Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Xipamide”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 109 records · Page 6Linked to original sources
PubMed1989

Comparison of two combined diuretics in the treatment of essential hypertension.

The efficacy and safety of two combination drugs, consisting of a diuretic + a K-sparing agent, were investigated in the treatment of essential hypertension. A double-blind, randomized, parallel group study design was employed. After randomization, 14 patients were treated with 10 mg xipamide + 30 mg triamterene (A) and 16 with 25 mg hydrochlorothiazide + 50 mg triamterene (B). The patients suffered from essential hypertension with a systolic blood pressure (SBP) at entry of greater than or equal to 150 mmHg and a diastolic blood pressure (DBP) of greater than or equal to 95 mmHg. After 6 weeks, mean decline in DBP was 12% in group A and 9% in group B, respectively. With treatment A, one patient became hypokalemic and with treatment B one patient became hyperkalemic.

Adult↗
PubMedDate not supplied

A decade of developments in diuretic drug therapy.

New diuretics introduced into clinical medicine during the past decade include potent new loop diuretics such as bumetanide and piretanide, the uricosuric indanyloxyacetic acid derivative indacrinone, and a new generation of sulfamoyl diuretics such as indapamide and xipamide, which are recommended primarily for the treatment of hypertension. Pharmacokinetic studies of individual diuretics have demonstrated that the diuretic and natriuretic responses to the newer agents generally follow the plasma drug concentration-time curves and urinary drug excretion rates. Therapeutic monitoring can therefore be achieved in most patients with edema or hypertension by close clinical observation and laboratory analysis of plasma electrolyte and creatinine concentrations and urinary electrolyte excretion rates. Interest in the mechanisms involved in the renal and extrarenal vascular actions of the newer diuretics has led to a better understanding of how changes in venous compliance, peripheral vascular resistance, and renal blood flow distribution may contribute to the overall therapeutic response to these agents, especially in patients with severe congestive heart failure, renal insufficiency with low glomerular filtration rates, and hypertension with cardiorenal complications. Adverse reactions to modern diuretics, which are mainly an extension of their renal pharmacodynamic effects, have proved to be minimal, provided that the dosage is adjusted to meet but not exceed individual patient requirements. However, the long-term consequences of prolonged periods of diuretic-induced alterations in plasma potassium levels, and metabolic effects that include elevated blood lipids, are still under investigation.

Diuretics↗
PubMed1992

Cicletanine sulfate: inhibition of anion transport systems and natriuretic activity.

In contrast with cicletanine, its urinary sulfoconjugate metabolite (cicletanine sulfate) was active on membrane ion transport in human red blood cells. Cicletanine sulfate was a more potent inhibitor of the Na+ dependent [Cl-/HCO3-] exchanger (IC50 = 9 +/- 3 x 10(-5) mol/l; mean +/- SD of 4 experiments) than cicletanine (IC50 = 10(-3) mol/l). This inhibitory potency was intermediate between that of xipamide (IC50 = 2 x 10(-5) mol/l) and that of furosemide (IC50 = 2 x 10(-4) mol/l). Moreover, cicletanine sulfate exhibited modest inhibitory potency against the [Na+,K+,Cl-]-cotransport system (IC50 = 1 +/- 0.3 x 10(-3) mol/l; mean +/- SD of 4 experiments) and poor inhibitory activity against the [K+,Cl-]-cotransport system. Cicletanine sulfate was unable to modify the activity of Cl(-)-independent membrane carriers (Na+:H+ exchanger, Ca2+ pump, Na+:Li+ countertransport system and Na+,K+ pump). Following renal intraarterial administration in rats, cicletanine sulfate and not cicletanine, exhibited salidiuretic activity. In conclusion, the urinary sulfo-conjugate of cicletanine is an active anion transport inhibitor and natriuretic metabolite. In fact, this metabolite may be responsible for the salidiuretic action of cicletanine.

