A new class of nonhormonal pregnancy-terminating agents. Synthesis and contragestational activity of 3,5-diaryl-s-triazoles.

A series of 3,5-diaryl-s-triazoles were synthesized and evaluated as postimplantation contragestational agents. The introduction of various substituents (e.g., an o-alkyl chain on one phenyl and a m-alkoxy group on the other) was found to increase the potency. Several compounds with very high pregnancy-terminating activity in both hamsters and rats were obtained. One of these, 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-s-triazole, DL 111 (36), was selected for detailed evaluation in various animal species. A synthetic scheme for the preparation of these compounds and preliminary structure-activity relationships are presented.

Laparoscopic unroofing of simple renal cysts.

OBJECTIVE: The aim of this study was to assess the clinical reliability of laparoscopic treatment for simple renal cysts. METHODS: Twenty patients with symptomatic simple renal cysts underwent laparoscopic unroofing of the cysts. Four of these patients also underwent concomitant laparoscopic cholecystectomy because of symptomatic gallbladder stones. RESULTS: In all cases the cyst wall was widely resected with no significant surgical complication. Cholecystectomy was easily performed without additional morbidity. Postoperative renal ultrasonography and intravenous urography demonstrated the absence of cyst recurrences and the integrity of the excretory tract. Symptoms were resolved by the operation in all cases. CONCLUSIONS: Laparoscopic unroofing is a safe, effective, and minimally invasive treatment for selected symptomatic simple renal cysts.

[Repeated ultrasound-guided transrectal prostate biopsy in patients with negative histologic test]. / Il campionamento bioptico prostatico transrettale ecoguidato iterativo in pazienti con esame istologico negativo.

The screening programs for prostate cancer will affect a number increasing of patients over 50 years with consequence rising the bioptic demand. Nevertheless the istopathologic results are negatives for carcinoma in the most part of patients. It's evident that a part of carcinomas are lost at biopsy. Two hundred four patients where submitted at second bioptic session after a maximum of 12 months. Our results show a percent probability of positive findings in 12%. In 75% cancer diagnosed in that second session had clinically significance. Prostate specific antigen (PSA) value, in our study, is the most positive predictive parameter for prostate cancer at second biopsy. Patients with PSA > 10 ng/ml have a risk 7 times greater of having a prostatic cancer respect to patients with PSA < 10 ng/ml. PSA density, PSA velocity and the presence of ipoecoic areas previously biopsied, aren't risk factors for detection of prostate cancer at second bioptic session.

[Complications of multiple transrectal ultrasound-guided biopsy of the prostate]. / Complicanze del campionamento bioptico multiplo prostatico transrettale.

The screening programs for prostate cancer will affect a number increasing of patients over 50 years with consequence rising the bioptic demand. For these reason it's important to know the real morbidity correlate with these widespread diagnostic method that will know a larger use in the future. Our study involve 1.467 patients with median age of 66.7 years (range 45-93). Forty-five were diabetics, 80 took a chronic anti-aggregant salicylic therapy, 25 took a chronic coumarolic anticoagulation therapy, 54 had a recent history of prostatitis. Our major complication rate was 0.7% of patients requesting hospital admission and care. An intermediate category of complications was considered, with complication rate of 6.9% and indication for out-patient treatment. Minor complication rate was 76% without need of therapy. In spite of high number of biopsies per patient, our major complication rate is similar of that demonstrate from other authors. In conclusion, whole complication rate is high, but the incidence of major complications is very low. The complications that need out-patient treatment are limited and acceptable.

[Echo-guided transperineal and transrectal prostatic biopsy: complications of the 2 methods]. / Biopsia prostatica ecoguidata transperineale e transrettale: complicanze delle due metodiche.

We evaluated the complications of transrectal and transperineal ultrasound-guided prostatic biopsy in 280 patients. All patients underwent antibiotic prophylaxis with a different scheme according to the approach for the biopsy. Urine culture and, in some patients, blood culture have been collected after biopsy. We have reported the same rate of complications for the two modalities except for a lower rate of positive urine culture and blood culture in the group of patients submitted to transperineal biopsy; this type of approach, then, should be considered of first choice in some patients with a higher risk of infections.

[Laparoscopic adrenalectomy: a case report]. / Surrenalectomia laparoscopica: case report.

The authors report the first case of laparoscopic adrenalectomy for Conn's disease. The operative technique and clinical results are thoroughly discussed.

[Percutaneous echo-guided drainage and sclerotherapy of symptomatic renal cysts: critical comparison with laparoscopic treatment]. / Drenaggio percutaneo ecoguidato e sclerotizzazione delle cisti renali sintomatiche: confronto critico con il trattamento laparoscopico.

