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At least 19 recordsLinked to original sources
PubMed2006

Preparation of anti-pefloxacin antibody and development of an indirect competitive enzyme-linked immunosorbent assay for detection of pefloxacin residue in chicken liver.

Pefloxacin has been increasingly used in veterinary medicine to treat microbial infections. To avoid using a labor-intensive instrumental method to detect the residue of pefloxacin in food, a simple and convenient indirect competitive enzyme-linked immunosorbent assay method has been developed in this study. The antibody generated from immunogen cationized bovine serum albumin-pefloxacin showed high sensitivity toward pefloxacin with an IC50 value of 6.7 ppb in buffer and was suitable for a screening assay to detect the residue of pefloxacin in food products. The antibody has been assessed using rapid enzyme immunoassays to exploit its specificity. The antibody prepared shows cross-reactivity with a few other (fluoro)quinolones including fleroxacin (116%), enrofloxacin (88%), and ofloxacin (10%). The assay measured drug residue in chicken liver spiked with pefloxacin with an interassay coefficient of variation of 13.6% or less and an intra-assay coefficient of variation of 10.9% or less. The average recovery rates at 0.5, 5, 10, 50, and 100 ppb were in the range of 86-106% for interassay and in the range of 87-103% for intra-assay, respectively.

Animals↗
PubMedDate not supplied

[Pefloxacin + metronidazole versus netilmicin + metronidazole in the prevention of nosocomial infections in contaminated surgery. Pefloxacin Study Group].

Pefloxacin plus metronidazole versus netilmicin plus metronidazole in the prevention of nosocomial infections during contaminated surgery. Surgical prophylaxis is widely used in contaminated surgery, especially colorectal surgery. In this clinical trial the efficacy of pefloxacin 800 mg i.v. slow infusion associated to metronidazole 500 mg i.v. 1-2 hours before surgery and then metronidazole alone after 6 and 12 hours versus netilmicin 200 mg i.m. associated to metronidazole 500 mg i.v. 1-2 hours before surgery and then both after 6 and 12 hours were evaluated in 97 patients suffering by colorectal surgery. Efficacy of prophylaxis in patients was evaluated in terms of appearance of post-surgical infections (abdominal, urinary, respiratory and wound infections). In pefloxacin + metronidazole group (53 patients), two cases of wound infections (3.8%) and three cases of respiratory infections (5.8%) were observed. In netilmicin + metronidazole group (44 patients), two cases of wound infections (4.9%), three cases of urinary infections (7%), three cases of respiratory infections (7.5%) and one case of intra-abdominal infection were observed. Our data confirmed that in colorectal surgery, the association pefloxacin, drug with microbiological and pharmacokinetics characteristics suitable for prophylaxis + metronidazole, active against anaerobes pathogens, prevents post-surgical infections as well as a reference association (netilmicin + metronidazole), with the advantage of a single administration.

Adolescent↗
PubMed1997

Bactericidal effect of pefloxacin and fosfomycin against Pseudomonas aeruginosa in a rabbit endocarditis model with pharmacokinetics of pefloxacin in humans simulated in vivo.

The bactericidal activity of pefloxacin and fosfomycin alone and in combination against Pseudomonas aeruginosa was evaluated in an experimental rabbit endocarditis model after 24 h of treatment. Two strains with intermediate susceptibility to pefloxacin and good susceptibility to fosfomycin were tested. The serum kinetics obtained during administration of 400 mg every 12 h in humans were simulated in the animals using computer-controlled variable-flow infusion. Fosfomycin was administered as a continuous infusion at a constant flow, allowing a steady-state concentration of 47.4 +/- 11.9 mg/ml to be reached in serum. In valvular vegetations, pefloxacin was less bactericidal than fosfomycin, and in combination treatment, it reduced (but did not abolish) the bactericidal effect of fosfomycin. The duration of the pretreatment interval (12-48 h) had a negative effect on the bactericidal activity of both drugs, especially that of fosfomycin.

Animals↗
PubMed1997

[Pefloxacin versus ceftriaxone in single-dose antibiotic prophylaxis in general clean-contaminated surgery. The Pefloxacin Study Group].