Animals↗
PubMed1991

Evidence for the O-sulfo derivative of MK-447 as active metabolite of MK-447.

In contrast with furosemide (and other sulfamoylbenzoic and aryloxyacetic acids loop diuretics), MK-447 was unable to inhibit the [Na+,K+,Cl-] cotransport system in human red blood cells. Indeed, this compound was a very poor ion transport inhibitor (inactive on Ca(2+)-sensitive K+ channels, the Ca2+ pump, the Na+:Mg2+ exchange, the Na+:Li+ countertransport system and the [K+,Cl-] cotransport system, and only inhibiting the [Cl-/HCO3-] exchanger and the Na+,K+ pump at high concentrations). Conversely, its urinary metabolite (O-sulfo)-MK-447 was a very potent inhibitor of the [Na+,K+,Cl-] cotransport system (IC50 of 1.6 +/- 0.5 x 10(-6) M; mean +/- S.D. of four experiments). This compound was a much more potent [Na+,K+,Cl-] cotransport inhibitor than furosemide, and almost as active as bumetanide. In addition, (O-sulfo)-MK-447 was a moderate inhibitor of the [Cl-/HCO3-] exchanger (IC50 of 6 +/- 3 x 10(-5) M, n = 3), its potency being intermediate between that of xipamide and that of furosemide. Interestingly, it exhibited some inhibitory activity against Ca(2+)-sensitive K+ channels but only at high concentrations (it had no effect on the [K+,Cl-] cotransport system, the Ca2+ pump or the Na+:Mg2+ exchanger). The results suggest strongly that the O-sulfo derivative of MK-447 is an active natriuretic metabolite of MK-447. This metabolite may be responsible for the salidiuretic action of MK-447.

Biological Transport, Active↗
PubMed2004

Effects of pH and the presence of micelles on the resolution of diuretics by reversed-phase liquid chromatography.

A comparative study on the performance of two RPLC modes on the separation of 18 diuretics with diverse acid-base behaviour (acetazolamide, althiazide, amiloride, bendroflumethiazide, benzthiazide, bumetanide, canrenoic acid, chlorothiazide, chlorthalidone, ethacrynic acid, furosemide, hydrochlorothiazide, piretanide, probenecid, spironolactone, triamterene, trichloromethiazide and xipamide) was carried out. A conventional octadecylsilane column and acidic acetonitrile-water mobile phases, in the absence and presence of micelles of the anionic surfactant sodium dodecyl sulphate (SDS), were used. The effects of pH and the modifiers acetonitrile and SDS on peak asymmetry, efficiency, selectivity, resolution and analysis time, were examined. The comparison of both RPLC modes (aqueous- and micellar-organics) was done using the same processing tools, applying several polynomial and mechanistic equations to describe the retention. The best separations were obtained by maximising the product of peak purities, considering a wide range of experimental conditions. The study illustrates that, despite the theoretical and practical complexity of the problem, the predicted optimal chromatograms can be reproduced experimentally with great accuracy. None of the examined RPLC modes was able to yield baseline separation of the 18 diuretics. However, their selectivity was complementary, being appropriate for different combinations of a smaller number of the assayed diuretics.

Chromatography, Liquid↗
PubMed2000

Use of a three-factor interpretive optimisation strategy in the development of an isocratic chromatographic procedure for the screening of diuretics in urine samples using micellar mobile phases.

