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PubMed1977

Once daily treatment of mild to moderate hypertension with xipamid: a controlled study.

A double-blind, placebo controlled, crossover trial of 20 and 40 mg of xipamid once daily in the treatment of mild to moderate hypertension is reported and some of the difficulties and pitfalls of multicentre trials of this type are described. 2 Both doses were significantly more effective in reducing the blood pressure than the placebo and neither was superior to the other. Both produced some potassium loss. Xipamid acted for at least 22 h and was effective in up to 83% of the patients. 3 Further trials are suggested to investigate the activity of a lower dose than 20 mg.

Blood Pressure↗

PubMed1984

Xipamide: no advantage over bendrofluazide in hypertension.

In patients with uncontrolled hypertension addition of xipamide 20 mg daily to bendrofluazide 5 mg daily produced no significant additive antihypertensive effect, and the 95% confidence limits excluded a clinically important response. Xipamide treatment worsened hypokalaemia and increased the blood urea concentration significantly.

Bendroflumethiazide↗

PubMed1980

Xipamide ('Diurexan') in essential hypertension: a 24-month study.

Twenty-two patients with essential hypertension received xipamide as monotherapy for a continuous period of 2 years. At an average single daily dose of 23 mg, the patients showed a mean reduction in standing systolic pressure of 17%, and diastolic of 15% at the end of the study period. Serum potassium levels always remained within the normal range (without potassium supplements), and serum uric acid levels were only slightly above normal, even at the end of the 2-year trial period. Blood sugar levels in 8 patients with pre-existing diabetes mellitus were increased by 30% at the end of the first year of xipamide therapy, but remained stable at this level during the remaining 12 months. Adverse effects were mild and did not require the cessation of therapy.

Adult↗

PubMed1983

Comparison of the hypotensive effects of bendrofluazide, bumetanide and xipamide.

A randomized, triple crossover study was carried out in 24 elderly patients requiring chronic diuretic therapy to assess the different hypotensive effects of a fixed daily dose of 5 mg bendrofluazide, 1 mg bumetanide and 40 mg xipamide. Each treatment was given for 3 months. The results showed that no significant weight change took place during the study period. There was, however, a significant (p less than 0.001) decrease compared to baseline values both in systolic and diastolic blood pressure during the xipamide period and a decrease in diastolic blood pressure (p less than 0.05) when taking bumetanide. Only minor side-effects were reported.

Aged↗

PubMed1978

Xipamide in the management of renal, hepatic and cardiac oedema.

Xipamide (4-chloro-5-sulphamyl-salicylic acid 2', 6'-dimethylanilide) is a diuretic and antihypertensive agent. A clinical trial of the drug was performed in 11 patients, 8 with nephrotic syndrome, 1 with oedema and ascites due to hepatic cirrhosis, and 2 with congestive cardiac failure due to idiopathic cardiomyopathy. The drug proved to be potent, safe and efficacious. Side-effects were similar to those encountered with other thiazide-derived diuretics, but were not of a severe nature. Wider clinical usage of xipamide would appear to be warranted.

Adolescent↗

PubMed1975

[Structure-activity relationships in the diuretic xipamide (4-chloro-5-sulfamoyl-2', 6' -salicyloxylidide)].

The synthesis of various derivatives of 4-chlorosalicylic acid substituted in position 5 is described. The evaluation of their diuretic potency on the rat showed 4-chloro-5-sulfamoyl-2,6-salicyloxylidide (BE 1293, xipamide, Aquaphor) as the most effective one. The normal urinary volume is increased tenfold by a oral dose of 100 mg/kg body weight. All changes in the molecular structure of xipamide, even acetylation, the introduction of a second sulfamoyl group or the exchange of the sulfonic group for the carbonyl group, lead to a decrease in activity.

Acetylation↗

PubMed1975

[The saluretic effect of xipamide (4-chloro-5-sulfamoyl-2',6'-salicyloxylilide) in normal subjects].

The diuretic and saluretic effectiveness of xipamide (4-chloro-5-sulfamoyl-2',6'-salicyloxylidide, Aquaphor) is determined and compared to those of chlortalidone and furosemid in normal subjects. The substance is revealed as a potent diuretic agent. In the range of 0.035--0.750 mg/kg body weight the dose-response curve of orally administered xipamide for the increase of excretion of urine, sodium and potassium ion and chloride during 24 h is described. Observing the renal activity over a period of 3 days after a single administration the duration of action is found to be up to 24 h with its maximum within the first 12 h. In the following 2 days the degree of the physiological rebound effect depends on the preceding saluretic effect and thus on the given dose. The pattern of ion-excretion (Na

Administration, Oral↗

PubMed1975

[Inhibition of carbonic anhydrase by xipamide (4-chloro-sulfamoyl-2',6'-salicyloxylidide) in the modified Philpot test].

The inhibition of carbonic anhydrase by xipamide (4-chloro-5-sulfamoyl-2',6'-salicyloxylidide, Aquaphor), a poorly watersoluble saluretic agent, is determined with the Philpot method in the presence of 5 per cent N,N-dimethyl-formamide. The addition of the amide does not affect the enzyme. For xipamide 1.1 times 10-5 M is found as the 50 per cent inhibitory concentration.

Anilides↗

PubMed2003

Can xipamide or tacrolimus inhibit the glucuronidation of mycophenolic acid in rat liver slices?

The objective of this study was to investigate the effect of tacrolimus (Tac) and xipamide (X) on mycophenolic acid (MPA) glucuronidation in precision-cut rat liver slices. To assess a possible effect of these two drugs, the influence of the anti-inflammatory drug niflumic acid (NA)--a well-known inhibitor for MPA glucuronidation in human liver microsomes--was used as a standard. MPA and its main metabolite mycophenolic acid glucuronide (MPAG) were determined by means of high-performance liquid chromatography. MPA glucuronidation rate showed a significant linear correlation (p = 0.012) with MPA concentrations from 15.61 up to 124.88 microM in the medium. That means, the enzyme(s) responsible for the glucuronidation of MPA worked far below Km-value. With all MPA concentrations tested, neither the addition of Tac (31.30 nM) nor of X (28.25 nM) influenced the glucuronidation of MPA. In comparison, NA at a concentration of 70.92 nM showed a marked inhibitory effect (by 72%). The present pilot-study indicates that precision-cut rat liver slices are a suitable in vitro model to characterize the glucuronidation of MPA to its primary metabolite MPAG and interferences with other substances.

Animals↗

PubMed2004