride induced some changes in motor activity but did not accelerate the recovery of normal motility [12].
  • They were treated with rectal cisapride (30 mg three times daily) or placebo until the clinical resolution of ileus [12].
  • Statistical analysis compared symptom response among treatment and autonomic dysfunction groups and assessed the influence of absence of migrating motor complexes and presence of postprandial antral hypomotility on symptomatic responses to cisapride [11].
  • Cisapride improves gallbladder contractility and bile lipid composition in an animal model of gallstone disease [13].

Chemical compound and disease context of cisapride


Biological context of cisapride

  • Cisapride facilitates gastric emptying in patients with upper gut dysmotility [19].
  • The propulsive efficiency (i.e., number of peristalses and total amount of fluid ejected per unit of time) of isolated segments of ileum was enhanced by cisapride (100 nM to 3 microM) [20].
  • The amplitude of fast nicotinic excitatory postsynaptic potentials recorded from S cells was increased by cisapride in the concentration range of 10 nM to 1 microM [20].
  • Cisapride (10-300 nM) did not affect the membrane potential, resting properties, or active properties of S neurons [20].
  • Cisapride inhibited I(Kr), the major time-dependent outward current elicited by short pulses (I[K250]) to low depolarizing potentials, in a concentration-dependent manner with an IC50 of 15 nmol/L (therapeutic levels, 50 to 200 nmol/L) [21].

Anatomical context of cisapride

  • CONTEXT: Cisapride, a gastrointestinal tract promotility agent, can cause life-threatening cardiac arrhythmias in patients susceptible either because of concurrent use of medications that interfere with cisapride metabolism or prolong the QT interval or because of the presence of other diseases that predispose to such arrhythmias [22].
  • Cisapride renders biliary lipid composition towards normal by enhancing gallbladder (and possibly intestinal) motility and cycling of the bile salt pool, thereby increasing bile salt secretion [13].
  • These data indicate that cisapride facilitates cholinergic transmission in the myenteric plexus of guinea pig ileum and that this effect may be at least partially responsible for the increased propulsive efficiency observed in ileal segments [20].
  • Transiently expressed in COS-7 cells, this receptor stimulates adenylyl cyclase activity and is sensitive to the benzamide derivative cisapride [23].
  • Overall, 112 myocytes were exposed to seven concentrations of cisapride (10 nmol/L to 10 micromol/L) [21].

Associations of cisapride with other chemical compounds


Gene context of cisapride

  • All HERG channels had similar sensitivity to block by cisapride [29].
  • On the other hand, cisapride strongly inhibited CYP3A4 and markedly inhibited CYP2C9 [30].
  • Interaction of cisapride with the human cytochrome P450 system: metabolism and inhibition studies [31].
  • RESULTS: The rate of biotransformation of cisapride was greater by recombinant CYP3A4 than by CYP3A7 (0.77 +/- 0.5 and 0.01 +/- 0.01 nmol metabolites formed in 24 h, respectively), whereas CYP1A1, 1A2, 2C8, 2C9 and 3A5 showed no activity [32].
  • Formation rate of NORCIS from 10 microM cisapride in 14 HLMs was highly variable (range, 4.9-133.6 pmol/min/mg of protein) and significantly correlated with the activities of CYP3A (r = 0.86, P =. 0001), CYP2C19, and 1A2 [31].

