Ofloxacin concentration in human prostatic tissue after 3 days of administration

The present study was undertaken to evaluate the penetration of ofloxacin into prostatic tissue. Thirty-one patients with benign prostatic hypertrophy were entered in the study. Ofloxacin was administered orally in a dose of 200 mg three times daily for 3 days preoperatively. Blood samples were taken simultaneously at the time of tissue sampling. The patients were divided into 2 groups. In group 1, tissue sampling was done about 17 hours after the final drug administration. The mean concentration of ofloxacin was 6.88 +/- 3.98 micrograms/g in prostatic tissue and 2.14 +/- 0.81 micrograms/ml in serum. In group 2, sampling was done 5.5 hours after the final administration. The mean concentration of ofloxacin was 6.73 +/- 2.99 micrograms/g in prostatic tissue and 2.90 +/- 1.50 micrograms/ml in serum.     

Enoxacin concentration in human prostatic tissue after 3-day administration

The penetration of enoxacin into prostatic tissue was examined Thirty-five patients with benign prostatic hypertrophy entered the study. Enoxacin was administered orally in a dose of 200 mg three times daily for 3 days preoperatively. Blood samples were taken simultaneously at the time of tissue sampling. The patients were divided into groups 1 and 2. In group 1, tissue sampling was done after about 17 hours of final administration of the drug. The mean concentration of enoxacin in prostatic tissue was 1.87 +/- 1.23 micrograms/g and 1.05 +/- 0.458 micrograms/ml in serum. In group 2, sampling was done after 5.5 hours of final administration. The mean concentration of enoxacin in prostatic tissue was 2.51 +/- 0.725 micrograms/g and 1.78 +/- 0.586 micrograms/ml in serum.     

Norfloxacin concentration in human prostatic tissue after 3 days administration

The penetration of norfloxacin into prostatic tissue was evaluated on 36 patients with benign prostatic hypertrophy. Norfloxacin was administered orally in a dose of 200 mg three times daily for 3 days preoperatively, blood samples were taken simultaneously at the time of tissue sampling. The patients were divided into 2 groups, groups 1 and 2. In group 1, tissue sampling was done after about 17 hours of final administration of the drug. The mean concentration of norfloxacin in prostatic tissue was 0.38 +/- 0.18 micrograms/g and 0.18 +/- 0.09 micrograms/ml in serum. In group 2, sampling was done after 5.5 hours of final administration. The mean concentration of norfloxacin in prostatic tissue was 0.89 +/- 0.32 micrograms/g and 0.49 +/- 0.25 micrograms/ml in serum.     

Ciprofloxacin concentration in human prostatic tissue following 3 days' administration]

The penetration of Ciprofloxacin (CPFX) into the prostatic tissue and the serum was examined. Forty-four patients with benign prostatic hypertrophy treated with transurethral resection of the prostate were entered in this study. CPFX was administered orally in a dose of 200 mg three times daily for three days preoperatively. The blood samples were taken simultaneously at the time of the tissue sampling. The patients were divided into groups 1 and 2. In group 1 (16 patients), the tissue sampling was done about 17 hours after the final drug administration. The mean concentration of CPFX was 0.61 +/- 0.40 microgram/g in the prostatic tissue and 0.27 +/- 0.19 micrograms/ml in the serum. In group 2 (28 patients), tissue sampling was done 5.5 hours after the final drug administration. The mean concentration of CPFX was 1.32 +/- 0.64 micrograms g in the prostatic tissue and 0.65 +/- 0.31 microgram/ml in the serum.     

Diffusion of ofloxacin (OFLX) into prostatic tissue in patients with benign prostatic hypertrophy]

Diffusion of ofloxacin (OFLX) into prostatic tissue was studied in 31 patients with benign prostatic hypertrophy. Concentrations of OFLX in the serum and prostatic tissue were measured at scheduled intervals after 200 mg OFLX oral administration. The mean OFLX level in prostatic tissue and tissue/serum ratio at 2 hours, 4 hours and 6 hours was 3.33 +/- 0.96 micrograms/g (1.25 +/- 0.28) in 10 patients, 2.21 +/- 0.55 micrograms/g (0.92 +/- 0.32) in 9 patients and 2.10 +/- 0.99 micrograms/g (1.01 +/- 0.23) in 12 patients, respectively. OFLX levels in prostatic tissue covered the minimum inhibitory concentration for several pathogenic bacteria detected from the infected prostatic fluid. Therefore, OFLX was thought to be a very useful drug for the treatment of bacterial prostatitis and postoperative infection of prostatic surgery.     

