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Chemical Compound Review

loperamide     4-[4-(4-chlorophenyl)-4- hydroxy-1...

Synonyms: Loperacap, Ioperamide, Loperamida, Loperamidum, Diarr-Eze, ...
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Disease relevance of loperamide


Psychiatry related information on loperamide


High impact information on loperamide

  • A single dose of sulfamethoxazole-trimethoprim was also efficacious (28 vs 59 hours), but loperamide alone was significantly effective only when treatment failures were treated with antibiotics (33 vs 58 hours) [8].
  • Subjects treated with the combination had the shortest average duration of diarrhea compared with the placebo group (1 hour vs 59 hours), took the least amount of loperamide after the loading dose (3.8 mg), and had the shortest duration of diarrhea associated with fecal leukocytes or blood-tinged stools (4.5 hours) [8].
  • A pilot toxicity study with oral loperamide showed that this peripherally acting antidiarrheal agent gains potent opiatelike activity in the central nervous system of mdr1a (-/-) mice. mdr1a (-/-) mice also showed increased sensitivity to neurolepticlike side effects of oral domperidone [9].
  • Tissue distribution studies demonstrated that the relative brain penetration of radiolabeled ondansetron and loperamide (and their metabolites) is increased four- and sevenfold, respectively, in mdr1a (-/-) mice [9].
  • Secretagogue-induced changes in membrane calcium permeability in chicken and chinchilla ileal mucosa. Selective inhibition by loperamide [10].

Chemical compound and disease context of loperamide


Biological context of loperamide

  • When loperamide-pretreated vesicles were incubated with 2 microM calcium (free concentration) plus 5 microM calmodulin for 1 h at 5 degrees C, complete inhibition of the stimulatory effect of loperamide on Cl-/OH- antiport and Na+/Cl- cotransport was observed [16].
  • After application of loperamide (12 mg), cyclically recurring migrating motor complexes in the small intestine occurred at a significantly higher frequency than after application of placebo [5].
  • The area under the gastric emptying curve, a potentially more sensitive parameter for measuring gastric emptying, was significantly increased in the group receiving 12 and 18 mg of lidamidine (p less than 0.05) compared with the group receiving loperamide or placebo [17].
  • Loperamide is a well-established antidiarrhoeal agent with effects on gastrointestinal motility [18].
  • Average AUC of diarrhoea (1.9 v 4.5; p=0.09) and average number of loperamide tablets taken (0.4 v 2.6; p=0.002) were reduced in the glutamine arm [19].

Anatomical context of loperamide


Associations of loperamide with other chemical compounds


Gene context of loperamide

  • We investigated the modulation of the central nervous effects of loperamide resulting from ABCB1 genetic variants [27].
  • Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC(50) = 0.44 mM) [28].
  • Loperamide (10 micromol/l for 24 h) reversed the inhibition of insulin-stimulated 2-DG uptake by TNFalpha in a manner sensitive to blockade of opioid mu-receptors [29].
  • OBJECTIVE: The purpose of the present study was to elucidate the cytochrome P450 (P450) isoform(s) involved in the metabolism of loperamide (LOP) to N-demethylated LOP (DLOP) in human liver microsomes [30].
  • LVP increased ACTH levels after both loperamide (from 48 +/- 17.3 to a peak of 95 +/- 21 pmol/l) and placebo (from 231 +/- 59.5 to 365 +/- 86.6 pmol/l): the interaction between treatments and time was not significant [31].

Analytical, diagnostic and therapeutic context of loperamide

  • Loperamide also had no effect during steady-state perfusion when absorption rates were reduced by intravenous infusion of vasoactive intestinal polypeptide [32].
  • Management of radiation-induced diarrhea is similar but may not require hospitalization, and chronic low- to intermediate-grade symptoms can be managed with continued loperamide [33].
  • We examined the effect of two drugs, codeine phosphate and loperamide, on upper intestinal transit and carbohydrate absorption, measured non-invasively by serial exhaled breath hydrogen monitoring, in patients with postvagotomy diarrhoea who had previously failed to gain relief from drug therapy [34].
  • Each subject underwent tests during the administration of placebo, loperamide (12-16 mg po), naloxone (40 micrograms/kg/h by a three-hour intravenous infusion), and loperamide plus naloxone, carried out at intervals of one or two weeks [26].
  • In study II, as in study I, unlike loperamide and placebo, codeine induced pupillary constriction [35].


