Rufloxacin is a new long-acting, once-daily quinolone antibacterial agent. We evaluated inter-and intrasubject variations in pharmacokinetics of rufloxacin following oral administration of 400 mg (two capsules) under controlled conditions, at an interval of 2 weeks (periods I and II), to 12 healthy male subjects. Plasma and urine samples were collected up to 48 h after drug administration. Plasma drug levels determined by bioassay were higher than those measured by high-performance liquid chromatography, indicating that one or more active metabolites were formed. Individual high-performance liquid chromatography plasma rufloxacin concentrations were fitted with a one-compartment open model with first-order input. There were considerable variations in the plasma concentration-time profiles among subjects; for example, the elimination half-life in plasma varied from 14.6 to 95.5 h. However, pharmacokinetic parameters calculated for the two periods did not differ significantly. These results suggest that the intrasubject variation in the pharmacokinetics of rufloxacin is usually small in spite of the considerable intersubject variation.Rufloxacin (MF 934; Fig.

The in vitro activity of rufloxacin (MF 934), a new broad-spectrum fluoroquinolone, was tested against 1,032 gram-positive and gram-negative clinical isolates and compared to that of five other compounds of this class. All quinolones except for ciprofloxacin had limited activity against group A and B streptococci and pneumococci (MIC 90% of 4–64 mg/l) and no activity against enterococci. Most species of the enterobacteriaceae and staphylococci were found to be sensitive to rufloxacin (MIC 90% of 0.5–8 and 2–8 mg/l). Like the other quinolones except for ciprofloxacin, rufloxacin was not active against Pseudomonas aeruginosa.The antibacterial activity of rufloxacin was affected only minimally by an increase in the bacterial inoculum or by alterations in the pH of the medium. In spite of the relatively higher MICs of rufloxacin compared to those of the other quinolones, its favorable pharmacokinetic properties may account for its good clinical efficacy.

ABSTRACT— In 67 patients (mean age 51 years, range 26–79), at diagnosis of primary haemochromatosis (PH), grade III or IV liver iron overload was present in all cases, cirrhosis in 85%, transferrin saturation > 80% in 75%, serum ferritin > 1000 μg/1 in 84%, and overt diabetes in 48%. Alcohol intake was > 150 g/day in 11 patients; six were chronic hepatitis B surface antigen (HBsAg) carriers. HLA‐A3 and B7 antigens were present in 64% and 23% versus respectively 22% (p<0.01) and 9% (p<0.025) in controls. Iron overload was found in the stomach, duodenum, skin and bone marrow in 57, 43, 45 and 59% of the patients studied. Sixty‐three patients were followed for 1–260 months (median 24); 43 received regular iron‐depleting treatment and 20 did not because of liver failure, cancer or refusal. Cumulative survival was 79%, 67% and 61% at 1, 4 and 10 years, respectively. Ten patients died from hepatocellular carcinoma and two from extrahepatic cancer. The early high mortality rate was due to some cases of advanced disease or cancer. Cumulative survival in the regularly treated group was 95% at 1 year and 91% at 4 and 10 years, which was higher than in the untreated group.

The efficacy and safety of rufloxacin once daily was compared with that of ofloxacin b.i.d. for therapy of complicated cystitis and upper urinary tract infections. Eighty-three patients were randomly assigned to receive rufloxacin as a loading dose of 400 mg on the first day, followed by 200 mg s.i.d., and 80 received ofloxacin 300 mg b.i.d. Both agents were administered orally for a median duration of eight days. Bacterial elimination rates after treatment were 90% for rufloxacin and 81% for ofloxacin. Half of the treatment failures occurred in patients with infections caused by uropathogens that became either less sensitive or resistant to the quinolones being studied. At a two-week follow-up, recurrences had not occurred in any of the rufloxacin patients and had occurred in 17% of the ofloxacin patients. Minor adverse reactions were reported by 12 and 13 patients, respectively. Rufloxacin once daily is as effective as ofloxacin b.i.d. for the treatment of complicated cystitis and upper urinary tract infections.