Analytical, diagnostic and therapeutic context of cisapride


  1. Cisapride and fatal arrhythmia. Wysowski, D.K., Bacsanyi, J. N. Engl. J. Med. (1996) [Pubmed]
  2. A comparison of five maintenance therapies for reflux esophagitis. Vigneri, S., Termini, R., Leandro, G., Badalamenti, S., Pantalena, M., Savarino, V., Di Mario, F., Battaglia, G., Mela, G.S., Pilotto, A. N. Engl. J. Med. (1995) [Pubmed]
  3. Coprescribing and codispensing of cisapride and contraindicated drugs. Jones, J.K., Fife, D., Curkendall, S., Goehring, E., Guo, J.J., Shannon, M. JAMA (2001) [Pubmed]
  4. Cisapride in postoperative gastroparesis. Cullen, P.T., Campbell, F.C. Lancet (1987) [Pubmed]
  5. Impaired transit of chyme in chronic intestinal pseudoobstruction. Correction by cisapride. Camilleri, M., Brown, M.L., Malagelada, J.R. Gastroenterology (1986) [Pubmed]
  6. Effects of cisapride on jejunal motor activity in fasting healthy humans. Stacher, G., Steinringer, H., Schneider, C., Winklehner, S., Mittelbach, G., Gaupmann, G. Gastroenterology (1986) [Pubmed]
  7. Intravenous cisapride accelerates delayed gastric emptying and increases antral contraction amplitude in patients with primary anorexia nervosa. Stacher, G., Bergmann, H., Wiesnagrotzki, S., Kiss, A., Schneider, C., Mittelbach, G., Gaupmann, G., Höbart, J. Gastroenterology (1987) [Pubmed]
  8. Absent postprandial duodenal motility in a child with cystic fibrosis. Correction of the symptoms and manometric abnormality with cisapride. Hyman, P.E. Gastroenterology (1986) [Pubmed]
  9. Gastrointestinal motility disorders in scleroderma. Sjogren, R.W. Arthritis Rheum. (1994) [Pubmed]
  10. Cisapride for the treatment of constipation in children: A double-blind study. Nurko, S., Garcia-Aranda, J.A., Worona, L.B., Zlochisty, O. J. Pediatr. (2000) [Pubmed]
  11. Determinants of response to a prokinetic agent in neuropathic chronic intestinal motility disorder. Camilleri, M., Balm, R.K., Zinsmeister, A.R. Gastroenterology (1994) [Pubmed]
  12. Small bowel motility following major intra-abdominal surgery: the effects of opiates and rectal cisapride. Benson, M.J., Roberts, J.P., Wingate, D.L., Rogers, J., Deeks, J.J., Castillo, F.D., Williams, N.S. Gastroenterology (1994) [Pubmed]
  13. Cisapride improves gallbladder contractility and bile lipid composition in an animal model of gallstone disease. Xu, Q.W., Shaffer, E.A. Gastroenterology (1993) [Pubmed]
  14. Overexpression of serotonin4 receptors in cisapride-responsive adrenocorticotropin-independent bilateral macronodular adrenal hyperplasia causing Cushing's syndrome. Cartier, D., Lihrmann, I., Parmentier, F., Bastard, C., Bertherat, J., Caron, P., Kuhn, J.M., Lacroix, A., Tabarin, A., Young, J., Vaudry, H., Lefebvre, H. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
  15. Small bowel motility affects glucose absorption in a healthy man. Schwartz, M.P., Samsom, M., Renooij, W., van Steenderen, L.W., Benninga, M.A., van Geenen, E.J., van Herwaarden, M.A., de Smet, M.B., Smout, A.J. Diabetes Care (2002) [Pubmed]
  16. Clinical pharmacokinetics of drugs used in the treatment of gastrointestinal diseases (Part I). Lauritsen, K., Laursen, L.S., Rask-Madsen, J. Clinical pharmacokinetics. (1990) [Pubmed]
  17. A comparative study of cisapride and ranitidine at controlling oesophageal acid exposure in erosive oesophagitis. Pouderoux, P., Kahrilas, P.J. Aliment. Pharmacol. Ther. (1995) [Pubmed]
  18. Domperidone is more effective than cisapride in children with diabetic gastroparesis. Franzese, A., Borrelli, O., Corrado, G., Rea, P., Di Nardo, G., Grandinetti, A.L., Dito, L., Cucchiara, S. Aliment. Pharmacol. Ther. (2002) [Pubmed]
