Clinical pharmacokinetics of oral levofloxacin and sitafloxacin in epididymal tissue
| Autor: | Norifumi Morikawa, Takashi Yoshioka, Shinya Uehara, Ayano Ishii, Yasuyuki Kobayashi, Motoo Araki, Yasutomo Nasu, Takuya Sadahira, Hiroaki Kurahashi, Toyohiko Watanabe, Masami Watanabe, Kazuro Ikawa, Koichiro Wada, Yuichi Ariyoshi |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Microbiology (medical) Sitafloxacin Male medicine.medical_specialty Pathology 030106 microbiology 030232 urology & nephrology Urology Cmax Administration Oral Levofloxacin Microbial Sensitivity Tests 03 medical and health sciences 0302 clinical medicine Pharmacokinetics Oral administration medicine Humans Pharmacology (medical) Orchiectomy Adverse effect Aged Epididymis Epididymitis business.industry Prostatic Neoplasms medicine.disease Anti-Bacterial Agents Infectious Diseases business medicine.drug Fluoroquinolones |
| Zdroj: | Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy. 23(4) |
| ISSN: | 1437-7780 |
| Popis: | Objectives 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 (AUC 24 ) 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 AUC 24 was 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. |
| Databáze: | OpenAIRE |
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