Enterococcus is a normal constituent of the intestinal bacterial flora in humans, which occasionally causes opportunistic infections and induces sepsis in case of serious infections. The combination of aminoglycosides with penicillins is generally known to be one of the regimens for bacteremia due to Enterococcus The drug susceptibility of high-level aminoglycoside-resistant (HLAR) isolates which were detected in part of the En terococcus isolates derived from blood specimens and the resistance genes were investigated in the present study.
One hundred and forty-nine isolates of Enterococcus (2.2%) were detected in 6, 730 blood specimens taken between February 2001 and February 2002. The details are as follows: Enterococcus faecal is strains accounted for 94 (63.1%) followed by Entcrococcvs jacci um strains at 41 (27.5%), and both organisms accounted for 90.6% of all organisms. A total of 54 HLAR strains (36.2%) were detected in 149 strains of Enterococcus and the resistance rate of E. faccium was low, 4.9%, as compared with that of E. faccatis (50.0%). There were differences between E. faecium and E. faccalis in the resistance rate. The aac (6')-aph (2'') gene was detected in 49 of the 54 strains (90.7%) with PCR. In addition, the inactivation of gentamicin (GM) was investigated in the 5 isolates without resistant genes. As a result, these isolates inactivated GM. The MICs of penicillin G (PCG), vancomycin (VCM), teicoplanin (TEIC), linezolid (LZD), telithromycin (TEL) and gatifloxacin (GFLX) for 54 isolates of HLAR were determined. The strains resistant to PCG, TEL and GFLX were about 4 to 44%. In the present study there were no strains resistant to VCM, TEIC or LZD, which suggests that these antibiotics are usefully therapeutic drugs for the treatment of infections caused by HLAR strains.

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The efficacy and safety of telithromycin (TEL), an oral ketolide antibiotic, was evaluated in a double-blind, parallel-group, noninferiority comparative study with cefdinir (CFDN) as the control drug under minimized randomization method. Patients with deep-seated skin infections were assigned either to the TEL group (TEL 600mg once daily for 5 days) or the CFDN group (CFDN 100mg 3 times daily for 5 days).
1. Clinical outcome
In the 228 patients evaluated for clinical outcome, clinical efficacy was 88.9%(104/117) in the TEL group and 82.9%(92/111) in the CFDN group, and the noninferiority of TEL compared to CFDN was confirmed.
2. Bacteriological outcome
The bacteriological outcome was evaluated in 223 patients, and bacteriological efficacy in 143 patients, excluding 80 patients for whom the bacteriological outcome could not be determined, was 98.6%(71/72) in the TEL group and 93.0%(66/71) in the CFDN group. Total eradication, the sum of eradications for all causative pathogen isolated prior to administration, was 100.0%(114/114) in the TEL group and 94.1%(96/102) in the CFDN group.
3. Safety
Safety was evaluated in 245 patients. The incidence of side effects in 242, excluding 3 for whom safety could not be determined, was 30.6%(37/121) in the TEL group and 35.5%(43/121) in the CFDN group, with no significant, difference between groups.
Findings thus suggest that TEL 600mg once daily for 5 days is as clinically effective and safe as CFDN 100mg 3 times daily for 5 days in the management of skin and soft tissue infection.

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A clinical pharmacological study to evaluate telithromycin (TEL), an oral ketolide antibiotic, for its skin penetration, and a phase III Open clinical study of administration of TEL 600 mg once daily for 5 days to patients with superficial skin infection, secondary infection, and miscellaneous abscesses were conducted.
1. Penetration of skin tissues
In the 13 patients evaluated, mean skin concentration at 5 hours 20minutes to 6 hours 35 minutes was 0.64μg/g and plasma concentrations at the almost same time was 0.38μg/mL after a single oral dose of TEL 600mg, and the skin concentration plasma concentration ratio was 1.50.
2. Clinical outcome
In the 80 patients evaluated for clinical outcome, clinical efficacy was 81.3%(65/80). Clinical efficacy for superficial skin infection, secondary infection and miscellaneous abscesses was 96.0%(24/25), 85.7%(18/21), and 67.6%(23/34).
3. Bacteriological outcome
The bacteriological outcome was evaluated in 78 patients, and bacteriological efficacy in 67 patients, excluding 11 patients for whom the bacteriological outcome could not be determined, was 88.1%(59/67). Total eradication for all pathogens isolated prior to administration was 93.0%(106/114).
4. Safety
Safety was evaluated in 98 patients. The incidence of side effects in 95, excluding 3 for whom safety was not determined, was 30.5%(29/95). All side effects observed were mild or moderate.
Findings thus suggest that TEL penetrated skin well and that the administration of TEL 600 mg once daily for 5 days is clinically effective and safe in the treatment of skin and soft tissue infection.

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A clinical pharmacological study to evaluate telithromycin (TEL), an oral ketolide antibiotic, for its penetration of female genital organ tissues, and a clinical study of administration of TEL 600mg once daily for 5 days to patients with cervicitis caused by Chiamydia trachomatis or Neisseria gonorrhoeae were conducted, withthe following results:
1.Distribution to female genital organ tissues (clinical pharmacological study)
In the 11 patients evaluated, mean tissue concentration in female genital organs at 180-435 minutes after a single dose of TEL 600mg was 1.22μg/g in portio vaginalis, 1.97μg/g in cervix uteri, 2.37μg/g in endometrium, and 2.61μg/g g in myometrium, and distribution ratios (tissue concentration/plasma concentration) ranged from 2.29 to 4.90.
2.Clinical efficacy
TEL 600mg was administered once daily for 5 days, and clinical efficacy was evaluated on Days 14 and 28. Efficacy on Days 14 (53 patients) and 28 (50 patients) was 81.1%(43/53) and 96.0%(48/50).
3.Bacteriological efficacy
Bacteriological efficacy on Days 14 (53 patients) and 28 (50 patients) was 81.1%(43/53) and 96.0%(48/50). Eradication for C.trachoma tis was 80.4%(37/46) on Day 14 and 95.3%(41/43) on Day 28, and for N. gunorrhoeae was 90.0%(9 10) on Day 14 and 100.0%(9 9) on Day 28.
4. Safety
Safety was evaluated in 58 patients, and the incidence of side effects in 56, excluding 2 for whom incidence could not be determined, was 26.8%(15 56). All side effects observed were either mild or moderate.
Results show that the administration of TEL 600mg once daily for 5 days is clinically highly effective for cervicitis caused by C.trachomatis and N.gonorrhoeae, and this was backed by the fact that TEL was well distributed in female genital organ tissues.

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