Abstract | BACKGROUND AND OBJECTIVE: METHODS: This was a phase I, randomized, open-label, single-centre study involving 20 male Caucasian patients (mean age 63.1 years) requiring TURP for treatment of benign prostatic hyperplasia. Sixteen patients were randomized to receive prulifloxacin; the other four patients were not treated (controls) in order to validate the bioanalytical method. Patients in the active treatment groups were randomized to receive one or three once-daily doses of prulifloxacin 600 mg, with the last administration 3 hours prior to surgery. Central/transitional and peripheral zone prostatic tissue samples were obtained from the 6 o'clock and 9 o'clock positions in the prostate, and blood samples were collected concurrently. Ulifloxacin concentrations were determined in the tissue samples and plasma using liquid chromatography-tandem mass spectrometry. Safety was also assessed. RESULTS: Prostatic tissue concentrations of ulifloxacin always exceeded those in plasma. Mean ulifloxacin concentrations measured in samples collected from the 6 o'clock central/transitional zone of the prostate were higher in patients who received prulifloxacin for 3 days than in those who received a single dose. Mean prostatic tissue/plasma ulifloxacin concentration ratios after single and repeated prulifloxacin administration ranged from 3.8 to 7.1 and from 3.9 to 9.5, respectively. The highest mean ratio was found in the 6 o'clock central/transitional zone after repeated dosing. Prostatic levels of ulifloxacin were above the minimum inhibitory concentrations for the most common causative pathogens of bacterial prostatitis. No treatment-related toxicities were reported. CONCLUSION: These findings confirm the ability of prulifloxacin to penetrate prostatic tissues, indicating high exposure of the target tissue to ulifloxacin and, therefore, a potential therapeutic role for prulifloxacin in the treatment of bacterial prostatic infections.
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Authors | Claudio Giberti, Fabrizio Gallo, Maria T Rosignoli, Alessandro Ruggieri, Simona Barattè, Rossella Picollo, Paolo Dionisio |
Journal | Clinical drug investigation
(Clin Drug Investig)
Vol. 29
Issue 1
Pg. 27-34
( 2009)
ISSN: 1173-2563 [Print] New Zealand |
PMID | 19067472
(Publication Type: Clinical Trial, Phase I, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
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Chemical References |
- Anti-Bacterial Agents
- Dioxolanes
- Fluoroquinolones
- Piperazines
- prulifloxacin
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Topics |
- Administration, Oral
- Anti-Bacterial Agents
(administration & dosage, pharmacokinetics, therapeutic use)
- Biological Availability
- Dioxolanes
(administration & dosage, pharmacokinetics, therapeutic use)
- Fluoroquinolones
(administration & dosage, pharmacokinetics, therapeutic use)
- Humans
- Male
- Middle Aged
- Piperazines
(administration & dosage, pharmacokinetics, therapeutic use)
- Prostate
(metabolism)
- Prostatic Hyperplasia
(metabolism, surgery)
- Prostatitis
(drug therapy)
- Transurethral Resection of Prostate
(methods)
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