Cinoxacin concentrations in Plasma, Urine and Prostatic Tissue after Oral Administration to Man

Burt, Robert A.; Morgan, Timothy W.; Payne, J. P.; Bonner, R. M.

doi:10.1111/j.1464-410x.1977.tb04089.x

Cited by 13 publications

(4 citation statements)

References 7 publications

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“…Serum and urinary levels, as well as pharmacokinetic parameters of Cinoxacin determined in this study are in agreement with the data reported in the literature (1,2,3, 6,7,13,15,20). For pipemidic acid however we have found a larger percentage of urinary recovery (83% over 24 h) than cited by Humbert et al (12) (63% over 24 h) or Soussy et al (22) (48.3% over 24 h).…”

Section: Discussionsupporting

confidence: 82%

Comparative pharmacokinetic profiles of Cinoxacin and pipemidic acid in humans

Jm¹,

Comte²,

Lavillaureix³

1983

European Journal of Drug Metabolism and Pharmacokinetics

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Serum and urinary levels of Cinoxacin and pipemidic acid were determined at 7-day intervals in the same 10 healthy volunteers after a single oral dose of respectively 500 and 400 mg of the drugs. Comparison of results shows that Cinoxacin was absorbed faster (absorption half-life, ta 1/2cin = 0.25 h) than pipemidic acid (ta 1/2pip = 0.37 h) and distributed in a smaller apparent volume (AVDcin = 23.5 1/1.73 m2; AVDpip = 60.1 1/1.73 m2). Biological half-lives were identical (tb 1/2cin = 2.10 h; tb 1/2pip = 2.15 h). On the other hand, serum levels for Cinoxacin at 1, 2 and 4 hours (8.1 +/- 1.5 micrograms/ml, 10.6 +/- 1.5 micrograms/ml, 5.6 +/- 1.3 micrograms/ml respectively) were higher than those for pipemidic acid (3.3 +/- 0.3 micrograms/ml, 3.4 +/- 0.5 micrograms/ml, 2.1 +/- 0.5 micrograms/ml respectively). Urinary excretion of the two derivatives during the 12 hours following their administration was similar (Ucin0-12h = 86%; Upip0-12h = 83%). Mean urinary concentrations were particularly high, still attaining respectively 90 +/- 29 micrograms/ml and 131 +/- 38 micrograms/ml in samples collected between the 9th and the 12th hours; these levels were well above the M.I.C. for the Gram-negative organisms included within the spectrum of activity of these two quinolones. In addition, predictive calculations of serum levels reached after multiple dosing indicate that at an administration rate of 500 mg every 6 or preferably every 4 hours, Cinoxacin concentrations should be sufficiently high to be of interest in the treatment of systemic infections by sensitive organisms.

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Section: Discussionsupporting

confidence: 82%

Comparative pharmacokinetic profiles of Cinoxacin and pipemidic acid in humans

Jm¹,

Comte²,

Lavillaureix³

1983

European Journal of Drug Metabolism and Pharmacokinetics

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“…Other investigators reported this phenomenon in patients after 0.25-g (14) and 0.5-g doses (3,4). Similar variations in peak serum concentrations and time to reach peak concentrations have been observed with other orally administered agents (7,8).…”

Section: Resultsmentioning

confidence: 98%

“…Cinoxacin (Cinobac; 1-ethyl-1,4-dihydro-4-oxo [1,3] dioxolo- [4,5-g] cinnoline-3-carboxylic acid) is a synthetic organic antibacterial which has good in vitro antimicrobial activity against Enterobacteriaceae but negligible activity against Pseudomonas aeruginosa and gram-positive cocci (5,9,10,12,13,16). As expected from in vitro activity, cinoxacin has been shown to be clinically effective in the treatment of urinary tract infections caused by these microorganisms (2, 11, 14, 15, 17; C. E. Cox, Abstr.…”

mentioning

confidence: 99%

Pharmacology of Cinoxacin in Humans

Black

Israel

Wolen

et al. 1979

Antimicrob Agents Chemother

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Cinoxacin was almost completely absorbed when given orally and was found to be approximately 60 to 70% protein bound. Peak serum concentrations were reached within 2 h, and detectable serum concentrations persisted up to 12 h after administration of 0.25-, 0.5-, and 1-g multiple oral doses. Although food delayed the absorption and caused a 30% reduction in mean peak serum concentrations, the overall 24-h urinary recovery was not significantly altered. Approximately 50 to 55% of the drug was excreted in the urine as unchanged drug. At 12 h, urine concentrations were still above the minimal inhibitory concentration for most common gram-negative urinary pathogens. Cinoxacin was well tolerated when administered to 23 volunteers from 10 to 28 days. Resistance among fecal isolates initially susceptible to cinoxacin was not observed in nine volunteers who were administered 0.5 g every 12 h for 4 to 28 days.

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“…Except for day 1, a. serum sample was also taken just before administration of the morning dose. Urine was collected on the same days at 3,6, and 12 h after drug administration. To evaluate the safety of the drug, the following laboratory tests were performed before and at the end of the treatment: serum creatinine, blood urea nitrogen, creatinine clearance, total bilirubin, serum glutamic-oxaloacetic transaminase, and alkaline phosphatase, as well as leukocyte count, hemoglobin, and hematocrit.…”

mentioning

confidence: 99%

Cinoxacin: pharmacokinetics and tolerance in patients with normal and impaired renal function

Maigaard¹,

Frimodt‐Møller²,

Welling³

et al. 1979

Antimicrob Agents Chemother

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The pharmacokinetics of cinoxacin, a new antibacterial compound related to nalidixic acid and oxolinic acid, were investigated in 22 patients with varying degrees of renal impairment. After oral administration of cinoxacin at 500 mg every 12 h for 7 days to all patients, the drug was found to be well tolerated. The urine concentrations of cinoxacin in all patients far exceeded the minimal inhibitory concentrations for susceptible organisms commonly found in urinary tract infections. The serum half-life of cinoxacin in patients with normal renal function was approximately 2.7 h but increased to approximately 8.5 h in patients with creatinine clearance less than 30 ml/min. No undue drug accumulation was demonstrated in any patient group during the treatment. Highly significant correlations were found between the elimination rate constant and creatinine clearance and also between the elimination half-life and serum creatinine. The bioavailability of cinoxacin was independent of renal function.

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Cinoxacin concentrations in Plasma, Urine and Prostatic Tissue after Oral Administration to Man

Cited by 13 publications

References 7 publications

Comparative pharmacokinetic profiles of Cinoxacin and pipemidic acid in humans

Comparative pharmacokinetic profiles of Cinoxacin and pipemidic acid in humans

Pharmacology of Cinoxacin in Humans

Cinoxacin: pharmacokinetics and tolerance in patients with normal and impaired renal function

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