Ceftazidime concentration in human prostatic tissue and serum following intravenous injection]

The present study was undertaken to evaluate the penetration of Ceftazidime (CAZ) into prostatic tissue (P) and serum (S). Thirty-seven patients with benign prostatic hypertrophy took part in this study. CAZ was administered intravenously at a dose of 1g preoperatively. Blood samples were taken simultaneously at the time of tissue sampling by transurethral resection of the prostate (TUR-P). The patients were divided into 3 groups. In group 1 (twelve patients), intravenous injection of the drug was given 60 minutes before tissue sampling. The mean concentrations of CAZ were 23.4 +/- 7.4 micrograms/g in the prostatic tissue and 45.0 +/- 15.9 micrograms/ml in the serum. In group 2 (thirteen patients), the injections were given 120 minutes before tissue sampling. The mean concentrations of CAZ were 18.0 +/- 8.2 micrograms/g in the prostatic tissue and 39.8 +/- 21.3 micrograms/ml in the serum. In group 3 (twelve patients), the injections were given 240 minutes before tissue sampling. The mean concentrations of CAZ were 11.3 +/- 3.2 micrograms/g in the prostatic tissue and 22.3 +/- 9.6 micrograms/ml in the serum. These findings indicate that CAZ is useful for the treatment of prostatitis and preventive medication before TUR-P.     

Minocycline diffusion into prostatic tissue

We evaluated the concentration of minocycline in human prostatic tissue. Twenty-six patients undergoing transurethral resection of prostate, two patients undergoing open prostatectomy for benign prostatic hyperplasia and two patients undergoing radical cystoprostatectomy for bladder cancer were studied. Prostatic tissue and blood were sampled at 1, 2 or 3 hours after the intravenous administration of 200 mg of minocycline. The concentration of minocycline was 2.95 +/- 1.39 micrograms/ml (mean +/- SD) in serum and 1.97 +/- 0.79 cg/g (mean +/- SD) in the prostatic tissue. The ratio of the prostatic concentration/serum concentration was 0.76 +/- 0.33 (mean +/- SD).     

Study on the concentration of cefminox sodium in serum and prostatic tissue]

The concentration of cefminox sodium (CMNX) in serum and prostatic tissue was determined in 25 patients with benign prostatic hypertrophy. One gram of CMNX was intravenously administered prior to transurethral prostatectomy. Blood and prostatic tissue were obtained 1 hour after the administration of CMNX. The concentration of CMNX was 69.17 +/- 17.47 micrograms/ml (mean +/- SD) in serum and 5.33 +/- 2.33 micrograms/g (mean +/- SD) in the prostatic tissue. The ratio of the prostatic tissue concentration/serum concentration was 8.18 +/- 4.45% (mean +/- SD). There was no correlation between serum and prostatic tissue level of CMNX.     

Prostatic tissue levels of ceftizoxime

The concentration of Ceftizoxime (CZX) was determined in the prostatic tissue and serum of 130 patients with benign prostatic hypertrophy. Two grams of CZX was given by intravenous injection prior to TUR. The mean value of CZX levels in prostatic tissue and prostatic level/serum levels ratio (p/s ratio) after administration were 47.2 +/- 2.8 micrograms/g, 49.1% at 30 minutes, 33.3 +/- 2.2 micrograms/g, 51.4% at one hour, 22.2 +/- 2.7 micrograms/g, 60.8% at 2 hours, 13.6 +/- 3.9 micrograms/g, 64.2% at 4 hours, 3.04 +/- 0.54 micrograms/g, 74.5% at 8 hours, respectively. In conclusion, the concentration of CZX in the prostatic tissues attained the minimal inhibitory concentration of 80% for the gram-negative bacteria, the excluding P. aeruginosa. Thus clinical effectiveness of CZX could be expected on bacterial prostatitis and bacterial infection after prostatic operations.     