Single-shot surgical prophylaxis is today used in all clean-contaminated surgery, because it is able to reduce the incidence of post-surgical infections. The aim of this clinical trial is to evaluate the efficacy of Pefloxacin 800 mg i.v. slow infusion in single administration 1-2 hours before surgery versus ceftriaxone 2 g i.v. 1-2 hours before surgery in 297 patients suffering from clean-contaminated surgery, especially biliary surgery and gastrectomy. Efficacy of prophylaxis in 259 patients, evaluable according to the protocol, was evaluated in terms of appearance of post-surgical infections (urinary, respiratory and wound infections). In the Pefloxacin group (128 patients), no cases of wound infections were observed, except one case of wound sterile secretion, without dehiscence, (0.81%), one case of urinary infection (0.81%) and three cases of respiratory infections (2.34%). In the ceftriaxone group (131 patients), three cases of wound sterile secretion without dehiscence (2.36%), one case of urinary infections (0.76%) and four cases of respiratory infections (3.05%) were observed. From this study we can conclude that single-shot surgical prophylaxis with pefloxacin, drug with microbiological and pharmacokinetics characteristics suitable for prophylaxis, is able to prevent postsurgical nosocomial infections as well as ceftriaxone, considered a reference drug largely used in this indication.

Adolescent↗
PubMed1986

Pharmacokinetics of pefloxacin after repeated intravenous and oral administration (400 mg bid) in young healthy volunteers.

Multiple-dose kinetics of pefloxacin was determined in 12 normal male subjects given 400 mg pefloxacin by iv 1 h-infusion every 12 h for 16 doses. Twelve other subjects (6 men and 6 women) were given 400 mg pefloxacin by mouth every 12 h for 18 doses. Plasma and urine concentrations of pefloxacin and its main metabolites (N-desmethyl pefloxacin or norfloxacin and pefloxacin N-oxide) were measured by high performance liquid chromatography. The bioavailability of pefloxacin was complete and plasma concentrations after iv or oral administration were similar. Pefloxacin was rapidly absorbed from the gastrointestinal tract and reached maximum plasma concentrations about 1 h after dosing. Pefloxacin elimination (T 1/2 beta) increased from 11.00 +/- 2.64 h after the first iv dose to 13.93 +/- 3.58 h after the last iv dose (P less than 0.01). Apparent total body clearance decreased from 148.5 +/- 47.6 to 106.9 +/- 39.2 ml/min (P less than 0.01) because of decreased non-renal clearance (apparent volume of distribution did not significantly change over the repeated pefloxacin administration). Similar results were obtained after repeated oral dosing. Renal clearance of pefloxacin was low (7.47 +/- 2.28 ml/min) indicating that non-renal clearance represents the major route of elimination of this quinolone. Urinary excretion of pefloxacin and N-desmethyl and N-oxide metabolites was approximately 31% of the pefloxacin dose and beta-elimination half-lives of these metabolites were very close to that of pefloxacin (13.34 +/- 2.72 h and 11.95 +/- 2.64 h respectively). Due to a possible saturable process in the metabolic pathway, some accumulation occurred during repeated iv or oral treatment (accumulation ratio = 1.37 +/- 0.20). These results show that concentrations of pefloxacin in excess of the minimum inhibitory concentrations for many important pathogens can be rapidly achieved in plasma and urine with the 400 mg bid regimen with both iv and oral routes.

Administration, Oral↗
PubMed1986

The comparative in-vitro activity of pefloxacin.

