Phenolphthalein

IARC Monographs on the Evaluation of Carcinogenic Risks to Humans

Volumn 76, Issue , 2000, Pages 387-415

[No Author Info available]

Author keywords

[No Author keywords available]

Indexed keywords

PHENOLPHTHALEIN;

ANIMAL EXPERIMENT; COLON CANCER; DRUG ANALYSIS; DRUG INDICATION; DRUG STRUCTURE; FEMALE; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; REVIEW;

EID: 0033941610     PISSN: 02509555     EISSN: None     Source Type: Book Series    
DOI: None     Document Type: Review

References (90)

1. Al-Shammary, F., Mian, M.S. & Mian, N.A.A (1991) Phenolphthalein. In: Florey, K., ed., Analytical Profiles of Drug Substances. New York, Academic Press, Vol. 20, pp. 627-664
2. American Hospital Formulary Service (1995) AHFS Drug Information® 95, Bethesda, MD, American Society of Health-System Pharmacists, pp. 1986-1995
3. American Hospital Formulary Service (1997) AHFS Drug Information® 97, Bethesda, MD, American Society of Health-System Pharmacists, pp. 2241-2242
4. Ayass, M., Bussing, R. & Mehta, P. (1993) Munchausen syndrome presenting as hemophilia: A convenient and economical 'steal' of disease and treatment. Pediatr. Hematol. Oncol., 10, 241-244
5. Bergan, T., Fotland, M.H. & Sund, R.B. (1982) Interaction between diphenolic laxatives and intestinal bacteria in vitro. Acta pharmacol. toxicol., 51, 165-172
6. Bishop, M.E., Aidoo, A., Domon, O.E., Morris, S.M. & Casciano, D.A. (1998) Phenolphthalein induces micronuclei in transgenic human lymphoblastoid cells. Environ. mol. Mutag., 32, 286-288
7. Bonin, A.M., Farqhuarson, J.B. & Baker, R.S.U. (1981) Mutagenicity of arylmethane dyes in Salmonella. Mutat. Res., 89, 21-34
8. British Pharmacopoeial Commission (1993) British Pharmacopoeia 1993, London, Her Majesty's Stationery Office, Vol. I, pp. 502-503
9. Budavari, S., ed. (1996) The Merck Index, 12th Ed., Whitehouse Station, NJ, Merck & Co., pp. 1248, 1726-1727
10. Canadian Pharmaceutical Association (1997) CPS Compendium of Pharmaceuticals and Specialties, 32nd Ed., Ottawa, Ontario, pp. 40, 490, 564
11. Canadian Pharmacists Association (1999) Drug Brief - Phenolphthalein [http://www. cdnpharm.ca/drugbrf2.htm]
12. Chapin, R., Gulati, D., Mounce, R. & Russell, S. (1997a) Phenolphthalein. Environ. Health Perspectives, 105, 335-336
13. Chapin, R.E., Sloane, R.A. & Hasemen, J.K. (1997b) The relationships among reproductive endpoints in Swiss mice, using the Reproductive Assessment by Continuous Breeding database. Fundam. appl. Toxicol., 38, 129-142
14. CIS Information Services (1998) Worldwide Bulk Drug Users Directory 1997/98 Edition, Dallas, TX [CD-ROM]
15. Cleves, M. (1932) Poisoning by Exlax tablets. J. Am. med. Assoc., 99, 654-655
16. Colburn, W.A., Hirom, P.C., Parker, R.J. & Milburn, P. (1979) A pharmacokinetic model for enterohepatic recirculation in the rat: Phenolphthalein, a model drug. Drug Metab. Dispos., 7, 100-102
17. Cooke, W.T. (1977) Laxative abuse. Clin. Gastroenterol., 6, 659-673
18. Copeland, P.M. (1994) Renal failure associated with laxative abuse. Psychother. Psychosom., 62, 200-202
19. Cummings, J.H. (1974) Laxative abuse. Gut, 15, 758-766
