Pefloxacin Clinical Pharmacokinetics

Bressolle, Françoise; Gonçalves, Fátima; Gouby, A.; Galtier, M.

doi:10.2165/00003088-199427060-00003

Cited by 30 publications

(9 citation statements)

References 71 publications

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“…The concentrations of pefloxacin and enoxacin and their derived pharmacokinetic parameters in this study were very similar to those observed in previous multiple‐dose studies with 400 mg twice a day 26 , 27 , 28 . Likewise, caffeine pharmacokinetics without coadministration of a quinolone corresponded to published data 21 .…”

Section: Discussionsupporting

confidence: 87%

Interaction of pefloxacin and enoxacin with the human cytochrome P450 enzyme CYP1A2

Kinzig‐Schippers

Fuhr

Zaigler

et al. 1999

Clinical Pharmacology & Therapeutics

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Section: Discussionsupporting

confidence: 87%

Interaction of pefloxacin and enoxacin with the human cytochrome P450 enzyme CYP1A2

Kinzig‐Schippers

Fuhr

Zaigler

et al. 1999

Clinical Pharmacology & Therapeutics

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“…A chemical reaction was thought to occur between the chemical species in solution. The impregnated disc for the microbiological evaluation of pefloxacin was therefore based on the amount of pefloxacin effectively present for impregnation (Bressole et al, 1994).…”

Section: Discussionmentioning

confidence: 99%

The Pharmacokinetic and Biopharmaceutical Effect of Ascorbic acid (Vitamin C) on Pefloxacinon Concurrent Administration in Human

Awofisayo¹

2012

J. App. Pharm. Sci.

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The aim of the study was to assess the pharmacokinetic and biopharmaceutical effect of ascorbic acid (Vitamin C) on pefloxacin on concurrent administration in man through urine excretion data and microbiological evaluation. A two way crossover study was performed in ten healthy male volunteers aged (Mean ± SD) 45 ± 5.5 years and weight (Mean ± SD) 75.4 ± 12.5 Kg recruited and given pefloxacin 400mg as single dose and urine samples collected and pooled up at time intervals. The drug was concurrently given with 500mg vitamin C after a washout period of 4 weeks and urine samples similarly collected. Urine samples collected were analyzed and pefloxacin concentrations were determined with UV spectrophotometer from a validated calibration curve. The pharmacokinetic parameters Cmax, tmax, K e and t 1/2 were determined and compared. Microbial evaluation of the interaction of the drugs was performed through MIC determination using urinary isolate S. aureus (U-11420). The k e for pefloxacin alone was significantly lower than that for pefloxacin concurrently administered with vitamin C (0.1hr -1 and 0.3hr -1 ) P<0.05. The amount of pefloxacin excreted was significantly lower on single administration of pefloxacin compared to the co-administration with vitamin C, (44.13mg against 141.99mg) at P<0.05. The MIC obtained against S. aureus was 0.025mg/ml for pefloxacin alone while the co-solution with vitamin C at below 2hr and 4hr impregnation period was 0.05mg/ml and 0.1mg/ml respectively. There was significant chemical, microbiological and biopharmaceutical interaction on co-administration of pefloxacin with vitamin C.

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“…In humans, the bioavailability of numerous fluoroquinolones exceeds 90%, evidencing a good overall absorption (4,15,24). In the case of ciprofloxacin, an "absorption window" along the human gastrointestinal tract has been suggested (10).…”

Section: Discussionmentioning

confidence: 99%

Absorption of ofloxacin isomers in the rat small intestine

Rabbaa

Dautrey

Colas-Linhart

et al. 1997

Antimicrob Agents Chemother

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Ofloxacin, a chiral fluoroquinolone, possesses two optical isomers. The antibacterial activity of S-(-)-ofloxacin is 8 to 128 times higher than that of R-(+)-ofloxacin. In the rat, a saturable absorption process has been described for racemic ofloxacin. In the present study we investigated the mechanism underlying the in vivo intestinal absorption of ofloxacin enantiomers in the rat. Blood samples were collected from the portal vein. Our results show that the intestinal absorption of ofloxacin isomers is pH dependent, both enantiomers being best absorbed at neutral pH. S-(-)-Ofloxacin seems to have a greater affinity for the intestinal transporter (initial concentrations at 5 min [C(init)] are 0.17 +/- 0.04 and 0.12 +/- 0.03 microg/ml for S-(-)- and R-(+)-ofloxacin, respectively). Dipeptides fail to modify ofloxacin absorption, but amino acids reduce both isomers' absorption (C(init) is reduced by 53 and 33% with glycine for S-(-)- and R-(+)-ofloxacin, respectively, and by 59 and 42% with L-leucine). Gamma amino butyric acid interferes with the absorption of ofloxacin isomers, but less seriously than do amino acids. Furthermore, ofloxacin competes with other fluoroquinolones or P-glycoprotein substrates for a common secretory pathway, resulting in an increased rate of absorption for both ofloxacin isomers; this is probably an indirect result of their reduced efflux from the apical side of intestinal cells.

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Pefloxacin Clinical Pharmacokinetics

Cited by 30 publications

References 71 publications

Interaction of pefloxacin and enoxacin with the human cytochrome P450 enzyme CYP1A2

Interaction of pefloxacin and enoxacin with the human cytochrome P450 enzyme CYP1A2

The Pharmacokinetic and Biopharmaceutical Effect of Ascorbic acid (Vitamin C) on Pefloxacinon Concurrent Administration in Human

Absorption of ofloxacin isomers in the rat small intestine

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