Weissbach L, Lobe H, Jost M, Gillissen J
Med Klin. 1976 Aug 6;71(32-33):1300-7.
In a study with 30 randomized patients the pharmacokinetics, efficacy and side effects of Sisomicin were determined. Half of the patients received one single intramuscular injection of 75 or 100mg (1.4 mg/kg) Sisomicin/day. The other cases were injected 50 or 75mg (1.9 or 2.1 mg/kg) b.i.d. The serum concentrations determined on the first and last days of treatment 1 hour after the application ranged between 4 and 5.3 mug/ml. After 6 hours the values decreased to 0.7-0.8 mug/ml. The elimination rate within 24 h amounted to 63-77%. Depending on the dosage group, the mean urinary concentrations/24 h amounted to 46-51 mug/ml or 63 to 92 mug/ml, respectively. The highest concentration measured during the first 8 hours amounted to 129 mug/ml after an administration of 1.4 mg/kg. In 18 of 29 cases a "cure" of urologic infections, most of which had been treated previously without success, could be achieved. Furthermore we observed 5 relapses, 3 failures and 3 reinfections, but no superinfection. The local and general tolerance of Sisomicin was good. 5 patients showed toxic reactions of the vestibular organ in the form of dizziness. In 1 case there was an excretion of granulated casts.
在一项针对30名随机分组患者的研究中，测定了西索米星的药代动力学、疗效和副作用。一半患者每天接受一次75或100毫克（1.4毫克/千克）西索米星的单次肌内注射，另一半患者每天两次注射50或75毫克（1.9或2.1毫克/千克）。在治疗的第一天和最后一天给药后1小时测定的血清浓度在4至5.3微克/毫升之间，6小时后降至0.7 - 0.8微克/毫升。24小时内的消除率为63% - 77%。根据剂量组不同，平均24小时尿浓度分别为46 - 51微克/毫升或63至92微克/毫升。在给予1.4毫克/千克剂量后，最初8小时内测得的最高浓度为129微克/毫升。29例中有18例泌尿系统感染得到“治愈”，其中大多数此前治疗未成功。此外，我们观察到5例复发、3例治疗失败和3例再感染，但未出现二重感染。西索米星的局部和全身耐受性良好。5名患者出现以头晕形式表现的前庭器官毒性反应。1例出现颗粒管型排泄。
