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腎結石患者12例に対してYACHIYODA SZIによるESWL前後にMRIを用い腎実質および周囲組織への影響を検討した. 1)12例中6例の患者に術後MRIにて何らかの変化を認め, CMJの消失を2例, 腎被膜下出血を2例, 腎周囲軟部組織の信号強度の増強を6例に認めた. 2)MRIはESWLによる腎の変化を鋭敏にとらえることができ治療後異常が認められた場合は積極的に検査を行うべきと思われた, Extracorporeal shock wave lithotripsy (ESWL) using YACHIYODA SZI was performed on 12 patients with renal stones and the effect on the kidney and adjacent tissue was evaluated by magnetic resonance imaging (MRI) before and after treatment. Some changes were seen in 6 of the 12(50%) patients; perirenal fluid collection in 2 of the 12 (16.7%) patients, subcapsular hematoma in 2 of the 12 (16.7%) patients, renal enlargement in 5 of the 12 (31.3%) patients, increased signal intensity in perirenal tissue in 6 of the 12 (50%) patients, and loss of the corticomedullary junction 2 out of 9 patients (22%). These findings indicated fewer changes in the kidney after ESWL using YACHIYODA SZI than in the other reports. MRI is also concluded to be effective to detect the changes of the kidney after ESWL.

尿路結石患者32名(34結石)に対してYACHIYODA-SZ 5000による臨床試験を行った。治療成績は著効26結石, 有効3結石で有効率は85%であった, YACHIYODA SZ-5000 is a new model of lithotriptor made in Japan, of which the energy source is microexplosion. Compared with the old type of SZ-1, the water bag is substituted for a hot water bath and ultrasonography as well as fluoroscopy can be used for stone localization. Moreover, this new model is extremely small. The first clinical trial of 32 candidates with urinary tract calculi (34 stones) was performed at our hospital between September 1991 and June 1992. They were 10 women and 22 men between 25 and 71 with a mean of 47.3 years. All patients received no anesthesia. The stone location was: R2 for 16 stones, R3 for 5, U1 for 9, U2 for 1, and U3 for 3. The mean size was 14.1 mm. A mean number of 364, 326 and 324 shock waves were given for the R2, 3, U1, and U2, 3 stones, respectively. The second or third sessions were performed on 7 patients. Obvious symptoms and signs observed during the treatment were; local pain in 9 patients, nausea in 3, hypotension and bradycardia in 6, and hypertension in 3. Posttreatment fever up was found in two patients. In 34 stones, the efficiency evaluated 3 months later was 85.0% as determined by kidney-ureter-bladder X-ray and intravenous pyeography. In conclusion, YACHIYODA SZ-5000 is useful and safe in the management of patients with urinary tract stones.

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.

淋菌に対するLVFXの抗菌力は≦0.003 μg/ml～0.39 μg/mlに分布, MIC50 0.0125 μg/ml, MIC90 0.1 μg/mlでありCPFX, TFLX, SPFX, FLRX, OFLXとほぼ同程度であり, NFLX, ENX, LFLXと比べやや優れていた.PPNGに対する抗菌力はnon-PPNGと比べ差はなくβ-lactamaseに対する安定性を認めた.臨床的有用性については対象10例中, LVFXを1回200 mg, 1日2回を8例に, 1回100 mg, 1日2回を2例に, いずれも3日間投与した.総合有効率は著効4例, 有効4例であった.Chlamydia trachomatis(クラミジア)混合感染例は2例あり, ともに有効であった.副作用の発現はなかった, We performed basic and clinical studies in male gonococcal urethritis on a new oral antimicrobial agent, levofloxacin (LVFX, DR-3355), a new quinolone derivative. The antibacterial activity of LVFX against clinical strains of Neisseria gonorrhoeae was roughly comparable to that of ofloxacin, and ciprofloxacin. LVFX was administered to 10 males with gonococcal urethritis, 200 mg twice a day (8 cases) or 100 mg twice a day for 3 days (2 cases). Clinical evaluation was made according to the criteria of the Japanese UTI Committee. Overall efficacy rate was 100% (10/10). In the complication of chlamydia trachomatis (2 cases), efficacy rate was 100% (2/2). No subjective or objective adverse reactions occurred.