Diffusion of cefmenoxime into prostatic fluid in the patients with acute bacterial prostatitis

Expressed prostatic fluid (EPS) levels and serum levels of cefmenoxime (CMX) after intravenous administration were examined in 16 patients with acute bacterial prostatitis and 23 patients without prostatic diseases. Blood was drawn at 30, 60, 120 minutes and EPS was taken by prostatic massage at 60 minutes after the intravenous administration of 2 g CMX to evaluate the concentration of CMX. The concentration of CMX was determined by the bioassay using the E. coli NIHJ JC strain. The relationships between the EPS/serum ratio and peripheral WBC counts, CRP value and ESR 1h value were also analyzed. The serum levels of CMX at 60 minutes ranged between 20.3 micrograms/ml and 73.5 micrograms/ml (mean +/- S.D.: 41.8 +/- 14.2 micrograms/ml) in 16 patients with acute prostatitis, and between 21.5 micrograms/ml and 89.5 micrograms/ml (mean +/- S.D.: 49.5 +/- 18.7 micrograms/ml) in 23 patients without prostatic diseases. The EPS levels ranged between 0.4 micrograms/ml and 30.8 micrograms/ml (mean +/- S.D.: 12.6 +/- 9.6 micrograms/ml) in 16 patients with acute prostatitis, and between 0 and 2.3 micrograms/ml (mean +/- S.D.: 0.7 +/- 0.8 microgram/ml) in 19 patients without prostatic diseases. In 4 patients without prostatic diseases, the EPS amount was not large enough to evaluate the concentration of CMX. The EPS/serum ratio ranged between 0.006 and 0.697 (mean +/- S.D.: 0.31 +/- 0.21) in patients with acute prostatitis and between 0 and 0.058 (mean +/- S.D.: 0.015 +/- 0.018) in patients without prostatic diseases. The diffusion of CMX into the prostatic fluid in patients with acute prostatitis was strikingly higher than that in patients without prostatic diseases (p less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)     

Astromicin sulfate concentration in human prostatic tissue after an intramuscular injection

The present study was undertaken to evaluate the penetration of astromicin sulfate into prostatic tissue. Twenty eight patients with benign prostatic hypertrophy entered the study. Astromicin sulfate was administered as an intramuscular injection in a dose of 200 mg one hour preoperatively. Blood samples were taken simultaneously with the tissue sampling at the transurethral resection of the prostate. The mean concentration of astromicin sulfate in prostatic tissue was 3.79 +/- 1.01 micrograms/g and that in serum was 10.25 +/- 2.70 micrograms/ml.     

A study on enoxacin concentration in human prostatic tissue]

To examine the penetration of enoxacin into prostatic tissue of patients with benign prostatic hypertropHy, the serum concentration and prostatic tissue level of enoxacin were measured. Enoxacin was administered orally at a dose of 200 mg, three times 2 days and one day before and once on the day of the operation. Blood and prostatic tissue samples were taken during the operation. The mean concentration of enoxacin was 2.84 +/- 0.349 g/ml in serum and 4.60 +/- 0.631 micrograms/ml in the prostatic tissue.     

A study on transfer of ceftizoxime into prostatic and vesical tissues

Prostatic and vesical tissue levels of Ceftizoxime (CZX) were determined in 21 patients with prostatic hyperplasia after the intravenous administration of 1 g of CZX. Serum concentration on prostatic surgery continued to be 1.3 fold higher than that of healthy adults. Prostatic tissue levels attained a peak of 40.7 +/- 1.6 micrograms/g (mean +/- SE) at 30 minutes after administration and vesical tissue levels attained a peak of 72.4 +/- 24.8 micrograms/g at 30 minutes. The mean value was 21.0 +/- 6.4 micrograms/g in prostatic tissue after administration for 120 minutes with the tissue/serum ratio of 0.91. Prostatic tissue level in glandular dominant were slightly higher than those of myoglandular hyperplasia (P less than 0.1). Judging from its favorable transfer into the prostatic tissue and MIC against clinically isolated E. coli, Proteus sp. and Klebsiella, CZX seemed to be clinically useful in the treatment of prostatic infection.     