  1. Comparison of loperamide with bismuth subsalicylate for the treatment of acute travelers' diarrhea. Johnson, P.C., Ericsson, C.D., DuPont, H.L., Morgan, D.R., Bitsura, J.A., Wood, L.V. JAMA (1986) [Pubmed]
  2. Loperamide to diagnose Cushing's syndrome. Ambrosi, B., Bochicchio, D., Colombo, P., Fadin, C., Faglia, G. JAMA (1993) [Pubmed]
  3. Toxic megacolon associated with loperamide therapy. Brown, J.W. JAMA (1979) [Pubmed]
  4. Irinotecan (CPT-11) high-dose escalation using intensive high-dose loperamide to control diarrhea. Abigerges, D., Armand, J.P., Chabot, G.G., Da Costa, L., Fadel, E., Cote, C., Hérait, P., Gandia, D. J. Natl. Cancer Inst. (1994) [Pubmed]
  5. Human intestinal motor activity and transport: effects of a synthetic opiate. Kachel, G., Ruppin, H., Hagel, J., Barina, W., Meinhardt, M., Domschke, W. Gastroenterology (1986) [Pubmed]
  6. Loperamide improves anal sphincter function and continence after restorative proctocolectomy. Hallgren, T., Fasth, S., Delbro, D.S., Nordgren, S., Oresland, T., Hultén, L. Dig. Dis. Sci. (1994) [Pubmed]
  7. Misuse of loperamide in anxiety disorder patients. Lavin, M.R. Depression and anxiety. (1996) [Pubmed]
  8. Treatment of traveler's diarrhea with sulfamethoxazole and trimethoprim and loperamide. Ericsson, C.D., DuPont, H.L., Mathewson, J.J., West, M.S., Johnson, P.C., Bitsura, J.A. JAMA (1990) [Pubmed]
  9. P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. Schinkel, A.H., Wagenaar, E., Mol, C.A., van Deemter, L. J. Clin. Invest. (1996) [Pubmed]
  10. Secretagogue-induced changes in membrane calcium permeability in chicken and chinchilla ileal mucosa. Selective inhibition by loperamide. Chang, E.B., Brown, D.R., Wang, N.S., Field, M. J. Clin. Invest. (1986) [Pubmed]
  11. Ciprofloxacin and loperamide in the treatment of bacillary dysentery. Murphy, G.S., Bodhidatta, L., Echeverria, P., Tansuphaswadikul, S., Hoge, C.W., Imlarp, S., Tamura, K. Ann. Intern. Med. (1993) [Pubmed]
  12. Intestinal transit, deoxycholic acid and the cholesterol saturation of bile--three inter-related factors. Marcus, S.N., Heaton, K.W. Gut (1986) [Pubmed]
  13. Inhibition of postprandial pancreatic and biliary secretion by loperamide in patients with short bowel syndrome. Remington, M., Fleming, C.R., Malagelada, J.R. Gut (1982) [Pubmed]
  14. Increased drug delivery to the brain by P-glycoprotein inhibition. Sadeque, A.J., Wandel, C., He, H., Shah, S., Wood, A.J. Clin. Pharmacol. Ther. (2000) [Pubmed]
  15. Effects of loperamide on the human hypothalamo-pituitary-adrenal axis in vivo and in vitro. Auernhammer, C.J., Stalla, G.K., Lange, M., Pfeiffer, A., Müller, O.A. J. Clin. Endocrinol. Metab. (1992) [Pubmed]
  16. Calmodulin-mediated effects of loperamide on chloride transport by brush border membrane vesicles from human ileum. Stoll, R., Ruppin, H., Domschke, W. Gastroenterology (1988) [Pubmed]
  17. Effect of lidamidine hydrochloride and loperamide on gastric emptying and transit of the small intestine. A double-blind study. Sninsky, C.A., Davis, R.H., Clench, M.H., Thomas, K.D., Mathias, J.R. Gastroenterology (1986) [Pubmed]
  18. Antidiarrhoeal activity of loperamide: studies of its influence on ion transport across rabbit ileal mucosa in vitro. Hughes, S., Higgs, N.B., Turnberg, L.A. Gut (1982) [Pubmed]
