Flomoxef (FMOX) was examined for its efficacy and safety in treating paranasal sinusitis by clinical studies and laboratory examination of its tissue concentration and antibacterial potency. 1. The C_max of 1g of FMOX after an intravenous injection were 55.8μg/g, 57.6μg/g and 8.0μg/ ml in the maxillary sinus mucosa, nasal polyp, and maxillary sinus secretion, respectively. The T1/2 of the serum concentration was at 1.49 hours. 2. The MIC₈₀ of FMOX against Gram-positive and Gram-negative bacteria isolated from patients with sinusitis were 0.39μg/ml and 1.56μg/ml, respectively. 3. The treatment was considered effective by the attending physicians in 88.9% of those patients with acute exacerbation of chronic sinusitis, in 41.7% of those with chronic sinusitis, and in 74.5% of all patients. 4. In a standardized evaluation, the clinical efficacy rate of FMOX was judged to be 88.9% against acute sinusitis, 88.2% against acute exacerbation of chronic sinusitis, 41.7% against chronic sinusitis, and 76.6% against all patients. 5. The rates of bacterial disappearance when using FMOX against the different types of bacteria encountered were as follows: 79.2% for Gram-positive bacteria, 89.5% for Gram-negative, and 100% for anaerobic bacteria. The overall disappearance rate for all types of bacteria was 84.7%. 6. Side effects were noted in two of the 56 patients. One reported discomfort in the lower abdomen, and the other, a strange feeling in the mouth. These side effects were minor, which the patients could tolerate, and treatment was continued. No abnormal value was observed in laboratory findings. 7. FMOX was judged to be effective in treating acute sinusitis by 83.3% of the physicians, for acute exacerbation of chronic sinusitis by 82.4%, for chronic sinusitis by 33.3% and against all sinusitis cases, by 70.2%. From these results, FMOX is considered to be highly useful for the treatment of paranasal sinusitis.

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Fundamental and clinical evaluations of the safety and effectivity of FMOX in treating diseases caused by bacterial infections concerning the otorhinolaryngological field were done, and the following results were obtained. 1. FMOX was effective against S. aureus, S. pyogenes, Klebsiella sp., H. influenzae, B. catarrhalis, Anaerobic streptococci and Peptostreptococcus sp. isolated from patients with Various types of otorhinolaryngological infections, most notably, suppurative otitis media. The following data correspond to the MIC of FMOX for each of the above bacteria:≤6.25μg/ml, ≤0.78μg/ml, ≤0.39μg/ml, ≤0.78μg/ml, ≤0.78μg/ml, ≤1.56μg/ ml and≤0.78μg/ml, respectiVely. For S. aureus, FMOX had a far greater antibacterial effect than CTM or LMOX. 2. The maximum concentration in tissue (C_max) of 1g FMOX administered intravenously, was 25.6μg/g in the middle ear and 11.1μg/ml in the tonsils. 3. The percent efficiency of FMOX was measured against a standardized evaluation. FMOX was 56.9% effective against otitis media, 93.4% effective against tonsillitis, 100% effective against pharyngitis and laryngitis, and 75.2% effective against all infections. Physicians evaluated FMOX to have an efficacy of 79.7% against all infections. 4. The rate of bacterial disappearance was high: in infections of Gram-positive bacteria alone, 89.8%, and 75.0% in infections of Gram-negative bacteria alone. FMOX was also rated high at dealing with complex bacterial infections, including those with S. aureus. 5. The percent utility of FMOX was 62.1% against otitis media, 96.7% against tonsillitis, 64.7% against other infections, and 76.5% against all infections. 6. Mild side effects were noted in 5 patients (2.8%: gastrointestinal symptoms and hypersensitivity of the skin). Laboratory examinations uncovered abnormal findings primarily suggesting mild hepatic and renal dysfunction in 7 patients (6.2%), but these Were all temporary. From these results, FMOX is considered to be highly useful for the treatment of otorhinolaryngological infections, most notably suppurative otitis media.