Concentration level of latamoxef sodium (LMOX) in prostatic tissue

The concentration of latamoxef sodium (LMOX) in serum and prostatic tissue was evaluated. Thirty seven patients with benign prostatic hypertrophy were given 1 g LMOX intravenously prior to prostatectomy. Prostatic tissue and blood were sampled at 1, 2 or 3 hrs after administration of LMOX. The concentration of LMOX in prostatic tissue was 17.4 +/- 3.4 micrograms/g tissue, 11.1 +/- 1.3 microgram/g tissue and 8.9 +/- 1.3 microgram/g tissue 1, 2 and 3 hrs after injection, respectively (mean +/- S.E.). The penetration ratio of LMOX (concentration in tissue/in serum) to prostate was 30-45%. Therefore, the 80% MIC of LMOX is lower than 8 micrograms/ml for most gram negative bacteria, the results suggest that LMOX is very effective against prostatitis caused by these organisms.     

Ofloxacin concentration in human benign prostatic tissue after oral administration

The penetration of ofloxacin (OFLX) into prostatic tissue was examined on 11 patients with benign prostatic hypertrophy. OFLX was administered orally in a dose of 200 mg, three times one day before and twice on the day of operation. The blood sample was taken 30 minutes before operation and prostatic tissue specimens were collected during operation. The mean concentration of OFLX in prostatic tissue was 5.51 +/- 1.79 micrograms/g (mean +/- SD) and 5.36 +/- 1.28 micrograms/ml in serum. The mean ratio of these concentrations was 1.06 +/- 0.31 (range 0.55-1.54). These findings indicate that OFLX will be valuable against bacterial prostatitis.     

Study of the prostatic tissue cefbuperazone (CBPZ) level

The concentration of Cefbuperazone (CBPZ) was determined in the prostatic tissue and serum of 23 patients with benign prostatic hypertrophy. One or 2 of CBPZ was injected intravenously prior to transurethral prostatectomy. The mean CBPZ level in prostatic tissue and tissue/serum ratio at 1 hour was 17.4 +/- 7.2 micrograms/g (28.9 +/- 9.1%) in 10 patients administered 1 g of CBPZ, and 34.7 +/- 1C.2 micrograms/g (35.7 +/- 13.2%) in 13 patients administered 2 g of CBPZ. Serum and prostatic tissue CBPZ levels responded satisfactorily to the dose of CBPZ. Weights of resected prostatic tissue were not correlated to the tissue CBPZ level. Judging from the inhibitory concentration of CBPZ (minimum inhibitory concentration 80), the prostatic tissue CBPZ level was sufficient against pathogenic bacteria, particularly E. coli, K. pneumoiae and P. mirabilis for a relatively long time. For this reason CBPZ is a very useful drug for treatment of bacterial prostatitis and postoperative infection of prostate.     

Prostatic tissue levels of cefpiramide (CPM)

The concentration of CPM in prostatic tissue and serum in 12 patients with benign prostatic hypertrophy was measured. One gram of CPM was injected intravenously prior to prostatectomy. One, 2, 3 and 5 hours following the administration of CPM, the mean serum level of CPM was 142, 88.2, 87.4 and 61.2 micrograms/ml, respectively, while the mean level in the prostatic tissue was 48.3, 15.1, 15.6 and 8.3 micrograms/g, respectively. The prostatic tissue level of CPM was thought to be enough to eradicate gram-negative and gram-positive bacteria in the prostate. It is presumed from our study that clinical effectiveness of CPM might be expected in the case of acute or chronic bacterial prostatitis.     

Diffusion of sulbactam and cefoperazone into the prostatic tissue

Diffusion of sulperazone (SBT) and cefoperazone (CPZ) into the prostatic tissue was studied in 20 cases. Two g of SBT/CPZ was injected intravenously and 1 hour later, prostatic tissue was obtained surgically and venous blood was drawn simultaneously. The serum concentration of CPZ (58.0 micrograms/ml +9.2) was higher than that of SBT (25.9 micrograms/ml +/- 9.3) and the prostatic tissue concentration of CPZ (14.9 micrograms/ml +/- 6.1) was higher than that of SBT (10.9 micrograms +/- 6.1). However, the SBT concentration ratio of prostatic tissue to serum level (P/S ratio) was significantly higher (42.5%) than that of CPZ (25.9%). The SBT concentration in the prostatic tissue was high enough to enhance the antibacterial activity of CPZ. SBT/CPZ was appraised to be an effective chemotherapeutic agent for infections of prostate caused by susceptible organisms, especially by beta-lactamase producing bacteria.     

