Streptococcus pneumoniae is the most common organism causing acute otitis media (AOM). However, there have been some recent reports of clinical resistance to penicillin by S. pneumnoniae. The sequences of pemicillin-birlding pmtein (PBP), pbp 1a, pbp 2b, and pbp 2x, genes of penicillin-resistant S. pneumoniae (PRSP). were more highly divergent than those of penicillin-susceptible S. pneumoniae (PSSP). Polymerase chain reaction (PCR) can easily determine whether an S. pneumoniae isolate is susceptible or resistant to penicillin by amplifying the target gene through a combination of primers. In this study, S. pneumoniae (n=44) were obtained from the nasopharynx of infants and children with AOM. PCR was used to confirm the identification of isolates as S. pneumoniae by amplifying the autolysin gene (lyt A), and to detect three PBP genes by amplifying parts of pbp 1a, pbp 2 b and pbp 2x and macrolide-resistant gene by amplifying parts of ermAM and mef E. The resistance of S. pneumoniae to PCG and other β-lactams has been shown to be associated with mosaic mutations in the pbp 1 a, pbp 2 b and pbp 2x genes, and the resistance of S. pneumoniae to erythromycin and rokitamycin has been shown to be associated with ermAM and mefE genes. These findings suggest that rapid identification of PSSP, PISP and PRSP, or macrolide-resistant S. pneumoniae is possible and very useful for the effective treatment of AOM.

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This randomized, double-blind clinical study was conducted to compare the clinical efficacy, safety, and usefulness of gatifloxacin (GFLX, AM-1155), a new 8-methoxyquinolone, with that of levofloxacin (LVFX) in pneumonia. GFLX was administered at an oral dose of 200mg, twice a day, and LVFX at an oral dose of 100mg, three times a day, for 14days, and the following results were obtained:
1. Of the total of 226 patients enrolled, 200 (GFLX group: 100, LVFX group: 100) were eligible for evaluation of clinical efficacy.
2. The clinical efficacy rate was 98.0%(98/100) in the GFLX group, and 95.0%(95/100) in the LVFX group, and thus high efficacy was shown in both groups. The clinical equivalency of GFLX to LVFX was confirmed at Δ=10%, and the difference between the groups was not significant.
3. The bacteriological elimination rate was 100%(39/39) in the GFLX group and 87.5%(21/24) in the LVFX group, with no significant difference.
4. Side effects were noted in 10.4%(12/115) in the GFLX group and in 4.5%(5/110) in the LVFX group, and the difference between the two groups was not significant. The major events were diarrhea, sleepiness and dizziness.
5. Abnormal laboratory findings were observed in 14.2%(15/106) in the GFLX group and in 19.6%(21/107) in the LVFX group, and the difference between the two groups was not significant. The major events were mild elevations of transaminases.
6. The safety rate (“safe” in overall safety) was 76.4%(84/110) in the GFLX group and 76.6%(82/107) in the LVFX group, with no significant difference.
7. The usefulness rate (markedly useful+useful) was 92.9%(92/99) in the GFLX group and 89.8%(88/98) in the LVFX group, and the difference between the two groups was not significant.
The clinical equivalency of GFLX to LVFX was confirmed at Δ=10%. The bacteriological elimination rate was 100% in the GFLX group. There were no significant differences between the two groups in the incidence of side effects or abnormal laboratory findings. These results indicate that GFLX is a highly effective drug for the treatment of community-acquired pneumonia (bacterial, mycoplasmal, and chlamydial pneumonia).

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The present randomized, double-blind clinical study was conducted to compare the clinical efficacy, safety, and usefulness of gatifloxacin (GFLX, AM-1155), a new 8-methoxyquinolone, with that of levofloxacin (LVFX) in chronic respiratory tract infections. GFLX was administered at an oral dose of 200 mg, twice a day, and LVFX at an oral dose of 100 mg, three times a day, for 14 days. The results obtained are as follows:
1. Of the total 227 patients enrolled, 183 were eligible for evaluation of clinical efficacy (GFLX group: 93, LVFX group: 90).
2. The clinical efficacy rate was 98.9%(92/93) in the GFLX group and 77.8%(70/90) in the LVFX group, and the difference in clinical efficacy between the two groups was significant.
3. The bacteriological elimination rate was 90.9%(50/55) in the GFLX group and 85.4%(41/48) in the LVFX group, and the difference between the two groups was not significant.
4. Side effects were noted in 8.0%(9/112) in the GFLX group and in 9.3%(10/108) in the LVFX group, with no significant difference.
5. Abnormal laboratory findings were observed in 14.7%(15/102) in the GFLX group and in 11.7%(12/103) in the LVFX group, with no significant difference. The major events were mild elevations of transaminases.
6. The safety rate (“safe” in the overall safety) was 77.1%(81/105) in the GFLX group and 79.6%(82/103) in the LVFX group.
7. The usefulness rate (markedly useful + useful) was 93.5%(86/92) in the GFLX group and 78.2%(68/87) in the LVFX group, and the difference in usefulness rate between the two groups was significant.
Significant differences were observed between the two groups in clinical efficacy and usefulness rates, but there were no significant differences between the two groups in the incidences of side effects or abnormal laboratory findings. These results indicate that GFLX is one of the most highly effective drugs for the treatment of chronic respiratory tract infections.

