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Results for “Oxyphenisatin Acetate”

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At least 19 recordsLinked to original sources
PubMed1981

Effects of sodium picosulfate and other laxatives in cultured Chang cells.

Cytotoxic effects were studied in Chang liver cells exposed to 4,4'-dihydroxy-diphenyl-(2-pyridyl)-methane-bis(hydrogen sulfate) (ether)-disodium salt (sodium picosulfate) and the results were compared with the effects of other laxatives. Sodium picosulfate caused a decrease in cell growth parallel to a decrease in glucose consumption and lactate production at 2000 and 4000 microgram/ml. On the contrary, 4,4'-dihydroxy-diphenyl-(2-pyridyl)-methane (bis-acodyl) decreased cell growth at 25 and 50 microgram/ml, while glucose consumption, lactate production and the molar ratio of glucose converted to lactate were increased. These effects were also observed with 4,4'-dihydroxy-diphenyl-(2-pyridyl)-methane (La 96), 3,3-bis(p-hydroxyphenyl)oxindole (oxyphenisatin acetate) and 3,3-bis(p-acetoxyphenyl) phthalide (phenolphthalein) at doses of 25 and 50 microgram/ml. Diphenolic compounds seem to increase anaerobic glycolysis by inhibition of respiration. This assumption was confirmed with potassium cyanide, which is known to inhibit the electron transport in the respiratory chain. Actinomycin D, cycloheximide and hydroxyurea did not show such effects.

Cathartics↗
PubMed1976

Pathway of sodium moving from blood to intestinal lumen under the influence of oxyphenisatin and deoxycholate.

The transfer of (51)CrEDTA and inulin--substances which are distributed only in the extracellular space--across the rat colonic mucosa in vivo is increased by oxyphenisatin O (3.5 times 10(-5)M) and deoxycholate D(3 times 10(-3)M). O and D do not change the size of the intra- and extracellular fluid compartments of the mucosa as measured with (51)CrEDTA from the blood side. The sodium and potassium content of the mucosal tissue is not altered. Therefore the calculated intracellular concentrations of sodium and potassium remain constant. The time course of the (22)Na uptake into the mucosal epithelium is not influenced by O and D up to 5 min after i.v. injection. The specific activity of sodium, however, in the luminal fluid increases under the influence of O(twofold) and D(fivefold). The uptake of (22)Na into the mucosal tissue after administration of (22)Nainto the intestinal lumen is not changed in presence of O and D. We conclude that the net transport of sodium and water from blood to lumen under the influence of O and D occurs mainly via the intercellular way.

Animals↗
PubMed1977

Transfer of sodium and water through isolated rat colonic mucosa under the influence of deoxycholate and oxyphenisatin.

1. The influence of oxyphenisatin (OP), a diphenolic laxative, and deoxycholate (DC) on the transfer of sodium and water in an everted sac preparation of stripped rat colon was investigated. 2. OP (10(-5) M, mucosal side) and DC (3 X 10(-4) M, mucosal side) completely blocked net water and sodium absorption. Net movements from the serosal to the mucosal side could not be induced by higher concentrations of the drugs. 3. Unidirectional sodium movements in both directions were increased by OP and DC. 4. The effect of DC on the sodium flux from the serosal to the mucosal side was reversible. 5. The potassium content of the mucosal epithelium was not changed by DC and OP. 6. The integrity of the epithelium, as judged by light microscopy, was not disturbed by either drug under the experimental conditions. 7. It is concluded that DC and OP do not interfere with active transport mechanisms but increase the permeability of the epithelium to sodium.

Animals↗
PubMed1977

Influence of hydrostatic pressure gradients on net transfer of sodium and water across isolated rat colonic mucosa.

1. The dependence of net transfer of water and sodium on hydrostatic pressure gradients from the serosal to the mucosal side was investigated in everted sacs of the stripped mucosa of the rat colon. 2. In the range of 3-20 cm H2O both, net sodium and water transfer were linearly dependent on hydrostatic pressure. The hydraulic permeability coefficient was 1.1 ml per gram dry weight, hour and cm H2O. At a pressure gradient of 5.8 cm H2O the net movement of water from the mucosal to the serosal side ceased. Above this pressure a net movement in the opposite direction occurs. Sodium net movement from the mucosal to the serosal side ceased at 11 cm H2O. The fluid, which appears-driven by higher values of hydrostatic pressure-on the mucosal side, is hypotonic. 3. Oxyphenisation increases the hydraulic permeability of the colonic epithelium. The fluid, which appears--driven by the hydrostatic pressure gradient--on the mucosal side, is isotonic.

Animals↗
PubMed1983

Differentiation of secretagogue drugs by chlorpromazine in rat intestine in vivo.

The effect of chlorpromazine (CPZ) on passive epithelial permeability and net fluid movement induced by secretagogues was tested in the rat intestine in vivo. CPZ, in a dose of 20 mg/kg intramuscularly, did not alter colonic permeability either in control conditions or during increased permeability caused by deoxycholic acid (DOC) or bisacodyl. Fluid secretion induced by cholera toxin and theophylline was strongly reduced by CPZ. The effects of oxyphenisatin and bisacodyl were only slightly but significantly inhibited by CPZ, whereas the action of DOC was unaffected. It is concluded, that the increase of the epithelial permeability is the main reason for the augmented fluid secretion caused by DOC. Bisacodyl and oxyphenisatin seem to act partly via an increase in permeability and to some degree via an induction of an active secretory process.

Animals↗
PubMed1980

Intestinal filtration as a consequence of increased mucosal hydraulic permeability. A new concept for laxative action.