The in-vitro antibacterial activities of pefloxacin, other 4-quinolones and representative beta-lactams and aminoglycosides were assessed by determination of minimum inhibitory concentrations (MICs). Pefloxacin (MICs mostly 0.03-2 mg/l) was highly active against Enterobacteriaceae. Gentamicin had slightly lower activity, and ceftazidime and norfloxacin similar activities to pefloxacin whereas ciprofloxacin was more active. Pefloxacin (MICs 0.03-2 mg/l) was active against Acinetobacter but again ciprofloxacin was more active. Aeromonas was highly susceptible to pefloxacin and norfloxacin (MICs 0.008-0.03 mg/l) as well as to ciprofloxacin (MICs 0.001-0.008 mg/l). Pefloxacin (MICs 1-8 mg/l) had similar activities to ceftazidime and gentamicin against Pseudomonas aeruginosa but tobramycin (MICs 0.25-32 mg/l), norfloxacin (MICs 0.25-4 mg/l) and ciprofloxacin (MICs 0.06-1 mg/l) were generally more active. Haemophilus influenzae was susceptible to pefloxacin (MICs 0.008-0.06 mg/l) and to norfloxacin and ciprofloxacin, all of which were more active than ampicillin or ceftazidime. Gardnerella vaginalis was not very susceptible to pefloxacin (MICs 2-8 mg/l), the other 4-quinolones or gentamicin but ampicillin and ceftazidime were highly active. Neisseria gonorrhoeae was very susceptible to pefloxacin and norfloxacin (MICs 0.016-0.12 mg/l) and ciprofloxacin (MICs 0.002-0.008 mg/l). The activity of pefloxacin (MICs 0.25-1 mg/l) was similar to that of ciprofloxacin (MICs 0.12-2 mg/l) but greater than that of norfloxacin (MICs 0.5-4 mg/l) against Staphylococcus aureus. Vancomycin (MICs 1-2 mg/l) had similar activity in vitro but whilst gentamicin was highly active against some isolates, others were resistant. Pefloxacin (MICs mostly 4-32 mg/l) and the other 4-quinolones had lower activity against streptococci (including alpha-, beta-, and non-haemolytic strains, enterococci and pneumococci) than against staphylococci. Benzylpenicillin (or ampicillin in the case of enterococci) were usually more active than any of the 4-quinolones. Bacteroides species, both of the fragilis and melaninogenicus/oralis groups were generally moderately resistant to pefloxacin (MICs 2-32 mg/l) and norfloxacin though ciprofloxacin was more active. Whilst the activity of pefloxacin and the other 4-quinolones was generally somewhat higher against the other anaerobes, ampicillin generally had greater activity.

Acinetobacter↗
PubMed1990

Pefloxacin versus ceftazidime in therapy of soft tissue infections in compromised patients.

Soft tissue infections in compromised patients are frequently caused by Gram-negative organisms and particularly by Pseudomonas aeruginosa. These pathogens are effectively eradicated by pefloxacin as well as by ceftazidime. The effectiveness and safety of these two agents were compared in a prospective randomized study in 67 patients with soft tissue infections. Underlying conditions included malignant diseases, diabetes mellitus and chronic renal failure. The infections included: post operative infection, septic foot, soft tissue abscess and cellulitis. Thirty-three patients were treated with intravenous ceftazidime for a mean duration of ten days. More than half the 34 patients given pefloxacin were treated only orally for a mean period of 13 days. The clinical and bacteriological outcomes were similar in both groups. There was clinical cure or improvement in 26 pefloxacin cases and in 23 ceftazidime cases, failure in six pefloxacin cases and in seven ceftazidime and relapse in two pefloxacin and in three ceftazidime patients. The bacteriological responses were eradication in 23 pefloxacin cases and in 22 ceftazidime cases, persistence in five pefloxacin cases and in six ceftazidime cases, relapse in one pefloxacin case and in none of the ceftazidime group, reinfection in four pefloxacin cases and in three ceftazidime cases and there was one unassessed patient in the pefloxacin group and two in the ceftazidime group. Nausea and vomiting occurred in three patients and elevation of liver enzymes in another patient; all side effects were observed only in the pefloxacin treated patients. These results suggest that oral pefloxacin could offer an alternative to intravenous ceftazidime in half the compromised patients with tissue infections. However, adverse reactions due to pefloxacin administration should be watched for during such therapy.

Administration, Oral↗
PubMed1989

Antimicrobial activity and interaction of pefloxacin and its principal metabolites. Collaborative Antimicrobial Susceptibility Testing Group.

