An uncontrolled, open label study of 10% tosufloxacin granules in pediatric pneumonia

Tosufloxacin(TFLX) granules, a fluoroquinolone antibiotic agent, was administered at 4 mg/kg or 6 mg/kg twice daily in children with bacterial pneumonia to evaluate its ease of administration, efficacy, safety and plasma concentration. The efficacy at dosing completion or discontinuation was 100% (48 of 48 cases), eradication was 70.9% (39 of 55 strains) and 23 (63.9%) of 36 patients showed bacteria eradication. In administration, 28.6% (18 of 63) of patients reported it "very easy to take" and 68.3% (43/63) "easy to take." Adverse events reported by 45 patients numbered 109 and occurrence was 71.4% (45 of 63). The most frequently reported adverse reactions were diarrhea (22.2%, 14 of 63 patients) and vomiting (20.6%, 13 of 63 patients). No severe adverse events were reported and 6 adverse events moderate in severity were reported by 6 patients (2 cases of diarrhea and 1 case each of vomiting, bronchitis, thermal burns and rhinorrhoea). Mild adverse events reported by 45 patients numbered 103. Of 63 patients, 28 reported 41 adverse reactions at an occurrence of 44.4%. Frequently reported adverse reactions were diarrhea (11.1%, 7 of 63 patients) and vomiting (9.5%, 6 of 63 patients). One moderate adverse reaction was reported by a patient (diarrhea) and 40 cases of mild adverse reactions were reported by 28. Five cases of joint-related adverse reactions in the use of quinolone antibiotics were reported by as many children (2 cases of arthralgia and 1 case each of neck pain, pain in extremity, and pain). Neck pain, pain in extremity, and pain were deemed unrelated to the study drug and two cases of arthralgia were deemed possibly related. MMP-3 collected from 2 patients with arthralgia was not elevated from values measured before dosing and arthralgia resolved within a short time and was not clinically significant. No clear correlation was observed between subject background factors and adverse event occurrence. Adverse event occurrence by dose regimen was 65.8% (25 of 38 patients) in the 4 mg/kg group and 80.0% (20 of 25 patients) in the 6 mg/kg group, meaning that adverse events occurred more frequently in the higher dosage group. Plasma drug concentration in children with bacterial pneumonia dosed at 4 mg/kg or 6 mg/kg fell within the range of plasma concentrations in adults dosed at 102 mg and 204 mg (approved dosage), suggesting the same level of efficacy in both. TFLX administration at 4 mg/kg or 6 mg/kg twice daily in children with bacterial pneumonia is thus expected to be clinically highly beneficial.