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Arzneimittel-Forschung Sep 1997The oral hypoglycemic drugs carbutamide, chlorpropamide, glibenclamide, glubornuride, gliclazide, glipizide, gliquidone, glisoxepide, glymidine, tolazamide and...
The oral hypoglycemic drugs carbutamide, chlorpropamide, glibenclamide, glubornuride, gliclazide, glipizide, gliquidone, glisoxepide, glymidine, tolazamide and tolbutamide, and the diuretics acetazolamide, bemetizide, bendroflumethiazide, benzthiazide, benzylhydrochlorothiazide, bumetanide, butizide, chlorazanile, chlorothiazide, chlortalidone, clopamide, cyclopenthiazide, cyclothiazide, diazoxide, etozoline, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, mefruside, metolazone, piretanide, polythiazide, trichlormethiazide, and xipamide were investigated for photohemolytic properties in vitro. Irradiation with a SOL 3 apparatus (solar simulating irradiation) revealed hemolysis in the presence of five oral hypoglycemic agents and in the presence of 19 out of the 25 tested diuretics. Photohemolysis was induced in the presence of three substances, respectively, after exposure to UVA or visible light. UVB alone did not induce phototoxic hemolysis in the presence of the tested drugs. Compared to clinical reports on photosensitivity reactions, the photohemolysis model seems a good predictive model in recognizing potential photosensitizing sulfonamides.
Topics: Dermatitis, Phototoxic; Diuretics; Drug Evaluation, Preclinical; Hemolysis; Humans; Hypoglycemic Agents; In Vitro Techniques; Photosensitivity Disorders; Sunlight; Ultraviolet Rays
PubMed: 9342417
DOI: No ID Found -
Naunyn-Schmiedeberg's Archives of... Sep 1997The NHIK 3025 cell line (Norsk Hydro Institutt for Kreftforskning), a human in situ carcinoma of the cervix cell line, was used to investigate the thiazides bemetizide,... (Comparative Study)
Comparative Study
The NHIK 3025 cell line (Norsk Hydro Institutt for Kreftforskning), a human in situ carcinoma of the cervix cell line, was used to investigate the thiazides bemetizide, bendroflumethiazide, benzylhydrochlorothiazide, bumetanide, butizide, chlortalidone, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, piretanide, polythiazide, trichlormethiazide and xipamide for their potential phototoxic properties. Cell death following UVA irradiation and dependent on test substance concentration was observed in the presence of all the tested substances except chlortalidone, furosemide, indapamide and xipamide. Bendroflumethiazide was phototoxic at concentrations of 0.05 mM and higher; bemetizide, benzylhydrochlorothiazide, bumetanide and hydroflumethiazide were phototoxic at 0.25 mM and higher and butizide, hydrochlorothiazide, piretanide, polythiazide and trichlormethiazide were phototoxic at 0.5 mM and higher.
Topics: Benzothiadiazines; Cell Death; Diuretics; Dose-Response Relationship, Drug; Dose-Response Relationship, Radiation; Humans; Photosensitizing Agents; Sodium Chloride Symporter Inhibitors; Tumor Cells, Cultured; Ultraviolet Rays
PubMed: 9303564
DOI: 10.1007/pl00005053 -
Clinical Nephrology Jul 1997Ten patients with chronic renal failure from different genesis (serum creatinine levels 150-200 mumol/l), were evaluated from the aspect of the effect of the diuretic... (Clinical Trial)
Clinical Trial Comparative Study
Ten patients with chronic renal failure from different genesis (serum creatinine levels 150-200 mumol/l), were evaluated from the aspect of the effect of the diuretic therapy. The effects of furosemide (FUR) and polythiazide (POL) were assessed after 3-month application. The mean values of the estimated parameters before treatment, after 3-month administration of FUR as a monotherapy and after the next 3 months simultaneously used (FUR + POL), presented a stable increase of the diuresis, without statistically significant changes of the global renal function, and triglyceride disorders. On the contrary, the improvement of calciuria through combined using of furosemide and polythiazide is statistically and clinically significant.
