Non-antibiotic anti-diarrhoeal drugs: Factors affecting oral bioavailability of berberine and loperamide in testinal tissue

Advanced Drug Delivery Reviews

Volumn 23, Issue 1-3, 1997, Pages 111-120

  Baird, Alan W ^a   Taylor, Cormac T ^a   Brayden, David J ^b  

^a UNIVERSITY COLLEGE DUBLIN   (Ireland)

^b ELAN PHARMACEUTICALS   (United States)

Author keywords

berberine; diarrhoea; intestinal epithelium; loperamide; potassium channels; rat colon mucosae; tight junction; Ussing chamber

Indexed keywords

AGENTS; DISEASES; DRUG INTERACTIONS; DRUG THERAPY; PHARMACOKINETICS; POTASSIUM; TISSUE;

BERBERINE; DIARRHOEA; INTESTINAL EPITHELIUM; LOPERAMIDE; NON ANTIBIOTIC ANTI DIARRHOEAL DRUGS; ORAL BIOAVAILABILITY; POTASSIUM CHANNELS; RAT COLON MUCOSAE; TIGHT JUNCTION; USSING CHAMBER;

DRUG PRODUCTS;

ALPHA ADRENERGIC RECEPTOR STIMULATING AGENT; ANTIDIARRHEAL AGENT; BERBERINE; BISMUTH SALICYLATE; CARBACHOL; CHOLINERGIC RECEPTOR BLOCKING AGENT; CORTICOSTEROID; CYTOCHALASIN D; DIPHENOXYLATE; ENKEPHALINASE INHIBITOR; FORSKOLIN; KAOLIN; LOPERAMIDE; MESALAZINE; NONSTEROID ANTIINFLAMMATORY AGENT; OPIATE; PECTIN; PENETRATION ENHANCING AGENT; POTASSIUM CHANNEL; SALAZOSULFAPYRIDINE; SOMATOSTATIN DERIVATIVE;

BASOLATERAL MEMBRANE; CHLORIDE TRANSPORT; DIARRHEA; DRUG BIOAVAILABILITY; DRUG MECHANISM; INTESTINE EPITHELIUM; INTESTINE MOTILITY; INTESTINE SECRETION; NONHUMAN; PRIORITY JOURNAL; REVIEW; SHORT CIRCUIT CURRENT; TIGHT JUNCTION;

EID: 0031015137     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-409X(96)00429-2     Document Type: Review

References (77)