20. Cummings, J.H., Sladen, G.E., James, O.F.W., Sarner, M. & Misiewicz, J.J. (1974) Laxative-induced diarrhoea: A continuing clinical problem. Br. med. J., i, 537-541
21. Davies, D.M., ed. (1985) Textbook of Adverse Drug Reactions, 3rd Ed., New York, Oxford University Press, pp. 110, 121, 475-479
22. Dietz, D.D., Elwell, M.R., Chapin, R.E., Shelby, M.D., Thompson, M.B., Filler, R. & Stedham, M.A. (1992) Subchronic (13 week) toxicity studies of phenolphthalein in Fischer 344 rats and B6C3F1 mice. Fundam. appl. Topical., 18, 48-58
23. Dunnick, J.K. & Hailey, J.R. (1996) Phenolphthalein exposure causes multiple carcinogenic effects in experimental model systems. Cancer Res., 56, 4922-4926
24. Dunnick, J.K., Hardisty, J.F., Herbert, R.A., Seely, J.C., Furedi-Machacek, E.M., Foley, J.F., Lacks, G.D., Stasiewicz, S. & French, J.E. (1997) Phenolphthalein induces thymic lymphomas accompanied by loss of the p53 wild type allele in heterozygous p53-deficient (±) mice. Toxicol. Pathol., 25, 533-540
25. Everhart, J.E., Go, V.L.W., Johannes, R.S., Fitzsimmons, S.C., Roth, H.P. & White, L.R. (1989) A longitudinal survey of self-reported bowel habits in the United States. Dig. Dis. Sci., 34, 1153-1162
26. Food & Drug Administration (1999) Laxative drug products for over-the-counter human use. Fed. Regist., 64, 4535-4540
27. Francesco International (1998) Major Rx-to-OTC Switched Products: The Important Switches of 1997 in Major Markets [http://www.rxtootcswitch.com/data.htm]
28. Furst, S.M., Blanchard, K.T., Lilly, P.D., Holden, H.E., Stoltz, J.H., Barthel, C. & Stoll, R.E. (1999) Six month oral gavage and diet carcinogenicity study with phenolphthalein in the heterozygous p53 +/-mouse (Abstract No. 1202). Toxicologist, 48
29. Gennaro, A.R. (1995) Remington: The Science and Practice of Pharmacy, 19th Ed., Easton, PA, Mack Publishing, Vol. II, p. 897
30. Gibson, D.P., Brauninger, R., Shafti, H.S., Kerckaert, G.A., LeBoeuf, R.A., Isfort, R.J. & Aardema, M.J. (1997) Induction of micronuclei in Syrian hamster embryo cells: Comparison to results in the SHE cell transformation assay for National Toxicology Program test chemicals. Mutat. Res., 392, 61-90
31. Griffin, R.J., Godfrey, V.B. & Burka, L.T. (1998) Metabolism and disposition of phenolphthalein in male and female F344 rats and B6C3F1 mice. Toxicol. Sci., 42, 73-81
32. Harari, D., Gurwitz, J.H., Avorn, J., Bohn, R. & Minaker, K.L. (1989) Bowel habit in relation to age and gender. Findings from the National Health Interview Survey and clinical implications. Arch, intern. Med., 156, 315-320
33. Hardman, J.G., Limbird, L.E., Molinoff, P.B. & Ruddon, R.W., eds (1996) Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th Ed., New York, McGraw-Hill, pp. 921-925
34. Harvey, M., McArthur, M.J., Montgomery, C.A., Jr, Butel, J.S., Bradley, A. & Donehower, L.A. (1993) Spontaneous and carcinogen-induced tumorigenesis in p53-deficient mice. Nature Genet., 5, 225-229
35. Hegi, M.E., Söderkvist, P., Foley, J.F., Schoonhoven, R., Swenberg, J.A., Kari, F., Maronpot, R., Anderson, M.W. & Wiseman, R.W. (1993) Characterization of p53 mutations in methylene chloride-induced lung tumors from B6C3F1 mice. Carcinogenesis, 14, 803-810
