BASIC AND CLINICAL STUDIES ON BIAPENEM (L-627) IN OBSTETRICS AND GYNECOLOGY

Abstract

We investigated biapenem (BIPM, L-627) a newly carbapenem antibiotic, for its antibacterial activity, tissue penetration, clinical efficacyand bacteriological effect in obstetric and gynecological infections, and obtained the following results.
1. Antibacterial activity
MICs of L-627 against 149 strains isolated from80 patients in this clinical trial were examined and compared with those of imipenem (IPM) and ceftazidime (CAZ). The MICK₅₀, and MICK₉₀, of L-627 against the isolates were 0.2and 12.5 μg/ml, respectively. Those of IPM were 0.2and 6.25μg/ml, respectively.
The antibacterial activity of L-627 was quite similar to that of IPM, and was superior to that of CAZ.
2. Tissue and retroperitoneal fluid penetration
The peak levels in venous and uterine arterial sera were 24.0 and 26.2μg/ml, respectively, after 300mg drip infusion. The peak levels in the uterine or adnexal tissues were 2.39-9.60μg/g, and 0.2μg/g of L-627 was detected at 275 minutes after administration.
Peak levels in retroperitoneal fluid were 8.7±1.7 ktg/ml at 1 hour after the completion of 30 minutes drip infusion (300 mg) and 7.9±0.2, ug/ml at 30 minutes after 300 mg 60 minutes drip infusion (300 mg). These levels expected the MICs against main pathogenic organisms.
3. Clinical results
L-627 was given to the following 144 patients (No.of analytical subjects) at a daily dose of0.3-1.2 g for 2-13 days: intrauterine infections (54), adnexitis (36), parametritis (17), pelvic peritonitis (27), bartholins abscess (6) and other infections (4). The clinical efficacy was93.1% (134/144) and the eradication rate against isolated organisms was 88.7% (110/124). Side effects were observed in 2 patients: eruption (1) and vomiting with numbness of the tongue (1). Abnormal change in laboratory test results included increase in eosinophiles in 1, increase in GOT, GPT and γ-GTP in 1 and increase in GPT and Al-P in 1, but all of these abnormalities were very mild and withdrawal of the drug was not required.
Our results suggest that this drug is useful inthe treatment of gynecological infections.