The in vitro antimicrobial activity of pefloxacin and its major metabolites was determined and the interaction of pefloxacin and N-demethyl pefloxacin (norfloxacin) assessed at the ratio naturally occurring in urine (1:2). Pefloxacin and N-demethyl pefloxacin had approximately the same spectrum but were markedly more active than N-oxide pefloxacin (MIC90s greater than or equal to 64 micrograms/ml) against 867 stock strains. When combined with N-demethyl pefloxacin, pefloxacin had greater potency and a broader spectrum in tests against 5869 fresh clinical organisms. For approximately 10% more strains pefloxacin MICs were less than or equal to 2 micrograms/ml when pefloxacin was combined with 2 parts (4 micrograms/ml) of N-demethyl pefloxacin. The most significant extension of the pefloxacin spectrum was to include non-enteric gram-negative bacilli (inhibition of 67% versus 88%) and enterococci-streptococci (inhibition of 33% versus 86%). These results are similar to those previously noted for enoxacin plus 3-oxo-enoxacin, and potentially achievable with other newer fluoro-quinolones undergoing significant metabolism.

Anti-Bacterial Agents↗
PubMed1999

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

BACKGROUND AND OBJECTIVES: Pefloxacin is reported to cause clinically relevant inhibition of theophylline metabolism in vivo, but in vitro pefloxacin was only a weak inhibitor of the cytochrome P450 CYP1A2, mediating main theophylline biotransformation. We therefore further characterized the interaction between pefloxacin and CYP1A2. METHODS: A randomized 3-period change-over study was conducted in 12 healthy young volunteers on the steady-state interactions between pefloxacin or enoxacin (400 mg twice a day) with caffeine (183 mg once daily), a validated marker of CYP1A2. Caffeine pharmacokinetics were estimated after its fifth dose. Studies in human liver microsomes were carried out to measure the effect of pefloxacin and norfloxacin on caffeine 3-demethylation, an in vitro CYP1A2 probe, and to identify the enzyme(s) that mediate pefloxacin N-4'-demethylation with selective inhibitors. RESULTS: For the in vivo study, ANOVA-based point estimates (90% confidence intervals [CI]) for the ratios of caffeine pharmacokinetics with and without pefloxacin coadministration were 1.11 for maximal steadystate plasma concentrations (Cmax,ss; 90% CI, 0.99 to 1.26), 0.53 for total clearance (CLt,ss; 90% CI, 0.49 to 0.58), and 1.04 for the beta-phase distribution volume (Vdbeta; 90% CI, 0.96 to 1.13). The values for enoxacin were 1.99 for Cmax,ss (90% CI, 1.77 to 2.23), 0.17 for CLt,ss (90% CI, 0.16 to 0.19), and 1.01 for Vdbeta (90% CI, 0.90 to 1.13). Thus pefloxacin caused a 2-fold decrease in caffeine clearance, and enoxacin caused a 6-fold decrease in caffeine clearance. In vitro, norfloxacin and pefloxacin competitively inhibited CYP1A2, with inhibition constant (Ki) values of 0.1 and 1 mmol/L, respectively, and CYP1A2 was the only enzyme with a relevant contribution (approximately 50%) to pefloxacin N-4'-demethylation. CONCLUSIONS: Enoxacin and to a lesser extent pefloxacin may cause clinically relevant interactions with further CYP1A2 substrates. The data suggest that the pefloxacin interaction is partly mediated by its major metabolite norfloxacin.

Adult↗
PubMed2001

Pharmacokinetics of pefloxacin and its interaction with cyclosporin A, a P-glycoprotein modulator, in rat blood, brain and bile, using simultaneous microdialysis.

1. In vivo microdialysis with HPLC was used to investigate the pharmacokinetics of pefloxacin and its interaction with cyclosporin A. Microdialysis probes were inserted into the jugular vein/right atrium, the striatum and the bile duct of male Sprague-Dawley rats. Biological fluid sampling thereby allowed the simultaneous determination of pefloxacin levels in blood, brain and bile. 2. Following pefloxacin administration, the brain-to-blood coefficient of distribution was 0.036. This was calculated by dividing the area under the concentration curve (AUC) of pefloxacin in brain by its AUC in blood (k=AUC(brain)/AUC(blood)). 3. When the P-glycoprotein cyclosporin A (10 mg kg(-1)) was co-administered with pefloxacin (10 mg kg(-1)), the AUC and the mean residence time in rat blood did not differ significantly (P>0.05). Similarly, the pharmacokinetics of pefloxacin in rat brain was not affected by the presence of cyclosporin A. 4. The AUC of unbound pefloxacin in bile was significantly greater than that in blood. The disposition of pefloxacin in rat bile shows a slow elimination phase following a peak concentration 30 min after pefloxacin administration (10 mg kg(-1), i.v.). The bile-to-blood coefficient of distribution (k=AUC(bile)/AUC(blood)) was 1.53. 5. The results indicated that pefloxacin was able to penetrate the blood-brain barrier and that the concentration in bile was greater than that in the blood, suggesting active biliary excretion of pefloxacin. Current data obtained from rats show no significant impact of cyclosporin A on the pharmacokinetics of pefloxacin in rat blood and brain when administered by concomitant i.v. bolus.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed2005

