Absorption, excretion, and metabolism of a new antibacterial agent, nalidixic acid

McChesney, Evan W.; Froelich, Ernest J.; Lesher, George Y.; Crain, A.V.R.; Rosi, D.

doi:10.1016/0041-008x(64)90070-5

Cited by 121 publications

(42 citation statements)

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“…The renal concentration of sulphonamides is low, but the renal-cortex/plasma ratio for nalidixic acid is eight to one in the rat (Schlegel, 1962a). In the monkey nalidixic acid has a high concentration in the kidney but no marked affinity for any other tissue (McChesney et al, 1964).…”

Section: Discussionmentioning

confidence: 99%

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Tissue Concentration of Nalidixic Acid in Chronic Pyelonephritis

Jameson¹

1965

BMJ

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Section: Discussionmentioning

confidence: 99%

“…Care was taken that the adjacent tissue was submitted for histological study. The spectrophotofluorinietric technique described (McChesney et al, 1964) measures free and protein-bound nalidixic acid; the biologically inactive metabolites are not determined.…”

Section: Methodsmentioning

confidence: 99%

Tissue Concentration of Nalidixic Acid in Chronic Pyelonephritis

Jameson¹

1965

BMJ

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“…Historically, nalidixic acid (Fig. 6) has been reserved for use only in urinary tract infections due to its poor tissue distribution and the rapid emergence of bacterial resistance (59,101). Many new fluoroquinolone derivatives of nalidixic acid have been developed, and these compounds possess much greater antibacterial potency than the original compound.…”

Section: Quinolonesmentioning

confidence: 99%

Discovery and development of new antimicrobial agents

Gootz

1990

Clin Microbiol Rev

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The unprecedented growth in the number of new antibiotics over the past two decades has been the result of extensive research efforts that have exploited the growing body of knowledge describing the interactions of antibiotics with their targets in bacterial cells. Information gained from one class of antimicrobial agents has often been used to advance the development of other classes. In the case of beta-lactams, information on structure-activity relationships gleaned from penicillins and cephalosporins was rapidly applied to the cephamycins, monobactams, penems, and carbapenems in order to discover broad-spectrum agents with markedly improved potency. These efforts have led to the introduction of many new antibiotics that demonstrate outstanding clinical efficacy and improved pharmacokinetics in humans. The current review discusses those factors that have influenced the rapid proliferation of new antimicrobial agents, including the discovery of new lead structures from natural products and the impact of bacterial resistance development in the clinical setting. The development process for a new antibiotic is discussed in detail, from the stage of early safety testing in animals through phase I, II, and III clinical trials.

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“…Its two major metabolites are 7-hydroxynalidixic acid (HNA), which exhibits antibacterial properties equal to NA (McChesney et al, 1964;Moore et al, 1965;Portmann et al, 1966) and 7-carboxynalidixic acid (CNA), which is inactive.…”

Section: Methodsmentioning

confidence: 99%

Nalidixic acid kinetics in renal insufficiency.

Cuisinaud¹,

Ferry²,

Pozet³

et al. 1982

Brit J Clinical Pharma

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1 A pharmacokinetic study of nalidixic acid (NA) and metabolites was carried out in 23 patients with differing renal function so as to determine the influence of renal insufficiency on the excretion and biotransformation rate of this antibacterial agent. Plasma and urine concentration of NA and of its 7-hydroxy (HNA) and 7-carboxy (CNA) derivatives were measured after a single oral administration. 2 Renal insufficiency did not markedly affect the renal clearance of NA while it significantly decreased the elimination rate of HNA, a compound which largely excreted into the urine. 3 Interestingly, CNA which could never be detected in the plasma of patients with normal renal function appeared in that of patients with renal insufficiency. Plasma concentrations of CNA and creatinine were positively related, and the amount of urinary CNA increased with the renal impairment.4 These results suggest that HNA can still be biotransformed into CNA by the impaired kidney. Since CNA cannot be easily excreted in the urine of patients with renal insufficiency it is hypothesized that this compound back diffuses into the plasma. 5 Finally, the study of the urinary concentrations of NA and metabolites shows that a standard NA dosage can be used, at least in patients with mild renal insufficiency.

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Absorption, excretion, and metabolism of a new antibacterial agent, nalidixic acid

Cited by 121 publications

References 1 publication

Tissue Concentration of Nalidixic Acid in Chronic Pyelonephritis

Tissue Concentration of Nalidixic Acid in Chronic Pyelonephritis

Discovery and development of new antimicrobial agents

Nalidixic acid kinetics in renal insufficiency.

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