Drugs online research references
Pathol Biol (Paris). 1988 Jun;36(5 Pt 2):719-23.
[The role of ciprofloxacine metabolites in its biliary and urinary elimination in man]
[Article in French]
Brogard JM, Jehl F, Blickle JF, Arnaud JP, Monteil H.
Service de Medecine Interne, Faculte de Medecine, Centre Hospitalo-Universitaire, Strasbourg.
The purpose of the present work was the investigation of the urinary and biliary eliminations of M1, M2, M3 and M4, the four metabolites of ciprofloxacin in twelve recently cholecystectomized patients provided with a T-drain. The four metabolites were measured by HPLC under isocratic conditions for M2 and M4, and by gradient elution for M1 and M3. After a single oral dose of 500 mg of ciprofloxacin, the 24th urinary elimination of the parent compound and its metabolites respectively amounted to 130.1 +/- 15.6; 13 +/- 11; 46.6 +/- 8.2; 13 +/- 3.7 and 0 mg, representing 26.02; 0.54; 1.32; 2.60 and 0% of the administered dose (total: 192.4 mg; 38.5%). During the same investigation period, the biliary elimination respectively reached 1,587 +/- 222; 241 +/- 38; 11,042 +/- 2,489; 144 +/- 51 and 19 +/- 13 micrograms (total: 13 mg) corresponding to 0.32; 0.05; 2.21; 0.03 and 0% (total: 2.61%) of the dose. The urinary and biliary elimination of ciprofloxacin as metabolites respectively represents 12.5 and 2.3% of the dose (total: 14.8%). The important amount of M2 recovered in bile (7 times more than ciprofloxacin itself) let suggest a hepatic biotransformation of ciprofloxacin.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3054754&dopt=Abstract
Antimicrob Agents Chemother. 1987 Mar;31(3):430-3.
In vitro and in vivo activity of ciprofloxacin against enterococci isolated from patients with infective endocarditis.
Fernandez-Guerrero M, Rouse MS, Henry NK, Geraci JE, Wilson WR.
In vitro activity of ciprofloxacin against 27 strains of enterococci was inoculum dependent. Using inocula of 10(5) to 10(6) or 10(7) to 10(8) CFU of enterococci per ml, the MICs for 50 and 90% of strains tested increased from 1 to greater than or equal to 128 micrograms of ciprofloxacin per ml with the higher inoculum compared with the lower inoculum. The MBC for 50% of strains tested increased from 2 to greater than 128 micrograms/ml and the MBC for 90% of strains tested increased from 8 to greater than 128 micrograms of ciprofloxacin per ml with the lower and higher inocula, respectively. The combination of penicillin-gentamicin was more effective in vitro than the combination of ciprofloxacin-gentamicin against the low or high inoculum of enterococci. Using two strains of enterococci, we studied the efficacy of ciprofloxacin in the treatment of enterococcal experimental endocarditis in rabbits. Ciprofloxacin used alone or combined with gentamicin was significantly less effective (P less than 0.01) than procaine penicillin alone or procaine penicillin combined with gentamicin for the treatment of enterococcal experimental endocarditis. The combination of ciprofloxacin-procaine penicillin was not a more effective therapy than procaine penicillin alone.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3579260&dopt=Abstract
Scand J Infect Dis Suppl. 1986;49:115-23.
Frequency and expression of mutational resistance to the 4-quinolone antibacterials.
Smith JT.
The frequency with which Escherichia coli mutated to resist a series of ten 4-quinolone antibacterials was studied. It was found that the mutation frequency could not be predicted from the potency of the drugs against sensitive bacteria. The mutation rates were lowest with ofloxacin, norfloxacin and ciprofloxacin. No mutants were observed with ofloxacin while less mutants were observed with norfloxacin than with ciprofloxacin, despite the latter possessing greatest activity against susceptible bacteria. The mutation frequencies observed with nalidixic acid, cinoxacin, pipemidic acid, flumequine, rosoxacin, oxolinic acid, and enoxacin were much higher than those observed with the three 4-quinolones mentioned earlier. When the sensitivities of the mutants to 4-quinolones were investigated, it was again found that the potency of each 4-quinolone against sensitive bacteria did not correlate with the levels of resistance of mutants to that drug. However, when the relative activities of the 4-quinolones against the mutants were investigated, it was found that no mutant isolated resisted a concentration exceeding the peak serum levels of ciprofloxacin, norfloxacin or ofloxacin. Although some mutants exhibited more resistance than the maximum attainable serum levels of the other 4-quinolones, the sensitivity of all the mutants fell well within the urine levels of pipemidic acid, flumequine, rosoxacin, oxolinic acid, enoxacin, norfloxacin, ofloxacin, and ciprofloxacin.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3547618&dopt=Abstract
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