Two mechanisms have been proposed to explain the secretory action of laxative compounds in the intestine: 1. increase of the intracellular amount of cyclic adenosine monophosphate due to stimulation of the adenylate cyclase system and 2. inhibition of intestinal transfer processes, in particular the Na,K-ATPase activated sodium absorption. In a set of in vivo and in vitro experiments in rat colon it could be demonstrated that dihydroxy bile acids (deoxycholate) and diphenolic laxatives (oxyphenisatin) enhance the hydraulic permeability of the mucosal tissue. The permeability changes take place--and there is good experimental evidence--at the zonulae occludentes which bind the epithelial cells together at their luminal borders. Due to laxative action the hydraulic permeability of the colonic mucosa increases to such an extent that according to the Starling forces the normal subepithelial hydrostatic pressure is a sufficient driving force to reverse net sodium, chloride, and water absorption into net secretion. A new concept of "intestinal filtration as a consequence of increased mucosal hydraulic permeability" is proposed to explain the laxative action of deoxycholate and oxyphenisatin in the colon. The question whether inhibition of Na,K-ATPase activity, cyclic AMP-mediated secretion or increased hydraulic permeability of the colonic mucosa are causatively linked to and quantitatively meaningful in intestinal secretion remains open.

Adenosine Triphosphatases↗
PubMed1979

Drug-induced chronic hepatic disease.

A number of chronic hepatic lesions can result from adverse reactions to medicinal agents. Such lesions include a form of chronic active hepatitis; hepatic steatosis, phoepholipidosis and granulomatosis; several vascular lesions; two types of noncirrhotic portal hypertension; several types of cirrhosis and several neoplasms.

Carcinoma, Hepatocellular↗
PubMed1977

Genetic factors in the development of chronic active hepatitis.

In 14 of 16 patients with chronic active hepatitis (C.A.H.) who did not have HLA antigens B8 and/or B12 an external triggering factor (drug or virus) could be demonstrated at onset of symptoms. In contrast external factors were involved in only 11 of 25 cases of C.A.H. in patients with HLA-B8 and/or B12. In the latter group antinuclear antibodies were less common in cases possible triggered by external agents compared with cases in which no such factor was demonstrated. The results suggest that there are at least two pathogenetically different types of C.A.H.---one genetically determined type in which no external factor is involved and in which autoimmune phenomena are common, and another type triggered by environmental agents and not involving predisposing genetic factors.

Autoantibodies↗
PubMed1981

Qualitative and quantitative analysis of some synthetic, chemically acting laxatives in urine by gas chromatography-mass spectrometry.

A method for the qualitative and quantitative simultaneous analysis of dioxyanthraquinone, desacetyl-Bisacodyl, phenolphthalein and Oxyphenisatin in human urine using gas chromatography-mass spectrometry (GC-MS) has been developed. The compounds were extracted from urine at pH 7.5 with diethyl ether using Extrelut extraction columns, followed by evaporation and trimethylsilylation. The method used electron beam ionization GC-MS employing a computer-controlled multiple-ion detector (mass fragmentography). The recovery from urine for the various compounds was between 80% and 100%. The detection limit for these compounds was in the range 0.01--0.05 micrograms/ml of urine. The method proved to be suitable for measuring urine concentrations for at least four days after administration of a single oral low therapeutic dose of the laxatives to sixteen healthy volunteers.

Anthraquinones↗
PubMed1975

[Oxyphenisatin-induced liver disease (author's transl)].

Over a period of 18 months the development of hepatitis after intake of oxyphenisatin, a laxative, was established in 14 patients by re-exposure to the drug. The characteristic feature was nonspecific upper abdominal pain up to colic-like pain, lact of appetite, nausea or vomiting, and pruritus. The biochemical changes were those of chronic hepatitis with varying severity of biliary stasis and abnormal immunofluorescence. On re-exposure there was a particularly remarkable rise in GLDH activity. The histological picture showed acute inflammatory changes in the biliary passages on re-exposure, while the liver cells were clearly involved only secondarily. At a latter point the histological picture became non-specific. At laparoscopy there were different stages of minor periportal hepatic fibrosis to marked postnecrotic liver scars with portal hypertension and decompensation. Early diagnosis is difficult but crucial to the patient's fate, because this form of hepatitis regresses completely after oxyphenisatin has been stopped. Laxatives containing this drug should be withdrawn from the market.

Adult↗
PubMed1978

Outcome of chronic active hepatitis: influence of histocompatibility antigens and triggering factors.

Twenty-five patients with chronic active hepatitis triggered by external factors (viruses or drugs) and 20 patients with cryptogenic chronic active hepatitis were studied for two to five years. The first group showed a significantly higher frequency of clinical and biochemical resolution at the end of the observation period than did the second group. The group with cryptogenic disease had a predominance of females carrying the histocompatibility antigen HLA-B8, whereas the group with virus- or drug-induced hepatitis did not differ from normal controls in regard to the distribution of HLA antigens. HLA-B8 and HLA-B12 were found in all but two patients in the group with cryptogenic hepatitis; this group of patients had elevated levels of gamma-globulin and autoantibodies in their sera more frequently than did the group with virus- or drug-induced disease. The results suggest that there are at least two types of chronic active hepatitis: one genetically determined, with signs of enhanced immunoreactivity and with a low degree of healing in five years; and another type triggered by external factors and without predisposing genetic factors. The data suggest that the clinical outcome is more favorable for patients with the second type of chronic active hepatitis.

Chemical and Drug Induced Liver Injury↗