急性精巣上体炎に対するLevofloxacinの基礎的・臨床的検討

Abstract

本剤200 mg内服2時間後の精巣及び精巣上体の組織濃度はそれぞれ4.57～4.90 μg/g, 3.38～3.48 μg/gであり, 血清中濃度2.85 μg/mlに比し高く, それぞれ1.60～1.72倍, 1.19～1.22倍と移行は良かった.1回100 mg, 1日3回・13日間連続投与による精液中への移行は, 7日目1.19±0.08 μg/ml, 13日目1.32±0.15 μg/mlで対血清比はそれぞれ1.12±0.11, 1.26±0.14であった.精子への影響は認めなかった.クラミジアに対するMIC(最小発育阻止濃度)は0.25～1.0 μg/mlに分布し, MIC50, MIC90はそれぞれ0.5 μg/ml, 1.0 μg/mlであった.急性精巣上体炎23例に1回100 mgを1日2～3回投与し, 原則として14日治療を行った場合, 14日目の統一判定可能症例では著効16例, 有効4例であった.また, クラミジアが原因と考えられた12例では, 7日目に著効5例, 有効5例, 無効2例, 14日目に著効9例, 有効2例であった

We performed basic and clinical studies on the effects of a new oral quinolone derivative, levofloxacin (LVFX, Code No. DR 3355) which is an optical l-isomer of ofloxacin, in acute epididymitis. LVFX was administered in a dose of 200 mg to prostatic cancer patients 2 hours before operation. The mean concentration of LVFX in the tissues of testis and epididymis were 4.73 micrograms/g and 313-3.6 micrograms/g, respectively. Tissue/Serum ratios were 1.63 and 1.16-1.32, respectively. LVFX was administered in a dose of 100 mg three times daily for 13 days to healthy male volunteers. Semen and blood samples were taken 2 hrs after 7th and last day of administration. The concentration of LVFX in semen were 1.19 micrograms/ml (7th day) and 1.32 micrograms/ml (13th day). Semen/serum ratios were 1.12 and 1.26, respectively. No affection of LVFX on the sperm was observed. Antimicrobial activity of LVFX to C. trachomatis showed good MICs of 0.25-1.0 micrograms/ml. LVFX was administered in a dose of 100 mg two or three times daily for 14 days to 23 patients with acute epididymitis. The overall efficacy rate based on a criteria for acute epididymitis showed 100% (excellent: 16, good: 4, 20/20). A better efficacy rate was obtained on the 14th day than 7th day. No subjective or objective adverse reactions were observed.