Pharmacokinetics and tissue residues of pefloxacin and its metabolite norfloxacin in broiler chickens.

1. The pharmacokinetics of pefloxacin and its active metabolite norfloxacin were investigated in chickens after a single oral administration of pefloxacin at a dosage of 10 mg/kg. To characterise the residue pattern, another group of chickens was given 10 mg of pefloxacin/kg body once daily for 4 d by oral route; the tissue concentrations of pefloxacin and norfloxacin were determined at 1, 5 and 10 d after the last administration of the drug. 2. The concentrations of pefloxacin and norfloxacin in plasma and tissues were determined by HPLC assay. The limit of detection for pefloxacin and norfloxacin was 0.03 microg/ml in plasma or microg/g in tissue. 3. The plasma concentration-time data for pefloxacin and norfloxacin were characteristic of a one-compartment open model. The elimination half-life, maximum plasma drug concentration, time to reach maximum plasma drug concentration and mean residence time of pefloxacin were 8.74 +/- 1.48 h, 3.78 +/- 0.23 microg/ml, 3.33 +/- 0.21 h and 14.32 +/- 1.94 h, respectively, whereas the respective values of these variables for norfloxacin were 5.66 +/- 0.81 h, 0.80 +/- 0.07 microg/ml, 3.67 +/- 0.21 h and 14.44 +/- 0.97 h. 4. Pefloxacin was metabolised to norfloxacin to the extent of 22%. 5. The concentrations of pefloxacin (microg/g) 24 h after the fourth dose of the drug declined in the following order: liver (3.20 +/- 0.40) > muscle (1.42 +/- 0.18) > kidney (0.69 +/- 0.04) > skin and fat (0.06 +/- 0.02). Norfloxacin was also detectable in all the tissues analysed except muscle. No drug and/or its metabolite was detectable in tissues except skin and fat 5 d after the last administration. The concentrations of pefloxacin and norfloxacin in skin and fat 10 d after the last dose of pefloxacin were 0.04 +/- 0.02 and 0.03 +/- 0.01 microg/g, respectively.

Adipose Tissue↗
PubMed1986

Transfer kinetics of pefloxacin into cerebro-spinal fluid after one hour i.v. infusion of 400 mg in man.

Nine subjects (5 women) aged between 17-66 years, with hydrocephalus were studied. An external ventricular drain was introduced for diagnostic purposes. Cerebro-spinal fluid (CSF) and plasma samples were obtained at suitable intervals after 1 h infusion of 400 mg pefloxacin. In plasma, pefloxacin Cmax was 8.54 +/- 1.53 (mean +/- S.E.M.) mg/l, at the end of infusion, whereas N-desmethyl pefloxacin concentration was 0.17 +/- 0.03 mg/l. The metabolite accounted for only 2% of plasma levels of pefloxacin. In CSF, pefloxacin Cmax was 2.97 +/- 0.32 mg/l, 5-6 h after the start of infusion, whereas N-desmethyl pefloxacin Cmax varied between 0.1-0.2 mg/l. Apart from the 1 h sample, the CSF/plasma ratio of pefloxacin was 60% which is similar to the unbound fraction of pefloxacin in plasma. The apparent half-life (T1/2) of transfer of pefloxacin from plasma to CSF was 1.26 +/- 0.18 h, assuming a first order process, while the apparent elimination T1/2 in CSF was 13.40 +/- 1.76 h, which is similar to the elimination T1/2 found previously in plasma, thus accumulation of pefloxacin in CSF is unlikely. With the present dosage regimen, CSF quickly attains therapeutic levels of pefloxacin.

