Fleroxacin is a new synthetic fluorinated quinolone antimicrobial agent. The in-vitro activity of fleroxacin and five comparative quinolones against 541 clinical isolates was studied. Minimum inhibitory concentrations (MIC90) of fleroxacin were less than or equal to 2.0 mg/l for Enterobacteriaceae, less than or equal to 8.0 mg/l for Pseudomonas aeruginosa and 1.0 mg/l for Acinetobacter calcoaceficis and 8 mg/l for streptococci. The activity of fleroxacin was comparable with that of ofloxacin, pefloxacin and norfloxacin, but less than that of ciprofloxacin. All quinolones showed little difference between MIC and minimum bactericidal concentrations (MBCs).

In an open non-comparative clinical trial with the aim of evaluating the clinical efficacy and safety of a 14 day course of 2 g ceftriaxone once daily, 46 patients with neuroborreliosis were entered at the Infectious Diseases Teaching Hospital in Prague 8. In 39 patients the diagnosis was early Lyme neuroborreliosis. Seven patients suffered from late stage disease. Clinical results were 30% of patients cured at the end of treatment and 85% after 9 months in early stage disease. In late stage disease two patients out of seven were cured and four had improved after 12 months. One patient died because of cardiac infarction. In no patient had treatment to be discontinued because of adverse reactions to antibiotics.

A total of 35 patients with late stage Lyme borreliosis with involvement of the joints was followed up until 3 years after a 14 day course of 2 g ceftriaxone once daily i.v. Diagnosis was confirmed by indirect and direct microbiological methods as well as clinical signs and symptoms. Long term clinical results in 26 patients at 36 months were complete response or marked improvement in 19, relapse in six and new manifestations in four of the cases, respectively. Possible mechanisms for non-responding to therapy are discussed. Therapy was well tolerated; in no case discontinuation of treatment was necessary due to adverse drug reactions. The treatment results in this group of 35 patients with Lyme arthritis are considered successful. The data obtained are consistent with expectations based on the published experiences with ceftriaxone in this indication.

A randomized double blind study in long term malaria chemoprophylaxis was performed to compare the tolerability of Fansimef (1 tablet containing 250 mg mefloquine + 500 mg sulfadoxine + 25 mg pyrimethamine per week) with chloroquine (300 mg per week). 211 Austrian industrial workers and their families in Warri, Nigeria, participated in this study; 101 received Fansimef and 110 chloroquine for 3-18 months (mean 41 weeks). Prophylaxis was discontinued because of adverse effects in 7 volunteers in the Fansimef group (mainly insomnia, palpitations, dizziness, nausea and headache) and in 2 volunteers of the chloroquine group (headache and loss of hair in one volunteer, nausea, dizziness and vomiting in the other). Most of the adverse effects could be due to the mefloquine component. A few minor complaints of burning eyes, nausea and gastric pain were reported in both groups. Laboratory checks performed at 3-monthly intervals showed a slight, transient and clinically irrelevant (but statistically significant) increase of serum glutamic-oxalacetic transaminase and gamma-glutamyl transpeptidase at month 3 in the Fansimef group. An attack of acute Plasmodium falciparum malaria occurred in one volunteer 6 weeks after discontinuation of prophylaxis with Fansimef. Antibodies against blood stage parasites could be demonstrated by the indirect immunofluorescence test at different stages of the study, indicating that these two antimalarials are not causal prophylactic agents.

We report the results of several trials aimed at evaluating the quinolones in urogenital infections. In Chlamydia trachomatis infections, ofloxacin (200 mg b.i.d. for 10 days) gave a cure rate of 98% (n = 66), and fleroxacin (400 mg s.i.d. for 7 days) provided a cure rate of 89% (n = 19). A double-blind study comparing fleroxacin (600 mg s.i.d.) to doxycycline (100 mg b.i.d.) for 7 days showed similar high cure rates for both regimens (100%; n = 23). In Mycoplasma hominis infections, ofloxacin (200 mg b.i.d. for 10 days) yielded a cure rate of 86% (n = 50) for M. hominis and 55% (n = 43) for Ureaplasma urealyticum. Gonococcal infections (n = 122) were all cured by a single dose of 200 mg ofloxacin. Both ofloxacin and fleroxacin were well tolerated and may be recommended for patients with chlamydial or uncomplicated gonococcal infections, although 600 mg fleroxacin showed a higher incidence of adverse events compared to doxycycline.