36. Heizer, W.D., Warshaw, A.L., Waldmann, T.A. & Laster, L. (1968) Protein-losing gastroenteropathy and malabsorption associated with factitious diarrhea. Ann. intern. Med., 68, 839-852
37. Hoyer, P.B., Boese, B. & Sipes, I.G. (1997) The effect of phenolphthalein on B6C3F1 mouse ovaries (Abstract No. 1825). Toxicologist, 36, 359
38. Jacobs, E.J. & White, E. (1998) Constipation, laxative use, and colon cancer among middleaged adults. Epidemiology, 9, 385-391
39. Kada, T., Tutikawa, K. & Sadaie, Y. (1972) In vitro and host-mediated 'rec-assay' procedures for screening chemical mutagens; and phloxine, a mutagenic red dye detected. Mutat. Res., 16, 165-174
40. Kar, P.K., Dutta, R.K. & Shah, B.H. (1986) Toxic epidermal necrolysis in a patient induced by phenolphthalein. J. Indian med. Assoc., 84, 189-190, 193
41. Kendall, A.C. (1954) Fatal case of encephalitis after phenolphthalein ingestion. Br. med. J., ii, 1461-1462
42. Kerckaert, G.A., Brauninger, R., LeBoeuf, R.A. & Isfort, R.J. (1996) Use of the Syrian hamster embryo cell transformation assay for carcinogenicity prediction of chemicals currently being tested by the National Toxicology Program in rodent bioassays. Environ. Health Perspectives, 104, 1075-1084
43. Kune, G.A. (1993) Laxative use not a risk for colorectal cancer: Data from the Melbourne Colorectal Cancer Study. Z. Gastroenterol., 31, 140-143
44. Lambrianides, A.L. & Rosin, R.D. (1984) Acute pancreatitis complicating excessive intake of phenolphthalein. Postgrad, med. J., 60, 491-492
45. LaRusso, N.F. & McGill, D.B. (1975) Surreptitious laxative ingestion. Delayed recognition of a serious condition: A case report. Mayo Clin. Proc., 50, 706-708
46. Longnecker, M.P., Sandler, D.P., Haile, R.W. & Sandler, R.S. (1997) Phenolphthalein-containing laxative use in relation to adenomatous colorectal polyps in three studies. Environ. Health Perspectives, 105, 1210-1212
47. Medical Economics (1998) PDR®: Physicians' Desk Reference, 52nd Ed., Montvale, NJ, Medical Economics Data Production, pp. 2601-2602, 2979
48. Mehendale, H.M. (1990) Assessment of hepatobiliary function with phenolphthalein and phenolphthalein glucuronide. Clin. Chem. Enzyme Commun., 2, 195-204
49. Millburn, P., Smith, R.L. & Williams, R.T. (1967) Biliary excretion of foreign compounds. Biphenyl, stilboestrol and phenolphthalein in the rat: Molecular weight, polarity and metabolism as factors in biliary excretion. Biochem. J., 105, 1275-1281
50. Mortelmans, K., Haworth, S., Lawlor, T., Speck, W., Tainer, B. & Zeiger, E. (1986) Salmonella mutagenicity tests. II. Results from the testing of 270 chemicals. Environ. Mutag., 8 (Suppl. 7), 1-119
51. Mrvos, R., Swanson-Biearman, B., Dean, B.S. & Krenzelok, E.P. (1991) Acute phenolphthalein ingestion in children. A retrospective review. J. pediatr. Health Care, 5, 147-151
52. 1 Mice (Feed Studies) (Technical Report Series No. 465; NIH Publ. No. 97-3390), Research Triangle Park, NC
53. National Toxicology Program (1999) NTP Report on Carcinogens. Background Document for Phenolphthalein (Final, March 1999), Research Triangle Park, NC, NTP Board of Scientific Counselors
