We performed experimental and clinical studies with gatifloxacin (GFLX), a new synthetic antimicrobial agent for oral use, in the field of oral surgery.
1. GFLX, at 100mg, was administered orally to 10 patients, and its concentration in maxillary bone ranged from 0.35 to 0.80 peg at 1.75 to 5.5 hours in 4 subjects, in mandibular bone from not detectable to 1.85μg/g at 3.25 to 5 hours in 4 subjects, in maxillary alveolar bone was 0.37μg/g at 2.75 hours in 1 subject, and in mandibular alveolar bone was 0.45μg/g at 3 hours in 1 subject.
2. GFLX, at 100mg, was administered orally to 2 patients, and the concentrations in exudate during the operation ranged from 0.49 to 0.57μg/g at 2.83 to 4.17 hours after administration.
3. A clinical study was conducted in 104 patients with periodontitis, pericoronitis and osteitis of the jaw. The efficacy rate, judged by doctors, was 96.8% for 93 patients, whereas the comparative score evaluation was 93.4% for 91 patients.
4. Three hundred and thirteen strains of organisms were isolated from closed abscesses, and the bacteriological eradication rate was 100% in all strains.
5. Side effects were observed in 3 cases (diarrhea and rash etc.). Abnormal laboratory findings were recognized in 12 cases (increased S-GOT, S-GPT levels and eosinophil count etc.).
From these results, we conclude that GFLX is a useful antimicrobial agent for the treatment of odontogenic infections at the dose of 200 or 400mg/day.

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We performed a multicenter clinical trial of gatifloxacin (GFLX), a new 8-methoxy-quinolone antimicrobial agent, to examine its penetration into skin exudate and its clinical efficacy and safety in the field of dematology. GFLX was administered at a dose of 100 mg or 200 mg twice a day for 4 to 7 days in most patients. The clinical efficacy rate was 91.8%(56 of 61 patients): group-I a 95.2%(20/21), group-I b 100%(5/5), group-II a 100%(10/10), group-II b 84.6%(11/13), group-III 90.9%(10/11), group-IV 0%(0/1). The bacteriological response rate was 87.5%(49/56 strains). Adverse reactions were observed in 4 of 73 patients (5.5%), and manifested as either slight or moderate gastrointestinal symptoms. Abnormal laboratory findings were observed in 7 of 67 patients (10.4%), and were composed of slightly elevated serum liver enzymes in most cases. The ratio of skin exudate concentration to serum concentration was 1.24 at 2 hours after the oral administration of GFLX 100 mg twice a day. These results suggest that GFLX will be an effective and safe drug in thetreatment of skin and skin structure infections.

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Gatifloxacin (GFLX), a new oral fluoroquinolone, was evaluated for its tissue penetration into female genital organs and its clinical efficacy, safety and utility in obstetric and gynecological infections.
1. Tissue penetration
The peak serum levels were 1.85μg/ml after a single oral dose of 200 mg. The mean tissue concentrations (μg/g) were 0.50 in myometrium, 0.77 in endometrium, 0.42 in portio vaginalis, 0.44 in cervix uteri, 0.46 in oviduct and 1.24 in ovary, respectively, with the mean relative tissue/serum concentration ratios of 1.00 to 1.65 in these tissues.
2. Clinical effect
GFLX was administered to 69 patients with obstetric and gynecological infections: 100 mg b. i. d. for 37, 200 mg o.d. for 8 and 200 mg b.i.d. for 24. The overall clinical efficacy rate was 89.9%(62/69). In 23 patients with chlamydial infection, the clinical efficacy rate was 95.7%(22/23).
3. Bacteriological effect
The bacteriological response rate was 85.2%(23/27 patients), and the bacterial elimination rate was 92.5%(49/53 strains).
4. Safety
In adverse reactions, only one case of lightheadedness was observed in 75 patients. In the clinical laboratory test, one case of a decreased WBC count was reported in 61 patients. Neither case was serious.
5. Utility
The utility was markedly useful in 10, useful in 51 and useless in 8 patients, resulting in the utility rate (markedly useful and useful) of 88.4%(61/69).
The above results indicate that GFLX is well tolerated and useful in the treatment of obstetric and gynecological infections.

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To evaluate the clinical efficacy, clinical cure effect and safety of gatifloxacin (GFLX), 8-methoxyquinolone derivatives, in prostatitis and the penetration of GFLX into prostatic fluid in healthy volunteers, we performed a clinical study. Six healthy volunteers received 200 mg of GFLX as a single oral dose and the drug's penetration into prostatic fluid at 2 and 4 hours was evaluated. Thirty-two patients orally received 200 mg b.i.d. of GFLX for 14 days and were evaluated on Day 7, 14 and 28, and the clinical efficacy was assessed in accordance with the criteria of the Japanese UTI Committee.
1. The concentrations of GFLX in prostatic fluid ranged from 0.65 to 2.20 and from 1.02 to 1.56μg/mL, and concentration ratios to serum were 0.98 and 1.03 at 2 and 4 hours, respectively.
2. In acute bacterial prostatitis, including chronic bacterial prostatitis acutely aggravated, the overall clinical efficacy rate (excellent and moderate responses) was 100%(7/7) on Day 7. Also clinical cure rates on Day 14 (time of final dosing) and 28 (2 weeks after dosing) were 100%(6/6).
3. In chronic bacterial prostatitis, the overall clinical efficacy rate was 100%(9/9) on Day 14. On Day 28 (2 weeks after dosing), 7 of 7 patients were clinically cured.
4. The incidence of clinical adverse reactions was 6.3% of 32 patients, and of laboratory adverse reactions was 9.7% of 31 patients. None of the findings in adverse reactions were serious.
From the results of this study, we conclude that GFLX penetrates the prostatic fluid well, and is safe and effective in the treatment of prostatitis.

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To find the optimal dose of biapenem (BIPM), a new parenteral carbapenem, in the treatment of complicated urinary tract infections, we performed a randomized, prospective, well-controlled study using imipenem/cilastatin (IPM/CS) as the control drug. The subjects had complicated urinary tract infection with pyuria of at least 5 WBCs/HPF, bacteriuria of at least 10⁴CFU/ml and an identifiable underlying urinary tract disease. Only hospitalized patients aged from 50 to 79 years without indwelling catheters were enrolled in the study. Patients were randomly assigned to receive either 150 mg b. i. d. of BIPM (group L), 300 mg b. i. d. of BIPM (group H) or 500 mg/500 mg b. i. d. of IPM/CS (group C) by intravenous drip infusion for 5 days. Overall clinical efficacy was evaluated on the basis of criteria proposed by the Japanese UTI Committee as “excellent”, “moderate” or “poor”. Excellent and moderate responses were obtained in 80.0% of 10 patients in group L, and in 100% of 11 patients in group H and 14 patients in group C. The differences were not statistically significant. The bacteriological eradication rates achieved were 85.7% of 14 strains in group L, 100% of 21 strains in group H and 94.1% of 17 strains in group C, with no statistically significant differences. Clinical adverse reactions were experienced in 10.0% of the 10 patients in group L, and in 0% of the 13 patients in group H and the 15 patients in group C, with no statistically significant differences. Clinical value also was not significantly different between the three groups. Based on the results obtained in this study, we concluded that the optimal dose of BIPM in the treatment of complicated urinary tract infections is 300 mg b. i. d.

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