In Vitro Antimicrobial Activity of Cinoxacin Against 2,968 Clinical Bacterial Isolates

Jones, Ronald N.; Fuchs, Peter

doi:10.1128/aac.10.1.146

Cited by 22 publications

(4 citation statements)

References 6 publications

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“…Although older drugs of this class, such as nalidixic acid or cinoxacin, are active against a wide range of gram-negative bacteria, they are relatively inactive against Pseudomonas aeruginosa and gram-positive cocci (6). The MICs of the older agents against most enteric gram-negative organisms relative to achievable drug concentrations are such that use of those drugs has been generally limited to the treatment of urinary tract infections (1).…”

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In vitro activity of ciprofloxacin, a new carboxyquinoline antimicrobial agent

Eliopoulos¹,

Gardella²,

Moellering³

1984

Antimicrob Agents Chemother

175

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The in vitro activity of ciprofloxacin (Bay o 9867), a new carboxyquinoline antimicrobial agent, was compared with those of norfloxacin, nalidixic acid, and several other oral and parenteral antimicrobial agents. Ciprofloxacin was substantially more active than nalidixic acid or cinoxacin against all gramnegative bacteria tested. Virtually all strains of Enterobacteriaceae were inhibited by the new drug at concentrations of <0.125 p.g/ml. Ciprofloxacin was more active than norfloxacin against Klebsiella sp., Enterobacter sp., and Serratia marcescens, and it was the most active agent tested against Pseudomonas aeruginosa (MIC90, 0.5 ,ug/ml). The new drug also demonstrated significant activity against gram-positive cocci, inhibiting all strains of staphylococci at concentrations of '1.0 ,ug/ml. Ciprofloxacin was bactericidal at concentrations near the MIC against most isolates tested. Although stepwise increases in resistance were seen with Escherichia coli and P. aeruginosa during serial passage on plates containing incremental concentrations of the drug, significant resistance did not emerge during incubation of strains in broth containing concentrations of ciprofloxacin above the MBC.Ciprofloxacin (Bay o 9867) is a recently developed carboxyquinoline antimicrobial compound which is structurally related to nalidixic acid (20). Although older drugs of this class, such as nalidixic acid or cinoxacin, are active against a wide range of gram-negative bacteria, they are relatively inactive against Pseudomonas aeruginosa and gram-positive cocci (6). The MICs of the older agents against most enteric gram-negative organisms relative to achievable drug concentrations are such that use of those drugs has been generally limited to the treatment of urinary tract infections (1). Several new quinoline derivatives, including norfloxacin (7,8,10,11), AT-2266 (2, 9), and ofloxacin (14), are not only more potent than nalidixic acid against susceptible enteric gram-negative bacteria, but also demonstrate significant activity against organisms resistant to the older drugs, including P. aeruginosa and many gram-positive bacteria. The present study examines the in vitro activity of ciprofloxacin against routine clinical isolates of gram-negative bacteria and against selected gram-positive organisms in comparison with those of other orally or parenterally administered antimicrobial agents.(This work was presented in part at the 13th International Congress of Chemotherapy, Vienna, Austria, 28 August-2 September 1983.) MATERIALS AND METHODS Bacterial strains. Gram-negative bacteria used in this study were routine clinical isolates recently collected in our hospital. Duplicate isolates from individual patients were excluded, but organisms were otherwise unselected. Strains of Campylobacter jejuni and routine gram-positive isolates had been collected earlier at the Massachusetts General Hospital. Penicillin-resistant pneumococci and viridans streptococci were obtained as previously reported (4) Louis, Mo. Sultamicillin was simulated using...

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confidence: 99%

In vitro activity of ciprofloxacin, a new carboxyquinoline antimicrobial agent

Eliopoulos¹,

Gardella²,

Moellering³

1984

Antimicrob Agents Chemother

175

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“…Like nalidixic, oxolinic, piromidic and pipemidic acids, it is structurally centered by the cinnolin ring ( Figure I). Its antimicrobial spectrum includes the majority of gram-negative bacteria (except for Pseudomonas aeruginosa), in particular enterobacteriaceae (1, 9,11,14,16). Furthermore, Cinoxacin seems to inhibit the transfer of a number of R-factors, even in cases where either the donor or the recipient organism is nalidixic acid-resistant (19).…”

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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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“…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.…”

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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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In Vitro Antimicrobial Activity of Cinoxacin Against 2,968 Clinical Bacterial Isolates

Cited by 22 publications

References 6 publications

In vitro activity of ciprofloxacin, a new carboxyquinoline antimicrobial agent

In vitro activity of ciprofloxacin, a new carboxyquinoline antimicrobial agent

Comparative pharmacokinetic profiles of Cinoxacin and pipemidic acid in humans

Pharmacology of Cinoxacin in Humans

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