54. Nieto, A., Garciá, C. & López de Haro, S. (1990) In vivo estrogenic and antiestrogenic activity of phenolphthalein and derivative compounds. Biochem. int., 2, 305-311
55. Nishikawa, J. (1981) Effects of sodium picosulfate and other laxatives in cultured Chang cells. Arzneimittelforschung, 31, 1872-1875
56. Parker, R.J., Hirom, P.C. & Millburn, P. (1980) Enterohepatic recycling of phenolphthalein, morphine, lysergic acid diethylamide (LSD) and diphenylacetic acid in the rat. Hydrolysis of glucuronic acid conjugates in the gut lumen. Xenobiotica, 10, 689-703
57. Pietrusko, R.G. (1977) Use and abuse of laxatives. Am. J. Hosp. Pharm., 34, 291-300
58. Pohl, A. & Lowe, J.P. (1978) Phenolphthalein poisoning - four cases. Proc. Mine med. Off. Assoc. S.A., 51, 84-86
59. Pouchert, C.J. (1981) The Aldrich Library of Infrared Spectra, 3rd Ed., Milwaukee, WI, Aldrich Chemical Co., p. 1471
60. Pouchert, C.J. (1985) The Aldrich Library of FT-IR Spectra, Vol. 1-2-3, Milwaukee, WI, Aldrich Chemical Co., p. 1006
61. Ravdin, P.M., van Beurden, M. & Jordan, V.C. (1987) Estrogenic effects of phenolphthalein on human breast cancer cells in vitro. Breast Cancer Res. Treat., 9, 151-154
62. Rote Liste Sekretariat (1998) Rote Liste 1998, Frankfurt, Rote Liste Service GmbH, pp. 56-068
63. Royal Pharmaceutical Society of Great Britain (1999) Martindale, The Extra Pharmacopoeia, 13th Ed., London, The Pharmaceutical Press [MicroMedex Online: Health Care Series]
64. Sadtler Research Laboratories (1980) Sadtler Standard Spectra, 1980 Cumulative Index, Philadelphia, PA, p. 1048
65. Sarcinelli, L., Signore, L. & Malizia, E. (1970) Lethal phenolphthalein poisoning in a child. Proc. Eur. Soc. Study Drug Toxicol., 50, 261
66. Shelley, W.B., Schlappner, O.L.A. & Heiss, H.B. (1972) Demonstration of intercellular immunofluorescence and epidermal hysteresis in bullous fixed drug eruption due to phenolphthalein. Br. J. Dermatol., 86, 188-125
67. Sidhu, P.S., Wilkinson, M.L., Sladen, G.E., Filipe, M.I. & Toseland, P.A. (1989) Fatal phenolphthalein poisoning with fulminant hepatic failure and disseminated intravascular coagulation. Hum. Toxicol., 8, 381-384
68. Sipe, H.J., Jr, Corbett, J.T. & Mason, R.P. (1997) In vitro free radical metabolism of phenolphthalein by peroxidases. Drug Metab. Dispos., 25, 468-480
69. Steigmann, F., Barnard, R.D. & Dyniewicz, J.M. (1938) Phenolphthalein studies: Phenolphthalein in jaundice. Am. J. med. Sci., 196, 673-688
70. Stroud, M.B. & Rosio, T.J. (1987) A case of recurring painful red macules. Arch. Dermatol., 123, 1225-1230
71. Sugar, J.A., Belfer, M., Israel, E. & Herzog, D.B. (1991) A 3-year-old boy's chronic diarrhea and unexplained death. J. Am. Acad. Child adolesc. Psychiatr., 30, 1015-1021
72. Sund, R.B. & Hillestad, B. (1982) Uptake, conjugation and transport of laxative diphenols by everted sacs of the rat jejunum and stripped colon. Acta pharmacol. toxicol., 51, 377-387