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A double-blind comparative clinical trial was conducted on Lomefloxacin (NY-198), a new synthetic antibiotic, to objectively evaluate its efficacy, safety and usefulness in the treatment of acute lacunar tonsillitis using Norfloxacin (NFLX) as the control drug. Either NY-198 (n=115) or NFLX (n=117) was administered in a daily dosage of 600mg in 3 divided doses for 7 days. The following results were obtained: 1. The clinical efficacy rate as evaluated by the investigators was 82.2% in the NY-198 group and 83.8% in the NFLX group. The difference between the two groups was not statistically significant. 2. The clinical efficacy rate when evaluated by committee was 75.7% in the NY-198 group and 85.6% in the NFLX group. This was not a significant difference. 3. The bacteriological efficacy rates were high. Eradication rates of 92.1% and 96.5% were obtained in the NY-198 and NFLX groups, respectively, and the difference was not signifi cant. Nor were significant differences noted in the bacteriological efficacies of the two drugs towards the various causative bacterium. 4. No significant differences in terms of overall safety were observed between the two groups. Side effects were noted in 6 of 112 cases in the NY-198 group (5.4%) and 3 of 116 cases (2.6%), but the difference was not statistically significant. The side effects were mainly digestive tract symptoms and allergic reactions. All the side effects were transient, and mild or moderate in severity. Abnormal laboratory test values were recorded in 5 patients in the NY-198 group (11.6%) and one patient in the NFLX group (2.1%). The difference between the two groups was not statistically significant. None of the abnormal laboratory test values were severe, and all were transient. 5. The usefulness rate (satisfactory or better) was 80.7% in the NY-198 group, and 86.5% in the NFLX group. These rates were not statistically significant. On the basis of the above results, NY-198 was considered as useful as NFLX in the treatment of acute lacunar tonsillitis.

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A double-blind study was conducted on lomefloxacin (NY-198) to objectively compare its clinical effectiveness, safety and utility in patients with suppurative otitis media (acute suppur ative otitis media and acute exacerbation of chronic suppurative otitis media) to patients treated with pipemedic acid (PPA). Patients were given either 200mg t. i. d. of NY-198 or 500mg q. i. d. orally for 7 days. The following results were obtained. 1. The clinical efficacy rate in all cases was determined by the doctors in charge to be 61.7% (71/115) in the NY-198 group and 64.4% (76/ 118) in the PPA group. There was no statistically significant difference between the two groups (by either exact probability or the Wilcoxon rank sum test). The clinical efficacy was determined by the committee to be 60.0% (69/115) in the NY-198 group and 56.8% (67/118) in the PPA group. Again, the difference was not considered statistically significant. 2. The overall bacteriological effectivity, as measured by eradication rate, was 68.0% (68/100) for the NY-198 group and 66.7% (70/105) for the PPA group. This difference was not significant. However, in patients infected with a single strain of S. aureus, and in eradication or persistence of S. aurers, a higher eradica tion rate was observed for the NY-198 group (p<0.1, p<0.05, respectively). 3. Improvements in subjective and objective symptoms, and the overall improvement rate were assessed on the 3rd and 7th day of dosing. No significant differences were noted in either item for the two groups. 4. Side effects, consisting mainly of gastrointestinal tract symptoms, were observed in 4 cases out of 118 (3.4%) in the NY-198 group and in 7 out of 124 cases (5.6%) in the PPA group. Abnormal laboratory findings were noted in 5 out of 57 cases (8.8%) in the NY-198 group and in 4 out of 55 cases (7.3%) in the PPA group. Neither of these differences were statistically significant, nor was any significant difference observed in the overall safety between these two groups. 5. Utility was assessed by the doctors in charge of the cases by the clinical effectiveness and safety of the drugs. There was no statistical difference between the two groups. The utility rate was 60.0% (69/115) in the NY-198 group and 66.1% (80/121) in the PPA group. The above results suggest that NY -198 is a highly useful drug, when compared to PPA, in the treatment of suppurative otitis media.

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