Norfloxacin penetration into human renal and prostatic tissues

Abstract

Concurrent norfloxacin concentrations in serum, kidney, and prostatic tissue were determined in 14 patients. Mean ratios of norfloxacin concentration in tissue over concentration in serum were 6.6 +/- 2.8 for the kidney and 1.7 +/- 0.2 for the prostate samples. The levels were above the MICs of most urinary pathogens.

In vivo Diffusion of Enoxacin in Healthy Renal and Adenomatous Prostate Tissue in Man

“…The 3 late sam ples (collected 7-17 h after the last dose) seemed to point to the persistence of enoxacin in the renal tissue. Our concentrations of enoxacin in the kidney were higher than those obtained for pipemidic acid [Thaller et al, 1983] and equivalent to those obtained for ciprofloxacin [Daschner et ah, 1986] and norfloxacin [Bergeron et al, 1985]. The concentrations assessed in the kidney of 6 patients undergoing nephrectomy 1.7-6.3 h after the last of six 200-mg oral doses of enoxacin [Malmborg and Rannikko, 1988] ranged between 4.2 and 1.70 pg/g (cor tex) and 4.3 and 1.70 pg/g (medulla) with a mean tissue/ serum ratio of 3.8 ± 0.7 for the cortex and 3.2 ± 0.7 for the medulla.…”

“…The renal tissue concentrations in these patients were 4.6 and 22.5 pg/g and plasma concentrations 1.1 and 1.8 mg/1, yielding tissue-to-plasma concentration ratios of 4.18 and 12.5, respectively (table 5). ± 1.18 pg/g 3.9 h after the last dose, with a mean tissue/ serum ratio of 2.1 ± 0.6 in the study by Rannikko and Malmborg [1986] and 3.1 ± 1.8 pg/g with a mean tissue/ serum ratio of 2.53 in the study of White et al [1988], The tissue-to-plasma concentration ratio obtained for adenomatous prostate tissue was greater than or equal to those found for ciprofloxacin [Boerema et al, 1985;Wal dron and Arkell, 1986] and norfloxacin [Bergeron et al, 1985;Bologna et al, 1983Bologna et al, , 1985. The renal concentra tions were high, of the order of 14 pg/g renal tissue, with a tissue-to-plasma ratio of the order of 7.…”

Penetration of Norfloxacin into Human Prostatic Tissue following Single-Dose Oral Administration

“…Previous studies were limited to assay of tissue ¿ 5 h after administration of two doses of the drug [Bologna et al, 1983;Bergeron et al, 1985], Although other in vestigators have employed high-pressure liquid chromatography for assay of nor floxacin, data based on microbiologie as say may be more relevant clinically, since the effect of therapeutic material upon uri nary pathogens is examined.…”

“…Nor floxacin is active against a wide variety of urinary pathogens [Greenwood et al 1984], Preliminary investigations have suggested that norfloxacin is one of the few antibiotics which may achieve thera peutic concentrations in the prostate [Bo logna et al, 1983;Bergeron et al, 1985]. We have investigated the penetration of this agent into the prostatic tissue of pa tients undergoing elective suprapubic prostatectomy.…”

Review of Norfloxacin in Lower Urinary Tract Infections

“…Its efficacy and its safety profile in the treatment of uncomplicated lower urinary tract infections (UTIs) have been evaluated in many worldwide clinical trials. Norfloxacin has demonstrated excellent in vitro activity against the majority of pathogens isolated from the uri nary tract [1,2]. In vivo resistance has been observed infrequently [3,4], Pharmacokinetic studies have shown that norfloxacin has a high urinary excretion rate, a long elimination half-life and a low incidence of side effects [5,6], Because of these characteristics, norfloxacin ap pears to be well suited for the treatment of UTIs.…”