Madsen P O, Frimodt-Møller N, Maigaard S, Nielsen O S, Rodriguez N, Welling P G
Urology. 1981 May;17(5):496-9. doi: 10.1016/0090-4295(81)90204-1.
In dogs we found that cinoxacin concentrations in prostatic tissue, secretion, and interstitial fluid always were lower than the simultaneous serum concentrations, during constant infusion experiments. The cinoxacin concentrations in urethral and vaginal secretions were similar to those found in prostatic interstitial fluid, approximately one third to one fourth of the simultaneous serum concentrations. The concentrations of cinoxacin in human prostatic tissue after single or multiple doses of 500 mg. were found to be in the range of minimum inhibitory concentrations for most microorganisms found in urinary tract infections. Cinoxacin was found to have a half-life of 2.7 hours in patients with normal renal function, but increased to 8.5 hours in patients with impaired renal function. We found little or no drug accumulation during a seven-day treatment of patients with impaired renal function.
在犬类实验中，我们发现在持续输注实验期间，环丙沙星在前列腺组织、分泌物和间质液中的浓度始终低于同时期的血清浓度。环丙沙星在尿道和阴道分泌物中的浓度与在前列腺间质液中发现的浓度相似，约为同时期血清浓度的三分之一至四分之一。单次或多次服用500毫克后，人体前列腺组织中环丙沙星的浓度对于大多数尿路感染中发现的微生物而言处于最低抑菌浓度范围内。我们发现，肾功能正常的患者中环丙沙星的半衰期为2.7小时，但肾功能受损的患者中该半衰期延长至8.5小时。我们还发现，在对肾功能受损的患者进行为期七天的治疗期间，几乎没有药物蓄积现象。