Epoxycholesterols in secretions and tissues of normal, benign, and cancerous human prostate glands

Extracts of prostatic secretions taken from 25 control subjects, twenty-three to seventy-five years of age, were analyzed by gas-liquid chromatography (GLC) for cholesterol and possible epoxycholesterol content. Only subjects fifty-three years or older exhibited any signs of prostatic enlargement. Whereas cholesterol (893 +/- 133 micrograms/ml) was found in all prostatic secretions, the carcinogenic epoxycholesterols (22.6 +/- 3.3 micrograms/ml) were detected only in one third of the specimens examined. Prostatic secretion collected from 29 surgical patients prior to primary (20) and secondary (9) prostatectomies revealed cholesterol contents of 1,182 +/- 148 and 1,134 +/- 157 micrograms/ml, respectively. The epoxycholesterols were essentially present at concentrations of 33.7 +/- 7.9 and 24.0 +/- 10.3 micrograms/ml, respectively. Tissue extracts of the different prostatic lobes taken from 40 surgical BPH patients at the time of primary (26) and secondary (14) prostatectomy were examined by capillary GLC. Of these patients 8 had prostatic carcinoma. The cholesterol content of all tissues was essentially double that of normal prostates. The epoxycholesterols were present in all tissues. The mean cholesterol 5 alpha, 6 alpha-epoxide and cholesterol 5 beta, 6 beta-epoxide contents of all tissue were 120 +/- 23.4 and 9.9 +/- 5.2 micrograms/Gm dry tissue, respectively. There were no apparent differences beteeen the lobes nor between BPH and cancers. No epoxycholesterol could be detected in 8 seminal vesicles obtained at autopsy.     

A study of prostatic tissue levels of latamoxef, cefoperazone and cefotaxime

Although Cephem antibiotics are transferred to the prostatic fluid in relatively low levels, they are clinically effective for bacterial prostatitis. In the present study, the prostatic tissue concentration of Latamoxef (LMOX), Cefoperazone (CPZ) and Cefotaxime (CTX) were determined, and their penetration rates into the prostatic tissue were analyzed. Before the transurethral resection of the prostate (TUR-P), 2 g of LMOX (21 patients), 1 g of CPZ (15 patients) and 2 g of CTX (14 patients) were intravenously administered in a total of 50 patients with benign prostatic hypertrophy at our two Hospitals. The prostatic tissue was taken by TUR-P at 30 minutes and 60 minutes after the injection. The serum concentration and the prostatic tissue concentration of the three antibiotics were determined by the bioassay method. Additionally their serum concentration and the prostatic tissue concentration in the six cases of CTX-injected patients were also determined by high performance liquid chromatography (HPLC). The penetration rate into the prostatic tissue was obtained by the formula; the penetration rate = the prostatic tissue concentration/the serum concentration. The prostatic tissue concentrations determined by the bioassay method were, 36.9 +/- 10.6 micrograms/g at 30 minutes after the injection of 2 g of LMOX and 28.0 +/- 9.0 micrograms/g at 60 minutes, 31.0 +/- 8.3 micrograms/g at 30 minutes after the injection of 1 g of CPZ and 21.1 +/- 10.0 micrograms/g at 60 minutes, and 8.8 +/- 4.1 micrograms/g at 30 minutes after the injection of 2 g of CTX and 4.5 +/- 2.0 micrograms/g at 60 minutes (mean +/- S.D.). The penetration rates determined by the bioassay method were 36.2 +/- 10.9% at 30 minutes after the injection of LMOX and 34.8 +/- 15.3% at 60 minutes, 43.6 +/- 14.4% at 30 minutes after the injection of CPZ and 39.7 +/- 24.1% at 60 minutes, and 11.1 +/- 4.1% at 30 minutes after the injection of CTX and 9.6 +/- 3.8% at 60 minutes (mean +/- S.D.). The penetration rate of CPZ and LMOX were significantly higher than that of CTX (P less than 0.05, P less than 0.01). In 6 of the 14 CTX-injected patients, the serum and prostatic tissue concentrations of CTX and its metabolite, desacetyl-CTX, were also determined by HPLC. The penetration rate of CTX into the prostatic tissue was obtained by the formula; the penetration rate of CTX = the prostatic tissue concentration (CTX + Desacetyl-CTX)/the serum concentration (CTX + Desacetyl-CTX).(ABSTRACT TRUNCATED AT 400 WORDS)