73. Sund, R.B. & Lauterbach, F. (1986) Drug metabolism and metabolite transport in the small and large intestine: Experiments with 1-naphthol and phenolphthalein by luminal and contraluminal administration in the isolated guinea pig mucosa. Acta pharmacol. toxicol., 58, 74-83
74. Sund, R.B., Hetland, H.S. & Nafstad, I. (1986) Autoradiography in mice after intravenous and intragastric administration of phenolphthalein and desacetylated bisacodyl, two laxative diphenols of the diphenylmethane group. Norw. pharm. Acta, 48, 57-73
75. Swiss Pharmaceutical Society, ed. (1999) Index Nominum, International Drug Director, 16th Ed., Stuttgart, Medpharm Scientific Publishers [MicroMedex Online: Health Care Series]
76. Thomas, J., ed. (1998) Australian Prescription Products Guide, 27th Ed., Victoria, Australian Pharmaceutical Publishing, Vol. 1, pp. 286, 1190-1191, 1229, 1587, 1686
77. Tice, R.R., Furedi-Machacek, M., Satterfield, D., Udumudi, A., Vasquez, M. & Dunnick, J.K. (1998) Measurement of micronucleated erythrocytes and DNA damage during chronic ingestion of phenolphthalein in transgenic female mice heterozygous for the p53 gene. Environ, mol. Mutag., 31, 113-124
78. Tsutsui, T., Tamura, Y., Yagi, E., Hasegawa, K., Tanaka, Y., Uehama, A., Someya, T., Hamaguchi, F., Yamamoto, H. & Barrett, J.C. (1997) Cell-transforming activity and genotoxicity of phenolphthalein in cultured Syrian hamster embryo cells. Int. J. Cancer, 73, 697-701
79. Tyson, R.M., Shrader, E.A. & Perlman, H.H. (1937) Drugs transmitted through breast milk. Part I. Laxatives. J. Pediatr., 11, 824
80. US Pharmacopeial Convention (1994) The 1995 US Pharmacopeia, 23rd Rev./The National Formulary, 18th Rev., Rockville, MD, pp. 1205-1206
81. US Pharmacopeial Convention (1998) USP Dispensing Information, Drug Information for the Health Care Professional, 18th Ed., Rockville, MD, Vol. I, pp. 1798-1840
82. Velentzas, C.G. & Ikkos, D.G. (1971) Phenolphthalein as cause of factitious enteritis (Letter to the Editor). J. Am. med. Assoc., 217, 966
83. Visek, W.J., Liu, W.C. & Roth, L.J. (1956) Studies on the fate of carbon-14 labeled phenolphthalein. J. Pharmacol. exp. Ther., 117, 347-357
84. Weiss, B.D. & Wood, G.A. (1982) Laxative abuse causing gastrointestinal bleeding. J. Fam. Pract., 15, 177-181
85. WHO (1997) Alert No. 65: Laxatives Containing Phenolphthalein - Proposed Ban on Sale of OTC Products: Risk of Carcinogenicity [http://www.who.int/dmp/drugalert/alert65.htm]
86. WHO (1998) Regulatory matters: Phenolphthalein products withdrawn. WHO Drug Inf., 12, 13-14
87. Williams, R.T. (1959) Detoxication Mechanisms. The Metabolism and Detoxication of Drugs, Toxic Substances and Other Organic Compounds, 2nd Ed., New York, John Wiley & Sons, pp. 475-476
88. Witt, K.L., Gulati, D.K., Kaur, P. & Shelby, M.D. (1995) Phenolphthalein: Induction of micronucleated erythrocytes in mice. Mutat. Res., 341, 151-160
89. Wyatt, E., Greaves, M. & Søndergaard, J. (1972) Fixed drug eruption (phenolphthalein). Evidence for a blood-borne mediator. Arch. Dermatol., 106, 671-673
90. Zanolli, M.D., McAlvany, J. & Krowchuk, D.P. (1993) Phenolphthalein-induced fixed drug eruption: A cutaneous complication of laxative use in a child. Pediatrics, 91, 1199-1201