1. Onishchenko, G.G., Lomov, I.M.. Moskvitana, E.A., Usenko, U.G., Varivoda, A.G., Parfenov, A.I. and Kireev, I.G. (1994) The epidemic situation re: cholera in the world: a morbidity analysis and trends. Zh. Mikrobiol. Epidemiol. Immunobiol. 3, 34-39.
2. Bhattacharya, S.K., Goswami, A.G., Bhattacharay, M.K., Dutta, D., Deb, A., Sircar, B.K., Chowdhury, A.S., Das, K.P. and Nair, G.B. (1994) Epidemic of vibrio cholera 0139 in Calcutta. Indian J. Med. Res. 100, 213-216.
3. Fordtran, J.S. (1967) Speculations on the pathogenesis of diarrhoea. Fed. Proc. 26, 1405-1414.
4. Schiller, L.R. (1995). Review article: anti-diarrhoeal pharmacology and therapeutics. Aliment. Pharmacol. Ther. 9, 87-106.
5. Kaunitz, J.D., Barrett K.E. and McRoberts J.A. (1995) Electrolyte secretion and absorption: small intestine and colon. In Textbook of Gastroenterology, pp. 326-361, 2nd edition, ed. T. Yamada. J.B. Lippincott Co., Philadelphia.
6. Musch, M.W. and Chang, E.B. (1993) Diarrhea in inflammatory bowel diseases. In 'Inflammatory Bowel Disease: from Bench to Bedside'. pp. 239-254, ed. S.R. Targan and F. Shanahan, Williams and Wilkins, Baltimore, MD.
7. Cooke, H.J. (1986) Neurobiology of the intestinal mucosa. Gastroenterology 90, 1057-1081.
8. Cooke, H.J. (1989) Role of the little brain in the gut in water and electrolyte homesostasis. FASEB J. 3, 127-138.
9. Castro, G.A. (1982) Immunological regulation of epithelial function. Am. J. Physiol. 243 G321-G329.
10. Castro, G.A. and Arntzen, C.J. (1993) Immunophysiology of the gut: a research frontier for integrative studies of the common mucosal immune system. Am. J. Physiol. 265, G599-G610.
11. Shanahan, F. and Anton, P. (1988) Neuroendocrine modulation of the immune system. Possible implications for inflammatory bowel disease. Dig. Dis. Sci. 33, 41S-49S.
12. Wood, J.D. (1991) Communication between minibrain in the gut and enteric immune system. News Physiol. Sci. 6, 359-364.
13. Kowlessar, O.D. (1989) The carcinoid syndrome. In Gastrointestinal Disease: Pathophysiology, Diagnosis, Management. Ed M. Slesinger and J.S. Fordtran. W.B. Saunders and Co., Philadelphia, USA, pp. 1560-1569.
14. Kaufman, H.J. and Taubin, H.L. (1987) Non-steroidal antiinflammatory drugs activate quiescent bowel disease. Ann. Intern. Med. 107, 513-516.
15. Donowitz, M., Wicks, J. and Sharp, G.W.G. (1986) Drug therapy for diarrhoeal diseases: a look ahead. Rev. Infect. Dis. 8, S188-S201.
16. Burks, T.F. (1990) Mechanisms of opioid anti-diarrheal therapy. In Textbook of Secretory Diarrhea. Ed. Lebenthal, E. and Duffey, M., Raven Press Ltd, New York, pp. 409-419.
17. Macht, D.I. (1915) The history of opium and some of its preparations and alkaloids. J. Am. Med. Assoc. 64, 477-481.
18. Awouters, F., Niemegeers, C.J.E. and Janssen, P.A.J. (1983) Pharmacology of antidiarrheal drugs. Annu. Rev. Pharmacol. Toxicol. 23, 279-301.
19. Krueger, H. (1937) The action of morphine on the digestive tract. Physiol. Rev. 17, 618-645.
20. Turnberg, L.A. (1983) Anti-secretory activity of opiates in vitro and in vivo in man. Scand. J. Gastroenterol. 18 (Suppl. 84) 79-83.
21. Kromer, W., Pretzlaff, W. and Scheiblhuber, E. (1980) In vitro evidence for an involvement of intestinal endorphins in the control of peristalsis in the guinea pig ileum. Comparison to rabbit, cat and dog small intestine. In 'Endogenous and Exogenous Opiate Agonists and Antagonists. Ed. by E.L. Way, pp 337-340, Pergamon Press, New York.
22. Paton, W.D.M. (1957) The action of morphine and related substances on contraction and on acetylcholine output of coaxially stimulated gguinea-pigileum. Br. J. Pharmacol. 12, 115-118.
23. Burks. T.F. (1978) Central sites of action of gastrointestinal drugs. Gastroenterology 74, 332-324.
24. Schulz, R., Wuster, M. and Herz, A. (1979) Centrally and peripherally mediated inhibition of intestinal motility by opioids. Naunyn-Schmiedeberg's Arch. Pharmacol. 308, 255-260.
25. Porreca, F., Galligan, J.J. and Burks T.F. (1986) Central opioid receptor involvement in gastrointestinal motility. Trends Pharm. Sci. 7, 104-107.
26. Manara, L. and Bianchetti, A. (1985) The central and peripheral influences of opioids on gastrointestinal propulsion. Annu. Rev. Pharmacol. Toxicol. 25, 249-273.
27. Powell, D.W. (1981) Muscle or mucosa: the site of action of anti-diarrheal opiates? Gastroenterology 80; 406-408.