Screening of diuretics in urine is feasible through direct injection of the samples into the chromatographic system and isocratic reversed-phase liquid chromatography (RPLC) with micellar-organic mobile phases of sodium dodecyl sulfate (SDS) and 1-propanol. The surfactant coverage of the chromatographic column makes the addition of organic competing amines less necessary than in conventional aqueous-organic RPLC to achieve well-shaped peaks. Also, the range of elution strengths of micellar mobile phases required to elute mixtures of hydrophobic and hydrophilic diuretics is smaller. This allows the isocratic separation of the diuretics within adequate analysis times. An interpretive methodology is applied to optimise the resolution of a mixture of 15 diuretics of diverse polarity and acid-base behaviour (althiazide, amiloride, bendroflumethiazide, benzthiazide, bumetanide, canrenoic acid, chlorthalidone, ethacrynic acid, furosemide, piretanide, probenecid, torasemide, triamterene, trichloromethiazide and xipamide), using pH and concentrations of surfactant and organic modifier in the mobile phase as separation factors. Twelve diuretics were resolved in 25 min using 0.055 M SDS-6.0% 1-propanol at pH 3.0. The mixture of 15 diuretics was also resolved with two mobile phases showing complementary behaviour: 0.05 M SDS-5.6% 1-propanol at pH 5.4 and 0.11 M SDS-5.4% 1-propanol at pH 4.2. The results were applied to the analysis of urine samples with limits of detection similar to those usually reported for aqueous-organic RPLC, taking into account that the samples were injected without any previous treatment to separate or preconcentrate the analytes.

Calibration↗
PubMed2000

High-performance liquid chromatographic separation of a complex mixture of diuretics using a micellar mobile phase of sodium dodecyl sulphate. Application to human urine samples.

A systematic optimization of the HPLC separation of a complex mixture containing 19 diuretics by micellar liquid chromatography using sodium dodecyl sulphate (SDS), a Hypersil (150 mmx3.0 mm I.D., 5 microm) C18 column, a flow-rate of 0.5 ml min(-1) and UV absorbance detection has been carried out. Several mobile phases consisting of SDS and organic modifiers such as acetonitrile, tetrahydrofuran, propanol, butanol or pentanol, and the pH adjusted to 3.2, were tested. The effect of the organic modifier and SDS concentration on the retention behavior and separation of the diuretics was investigated. A mobile phase containing 40 mM SDS and 4% tetrahydrofuran was finally selected. Under these conditions, 14 out of 19 diuretics were separated in about 31 min. A bivariant optimization method for the mobile phase SDS-tetrahydrofuran corroborated the above results. The effect of temperature on the retention was also studied, and 50 degrees C was selected. The optimized method was applied to human urine samples of subjects administered Diurex (tablets containing 20 mg of the active ingredient xipamide) without sample preparation.

Calibration↗
PubMed1997

Inhibiting effects of antioxidants on drug-induced phototoxicity in cell cultures. Investigations with sulphonamide-derived oral antidiabetics and diuretics.

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.

Antioxidants↗
PubMed1992

Effects of diuretics on renal excretory function.

From a clinicopharmacological standpoint, the urinary excretory potency of diuretics should be assessed comparatively, on the basis of placebo-controlled changes in 24 h natriuresis, following single oral doses administered to healthy adult subjects who are in steady-state habitual external sodium balance. The potency of 30 diuretic formulations has been evaluated. Two formulations of loop diuretics (muzolimine 20 mg and torasemide 2.5 mg) are non-diuretic. The majority of the other formulations of loop diuretics studied (e.g. furosemide 40 mg and torasemide 5 and 10 mg) are comparatively less potent than most of the common formulations of early distal tubular diuretics studied (e.g. hydrochlorothiazide 25 and 50 mg, xipamide 10, 20 and 40 mg). Hydrochlorothiazide 25 mg and furosemide 80 mg have similar potencies. The presence of a rebound in natriuresis between 6 and 24 h after administration of loop diuretics make the majority of the common formulations of these drugs less potent than most common formulations of thiazide-type diuretics.

Circadian Rhythm↗
PubMed2005

Screening procedure for detection of diuretics and uricosurics and/or their metabolites in human urine using gas chromatography-mass spectrometry after extractive methylation.