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Clinical evaluation of a fluoroquinolone antimicrobial drug, gatifloxacin (GFLX) in the field of surgical infections were performed. The following results were obtained. GFLX was orally administered to 81 patients at a single dose of 100 mg or 200 mg twice a day for 3 to 7 days. Fourteen patients were excluded or dropped out, leaving 67 patients to be evaluated for clinical effects. The clinical responses at a dose of 100 mg twice a day were excellent in 21 cases, good in 7 cases, fair in 1 case and poor in 1 case, an efficacy rate of 93.3%(28/30), and at a dose of 200 mg twice a day were excellent in 19 cases, good in 12 cases, fair in 1 case and poor in 5 cases, an efficacy rate of 83.8%(31/37). The total efficacy rate was 88.1% in 67 patients with infections in surgery. The bacteriological efficacy rate was 84.5%(49/58). The eradication rate in 130 identified strains was 89.6%(43/48) in gram-positive bacteria, 100%(23/23) in gram negative bacteria, and 89.8%(53/59) in anaerobes, with a total rate of 91.5%(119/130). MIC₉₀ of GFLX against clinical isolates were 3.13μg/ml against 50 strains of gram-positive bacteria, 0.39μg/ml against 26 strains of gram negative bacteria and 1.56μg/ml against 65 strains of anaerobes. GFLX showed higher antibacterial activity against gram positive, gram-negative bacteria and anaerobes. With regard to safety, mild or moderate adverse reactions were observed in 3 cases, and abnormal changes of s-GOT, s-GPT and Al-Pase was observed in one patient and transient elevation of eosinophile was observed in one case. As mentioned above, GFLX is highly useful for infectious diseases in the surgical field.

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To evaluate objectively the clinical efficacy and cure rate of gatifloxacin (GFLX) 8-methoxyquinolone derivatives, in the 3-day and 7-day treatment of female acute uncomplicated cystitis, we performed a randomized double-blind comparative study. Only female patients with pain on micturition, pyuria of at least 10 WBCs/hpf and bacteriuria of at least 10⁴ CFU/mL were admitted to this study. Ninety-nine patients were randomly assigned to receive 100mg b. i. d. of GFLX for 3 days (group A) and 7 days (group B). The clinical efficacy was assessed on Day 7 and follow-up examinations were carried out on Day 14 and Day 35.
1. Using the criteria of the Japanese UTI Committee, clinical efficacy on Day 7 was evaluated in 34 patients in group A and 37 patients in group B. In this two groups, there were no significant differences in background characteristics of patients.
2. The overall clinical efficacy rate (excellent and moderate responses) was 97.1% in group A and 100% in group B, with no significant difference. The bacterial eradication rate was 97.1% of 35 strains in group A and 100% of 37 strains in group B, with no significant difference. The clinical efficacy rate as assessed by the doctor in charge was 97.1% in group A and 94.6% in group B, and assessments were performed in accordance with UTI criteria.
3. Final cure rate was 94.1%(32/34) in group A and 97.2%(35/36) in group B, with no significant difference.
4. The incidence of clinical adverse reactions was 4.3% of 46 patients in group A and 8.0% of 50 patients in group B, and of laboratory adverse reactions, 4.4% of 45 patients and 2.0% of 50 patients in group B, and the difference was not significant. None of the findings in adverse reactions were serious. Also no significant difference between the two groups in the overall safety rating and clinical value was noted.
From the results of this study, we conclude that GFLX is safe and effective for the treatment of acute uncomplicated cystitis, and 100mg b. i. d. for 3 days is sufficient as the dosage of GFLX.

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The clinical efficacies of gatifloxacin LX, a new 8-methoxyquinolone, on male urethritis were investigated. The subjects were 45 patients with gonococcal urethritis, 7 withgonococcal-chlamydial urethritis, 75 with chlamydial urethritis and 44 with nongonococcal-nonchlamydial urethritis. GFLX was administered orally at a dose of 200 mg twice a day for 3 days to the patients with gonococcal urethritis, and for 7 to 14 days to those with chlamydial urethritis and nongonococcal-nonchlamydial urethritis. Thirty-six patients with gonococcal urethritis, 33 patients with chlamydial urethritis and 20 patients with nongonococcal-nonchlamydial urethritis were assessable according to the criteria of the Japanese UTI Committee. The overall clinical responses were excellent in 30 cases and moderate in 6 cases with gonococcal urethritis, excellent in 25 cases, moderate in 7 cases and poor in 1 case with chlamydial urethritis, and excellent in all cases with nongonococcal-nonchlamydial urethritis, showing an overall efficacy rate of 100%, 97.0%, and 100%, respectively. MIC₉₀ of GFLX against 36 strains of Neisseria gonorrhoeae isolated in this study, was 0.063μg/mL, and its activity was 4-to 8-times higher than that of ciprofloxacin and ofloxacin, respectively. The incidence of clinical adverse reactions was 3.8%(6/160), and of laboratory adverse reactions 6.0%(5/83), and all adverse reactions were slight in degree. The results suggest that GFLX is an effective and safe drug in the treatment of both gonococcal and chlamydial urethritis.

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