  19. Oral glutamine in the prevention of fluorouracil induced intestinal toxicity: a double blind, placebo controlled, randomised trial. Daniele, B., Perrone, F., Gallo, C., Pignata, S., De Martino, S., De Vivo, R., Barletta, E., Tambaro, R., Abbiati, R., D'Agostino, L. Gut (2001) [Pubmed]
  20. Influence of loperamide on the internal anal sphincter in the opossum. Rattan, S., Culver, P.J. Gastroenterology (1987) [Pubmed]
  21. Pharmacologic treatment of the irritable bowel syndrome: a systematic review of randomized, controlled trials. Jailwala, J., Imperiale, T.F., Kroenke, K. Ann. Intern. Med. (2000) [Pubmed]
  22. Loperamide: a positive modulator for store-operated calcium channels? Harper, J.L., Shin, Y., Daly, J.W. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  23. A double blind crossover comparison of loperamide with diphenoxylate in the symptomatic treatment of chronic diarrhea. Pelemans, W., Vantrappen, F. Gastroenterology (1976) [Pubmed]
  24. Loperamide: studies on its mechanism of action. Sandhu, B.K., Tripp, J.H., Candy, D.C., Harries, J.T. Gut (1981) [Pubmed]
  25. Inhibitory actions of loperamide on absorptive processes in rat small intestine. Hardcastle, J., Hardcastle, P.T., Cookson, J. Gut (1986) [Pubmed]
  26. Effect of loperamide and naloxone on mouth-to-caecum transit time evaluated by lactulose hydrogen breath test. Basilisco, G., Bozzani, A., Camboni, G., Recchia, M., Quatrini, M., Conte, D., Penagini, R., Bianchi, P.A. Gut (1985) [Pubmed]
  27. Effects of ABCB1 (multidrug resistance transporter) gene mutations on disposition and central nervous effects of loperamide in healthy volunteers. Skarke, C., Jarrar, M., Schmidt, H., Kauert, G., Langer, M., Geisslinger, G., Lötsch, J. Pharmacogenetics (2003) [Pubmed]
  28. Hydrolysis of capecitabine to 5'-deoxy-5-fluorocytidine by human carboxylesterases and inhibition by loperamide. Quinney, S.K., Sanghani, S.P., Davis, W.I., Hurley, T.D., Sun, Z., Murry, D.J., Bosron, W.F. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  29. Effect of opioid mu-receptors activation on insulin signals damaged by tumor necrosis factor alpha in myoblast C2C12 cells. Ko, W.C., Liu, T.P., Cheng, J.T., Tzeng, T.F., Liu, I.M. Neurosci. Lett. (2006) [Pubmed]
  30. Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Kim, K.A., Chung, J., Jung, D.H., Park, J.Y. Eur. J. Clin. Pharmacol. (2004) [Pubmed]
  31. Loperamide, an opiate analog, differently modifies the adrenocorticotropin responses to corticotropin-releasing hormone and lysine vasopressin in patients with Addison's disease. Bochicchio, D., Ambrosi, B., Faglia, G. Neuroendocrinology (1988) [Pubmed]
  32. Mechanism of the antidiarrheal effect of loperamide. Schiller, L.R., Santa Ana, C.A., Morawski, S.G., Fordtran, J.S. Gastroenterology (1984) [Pubmed]
  33. Recommended guidelines for the treatment of cancer treatment-induced diarrhea. Benson, A.B., Ajani, J.A., Catalano, R.B., Engelking, C., Kornblau, S.M., Martenson, J.A., McCallum, R., Mitchell, E.P., O'Dorisio, T.M., Vokes, E.E., Wadler, S. J. Clin. Oncol. (2004) [Pubmed]
  34. Effect of codeine and loperamide on upper intestinal transit and absorption in normal subjects and patients with postvagotomy diarrhoea. O'Brien, J.D., Thompson, D.G., McIntyre, A., Burnham, W.R., Walker, E. Gut (1988) [Pubmed]
  35. Abuse potential of loperamide. Jaffe, J.H., Kanzler, M., Green, J. Clin. Pharmacol. Ther. (1980) [Pubmed]
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