title: Clinical pharmacokinetics of oral levofloxacin and sitafloxacin in epididymal tissue.
abstract: OBJECTIVE
  This study aimed to investigate the penetration of fluoroquinolones into human epididymal tissue.
  
  
  METHODS
  The penetration of levofloxacin (LVFX) 500 mg or sitafloxacin (STFX) 100 mg into epididymal tissue was examined. Patients with prostate cancer who were referred for orchiectomy were included. LVFX 500 mg (n = 9) or STFX 100 mg (n = 9) was administered orally 1 h before orchiectomy, and 0.5 g of epididymal tissue and blood samples were collected simultaneously during surgery. Drug concentrations were measured by high-performance liquid chromatography, and patient characteristics and adverse events were analyzed.
  
  
  RESULTS
  The mean ratio of the epididymal concentration to the serum concentration was 1.48 ± 0.45 for LVFX and 1.54 ± 0.81 for STFX. For LVFX, the simulated curves estimated the following: maximum concentrations (Cmax) of 8.84 μg/ml in serum and 14.1 μg/g in epididymal tissue and area under the concentration-time curve for 24 h (AUC24) of 68.5 μg h/ml in serum and 108.9 μg h/g in epididymal tissue. For STFX, the Cmax was 1.22 μg/ml in serum and 1.66 μg/g in epididymal tissue, and the AUC24was 9.58 μg h/ml in serum and 13.1 μg h/g in epididymal tissue. Neither treatment-related adverse events nor postoperative urogenital infections were observed.
  
  
  CONCLUSIONS
  The results of this study suggest that oral administration of LVFX 500 mg or STFX 100 mg achieves effective epididymal concentrations for treatment of epididymitis.
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Takuya
authors.initials: T
authors.lastname: Sadahira
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan. Electronic address: gmd17055@s.okadai.jp.
authors.forename: Koichiro
authors.initials: K
authors.lastname: Wada
authors.affiliation: Department of Clinical Pharmacotherapy, Hiroshima University, 1-2-3, Kasumi, Minami-ku, Hiroshima, 734-8551, Japan.
authors.forename: Kazuro
authors.initials: K
authors.lastname: Ikawa
authors.affiliation: Department of Clinical Pharmacotherapy, Hiroshima University, 1-2-3, Kasumi, Minami-ku, Hiroshima, 734-8551, Japan.
authors.forename: Norifumi
authors.initials: N
authors.lastname: Morikawa
authors.affiliation: Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Department of Urology, Tsukazaki Hospital, 68-1, Waku, Aboshi-ku, Himeji, 671-1227, Japan.
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Kurahashi
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Takashi
authors.initials: T
authors.lastname: Yoshioka
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Ariyoshi
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Yasuyuki
authors.initials: Y
authors.lastname: Kobayashi
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Motoo
authors.initials: M
authors.lastname: Araki
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Ayano
authors.initials: A
authors.lastname: Ishii
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Masami
authors.initials: M
authors.lastname: Watanabe
authors.affiliation: Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Department of Urology, Kawasaki Medical School, 577, Matsushima, Kurashiki, 701-0114, Japan.
authors.forename: Shinya
authors.initials: S
authors.lastname: Uehara
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Toyohiko
authors.initials: T
authors.lastname: Watanabe
authors.affiliation: Department of Urology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan; Okayama Urological Research Group (OURG), 2-5-1, Shikata-cho, Kita-ku, Okayama, 700-8558, Japan.
authors.forename: Yasutomo
authors.initials: Y
authors.lastname: Nasu
mesh_terms: D000284:Administration, Oral; D000368:Aged; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004822:Epididymis / Q000187:drug effects*; D004823:Epididymitis / Q000188:drug therapy; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D064704:Levofloxacin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008297:Male; D008826:Microbial Sensitivity Tests / Q000379:methods; D011471:Prostatic Neoplasms
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D064704:Levofloxacin; C076246:sitafloxacin
keywords: Antimicrobial pharmacokinetics; Epididymitis; Levofloxacin; Sitafloxacin; Urogenital tract infection