Matsuda S, Oh K, Ando S, Kawamata C, Shimizu T, Ishikawa M, Sengoku K, Saito S, Shibata S, Haga H
Department of Obstetrics and Gynecology, Kohto Hospital, Tokyo, Japan.
Jpn J Antibiot. 1994 Dec;47(12):1637-67.
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.
我们研究了新型碳青霉烯类抗生素比阿培南（BIPM，L-627）在妇产科感染中的抗菌活性、组织穿透性、临床疗效及细菌学效果，结果如下。1. 抗菌活性：检测了L-627对本次临床试验中80例患者分离出的149株菌株的最低抑菌浓度（MIC），并与亚胺培南（IPM）和头孢他啶（CAZ）的MIC进行比较。L-627对分离菌株的MIC50和MIC90分别为0.2和12.5微克/毫升。IPM的分别为0.2和6.25微克/毫升。L-627的抗菌活性与IPM相当，且优于CAZ。2. 组织及腹膜后液穿透性：静脉和子宫动脉血清中的峰值水平在300毫克滴注后分别为24.0和26.2微克/毫升。子宫或附件组织中的峰值水平为2.39 - 9.60微克/克，给药后275分钟检测到L-627为0.2微克/克。腹膜后液中的峰值水平在30分钟滴注（300毫克）结束后1小时为8.7±1.7微克/毫升，300毫克60分钟滴注（300毫克）后30分钟为7.9±0.2微克/毫升。这些水平超过了对主要病原菌的MIC。3. 临床结果：对以下144例患者给予L-627，日剂量0.3 - 1.2克，疗程2 - 13天：宫腔感染（54例）、附件炎（36例）、宫旁组织炎（17例）、盆腔腹膜炎（27例）、巴氏腺脓肿（6例）及其他感染（4例）。临床有效率为93.1%（134/144），对分离菌的根除率为88.7%（110/124）。2例患者出现副作用：皮疹（1例）和呕吐伴舌麻木（1例）。实验室检查结果异常包括1例嗜酸性粒细胞增多、1例谷草转氨酶（GOT）、谷丙转氨酶（GPT）和γ-谷氨酰转肽酶（γ-GTP）升高、1例GPT和碱性磷酸酶（A1-P）升高，但所有这些异常都非常轻微，无需停药。我们的结果表明该药物对治疗妇科感染有效。