Adolescent↗
PubMed2000

[Effectiveness of combined vancomycin and pefloxacine in gastrointestinal decontamination for preventing infections after chemotherapy-induced bone marrow aplasia. A randomized double-blind study].

OBJECTIVE: To test the value of the combination of pefloxacin and vancomycin as gastro-intestinal tract decontamination for the prevention of infections in patients with chemotherapy-induced neutropenia. PATIENTS AND METHODS: Oral pefloxacin plus vancomycin (48 patients), pefloxacin alone (51 patients), or placebo (52 patients) were administered in a randomized double-blind study. Evaluation was done by determining site and documentation of infections, organisms responsible for bacteriologically documented infections, organisms acquired in surveillance cultures and number of days with fever during aplasia. RESULTS: Patients receiving pefloxacin had significantly fewer episodes of bacteremia with enterobacteriacae. No differences were noted between patients treated by pefloxacin and those who received a combination of pefloxacin with vancomycin regarding gram-positive (Gram+) infections and infections with gram-negative (Gram-) organisms usually resistant to pefloxacin. However, placebo gave similar results. There was no induction of resistance to pefloxacin during the study. Tolerance of treatment was excellent. Only a prolonged aplasia has been observed in patients receiving pefloxacin. CONCLUSION: Thus, the combination of vancomycin with pefloxacin was not more efficacious than pefloxacin only for the prevention of Gram+ infections in the neutropenic patient. The systematic use of antibiotics as gastrointestinal tract decontamination for the prevention of infections in patients with aplasia may be questionable.

Adult↗
PubMed1988

Pharmacokinetics of pefloxacin and amikacin administered simultaneously to intensive care patients.

Ten adult patients with severe infections in an intensive care unit were treated simultaneously with 6 mg/kg pefloxacin and 7.5 mg/kg amikacin, infused i.v. over 1 h every 12 h for 5 days. Twelve h after the last infusion, pefloxacin alone was administered orally (400 mg tablet) every 12 h for 10 days. The pharmacokinetics of pefloxacin and its main metabolites, norfloxacin and pefloxacin N-oxide, were determined after the first (Day 1) and last (Day 5) infusions and after the last oral dose (Day 15). The kinetics of amikacin was determined after the first and the last infusion. The maximal and minimal steady-state plasma concentrations of amikacin were 27.3 and 3.3 mg/l. The total plasma clearance was 83.1 and 67.0 ml/min after the first and the last infusions, respectively, and the half-life was 3.9 and 5.0 h. The maximal and minimal steady-state plasma concentrations of pefloxacin were 13.1 and 7.9 mg/l after i.v. infusion and 13.4 and 9.0 mg/l after oral administration. Pefloxacin elimination (t1/2) increased from 11.3 h after the first infusion to 19.4 h after the last infusion and 21.1 h after the last oral dose. Total body clearance decreased from 90.8 (Day 1) to 51.9 (Day 5) and 56.4 ml/min (Day 15). The volume of distribution did not change significantly over the course of pefloxacin. Mean steady-state plasma concentrations of norfloxacin and pefloxacin N-oxide were respectively 0.5-0.6 mg/l and 0.9-1.3 mg/l after intravenous and oral administration of pefloxacin. There were no pharmacokinetic interaction between the drugs. The dosage regimen led to plasma concentrations of pefloxacin and amikacin within their therapeutic range.

Aged↗
PubMedDate not supplied

Urine bactericidal activity of pefloxacin versus norfloxacin in healthy female volunteers after a single 800-mg oral dose.

In an open randomised crossover study the antibacterial activity of pefloxacin and norfloxacin was assessed in the urine after a single 800-mg oral dose in 14 healthy female volunteers. Pefloxacin demonstrated lower peak concentrations in the urine than norfloxacin (mean, 217.2 mg/l versus 492.9 mg/l as determined by the microbiological assay) but pefloxacin was present over a longer period of time in sufficient concentrations than norfloxacin. Mean urine levels of at least 2 mg/l were present for 7 days after pefloxacin administration and 2 days after norfloxacin administration as determined by the microbiological assay. Overall, the urinary recovery of pefloxacin and norfloxacin amounted to 49.3% and 25.1%, respectively, of the total administered dose. The average urine bactericidal activity against the five test organisms was as follows: against reference strain Escherichia coli ATCC 25922 susceptible to nalidixic acid (Nal-S) for 5 days with pefloxacin and 2 days with norfloxacin; against three clinical isolates, one strain each of E. coli resistant to nalidixic acid (Nal-R), Klebsiella pneumoniae Nal-R, and Staphylococcus saprophyticus, for 3 days with pefloxacin and 24 h with norfloxacin; and against a clinical isolate of Enterococcus faecalis for 2 days with pefloxacin and 12 h with norfloxacin. In conclusion, pefloxacin as a single dose proved to have sufficiently high and long-lasting urine bactericidal activity against urinary pathogens. These findings support the results of a meta-analysis of seven clinical trials in patients with uncomplicated lower UTI, demonstrating a single oral dose of 800 mg pefloxacin to be as effective as a conventional treatment with comparative drugs.