新規注射用cephalosporin剤CPRの淋菌に対する抗菌力と前立腺, 腎臓の組織移行性を検討した.1)当科保存のNeisseria gonorrhoeae(非PPNG 34株, PPNG 20株)に対するCPRのMIC分布は非PPNGで≦0.003～0.1 μg/ml, PPNGで0.006～0.1 μg/mlで, MIC90はそれぞれ0.1 μg/ml, 0.05 μg/mlであった.2) CPR 1 g静注時の血中濃度と前立腺組織内濃度を30症例で検討した.組織内濃度は投与後15分で52.8 μg/gと最高値をとり, 以後経時的に漸減し, 60分平均値17.9 μg/g, 180分値10.1 μg/g, 320分値7.22 μg/g, 360分値2.70 μg/gであった.組織内濃度と組織採取時の血中濃度とは正相関をもち, 前立腺組織へは血中濃度に応じた組織移行が起こると考えられる.3)腎組織内濃度は4例で測定し, 投与90～100分後で皮質内濃度は107～148 μg/g, 髄質内濃度は80.6～88.6 μg/gといずれの症例も血中濃度を上回っていた.以上の点よりCPRは淋菌に対し優れた抗菌力を持つとともに十分な血中および組織内濃度を示し, 泌尿器感染症においても有用性が高い, The antibacterial activity of cefpirome (CPR), a new parenteral cephalosporin antibiotic having a cyclopentenopyridine group in the 3-position side chain, was evaluated against Neisseria gonorrhoeae and concentrations in human kidney and prostate was determined. The minimum inhibitory concentrations (MICs) of CPR against N. gonorrhoeae isolated clinically in our out-clinic (34 strains of non-PPNG and 20 of PPNG) were less than or equal to 0.003-0.1 microgram/ml in non-PPNG group and 0.006-0.1 microgram/ml in PPNG group. The 90% of MICs (MIC90s) was 0.1 microgram/ml in the non-PPNG group and 0.05 microgram/ml in the PPNG group. The concentration in the prostate was determined in 30 cases with benign prostatic hypertrophy. The maximum values was 52.8 micrograms/g at 15 minutes after administration of 1 g of CPR. The levels of CPR were gradually decreased with the lapse of time. The prostatic tissue concentration was 17.9 micrograms/g at 60 min., 10.1 micrograms/g at 180 min., 7.22 micrograms/g at 320 min. and 2.70 micrograms/g at 360 min. There was a positive correlation between concentration of the prostate and plasma collected at the time of the prostate. The concentration of CPR in human kidney, 90-100 min. after administration of 1 g to 4 cases with renal tumor, was 107-148 micrograms/g in the renal cortex, and 80.6-88.6 micrograms/g in the renal medulla. The concentration in kidney was higher than that in the plasma in all cases. In conclusion, CPR is suggested to be a useful drug for urological infection.

66歳男, 重量2, 258 g, 血中β-HCG陽性の巨大セミノーマの症例, A 66-year-old man visited our hospital with a history of a slowly growing left scrotal contents for the past 5 years. Serum beta-human chorionic gonadotropin and lactate dehydrogenase was greatly elevated. The resected mass was 26 cm x 16 cm x 13 cm in size, 2, 258 g in weight. It arose from left testis and grew to the left inguinal region. Histologically it was pure seminoma.

Extracorporeal shock wave lithotripsy (ESWL) using YACHIYODA SZI was performed on 12 patients with renal stones and the effect on the kidney and adjacent tissue was evaluated by magnetic resonance imaging (MRI) before and after treatment. Some changes were seen in 6 of the 12(50%) patients; perirenal fluid collection in 2 of the 12 (16.7%) patients, subcapsular hematoma in 2 of the 12 (16.7%) patients, renal enlargement in 5 of the 12 (31.3%) patients, increased signal intensity in perirenal tissue in 6 of the 12 (50%) patients, and loss of the corticomedullary junction 2 out of 9 patients (22%). These findings indicated fewer changes in the kidney after ESWL using YACHIYODA SZI than in the other reports. MRI is also concluded to be effective to detect the changes of the kidney after ESWL.

