[Clinical evaluation of lenampicillin in the treatment of superficial suppurative skin and soft tissue infection. A double-blind study comparing amoxicillin].

A double-blind controlled clinical study between lenampicillin (LAPC), a newly developed oral ampicillin (ABPC) prodrug, and amoxicillin (AMPC) was conducted for the treatment of suppurative skin and soft tissue infection as grouped in 6 disease types. LAPC or AMPC were orally administered at a daily dose of 1,000 mg, in 4 equally divided doses. Each group was treated for 14 days. The results indicated that LAPC was equal to AMPC in evaluations of effectiveness and usefulness, although incidence of severe side effects was slightly lower in LAPC. The number of cases studied was 235 (115 in the LAPC group, 120 in the AMPC group). Among these, 10 patients (4 in LAPC, 6 in AMPC) were excluded and 12 patients (5 in LAPC, 7 in AMPC) dropped out. Final global improvement rating was evaluated in 213 patients (106 in LAPC, 107 in AMPC). General usefulness rating was evaluated in 215 patients (106 in LAPC, 109 in AMPC), and overall safety rating was evaluated in 231 patients (115 in LAPC, 116 in AMPC). Final global improvement rating of LAPC was, "cured", 55.7% and "cured" and "remarkably improved", 79.2%. The rate increased to 88.7% when "improved" was included. On the other hand, in the AMPC group, "cured" was 50.5%, and "cured" and "remarkably improved" was 76.6%. The rate increased to 91.6% when "improved" was included. No significant difference was found between the 2 drug groups. In overall safety rating of LAPC, "safe" was 93.9%, while in the AMPC group, "safe" was 94.0%. No significant difference was found between the 2 drug groups. Side effects were noted in 2 of 115 patients (1.7%) among the LAPC group and in 5 of 116 patients (4.3%) among the AMPC group. Incidence of severe side effects was slightly lower in LAPC (P less than 0.1). General usefulness rating of LAPC was, "remarkably useful", 56.6% and the rate increased to 86.8% when "useful" was included. In the AMPC group, "remarkably useful" was 51.4%, and increased to 84.4% when "useful" was included. No significant difference was found between the 2 drug groups.

[Clinical studies on lenampicillin in the therapy of skin and soft tissue infections].

Clinical evaluation of newly developed oral ampicillin prodrug lenampicillin (LAPC, KBT-1585) applied to patients with superficial purulent infection at a dosage of 750 approximately 1,500 mg daily was conducted. Additionally, as part of the basic study, transition of the compound to the human skin tissue was observed. With regard to transition to human skin tissue in 11 presurgery dermatitis cases, 250 mg or 500 mg of LAPC was administered to 2 approximately 3 hours before surgery. Comparison was made between concentrations in serum and in skin tissue. Results in the case of 250 mg application showed serum concentration to be 1.28 approximately 3.32 micrograms/ml, and in skin tissue, 0.13 approximately 0.82 micrograms/g. At 500 mg, serum concentration was found to be 2.23 approximately 10.05 micrograms/ml, with skin tissue concentration at 0.45 approximately 1.34 micrograms/g. Rate of clinical efficacy in the treatment of the 183 cases of superficial purulent infection was 79.2%. By grouping of the infections (Table 3), high efficacy rates were obtained in the second group, at 85.7%; in the third at 88.9%; and in the fourth group at 96.4%. Evaluation of usefulness from the standpoint of safety was 77.6%. Good results were obtained in the third group with 88.9%; and in the fourth group with 96.4%. LAPC's efficacy rates against individual strains of bacteria in simple infection are as follows: Staphylococcus aureus, 74.6%; Staphylococcus epidermidis, 76.3%; GPC, 100%; anaerobes, 87.5%. In polymicrobial infections the rate was 84.6%. The rate of efficacy against all strains of bacteria was 76.0%. Adverse reactions were found in 13 cases (14 incidences) out of 193. The rate of incidence was 7.3%, with allergic response accounting for 5 cases, digestive tract disorders, 7 cases, and mouth odor, 1 case. There were 5 cases (6 incidences) of abnormal deviation of laboratory findings. In all cases, abnormal deviations were mild and their relation to the drug was unclear.

[Clinical evaluation of the TMS-19-Q.GC tablet on superficial suppurative disease. A comparative double blind study with midecamycin].

Clinical efficacy and safety of TMS-19-Q.GC tablet (TMS), a new macrolide preparation, were compared with those of midecamycin (MDM) in superficial suppurative skin and soft tissue infections. The study was made by the double-blind controlled trial at the dosage of daily 600 mg in TMS group and 1,200 mg in MDM group. Total 218 cases (106 in TMS, 112 in MDM) were analyzed and the final global improvement rating were 82.1% in TMS and 83.9% in MDM. The clinical effectiveness of TMS was favorable and significantly different from MDM in the aged patients (greater than or equal to 60 years old) and the patients infected with susceptible strains (MIC less than or equal to 3.13) of Staphylococcus aureus. TMS is prepared with a specific formulation to make the absorption easier in the patients with lower acidity of gastric juice, and the favorable effect of TMS is considered to be a contribution of the devise in older patients. Slight adverse reactions were observed at 5.0% (6 cases) in TMS and 2.4% (3 cases) in MDM. In conclusion, TMS at the daily half dose of MDM is as effective as MDM in superficial suppurative skin and soft tissue infections.