Reference

Fundamental and clinical studies of L-105 in obstetrics and gynecology

Fundamental and clinical studies of L-105 in obstetrics and gynecology. Cho, Nankun; Kimura, Takehiko; Kameda, Shogo; Watanabe, Hiroko; Fukunaga, Kango; Kunii, Katsuaki (Sch. Med., Showa Univ., Tokyo 142, Japan). Chemotherapy (Tokyo), 34(Suppl. 3), 661-76 (Japanese) 1986. CODEN: NKRZAZ. ISSN: 0369-4682. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 10 The antimicrobial activity, pharmacokinetics of the cephalosporin antibiotic L-105 [82219-78-1] were studied. The min. inhibitory concn. was 0.39 mg/mL for Staphylococcus aureus, 0.05 mg/mL for S. epidermidis, 3.13 mg/mL for Streptococcus faecalis, 0.05 mg/mL for Escherichia coli, 0.1 mg/mL for Klebsiella pneumoniae, 0.2 mg/mL for Enterobacter cloacae, 25 mg/mL for Citrabacter freundii and 0.78 mg/mL for Serratia marcescens. After i.v. administration of L-105 at 1 g the serum half-life was 1.35 h (AUC-area-under the concn. curve was 107.4 mg/h/mL), and the urinary excretion rate was 74% within 8 h. The half-life in uterine arterial serum was 56 min, and the AUC was 143 mg/h/mL. Similarly, the tissue level ranged from 9.4 to 51.8 mg/g, and the AUC ranged from 16.1 to 28.8 mg/h/g. The peak concn. of L-105 in the pelvic dead space exudate following 1 g i.v. injection was 10.2 mg/mL at 6 h with a half-life of >6.6 h. The levels in umbilical cord blood and amniotic fluid ranged from 0.3 to 5.9 mg/mL and 0.17 to 9.26 mg/mL, resp. These level are above the MIC80 for major pathogenic organisms. The penetration of L-105 into milk was very low.

Fundamental and clinical studies of L-105 in the surgical field

Fundamental and clinical studies of L-105 in the surgical field. Yura, Jiro; Shinagawa, Nagao; Ishikawa, Shu; Tachi, Yoshimasa; Shibata, Yoshitaka; Kobe, Akio; Mashita, Keiji (Med. Sch., Nagoya City Univ., Nagoya 467, Japan). Chemotherapy (Tokyo), 34(Suppl. 3), 593-600 (Japanese) 1986. CODEN: NKRZAZ. ISSN: 0369-4682. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 10 The antibacterial activity of L 105 (I) [82219-78-1], a new semisynthetic cephalosporin, was compared with that of latamoxef (LMOX), cefazolin (CEZ) and cefotiam (CTM). The min. inhibitory concns. (MICs) for I were the same or smaller than those of LMOX against surgical isolates of Escherichia coli and Klebsiella. The MIC for I was smaller than that of CEZ and CTM against Staphylococcus aureus. I, as well as LMOX, showed weak activity against Pseudomonas aeruginosa. The secretion of I into bile was measured in patients treated with I (1 g, i.v.). The max. concn. found in the bile was 3110 mg/mL. Clin. data are also reported.