The comparative pharmacokinetics of five quinolones

Wise, R.; Lister, D.; McNulty, C. A. M.; Griggs, Deborah; Andrews, J. M.

doi:10.1093/jac/18.supplement_d.71

Cited by 89 publications

(33 citation statements)

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“…Penetration of lomefloxacin into inflammatory fluid was 100%, which is comparable to that of oral norfloxacin (105%) (1), oral pefloxacin (99.3%) (9), oral fleroxacin (89.7%) (7), and intravenous or oral ciprofloxacin (121%) (11).…”

Section: Discussionmentioning

confidence: 74%

Pharmacokinetics and tissue penetration of orally administered lomefloxacin

Stone

Andrews

Ashby

et al. 1988

Antimicrob Agents Chemother

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The pharmacokinetics of the quinolone lomefloxacin were determined following a single 400-mg oral dose given to each of six male volunteers. Concentrations in serum, urine, and cantharidin-induced inflammatory fluid were determined by a microbiological assay. Samples from two volunteers were also assayed by high-performance liquid chromatography. The mean peak level in serum, 4.7 ,uglml, was attained within 1 h of administration. The mean elimination half-life from serum was 7 h. Inflammatory fluid was penetrated rapidly, with a mean peak level of 3.5 ,ug/ml occurring after 2.7 h. The mean recovery of lomefloxacin from urine over 48 h was 76% of the administered dose. There was a minor peak on the high-performance liquid chromatography trace, suggesting a small amount of unidentified metabolite. This was present only in urine; no detectable metabolites were found in serum. This study suggests that either once-daily or twice-daily dosage of lomefloxacin should be sufficient to treat urinary or systemic infections, respectively, caused by susceptible pathogens.

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Section: Discussionmentioning

confidence: 74%

Pharmacokinetics and tissue penetration of orally administered lomefloxacin

Stone

Andrews

Ashby

et al. 1988

Antimicrob Agents Chemother

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“…Total renal drug excretion (ofloxacin plus metabolites) after 200 mg i.v. reached means of 81.3% of the dose after 24 (25,50,100, and 200 mg) demonstrated a linear dose dependency of parenteral ofloxacin.…”

Section: Resultsmentioning

confidence: 92%

“…Ciprofloxacin, another parenteral quinolone, has biological half-lives of between 180 and 260 min (3,4,8,13,25), whereas biological half-lives of parenteral enoxacin (306 + 25 min [26]) and parenteral pefloxacin (630 + 90 min) were longer (10,26).…”

Section: Resultsmentioning

confidence: 99%

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Pharmacokinetics of ofloxacin after parenteral and oral administration

Lode

Höffken

Olschewski

et al. 1987

Antimicrob Agents Chemother

144

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In 10 volunteers, the pharmacokinetics of ofloxacin {HOE 280, DL 8280; (+)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido-[1,2,3-deI [1,4] 1.4 liters/kg of body weight) suggested effective diffusion into the extravascular space. High total and renal clearances indicated primarily renal excretion with additional elimination pathways, such as tubular secretion and extrarenal elimination. After oral administration, absorption was excellent, and the absolute bioavailability following 200 mg of ofloxacin could be calculated at >0.95. Maximal concentrations in serum were attained 1.2 to 1.9 h after dosing; areas under the curve increased in proportion to dose between 200 and 400 mg of oral ofloxacin. The amount of known metabolites (demethyl and N-oxide compounds) excreted in urine reached only 4.3% (intravenously) and 4.0% (orally). Transient headaches in some volunteers were the only side effects registered.6-Fluoro-7-piperazino-4-quinolones are noteworthy both for the wide range and intensity of activities against gramnegative bacilli and cocci in vitro and the capacity to control experimentally induced systemic infections with selected bacteria when administered orally in well-tolerated doses (9,15,27).Ofloxacin {HOE 280, DL 8280; (±)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl) -7-oxo-7H-pyrido[1,2,3-de] [1,4]benzoxacine-6-carboxylic acid} is a new quinolone carboxylic acid derivative showing a broad antimicrobial spectrum against gram-positive and gram-negative bacteria (1,11,17,22,27). This substance was found to be more active than norfloxacin and pipemidic acid (22), its in vitro antibacterial activity being almost comparable to those of gentamicin, tobramycin, and newer cephalosporins (9,11,27). When first introduced, ofloxacin could only be administered orally, but recently a parenteral form was developed.The purpose of this study was to investigate the pharmacokinetic properties of this quinolone after oral and intravenous (i.v.) administration of various doses to determine the bioavailability and metabolism of this drug.(Part of this study was presented at the 24th Interscience

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“…The same accounts for the elimination half-lives, about 4 and 7 h, respectively. Both compounds have relatively high distribution volumes: for ofloxacin, it is about 100 to 120 liters, and it is even higher for ciprofloxacin (33,36,61,62).…”

Section: Vitro Activitymentioning

confidence: 99%