28. Kromer, W. (1988) Endogenous and exogenous opioids in the control of gastrointestinal motility and secretion. Pharmacol. Rev. 40, 121-162.
29. Ooms, L.A.A. (1983) Alterations in intestinal fluid movement. Scand. J. Gastroenterol. 18, 65-77.
30. Heel, R.C., Brogden, R.N., Speight, T.M. and Avery G.S. (1978) Loperamide: a review of its pharmacological properties and therapeutic efficiency in diarrhoea. Drugs 15, 33-52.
31. Piercey, M.F. and Ruwart, M.J. (1979) Naloxone inhibits the anti-diarrhoeal activity of loperamide. Br. J. Pharmacol. 66, 373-375.
32. Awouters, F., Megens, A., Verlinden, M., Schuurkes, J., Niemegeers, C. and Janssen, P.A.J. (1993) Loperamide. Survey of studies on mechanism of its anti-diarrheal activity. Dig. Dis. Sci. 38, 977-995.
33. Burleigh, D.E. (1988) Opioid and non-opioid actions of loperamide on cholinergic nerve function in human isolated colon. Eur. J. Pharmacol. 152, 39-46.
34. Stoll, R., Ruppin, H. and Domschke,W. (1988) Calmodulinmediated effects of loperamide on chloride transport by brush border membrane vesicles from human ileum. Gastroenterology 95, 69-76.
35. Heykants, J., Michiels, M., Knaeps, A. and Brugmans, J. (1974) Loperamide (R18553) a novel type of anti-diarrhoeal agent. Part 5: The pharmacokinetics of loperamide in rats and man. Arzneim.-Forsch. 24, 1649-1655.
36. Miyazaki, H., Nambu, K. and Hashimoto, M. (1982) Loperamide in rat intestines: a unique disposition. Life Sci. 30, 2203-2206.
37. Ooms, L.A.A., DeGryse, A.D. and Janssen, P.A.J. (1984) Mechanisms of action of loperamide. Scand. J. Gastroenterol. 19 (suppl. 96) 145-155.
38. Wuster, M. and Herz, A. (1978) Opiate agonist action of anti-diarrheal agents in vitro and in vivo - findings in support of selective action. Naunyn-Schmeideberg's. Arch. Pharmacol. 301, 187-194.
39. Chopra, R.N., Dikshit, B.B. and Chowan, J.S. (1932) Pharmacological action of berberine. Indian J. Med. Res. 19, 1193-1203.
40. Zhang, M.F. and Chen, Z.L. (1991) Two new 8-oxotetrahydroprotoberberine alkaloids, gusanlung A and B from Acanalisia gusanlung. Planta Med. 57, 457-459.
41. Tang, W. and Eisenbrand, G. (1992) In Chinese Drugs of Plant Origin, pp. 361-371. Springer-Verlag Press: London.
42. Dutta, N.K., Marker, P.H. and Rao, N.R. (1972) Berberine in toxin induced experimental cholera. Br. J. Pharm. 44, 153-159.
43. Sabir, M., Akhter, M.H. and Bhide, N.K. (1977) Antagonism of cholera toxin by berberine in the gastrointestinal tract of adult rats. Indian J. Med. Res. 65, 305-313.
44. Sack, R.B. and Froehlich, J.L. (1982) Berberine inhibits intestinal secretory response of Vibrio choleras and Escherichia coli enterotoxins. Infect. Immun. 35, 471-475.
45. Yamamoto, K., Takase, H., Abe, K., Saito, Y. and Suzuki, A. (1993) Pharmacological studies on anti-diarrhoeal effects of a preparation containing berberine and gerainii herba. Nippon Yakurigaku Zasshi 101, 169-175.
46. Tai, Y.H, Feser, J.F., Marnane, W.G. and Desjeux, J.F. (1981) Anti-secretory effects of berberine in rat ileum. Am. J. Physiol. 241, G253-G258.
47. Guandalini, S., Fasano, A., Migliavacca, M., Marchesano, A.F. and Rubino, A. (1987) Effects of berberine on basal and secretagogue-modified ion transport in the rabbit ileum in vitro. J. Pediatr. Gastroenterol. 6, 953-960.
48. Taylor, C.T. and Baird, A.W. (1995) Berberine inhibition of electrogenic ion transport in rat colon. Br. J. Pharmacol. 116, 2667-2672.
49. Dawson, D.C. (1993) The molecular basis of gastrointestinal transport. Annu. Rev. Physiol. 55, 571-573.
50. Sandle, G.I., McNicholas, C.M. and Lomax, R.B. (1994) Potassium channels in colonie crypts. Lancet 343, 23-25.
51. Lohrmann, E., Burhoff, I., Nitschke, R.B., Lang, H.J., Mania, D., Englert, H.C., Hropot, M., Warth, R., Rohm, W., Bleich, M. and Greger, R. (1995) A new class of inhibitors of cAMP-mediated Cl secretion in rabbit colon, acting by the reduction of cAMP-activated K conductance. Pflugers Arch. 429, 517-530.
52. - secretion by phorbol esters: inhibition of basolateral potassium channels. Am. J. Physiol. 264, C161-168.
53. - secretion by T84 monolayers. Am. J. Physiol. 250, C486-C494.
54. Hua, Z. and Wang, X.L. (1994) Inhibitory effects of berberine on potassium channels in guinea pig ventricular myocytes. Yao Hsueh Hsueh Pao. 29, 576-580.
55. Sun, A.Y. and Li, D.X. (1993) Anti-fibrillatory effect of tetrahydroberberine. Acta Pharmacol. Sin. 14, 301-304.