  19. Effect of six weeks of treatment with cisapride in gastroparesis and intestinal pseudoobstruction. Camilleri, M., Malagelada, J.R., Abell, T.L., Brown, M.L., Hench, V., Zinsmeister, A.R. Gastroenterology (1989) [Pubmed]
  20. Effects of cisapride on cholinergic neurotransmission and propulsive motility in the guinea pig ileum. Tonini, M., Galligan, J.J., North, R.A. Gastroenterology (1989) [Pubmed]
  21. Block of the rapid component of the delayed rectifier potassium current by the prokinetic agent cisapride underlies drug-related lengthening of the QT interval. Drolet, B., Khalifa, M., Daleau, P., Hamelin, B.A., Turgeon, J. Circulation (1998) [Pubmed]
  22. Contraindicated use of cisapride: impact of food and drug administration regulatory action. Smalley, W., Shatin, D., Wysowski, D.K., Gurwitz, J., Andrade, S.E., Goodman, M., Chan, K.A., Platt, R., Schech, S.D., Ray, W.A. JAMA (2000) [Pubmed]
  23. The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants. Gerald, C., Adham, N., Kao, H.T., Olsen, M.A., Laz, T.M., Schechter, L.E., Bard, J.A., Vaysse, P.J., Hartig, P.R., Branchek, T.A. EMBO J. (1995) [Pubmed]
  24. Effect of cisapride on gastric emptying of indigestible solids in patients with gastroparesis diabeticorum. A comparison with metoclopramide and placebo. Feldman, M., Smith, H.J. Gastroenterology (1987) [Pubmed]
  25. Effect of different prokinetic agents and a novel enterokinetic agent on postoperative ileus in rats. De Winter, B.Y., Boeckxstaens, G.E., De Man, J.G., Moreels, T.G., Schuurkes, J.A., Peeters, T.L., Herman, A.G., Pelckmans, P.A. Gut (1999) [Pubmed]
  26. Inhibition of the effect of serotonin on rat ileal transport by cisapride: evidence in favour of the involvement of 5-HT2 receptors. Moriarty, K.J., Higgs, N.B., Woodford, M., Warhurst, G., Turnberg, L.A. Gut (1987) [Pubmed]
  27. Effects of ranitidine and cisapride on acid reflux and oesophageal motility in patients with reflux oesophagitis: a 24 hour ambulatory combined pH and manometry study. Inauen, W., Emde, C., Weber, B., Armstrong, D., Bettschen, H.U., Huber, T., Scheurer, U., Blum, A.L., Halter, F., Merki, H.S. Gut (1993) [Pubmed]
  28. Effects of a serotonin 5-HT(4) receptor antagonist SB-207266 on gastrointestinal motor and sensory function in humans. Bharucha, A.E., Camilleri, M., Haydock, S., Ferber, I., Burton, D., Cooper, S., Tompson, D., Fitzpatrick, K., Higgins, R., Zinsmeister, A.R. Gut (2000) [Pubmed]
  29. Molecular and functional characterization of common polymorphisms in HERG (KCNH2) potassium channels. Anson, B.D., Ackerman, M.J., Tester, D.J., Will, M.L., Delisle, B.P., Anderson, C.L., January, C.T. Am. J. Physiol. Heart Circ. Physiol. (2004) [Pubmed]
  30. Drug-drug interactions of Z-338, a novel gastroprokinetic agent, with terfenadine, comparison with cisapride, and involvement of UGT1A9 and 1A8 in the human metabolism of Z-338. Furuta, S., Kamada, E., Omata, T., Sugimoto, T., Kawabata, Y., Yonezawa, K., Wu, X.C., Kurimoto, T. Eur. J. Pharmacol. (2004) [Pubmed]
  31. Interaction of cisapride with the human cytochrome P450 system: metabolism and inhibition studies. Desta, Z., Soukhova, N., Mahal, S.K., Flockhart, D.A. Drug Metab. Dispos. (2000) [Pubmed]
  32. Evidence of impaired cisapride metabolism in neonates. Tréluyer, J.M., Rey, E., Sonnier, M., Pons, G., Cresteil, T. British journal of clinical pharmacology. (2001) [Pubmed]
  33. Measurement of gastric emptying in dyspeptic patients: effect of a new gastrokinetic agent (cisapride). Jian, R., Ducrot, F., Piedeloup, C., Mary, J.Y., Najean, Y., Bernier, J.J. Gut (1985) [Pubmed]
  34. Effect of cisapride on the gastrointestinal transit of a solid meal in normal human subjects. Edwards, C.A., Holden, S., Brown, C., Read, N.W. Gut (1987) [Pubmed]
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