Topics: Diuretics; Furosemide; Humans; Kidney Failure, Chronic; Middle Aged; Polythiazide; Sodium Chloride Symporter Inhibitors; Time Factors
PubMed: 9247782
DOI: No ID Found -
Journal of Photochemistry and... Mar 1997The sulphonamide-derived oral antidiabetics chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide, and the diuretics bemetizide,...
The sulphonamide-derived oral antidiabetics chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide, and the diuretics bemetizide, bendroflumethiazide, benzylhydrochlorothiazide, bumetanide, butizide, chlortalidone, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, piretanide, polythiazide, trichlormethiazide and xipamide were investigated for phototoxicity in a cell culture model. Cell death dependent on ultraviolet A (UVA) radiation fluence and test substance concentration was observed in the presence of the oral antidiabetics glibenclamide and gliquidone, as well as the diuretics bemetizide, bendroflumethiazide, benzylhydrochlorothiazide, bumetanide, butizide, hydrochlorothiazide, hydroflumethiazide, piretanide, polythiazide and trichlormethiazide. Bendroflumethiazide was phototoxic at concentrations of 0.05 mM and above; bemetizide, benzylhydrochlorothiazide, bumetanide and hydroflumethiazide were phototoxic at concentrations of 0.25 mM or more; the oral antidiabetics glibenclamide and gliquidone, as well as the diuretics butizide, hydrochlorothiazide, piretanide, polythiazide and trichlormethiazide were phototoxic at concentrations of 0.5 mM. To evaluate the effects of antioxidants, ascorbic acid, alpha-tocopherol, beta-carotene or ubiquinone was added to the tissue culture flasks before irradiation. The phototoxic inhibition of the colony-forming ability was largely reduced by the addition of ascorbic acid and alpha-tocopherole, indicating the involvement of reactive oxygen species in the phototoxic process.
Topics: Antioxidants; Ascorbic Acid; Cell Death; Cells, Cultured; Dermatitis, Phototoxic; Diuretics; Humans; Hypoglycemic Agents; Sulfonamides; Tumor Cells, Cultured; Ultraviolet Rays; Vitamin E
PubMed: 9134756
DOI: 10.1016/s1011-1344(96)07433-7 -
In Vivo (Athens, Greece) 1997The oral antidiabetics chlorpropamide, glibenclamide, glipizide, gliquiudone, glymidine, tolazamide and tolbutamide, and the diuretics bemetizide, bendroflumethiazide,... (Comparative Study)
Comparative Study
The oral antidiabetics chlorpropamide, glibenclamide, glipizide, gliquiudone, glymidine, tolazamide and tolbutamide, and the diuretics bemetizide, bendroflumethiazide, benzylhydrochlorothiazide, bumetanide, butizide, chlortalidone, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, piretanide, polythiazide, trichlormethiazide, and xipamide were investigated for potential phototoxicity in vitro using a cell culture model, and in vivo in hairless mice. After exposure to broad band UVA, the majority of the substances tested in vitro yielded a phototoxic action leading to loss of culture forming ability. In vivo, all tested substances induced edema or ulceration, and lead to a significantly increase in skin fold thickness of the mouse skin. In all, a number of substances not described to induce clinical photosensitivity nor phototoxicity in vitro or in vivo were detected in our testing. When determining potential photosensitizers, it seems important to utilize different test methods, as not all substances will exhibit action in a given assay.
Topics: Administration, Oral; Animals; Dimethyl Sulfoxide; Diuretics; Evaluation Studies as Topic; Female; Humans; Hypoglycemic Agents; Light; Mice; Mice, Hairless; Photochemistry; Photosensitizing Agents; Sulfonamides; Tumor Cells, Cultured; Uterine Cervical Neoplasms
PubMed: 9067780
DOI: No ID Found -
Arzneimittel-Forschung Jan 1997A number of sulphonamide derived oral antidiabetics (chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide) and diuretics...