A gas chromatography-mass spectrometry (GC-MS)-based screening procedure was developed for the detection of diuretics, uricosurics, and/or their metabolites in human urine after extractive methylation. Phase-transfer catalyst remaining in the organic phase was removed by solid-phase extraction on a diol phase. The compounds were separated by GC and identified by MS in the full-scan mode. The possible presence of the following drugs and/or their metabolites could be indicated using mass chromatography with the given ions: m/z 267, 352, 353, 355, 386, and 392 for thiazide diuretics bemetizide, bendroflumethiazide, butizide, chlorothiazide, cyclopenthiazide, cyclothiazide, hydrochlorothiazide, metolazone, polythiazide, and for canrenoic acid and spironolactone; m/z 77, 81, 181, 261, 270, 295, 406, and 438 for loop diuretics bumetanide, ethacrynic acid, furosemide, piretanide, torasemide, as well as the uricosurics benzbromarone, probenecid, and sulfinpyrazone; m/z 84, 85, 111, 112, 135, 161, 249, 253, 289, and 363 for the other diuretics acetazolamide, carzenide, chlorthalidone, clopamide, diclofenamide, etozoline, indapamide, mefruside, tienilic acid, and xipamide. The identity of positive signals in such mass chromatograms was confirmed by comparison of the peaks underlying full mass spectra with reference spectra. This method allowed the detection of the abovementioned drugs and/or their metabolites in human urine samples, except torasemide. The limits of detection ranged from 0.001 to 5 mg/L in the full-scan mode. Recoveries of selected diuretics and uricosurics, representing the different chemical classes, ranged from 46% to 99% with coefficients of variation of less than 21%. After ingestion of the lowest therapeutic doses, furosemide was detectable in urine samples for 67 hours, hydrochlorothiazide for 48 hours, and spironolactone for 52 hours (via its target analyte canrenone). The procedure described here is part of a systematic toxicological analysis procedure for acidic drugs and poisons.

Diuretics↗
PubMed1996

Inhibition of thiazide photohemolysis in vitro by antioxidants and a nitrogen atmosphere.

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.

Antioxidants↗
PubMed1996

Phototoxicity due to sulphonamide derived oral antidiabetics and diuretics: investigations in a cell culture model.

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.

Administration, Oral↗
PubMed1991

Effects of diuretics on outputs and flows of urine and urinary solutes in healthy subjects.

The effects of single oral doses of common formulations of diuretics (i.e. formulations on the market or designed to be marketed) on 24-hour diuresis and natriuresis in healthy subjects are considered as a measure of the renal excretory potency of diuretics. Common formulations of distal tubular diuretics (e.g. hydrochlorothiazide 25mg, xipamide 10mg and 20mg) are more potent diuretics and natriuretics than common formulations of loop diuretics [e.g. furosemide (frusemide) 40mg, torasemide 2.5, 5 and 10mg]. Indeed, some common formulations of loop diuretics, such as torasemide 2.5, do not increase 24-hour diuresis or natriuresis in healthy subjects. 24-hour kaliuresis and magnesiuresis are elevated by common formulations of distal tubular diuretics, but they are only slightly increased or (more usually) not affected by common formulations of loop diuretics, when single doses are administered to healthy individuals. Common formulations of loop diuretics have lower diuretic and natriuretic potency and lower kaliuretic and magnesiuretic effects than common formulations of distal tubular diuretics, because the pronounced elevations in urinary excretions caused by loop diuretics during the first 6 hours after dosing are followed by rebounds, with respect to post-placebo excretions, between 6 and 24 hours after dosing. These rebounds, which affect the urinary flows of fluid, chloride, sodium, potassium and magnesium, do not occur after administration of common formulations of distal tubular diuretics, at least during the first 24 hours after administration of single doses to healthy subjects. The time courses of urinary excretions after loop diuretics are dose dependent. Higher doses produce more rapid changes in the urinary flows of fluid, chloride, sodium, potassium and magnesium than lower doses, to the extent that single administration of torasemide 2.5 or 5mg to healthy subjects is followed by urinary fluid and solute flows whose time courses resemble those after administration of hydrochlorothiazide 25mg.

Administration, Oral↗
PubMed1992

[Effect of diuretics on serum lipoproteins].