56. Neto, F.R. (1993) Electropharmacological effects of berberine on canine cardiac purkinje fibres and ventricular muscle and artrial muscle of the rabbit. Br. J. Pharmacol. 108, 534-537.
57. Huang, W.M. (1992) A study of the anti-arrhythmic mechanism of berberine on delayed activation potassium current by voltage clamp. Chung Hua Hsin Hseuh Kuan Ping Tsa Chin. 20, 310-312.
58. Rennick, B.R. (1981) Renal tubule transport of organic cations. Am. J. Physiol. 240, F83-F89.
59. Iseki, K., Sugawara, M., Saitoh, N. and Miyazki, K. (1993) The transport mechanisms of organic cations and their zwitterionic derivatives across rat intestinal brush-border membrane vesicles. Biochem. Biophys. Acta 1152, 9-14.
60. Hughes, S., Higgs, N.B. and Turnberg, L.A. (1982) Antidiarrhoeal activity of loperamide: studies of its influence on ion transport across rabbit ileal mucosa in vitro. Gut 23, 974-979.
61. Cummins, A.G. and Roberts-Thomson, I.C. (1994) In Immunopharmacology of Epithelial Barriers. Ed. R. Goldie. Academic Press, pp. 213-223.
62. Hollander, D., Vadheim, C.M., Brettholz, E., Peterson, G.M., Delahunty, T. and Rotter, J.I. (1986) Increased intestinal permeability in patients with Crohn's disease and their relatives. A possible aetiological factor. Ann. Int. Med. 105, 883-885.
63. Cummins, A.G., Pentitila, I.A., LaBrooy, J.T., Shearman, D.J.C., Robb, T.A. and Davidson, G.P. (1991) Recovery of the small intestine in coeliac disease on a gluten free diet: changes in epithelial permeability, small bowel morphology and T-cell activity. J. Gastroenterol. Hepatol. 6, 53-57.
64. Aabakken, L., Bjornbeth, B.A., Hofstad, B., Olaussen, B., Larsen, S., and Osnes, M. (1989) Comparison of the gastrointestinal side effects of naproxen formulated as plain tablets, or enteric coated granules in capsules. Scand. J. Gastroenterol. (Suppl.) 163, 65-73.
65. Collins, S.M. and Croituru, K. (1993) Pathophysiology of inflammatory bowel disease: effect of inflammation on intestinal function. In: Inflammatory Bowel Disease: from Bench to Bedside. Ed. by S.R. Targan and F. Shanahan, Williams and Wilkins, Baltimore MD. pp. 194-209.
66. Sanderson, I.R. and Walker, W.A. (1993) Uptake and transport of macromolecules by the intestine: possible role in clinical disorders. Gastroenterology 104, 622-639.
67. Planchon, S.M., Martins, C.A.P., Guerrant, R.L. and Roche, J.K. (1994) Regulation of intestinal epithelial barrier function by TGF-β1. Evidence for its role in abrogating the effects of a T-cell cytokine. J. Immunol. 153, 5730-5739.
68. Madara, J.L.(1989) Loosening tight junctions: lessons from the intestine. J. Clin. Invest. 89, 1089-1094.
69. Colgan, S.P., Parkos, C.A., Delp, C., Arnaout, M.A. and Madara, J.L. (1993) Neutrophil migration across cultured intestinal epithelial monolayers is modulated by epithelial exposure to IFNγ in a highly polarised manner. J. Cell. Biol. 120, 785-798.
70. Perdue, M.H. and McKay, D.M. (1994) Integrative immunophysiology in the intestinal mucosa. Am. J. Physiol. 267 G151-G165.
71. Madara, J.L., Parkos, C., Colgan, S., Nusrat, A., Atisook, K. and Kaoutzani, P. (1992) The movement of solutes and cells across tight junctions. Ann. N.Y. Acad. Sci. 664, 47-60.
72. Fink, M.P. (1994) Effect of critical illness in microbial translocation and gastrointestinal mucosa permeability. Semin. Respir. Infect. 9, 256-260.
73. Lewis, S.A., Berg, J.R. and Kleine, T.J. (1995) Modulation of epithelial permeability by extracellular macromolecules. Physiol. Rev. 75, 561-589.
74. Dressman, J.B., Bass, P., Ritschel, W.A., Friend, D.R., Rubinstein, A. and Ziv, E. (1993) Gastrointestinal parameters that influence oral medications. J. Pharm. Sci. 82, 857-872.
75. Madara, J.L., Barenberg, D. and Carlson, S. (1986) Effects of cytochalasin D on occluding junctions of intestinal absorptive cells: further evidence that the cytoskeleton may influence paracellular permeability and junctional charge selectivity. J. Cell. Biol. 97, 2125-2135.
76. Artursson, P. and Karlsson, J. (1991) Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial cells. Biochem. Biophys. Acta 175, 880-885.
77. Madara, J.L., Stafford, J., Barenberg, D and Carlson, S. (1988) Functional coupling of tight junctions and microfilaments in T84 monolayers. Am. J. Physiol. 254, G416-G423.