A number of sulphonamide derived oral antidiabetics (chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide) and diuretics (bemetizide, bendroflumethiazide, benzylhydrochlorothaizide, bumetanide, butizide, chlortalidone, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, piretanide, polythiazide, trichlormethiazide and xipamide) were investigated for phototoxicity in a cell culture model. Cell death dependent on UVA fluence and test substance concentration was observed in the presence of the oral antidiabetics glibenclamide and gliquidone, as well as the diuretics bemetizide, bendroflumethiazide, benzylhydroxhlorothiazide, bumetanide, butizide, hydrochlorothiazide, hydroflumethiazide, piretanide, polythiazide and trichlormethiazide. Bendroflumethiazide was phototoxic at 5 x 10(-5) mol/l and higher concentrations, bemetizide, benzylhydrochlorothiazide, bumetanide and hydroflumethiazide were phototoxic at 2.5 x 10(-4) mol/l and higher concentrations, and the oral antidiabetics glibenclamide and gliquidone as well as the diuretics butizide, hydrochlorothiazide, piretanide, polythiazide and trichlormethiazide were phototoxic at 5 x 10(-4) mol/l and higher concentrations. The oral antidiabetics chlorpropamide, glipizide, glymidine, tolazamide and tolbutamide as well as the diuretics chlortalidone, furosemide, indapamide and xipamide did not induce phototoxicity in this assay.
Topics: Carcinoma in Situ; Cell Death; Dermatitis, Phototoxic; Diuretics; Female; Humans; Hypoglycemic Agents; Tumor Cells, Cultured; Ultraviolet Rays; Uterine Cervical Neoplasms
PubMed: 9037453
DOI: No ID Found -
Photodermatology, Photoimmunology &... Oct 1996The diuretics acetazolamide, bemetizide, bendroflumethiazide, benzthiazide, benzylhydrochlorothiazide, bumetanide, butizide, chlorazanile, chlorothiazide, chlortalidone,...
The diuretics acetazolamide, bemetizide, bendroflumethiazide, benzthiazide, benzylhydrochlorothiazide, bumetanide, butizide, chlorazanile, chlorothiazide, chlortalidone, clopamide, cyclopenthiazide, cyclothiazide, diazoxide, etozoline, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, mefruside, metolazone, piretanide, polythiazide, trichlormethiazide, and xipamide were screened in vitro for phototoxic effects by means of a photohemolysis test. In all, 19 out of the 25 test substances revealed phototoxic hemolytic properties after irradiation with either solar stimulating irradiation, UVA and/or visible light. Addition of the antioxidants ascorbic acid, alpha-tocopherole or superoxide dismutase significantly inhibited the phototoxic hemolysis, as well as did investigations carried out in a nitrogen rich atmosphere, findings which indicate the involvement of reactive oxygen species in the phototoxic process.
Topics: Antioxidants; Benzothiadiazines; Diuretics; Erythrocytes; Hemolysis; Humans; Nitrogen; Sodium Chloride Symporter Inhibitors; Superoxide Dismutase; Ultraviolet Rays; Vitamin E
PubMed: 9112280
DOI: 10.1111/j.1600-0781.1996.tb00202.x -
Photodermatology, Photoimmunology &... Feb 1996A number of sulphonamide-derived oral antidiabetics (chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide) and diuretics...
