Jaundice Due to Oxyphenisatin

Pearson, A J; Scheuer, P. J.; Grainger, John; McIntyre, Neil

doi:10.1016/s0140-6736(71)91388-2

Cited by 33 publications

(10 citation statements)

References 9 publications

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“…The authors suggested that the female preponderance was a result of their greater tendency, as compared with males, to take laxatives. Numerous reports have since followed, recounting instances of both acute and chronic hepatic injury caused by oxyphenisatin [7,10,11,19,22,25,40,47,58,62,69,89]. Of the more than 100 cases described to date, over 80% have shown features of CAH, many with established cirrhosis.…”

Section: Seminars In Liver Disease: 1 (21 1981mentioning

confidence: 99%

Drug-Induced Chronic Liver Disease, with Emphasis on Chronic Active Hepatitis

Seeff¹

1981

Semin Liver Dis

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Section: Seminars In Liver Disease: 1 (21 1981mentioning

confidence: 99%

Drug-Induced Chronic Liver Disease, with Emphasis on Chronic Active Hepatitis

Seeff¹

1981

Semin Liver Dis

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“…A single case of acute hepatitis in a 56-year-old female has also been reported (Pearson et al 1971). It is still available as an effective enema preparation which should only be used prior to radiological investigation or for short term use as a last resort in severely constipated patients because of the possibility of liver toxicity.…”

Section: Poly Phenolic Derivativesmentioning

confidence: 99%

Adverse Effects of Drugs Used in the Management of Constipation and Diarrhoea

1994

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Most laxatives, if used intermittently in the absence of contraindications, are relatively safe. Bulking agents may diminish absorption of some minerals and drugs, but this is not usually clinically significant. Ispaghula can cause serious allergic reactions. The chronic ingestion of stimulant laxatives has been blamed for the development of the 'cathartic colon', but there are no definitive studies which have demonstrated this. Dantron (danthron) preparations should only be used in older patients and the terminally ill because of the risk of hepatotoxicity with this drug. Oral oxyphenisatine should no longer be used. Senna would appear to be the stimulant laxative of choice during pregnancy and lactation. Bisacodyl is the polyphenolic derivative of choice. Lactulose, sorbitol and lactilol rarely cause significant adverse effects. Magnesium salt laxatives and phosphate enemas can cause serious metabolic disturbances in babies and young children. Liquid paraffin is contraindicated if there is any risk of aspiration. Interference with the absorption of fat soluble vitamins would not appear to be clinically significant. Docusate sodium may potentiate the hepatotoxicity of other drugs, but reports of this are rare. The role of cisapride in constipation has not been established. Antidiarrhoeal drugs are second line drugs whose use is aimed at minimising inconvenience and discomfort. No antidiarrhoeals can be recommended for children under 4 years of age. Loperamide is the drug of choice in older children and adults. The atropine component of diphenoxylate/atropine combinations can cause significant adverse effects. Bismuth salicylate is an inconvenient treatment for travellers' diarrhoea as large frequent doses of the liquid formulation are needed. Some bismuth can be absorbed and there is the potential to cause encephalopathy. Octreotide, methysergide and cholestyramine have a role for specific causes of diarrhoea only. Octreotide is effective in high output states from the small or large bowel, with few adverse effects. Clonidine and lidamidine may have a role in the treatment of chronic diabetic diarrhoea. The role of lidamidine in nondiabetic chronic diarrhoea has not been established.

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“…This nonprescription drug 1 was used for more than 40 years before it was taken off the market because of transient hepatotoxicity. [3][4][5] However, the hepatic reaction caused by 1 is presumably due to a hypersensitivity response rather than a nonspecific toxic effect. [3][4][5] In vitro, compound 2 is found to potently inhibit proliferation in the breast cancer cell line MDA-MB-468 (IC 50 =3 nM).…”

Section: Introductionmentioning

confidence: 99%

“…[3][4][5] However, the hepatic reaction caused by 1 is presumably due to a hypersensitivity response rather than a nonspecific toxic effect. [3][4][5] In vitro, compound 2 is found to potently inhibit proliferation in the breast cancer cell line MDA-MB-468 (IC 50 =3 nM). 1 Interestingly, this class of compounds has a broad but distinct selectivity for inhibition of cancer cells, some being very sensitive, others almost resistant as further discussed below.…”

Section: Introductionmentioning

confidence: 99%

“…Compound 2 is a substituted derivative of oxyphenisatin ( 1 , 3,3-bis(4-hydroxyphenyl)-2-oxindole) (Figure ), which has been extensively used in man as a laxative. This nonprescription drug 1 was used for more than 40 years before it was taken off the market because of transient hepatotoxicity. − However, the hepatic reaction caused by 1 is presumably due to a hypersensitivity response rather than a nonspecific toxic effect. − …”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Antitumor Effect in Vitro and in Vivo of Substituted 1,3-Dihydroindole-2-ones

Christensen¹,

Erichsen²,

Trojel-Hansen

et al. 2010

J. Med. Chem.

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Optimization of the anticancer activity for a class of compounds built on a 1,3-dihydroindole-2-one scaffold was performed. In comparison with recently published derivatives of oxyphenisatin the new analogues exhibited an equally potent antiproliferative activity in vitro and improved tolerability and activity in vivo. The best compounds from this series showed low nanomolar antiproliferative activity toward a series of cancer cell lines (compound (S)-38: IC(50) of 0.48 and 2 nM in MCF-7 (breast) and PC3 (prostate), respectively) and potent antitumor effects in well tolerated doses in xenograft models. The racemic compound (RS)-38 showed complete tumor regression at a dose of 20 mg/kg administered iv on days 1 and 7 in a PC3 rat xenograft.

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Jaundice Due to Oxyphenisatin

Cited by 33 publications

References 9 publications

Drug-Induced Chronic Liver Disease, with Emphasis on Chronic Active Hepatitis

Drug-Induced Chronic Liver Disease, with Emphasis on Chronic Active Hepatitis

Adverse Effects of Drugs Used in the Management of Constipation and Diarrhoea

Synthesis and Antitumor Effect in Vitro and in Vivo of Substituted 1,3-Dihydroindole-2-ones

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