Renal action, therapeutic use, and pharmacokinetics of the diuretic bumetanide

Davies, L M B David; Lant, A. F.; Millard, R B A Nicholas; Smith, Anthony J.; Ward, W M B John; Wilson, Graham M.

doi:10.1002/cpt1974152141

Cited by 126 publications

(59 citation statements)

References 7 publications

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“…The K t values of bumetanide for hOAT2, hOAT3, and hOAT4 were 7.52, 1.59, and 0.31 M, respectively (Hasannejad et al, 2004;Kobayashi et al, 2005), but the affinity of bumetanide for MCT6 (K t value at pH 7.4; 84 M) was lower. The clinical plasma concentration and plasma protein binding of bumetanide were reported to be about 0.27 M and 95%, respectively (Davies et al, 1974;Pentikainen et al, 1977). Consequently, the estimated plasma unbound concentration of bumetanide is 0.014 M, which is lower than K t values of MCT6, hOAT2, hOAT3, and hOAT4.…”

Section: Inhibitory Effects Of Anions and Cations On The Uptake Of ͓ mentioning

confidence: 89%

Functional characterization of human monocarboxylate transporter 6 (SLC16A5)

Murakami¹

2005

Drug Metabolism and Disposition

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Section: Inhibitory Effects Of Anions and Cations On The Uptake Of ͓ mentioning

confidence: 89%

Functional characterization of human monocarboxylate transporter 6 (SLC16A5)

Murakami¹

2005

Drug Metabolism and Disposition

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“…However IND produced an anticalciuria with very little change in magnesium excretion, other than a slight increase on the first day. These longer term effects on divalent cation excretion differ from the calciuria and magnesuria observed during the acute diuretic phase with both thiazides (Parfitt, 1969) and 'loop' diuretics (Davies et al, 1974).…”

mentioning

confidence: 77%

Renal actions of a uricosuric diuretic, racemic indacrinone, in man: comparison with ethacrynic acid and hydrochlorothiazide.

Brooks¹,

Lant²,

McNabb³

et al. 1984

Brit J Clinical Pharma

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3 During hydropenia with superimposed mannitol diuresis, both IND and EA caused a fall in fractional free-water reabsorption (TCH2O/GFR x 100%), AIND = -20.3% of control, AEA = -70.1% of control. HCTZ produced a significant increase in fractional free-water reabsorption, AHCTZ = -20.7% of control. 4 In all studies, single doses of IND were both uricosuric and hypouricaemic. Fractional urate excretion increased from a mean 6.7 + 0.1 to 15.2 + 2.1% of GFR whilst plasma urate concentration fell from a mean of 0.36 + 0.03 to 0.34 + 0.03 mM (P < 0.05) within 2-3 h post drug. HCTZ and EA, in single doses, had little effect on urate excretion. 5 In the second part of the study, a total of 16 healthy volunteers received either IND, 10 mg, or HCTZ 50 mg, orally for 8 days, whilst on a diet of controlled electrolyte content. 6 Both drugs were well tolerated by both sets of subjects with no adverse clinical or pathological findings. Both IND and HCTZ caused a significant reduction in weight and standing systolic blood-pressure during the first 48 h of therapy. At the doses administered, IND and HCTZ displayed similar diuretic responses with respect to water, Na+, Cl-, Ca2+ and P04 3-excretion. IND produced less kaliuresis than HCTZ during the first treatment day but cumulative K+ loss was similar for both drugs over the eight days of therapy. 7 Fractional urate excretion after IND remained elevated throughout the 8 days of therapy and the subjects remained isouricaemic for 7 days. HCTZ caused small reductions in fractional urate excretion during the first 4 h after each daily administration: however, plasma urate concentrations remained significantly elevated throughout the study, rising from a mean pre-drug value of 0.35 + 0.01 to 0.44 + 0.01 mM (P < 0.05) after 8 days of therapy.Keywords indacrinone ethacrynic acid hydrochorothiazide diuretics 497

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“…There was no evidence of a dose-response relationship and spontaneous variation from day to day was not assessed. Other workers have shown only small increases in Mgu following single doses of frusemide [81,82] and these did not reach statistical significance. Labeeuw et al [83] using 2 mg methylclothiazide by mouth (placebo, random order) found Mgu to be increased by only 14% whereas the average day to day spontaneous variation was 32% (range 11-60%).…”

Section: Animalsmentioning

confidence: 90%

Untitled

1993

Brit J Clinical Pharma

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2 Methods for the measurement of intracellular free magnesium levels are now available and are more relevant to the assessment of magnesium deficiency than total intracellular magnesium content; the complex relationship between intracellular free and total magnesium content remains to be defined. Future work involving the effect of diuretics on intracellular free magnesium measurements should make every attempt to avoid the errors of trial design and multiple publication that litter current and past literature.

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Renal action, therapeutic use, and pharmacokinetics of the diuretic bumetanide

Cited by 126 publications

References 7 publications

Functional characterization of human monocarboxylate transporter 6 (SLC16A5)

Functional characterization of human monocarboxylate transporter 6 (SLC16A5)

Renal actions of a uricosuric diuretic, racemic indacrinone, in man: comparison with ethacrynic acid and hydrochlorothiazide.

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