A number of sulphonamide-derived oral antidiabetics (chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide) and diuretics (bemetizide, bendroflumethiazide, benzylhydrochlorothiazide, bumetanide, butizide, chloratalidone, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, piretanide, polythiazide, trichlormethiazide and xipamide) were investigated for phototoxicity in a cell culture model. Cell death dependent on ultraviolet A fluence and test substance concentration was observed in the presence of the oral antidiabetics glibenclamide and gliquidone, as well as the diuretics bemetizide, bendroflumethiazide, benzyl-hydrochlorothiazide, bumetanide, butizide, hydrochlorothiazide, hydroflumethiazide, piretanide, polythiazide and trichlormethiazide. Bendroflumethiazide was phototoxic at 5x10(-5) M and higher concentrations, bemetizide, benzylhydrochlorothiazide, bumetanide and hydroflumethiazide were phototoxic at 2.5x10(-4) M and higher concentrations, and the oral antidiabetics glibenclamide and gliquidone as well as the diuretics butizide, hydrochlorothiazide, piretanide, polythiazide and trichlormethiazide were phototoxic at 5(-4) M and higher concentrations. Electron microscopic investigations showed swelling of mitochondria and endoplasmic reticulum as well as aggregation of euchromatin when the cells were irradiated in the presence of photosensitizers.
Topics: Administration, Oral; Cell Death; Cells, Cultured; Dermatitis, Phototoxic; Diuretics; Humans; Hypoglycemic Agents; Radiation Dosage; Sulfonamides; Ultraviolet Rays
PubMed: 8884891
DOI: 10.1111/j.1600-0781.1996.tb00235.x -
Pharmaceutical Research Oct 1994The interaction of a series of benzothiadiazides with human serum albumin (HSA) was investigated by equilibrium dialysis (ED) and spectroscopic methods including...
The interaction of a series of benzothiadiazides with human serum albumin (HSA) was investigated by equilibrium dialysis (ED) and spectroscopic methods including circular dichroism (CD). The primary binding site of benzothiadiazides was designated site II, the diazepam site on the HSA molecule, as indicated by displacement experiments using different site-selective probes. Tyrosine and lysine amino acid residues were probably involved in the binding site of these compounds to HSA. Both electrostatic and hydrophobic interactions were found to play a role in the binding of these compounds to HSA. Among the compounds tested, chlorothiazide had the highest affinity (K1 = 5.5 x 10(4) M-1, K2 = 5.8 x 10(3) M-1). The primary binding affinity of the compounds for HSA was of the order: chlorothiazide > cyclopenthiazide > polythiazide > ethiazide > trichlormethiazide = methyclothiazde > hydrochlorothiazide. Binding was insensitive to the N-B transition of HSA. The binding site is proposed to consist of a cationic site on the surface of the HSA molecular with a hydrophobic crevice to accommodate the aromatic ring of the compounds. Positions 3 and 7 of the benzothiadiazide molecule is thought to affect the binding affinity to HSA.
Topics: Benzothiadiazines; Binding Sites; Chemical Phenomena; Chemistry, Physical; Circular Dichroism; Dialysis; Electrochemistry; Humans; Hydrogen-Ion Concentration; Protein Binding; Serum Albumin; Spectrometry, Fluorescence; Spectrophotometry, Ultraviolet; Temperature
PubMed: 7855051
DOI: 10.1023/a:1018952108327 -
Tidsskrift For Den Norske Laegeforening... May 1991A number of studies indicate that hydrochlorothiazide doses above 50 mg daily provide little additional hypotensive effect but progressively greater hypokalemic effect....
A number of studies indicate that hydrochlorothiazide doses above 50 mg daily provide little additional hypotensive effect but progressively greater hypokalemic effect. From these and similar studies on other thiazides a daily dose range for thiazides of 12.5-50 mg for hydrochlorothiazide, 1.25-5 mg for bendroflumethiazide, 1-2 mg for trichloromethiazide, 0.5-1 mg for polythiazide, and 6.25-25 mg for chlorthalidone appears to be sufficient. Because amiloride enhances the natriuretic effect of thiazides, this agent has not only a Mg2+/K(+)-sparkling effect, but also a potential thiazide-sparing effect. For this reason, the recommended doses of fixed combinations of hydrochlorothiazide and amiloride should be lowered to the range 6.25 mg/0.625 mg--25 mg/2.5 mg.
Topics: Benzothiadiazines; Diuretics; Dose-Response Relationship, Drug; Humans; Hypertension; Sodium Chloride Symporter Inhibitors; Tablets
PubMed: 2063371
DOI: No ID Found