Oomomo Y, Maruhashi T, Hanaoka J, Minagawa Y, Yuzawa H, Tokunaga A, Takahashi T, Sasagawa S, Takeuchi S
Jpn J Antibiot. 1986 May;39(5):1342-9.
Tissue transfer and clinical effects of imipenem/cilastatin sodium (MK-0787/MK-0791), a new carbapenem antibiotic, were studied and the following results were obtained. Penetrations of MK-0787 into uterine arterial blood and into pelvic dead space exudate were good. When MK-0787/MK-0791 was administered at a dose of 500 mg/500 mg by a 30-minute intravenous drip infusion, the peak level of MK-0787 in uterine arterial blood was 22.2 micrograms/ml, 30 minutes after the completion of the drip infusion. The peak level of MK-0787 in pelvic dead space exudate was 12.9 micrograms/ml at 2 hours and it dropped to 2.6 micrograms/ml at 6 hours. MK-0791 levels were similar to those of MK-0787. Penetrations of MK-0787 into tissues were also good. When MK-0787/MK-0791 was administered at a dose of 500 mg/500 mg by a 30-minute intravenous drip infusion, the level of MK-0787 was 2.2 +/- 1.1 micrograms/g in the oviduct, 2.7 +/- 2.1 micrograms/g in the ovary, 2.5 +/- 1.2 micrograms/g in the endometrium, 3.0 +/- 1.6 micrograms/g in the myometrium, 3.1 +/- 1.9 micrograms/g in the cervix uteri and 3.8 +/- 2.0 micrograms/g in the portio vaginalis at 1 hour after administration. These levels were reduced to halves, respectively, in approximately 2 hours. Four patients with intrauterine infections and 2 with vaginal stump infections were treated with MK-0787/MK-0791 at a daily dose of 1 g/1 g (500 mg/500 mg X 2). Good clinical and bacteriological responses were observed in 5 patients and causative organisms were eradicated in 2 patients.(ABSTRACT TRUNCATED AT 250 WORDS)
对新型碳青霉烯类抗生素亚胺培南/西司他丁钠(MK - 0787/MK - 0791)进行了组织转移及临床效果研究,获得以下结果。MK - 0787在子宫动脉血及盆腔死腔渗出液中的穿透性良好。当以500mg/500mg的剂量经30分钟静脉滴注给予MK - 0787/MK - 0791时,子宫动脉血中MK - 0787的峰值水平在滴注结束后30分钟时为22.2微克/毫升。盆腔死腔渗出液中MK - 0787的峰值水平在2小时时为12.9微克/毫升,6小时时降至2.6微克/毫升。MK - 0791的水平与MK - 0787相似。MK - 0787在组织中的穿透性也良好。当以500mg/500mg的剂量经30分钟静脉滴注给予MK - 0787/MK - 0791时,给药后1小时,输卵管中MK - 0787的水平为2.2±1.1微克/克,卵巢中为2.7±2.1微克/克,子宫内膜中为2.5±1.2微克/克,子宫肌层中为3.0±1.6微克/克,子宫颈中为3.1±1.9微克/克,阴道部为3.8±2.0微克/克。这些水平在约2小时内分别降至一半。4例子宫内感染患者和2例阴道残端感染患者接受了每日剂量1g/1g(500mg/500mg×2)的MK - 0787/MK - 0791治疗。5例患者观察到良好的临床和细菌学反应,2例患者的致病微生物被根除。(摘要截于250字)