UNLABELLED: BASICS: Drug treatment of the risk factor hypertension has not led to the expected reduction in morbidity and mortality of coronary arterial disease. A negative effect of antihypertensive drugs on the lipid metabolism is under discussion as a possible cause. MAIN TOPICS: Both the commonly employed thiazide diuretics and chlorthalidone and the loop diuretics furosemide, piretanide and xipamide lead, to varying extents, to an increase in total and LDL cholesterol as well as triglycerides in subjects with normal metabolism. In addition, some diuretics lower the levels of protective HDL cholesterol. These side effects can be avoided--at least in part--by a combination with such drugs as prazosin, pindolol or captopril, which have a favorable effect on metabolism. CONCLUSION: It is recommended to carefully monitor serum Lipoproteins during diuretic treatment so that possible adverse changes may be counteracted by appropriate measures.

Arteriosclerosis↗
PubMed1989

[The effect of the beta 1 selective beta blocker, betaxolol, on metabolism in type II diabetics].

The effects of the highly beta 1-selective beta-blocker betaxolol (Kerlone) on carbohydrate and lipid metabolism in type II diabetic subjects were compared in a cross over study with those of a diuretic (xipamide-triamterene combination, Neotri). Betaxolol significantly lowered blood pressure with a tendency to better efficacy than the diuretic. The betaxolol-induced decrease in heart rate could be a contributing factor in attenuating the progression of atherosclerosis. No significant alterations were observed in postprandial blood glucose, glycosylated haemoglobin and 24-h urinary glucose excretion. The lack of noticeable influence on the carbohydrate metabolism during 4-week therapy is presumably related to the high beta 1-selectivity of betaxolol. Considering that diabetic hypertensive patients are at high risk for atherosclerosis it appears also favourable that betaxolol did not increase triglyceride levels and even decreased total cholesterol. The protective effect of beta-Blockers has been well established in the secondary and primary prevention of cardiovascular diseases. Especially diabetic patients might be expected to benefit from this therapy, if given preferably as beta 1-selective blocker that impairs carbohydrate and lipid metabolism in lesser extent.

Adrenergic beta-Antagonists↗
PubMed1987

Pharmacological properties of besulpamide, a new diuretic, in rats and dogs.

Besulpamide, a newly synthesized compound, has demonstrated significant diuretic activity in rats and dogs, similar to that of chlorthalidone, clopamide and xipamide. Antihypertensive activity of besulpamide is similar to that of hydrochlorothiazide and was demonstrated in rat one-kidney desoxycorticosterone acetate (DOCA)-salt hypertension. In addition, besulpamide, like hydrochlorothiazide, potentiated the antihypertensive activity of captopril in spontaneously hypertensive rats (SHR). Doses of besulpamide exceeding those normally required for pharmacological activity did not evoke adverse reactions in rats and mice.

Animals↗
PubMed1982

Diuretics and zinc.

Distal tubule diuretics (DTDs), including chlorothiazide, hydrochlorothiazide, bendroflumethiazide, chlorthalidone and xipamide, have been found to increase urinary zinc output through a poorly understood mechanism which could involve both direct and hormone-mediated processes. Significant zinc depletion may occur during long-term administration of DTDs, principally in conditions associated with diminished total body zinc levels such as hepatic cirrhosis, diabetes mellitus, gastro-intestinal disorders and several renal diseases. Attention to the early symptoms of zinc deficiency such as hypogeusia, hyposmia, abnormal dark adaptation and impotence and the monitoring of serum zinc levels are advisable during long-term treatment with common DTDs.

Adult↗
PubMed1981

Diuretics.

Diuretics of current interest are classified according to their potency or site of action. The pharmacokinetics of furosemide, xipamide hydrochlorothiazide and triamterene are briefly described, and important adverse reactions and drug interactions involving diuretics are reviewed. The clinical indications for diuresis are presented.

Diuretics↗