Basic and clinical studies on biapenem (L-627) in obstetrics and gynecology

• Published in: Japanese journal of antibiotics Vol. 47; no. 12; p. 1637
• Main Authors: Matsuda, S, Oh, K, Ando, S, Kawamata, C, Shimizu, T, Ishikawa, M, Sengoku, K, Saito, S, Shibata, S, Haga, H
• Format: Journal Article
• Language: Japanese
• Published: Japan 01-12-1994
• Subjects: Adolescent; Adult; Aged; Aged, 80 and over; Bacterial Infections - drug therapy; Bacterial Infections - metabolism; Female; Genital Diseases, Female - drug therapy; Genital Diseases, Female - metabolism; Humans; Japan; Microbial Sensitivity Tests; Middle Aged; Pregnancy; Pregnancy Complications, Infectious - drug therapy; Pregnancy Complications, Infectious - metabolism; Thienamycins - pharmacokinetics; Thienamycins - pharmacology; Thienamycins - therapeutic use; Tissue Distribution
• ISSN: 0368-2781
• DOI: 10.11553/antibiotics1968b.47.1637

We investigated biapenem (BIPM, L-627) a newly carbapenem antibiotic, for its antibacterial activity, tissue penetration, clinical efficacy and bacteriological effect in obstetric and gynecological infections, and obtained the following results. 1. Antibacterial activity: MICs of L-627 against 149 strains isolated from 80 patients in this clinical trial were examined and compared with those of imipenem (IPM) and ceftazidime (CAZ). The MIC50 and MIC90 of L-627 against the isolates were 0.2 and 12.5 micrograms/ml, respectively. Those of IPM were 0.2 and 6.25 micrograms/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 26.2 micrograms/ml, respectively, after 300 mg drip infusion. The peak levels in the uterine or adnexal tissues were 2.39-9.60 micrograms/g, and 0.2 microgram/g of L-627 was detected at 275 minutes after administration. Peak levels in retroperitoneal fluid were 8.7 +/- 1.7 micrograms/ml at 1 hour after the completion of 30 minutes drip infusion (300 mg) and 7.9 +/- 0.2 micrograms/ml at 30 minutes after 300 mg 60 minutes drip infusion (300 mg). These levels expected the MICs against main pathogenic organisms. 3.
L-627 was given to the following 144 patients (No. of analytical subjects) at a daily dose of 0.3-1.2 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 was 93.1% (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 eosinophils in 1, increase in GOT, GPT and gamma-GTP in 1 and increase in GPT and A1-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 in the treatment of gynecological infections.