YACHIYODA SZ-5000 is a new model of lithotriptor made in Japan, of which the energy source is microexplosion. Compared with the old type of SZ-1, the water bag is substituted for a hot water bath and ultrasonography as well as fluoroscopy can be used for stone localization. Moreover, this new model is extremely small. The first clinical trial of 32 candidates with urinary tract calculi (34 stones) was performed at our hospital between September 1991 and June 1992. They were 10 women and 22 men between 25 and 71 with a mean of 47.3 years. All patients received no anesthesia. The stone location was: R2 for 16 stones, R3 for 5, U1 for 9, U2 for 1, and U3 for 3. The mean size was 14.1 mm. A mean number of 364, 326 and 324 shock waves were given for the R2, 3, U1, and U2, 3 stones, respectively. The second or third sessions were performed on 7 patients. Obvious symptoms and signs observed during the treatment were; local pain in 9 patients, nausea in 3, hypotension and bradycardia in 6, and hypertension in 3. Posttreatment fever up was found in two patients. In 34 stones, the efficiency evaluated 3 months later was 85.0% as determined by kidney-ureter-bladder X-ray and intravenous pyeography. In conclusion, YACHIYODA SZ-5000 is useful and safe in the management of patients with urinary tract stones.

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.

We performed basic and clinical studies in male gonococcal urethritis on a new oral antimicrobial agent, levofloxacin (LVFX, DR-3355), a new quinolone derivative. The antibacterial activity of LVFX against clinical strains of Neisseria gonorrhoeae was roughly comparable to that of ofloxacin, and ciprofloxacin. LVFX was administered to 10 males with gonococcal urethritis, 200 mg twice a day (8 cases) or 100 mg twice a day for 3 days (2 cases). Clinical evaluation was made according to the criteria of the Japanese UTI Committee. Overall efficacy rate was 100% (10/10). In the complication of chlamydia trachomatis (2 cases), efficacy rate was 100% (2/2). No subjective or objective adverse reactions occurred.

A 66-year-old man visited our hospital with a history of a slowly growing left scrotal contents for the past 5 years. Serum beta-human chorionic gonadotropin and lactate dehydrogenase was greatly elevated. The resected mass was 26 cm x 16 cm x 13 cm in size, 2, 258 g in weight. It arose from left testis and grew to the left inguinal region. Histologically it was pure seminoma.

The antibacterial activity of cefpirome (CPR), a new parenteral cephalosporin antibiotic having a cyclopentenopyridine group in the 3-position side chain, was evaluated against Neisseria gonorrhoeae and concentrations in human kidney and prostate was determined. The minimum inhibitory concentrations (MICs) of CPR against N. gonorrhoeae isolated clinically in our out-clinic (34 strains of non-PPNG and 20 of PPNG) were less than or equal to 0.003-0.1 microgram/ml in non-PPNG group and 0.006-0.1 microgram/ml in PPNG group. The 90% of MICs (MIC90s) was 0.1 microgram/ml in the non-PPNG group and 0.05 microgram/ml in the PPNG group. The concentration in the prostate was determined in 30 cases with benign prostatic hypertrophy. The maximum values was 52.8 micrograms/g at 15 minutes after administration of 1 g of CPR. The levels of CPR were gradually decreased with the lapse of time. The prostatic tissue concentration was 17.9 micrograms/g at 60 min., 10.1 micrograms/g at 180 min., 7.22 micrograms/g at 320 min. and 2.70 micrograms/g at 360 min. There was a positive correlation between concentration of the prostate and plasma collected at the time of the prostate. The concentration of CPR in human kidney, 90-100 min. after administration of 1 g to 4 cases with renal tumor, was 107-148 micrograms/g in the renal cortex, and 80.6-88.6 micrograms/g in the renal medulla. The concentration in kidney was higher than that in the plasma in all cases. In conclusion, CPR is suggested to be a useful drug for urological infection.