Administration, Oral↗
PubMed1991

Influence of rifampin on the pharmacokinetics of pefloxacin.

Pefloxacin and rifampin are frequently associated in the antibiotic therapy of deep-seated, and especially bone-located, infections. The influence of rifampin, a potent drug metabolism enzyme inducer, on the pharmacokinetics of pefloxacin was studied in a randomized crossover trial involving eight young healthy male volunteers. Every volunteer received either pefloxacin alone (period A) or pefloxacin after a 10-day induction by rifampin (period B) given as a 900 mg daily oral dose, and both periods were separated by a 3-week washout period. During both periods, pefloxacin was given during 3 days as a 400 mg b.i.d. oral dose (six doses) followed by a 400 mg intravenous dose on the fourth day. The kinetics of pefloxacin are significantly influenced by rifampin: The minimum (12-hour) plasma concentration, area under the concentration-time curve, and elimination half-life decreased respectively from 4.26 +/- 1.57 to 2.70 +/- 1.00 mg/L, 78.91 +/- 22.82 to 57.81 +/- 16.69 mg.hr/L, 14.46 +/- 3.46 to 10.08 +/- 2.44 hours (p less than 0.05). The renal clearance of pefloxacin was unchanged, but the plasma clearance increased from 94.04 +/- 39.04 to 126.82 +/- 47.36 ml/min (p less than 0.05). The plasma clearance of N-demethyl and N-oxide metabolites were similar for both periods, but the cumulative renal excretion (0 to 96 hours) decreased significantly (p less than 0.01) for period B versus period A. This definite but moderate inductive effect of rifampin on the pharmacokinetics of pefloxacin does not suggest a dose modification of pefloxacin in therapeutic association with rifampin, but pefloxacin assay in plasma seems to be advisable.

Adult↗
PubMed1986

In-vitro activity of pefloxacin compared to other antibiotics.

Pefloxacin is a new quinolone carboxylic acid with a broad spectrum of antibacterial activity. A comparison was made of the in-vitro activity of pefloxacin and that of nine other antibiotics (ampicillin, ticarcillin, piperacillin, cefazolin, cefotaxime, ceftazidime, gentamicin, amikacin and norfloxacin). The MIC90 of pefloxacin against 500 strains of Enterobacteriaceae ranged from 0.25 mg/l (Escherichia coli, indole + Proteus spp., Enterobacter cloacae, Salmonella spp. and Shigella spp.) to 1 mg/l (Klebsiella pneumoniae). Pefloxacin inhibited 90% of 52 strains of Pseudomonas aeruginosa at 2.5 mg/l (range 0.25 mg/l-4 mg/l). The MIC90 of pefloxacin against 100 Staphylococcus aureus strains (78 oxacillin resistant strains) was 0.4 mg/l (range 0.12-0.5 mg/l). It was markedly less active against Streptococcus faecalis and Str. pneumoniae (37 strains of each species) the MIC90 being 4 mg/l against both species. Overall, pefloxacin was at least as active as the third-generation cephalosporins against Enterobacteriaceae and was more active than any other antibiotic tested against P. aeruginosa, S. epidermidis, and S. aureus. Against E. coli, pefloxacin had a more rapid anti-bacterial activity than piperacillin. A paradoxical effect was observed with pefloxacin. An optimal killing rate was observed at concentrations of pefloxacin compatible with those one can expect in blood of patients treated with this drug.

Anti-Bacterial Agents↗