Disease relevance of Pefloxacine

• Toxic reaction following treatment of typhoid fever with pefloxacin [1].
• Side-effects of pefloxacin in idiopathic nephrotic syndrome [2].
• Pefloxacin for falciparum malaria: only modest success [3].
• Pefloxacin may offer a new, efficacious, and safe therapy for gram-negative meningitis [4].
• Ten patients with acute meningitis caused by gram-negative bacteria were treated with pefloxacin intravenously for a mean period of 10 days [4].

Psychiatry related information on Pefloxacine

• An acute psychotic disorder caused by pefloxacin: a case report [5].
• Five patients given ciprofloxacin had to discontinue because of unwanted effects (mostly hallucinations), one patient given pefloxacin had gastric pain and two patients given ofloxacin developed a skin rash [6].
• Ocular films of pefloxacin mesylate were prepared with the objectives of reducing the frequency of administration, to improve patient compliance, obtaining controlled release and greater therapeutic efficacy in the treatment of eye infections such as conjunctivitis, keratitis, kerato conjunctivitis, corneal ulcers etc [7].

High impact information on Pefloxacine

• Pharmacokinetics of ciprofloxacin in maternal blood and amniotic fluid were studied after two doses of ciprofloxacin (200 mg intravenously every 12 hours), after two doses of pefloxacin (400 mg intravenously every 12 hours), and after two doses of ofloxacin (400 mg intravenously every 12 hours) [8].
• Pefloxacin treatment of meningitis caused by gram-negative bacteria [4].
• Eight patients responded clinically to pefloxacin treatment, and the causative organisms were eradicated from the cerebrospinal fluid in 9 of the 10 patients [4].
• The extent to which the fluoroquinolones undergo biotransformation in the liver ranges from approximately 50 percent for pefloxacin to about 6 percent for ofloxacin [9].
• The mean breast milk levels of pefloxacin were 3.54, 3.43, 2.93, 2.24, 1.79, and 0.88 micrograms/ml, and of ofloxacin, 2.41, 1.91, 1.25, 0.64, 0.29, and 0.05 micrograms/ml [8].

Chemical compound and disease context of Pefloxacine

• At 4 h, no bacteremia was observed in Cip-treated rats, whereas 93% of the Pef-treated rats and 80% of the Ofl-treated rats were bacteremic (P < 0.001) [10].
• UBTs for Proteus mirabilis of pefloxacin are significantly higher than those of fleroxacin [11].
• Systemic prophylaxis of experimental staphylococcal endophthalmitis: comparative efficacy of sparfloxacin, pefloxacin, imipenem, vancomycin, and amikacin [12].
• Once-daily pefloxacin + teicoplanin vs netilmicin + teicoplanin in empirical therapy for fever and neutropenia [13].
• Comparative efficacies of ciprofloxacin, pefloxacin, and vancomycin in combination with rifampin in a rat model of methicillin-resistant Staphylococcus aureus chronic osteomyelitis [14].

Biological context of Pefloxacine

• 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) [15].
• The relative bioavailability of pefloxacin after the antacid treatment was 44.4% +/- 23.8%, compared with that after a single administration [16].
• Effects on oral and intestinal microfloras of norfloxacin and pefloxacin for selective decontamination in bone marrow transplant patients [17].
• Our results indicate that ofloxacin and pefloxacin do not induce inhibition of myelopoiesis [18].
• Data from mainly non-comparative studies suggest that pefloxacin has the potential for use in a variety of serious or difficult-to-treat and nosocomially acquired infections in hospitalised and immunocompromised patients [19].

Anatomical context of Pefloxacine

• 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 [20].
• Randomized, double-blind comparison of single-dose regimens of rufloxacin and pefloxacin for acute uncomplicated cystitis in women. French Multicenter Urinary Tract Infection-Rufloxacin Group [21].
• The intracellular postantibacterial effects of 0.1 microgram of pefloxacin, ciprofloxacin, and ofloxacin per ml, which were left in contact with L. pneumophila-infected human macrophages for 24 h, were evaluated at various times after removal of the drugs [22].
• Pefloxacin-induced achilles tendon toxicity in rodents: biochemical changes in proteoglycan synthesis and oxidative damage to collagen [23].
• Despite a relatively low incidence of serious side effects, fluoroquinolones and the fluoroquinolone pefloxacin have been reported to occasionally promote tendinopathy that might result in the complication of spontaneous rupture of tendons [23].

Associations of Pefloxacine with other chemical compounds

• In animals with P. aeruginosa or S. marcescens infections, resistance to pefloxacin diminished or disappeared after treatment with the combinations of pefloxacin plus ceftriaxone or pefloxacin plus amikacin [24].
• CONCLUSIONS: Enoxacin and to a lesser extent pefloxacin may cause clinically relevant interactions with further CYP1A2 substrates [20].
• Mutant strains 34PEFr, which was resistant to pefloxacin (128-fold increase in the MIC), and 34CTXr, which was resistant to cefotaxime (32-fold increase in the MIC) and which was derived from the susceptible parent 34s, were obtained by serial passages on pefloxacin and cefotaxime gradient plates, respectively [25].
• Cmax and AUC of fleroxacin were statistically significantly greater (P less than 0.05) compared to pefloxacin (Cmax: 5.62 vs. 4.09 mg/l, AUC0-48: 65.9 vs. 48.7 mg/l.h, AUC0-infinity: 70.7 vs. 51.5 mg/l.h) [26].
• In-vitro activity of lomefloxacin in comparison with pefloxacin and ofloxacin [27].

Gene context of Pefloxacine

• We therefore further characterized the interaction between pefloxacin and CYP1A2 [20].
• The behavioral and convulsant effects of pefloxacin (PEFLO), a quinolone derivative, were studied after intraperitoneal (i.p.) administration to Dilute Brown Agouti DBA/2J (DBA/2) mice, a strain genetically susceptible to sound-induced seizures [28].
• No inhibitory activity against purified IL-1 or IL-2 could be demonstrated in the dialyzed supernatants from pefloxacin- or ciprofloxacin-treated monocytes [29].
• Neither pefloxacin nor ciprofloxacin modified the biological activity of preformed IL-1 [29].
• Moreover, IL-2, a known mediator of apoptosis was found to be downregulated, whereas TNF-alpha had been upregulated for the first 18 hours after pefloxacin administration [30].

Analytical, diagnostic and therapeutic context of Pefloxacine

• Comparison of plasma and dialysate concentrations of pefloxacin after intravenous, oral, or intraperitoneal administration shows excellent bidirectional diffusion of the quinolone through the peritoneal membrane, demonstrating that therapeutical concentrations can be achieved in the dialysate after intravenous or oral administration [31].
• The concentrations of pefloxacin and its metabolites in plasma and urine were determined by high-performance liquid chromatography assays [16].
• Pefloxacin pharmacokinetics and serum bactericidal activities (SBA) against Escherichia coli and Staphylococcus aureus were compared after intravenous infusion of either a single 800-mg dose or twice-daily 400-mg doses into 16 healthy volunteers [32].
• Clinical trials with pefloxacin in patients at risk for P. carinii pneumonia appear to be justified [33].
• The results (expressed as mean log10 CFU per milliliter +/- standard deviation) showed that pefloxacin significantly (P < 0.001) reduced the bacterial counts (4.39 +/- 0.97) compared with those in control eyes (6.46 +/- 0.69) [34].

References