Nowadays, the minimally invasive treatment of symptomatic renal cyst has been progressively gaining wide acceptance while classic open surgery has been almost abandoned. It is a still controversial which minimally invasive approach provides the major advantages and results. Fifty-two patients with symptomatic simple renal cyst underwent ultrasound guided percutaneous drainage and sclerotherapy (ethanol 95 degrees) and 20 patients underwent laparoscopic unroofing of simple renal cysts in our department. No major complication was recorded with both the techniques. Even if we reported a higher recurrence rate (82%) with sclerotherapy than that with laparoscopic treatment (5%) we consider the percutaneous drainage a valid approach because it is a safe, easy and at low cost procedure.

[Synthesis of 2-aminoisoindolin-1-ones with or without 6-substituents]. / Sintesi di 2-aminoisoindolin-1-oni-5 e/o 6-sostituiti

The synthesis of 5- and 6-chloro, 5- and 6-methoxy, 5,6-dimethoxy, 6-amino and 6-nitro-2-aminoisoindolin-1-ones (III b...h), starting from the substituted phthalides (Vb...g), are reported. Chloro and methoxy-derivatives (III b...f) have been prepared by reduction of phthalazin-1-(2H)-ones (Ib...f) with zinc and acids under controlled conditions to afford the 3,4-dihydrocompounds (II), that have been rearranged to (III b...f) with hydrazine hydrate or hydrochloric acid (Scheme 3). The synthesis of 6-nitro and 6-amino-derivatives (III g,h) have been respectively accomplished by hydrolysis and hydrogenolysis of 6-nitro-2-benzylidenaminoisoindolin-1-one (IV g), prepared by chlorination and ring closure with sodium carbonate of benzylidenhydrazide of 5-nitro-2-hydroxymethyl-benzoic acid (Scheme 2).

The synthesis of 2 14C-labelled 2-(3-alkoxyphenyl)-5,6-dihydro-5-trazolo[5, 1-a] isoquinoline compounds, novel antifertility agents.

PIP: 2 new compounds, L-10503, 2-(3-methoxyphenyl)-5,6-dihydro-s-triazolo [5,1-a] isoquinoline and DL-204 IT, 2-(3-ethoxyphenyl)-5,6-dihydro-s-triazolo [5,1-a] isoquinoline have been developed in the Lepetit Research Laboratories in Milan, Italy. These compounds have been tested in monkeys and rats and have been shown to terminate pregnancy after a single intramuscular injection. Pharmocokinetical, metabolic, and placental absorption studies of these compounds required synthesis of 14 C labelled forms for both. This article describes in details the laboratory procedures to obtain synthesis of these compounds.^ieng

Long-term clinical reliability of transurethral and open prostatectomy for benign prostatic obstruction: a term of comparison for nonsurgical procedures.

To elucidate the long-term reliability of prostatectomy, we evaluated 92 benign prostatic hyperplasia patients who had been submitted to either transurethral or open surgery at the 5-year follow-up. Ninety-five percent of the patients were still nonobstructed and subjectively satisfied of their urinary status. Postoperative mortality was presumably not related to the previous operation. Until now, nonsurgical procedures did not guarantee the results achieved by surgical treatment and should thus be reserved for patients at high operative risk or refusing surgery.

Extracorporeal lithotripsy and combined surgical procedures in the treatment of renoureteral stone disease: our experience with 2,955 patients.

From May, 1985 to August, 1987, a total of 2,955 patients with renoureteral stone disease presented at our institution and were treated either by extracorporeal lithotripsy alone or combined with percutaneous nephrolithotomy, ureteroscopy, or open surgery. Seventy-three percent of patients were stone-free at the 3 month follow-up date while 22% presented with negative urine culture and small (less than 5 mm) asymptomatic fragments deemed susceptible to spontaneous discharge. The rate of major complications was extremely low (sepsis, 0.03% and major renal bleeding, 1.55%). The application of this multimodal therapeutic strategy allowed successful treatment in almost every case of renoureteral lithiasis with minor iatrogenic damage to the renal parenchyma.

Prostatic UroLume Wallstent for urinary retention due to advanced prostate cancer: a 1-year followup study.

We attempt to clarify the long-term clinical reliability of the prostatic UroLume Wallstent in the treatment of urinary retention due to advanced prostate cancer. The stent was placed in 11 stage D prostate cancer patients at high surgical risk and with urinary retention unrelieved by total androgen blockade. At preoperative urethroscopy, the bladder neck and verumontanum were clearly visible and not massively infiltrated by tumor. All patients voided spontaneously at the end of the procedure. At 1 year maximum flow nomograms demonstrated the definite relief of bladder outlet obstruction and of related symptoms in the 10 cases evaluated. As expected, the stent had no evident effect on the natural history of prostate cancer. There were no major complications. Bladder outlet obstruction due to advanced prostate cancer and unrelieved by conventional medical therapy can be treated safely and effectively by the prostatic UroLume Wallstent.

Prostatic UroLume Wallstent for benign prostatic hyperplasia patients at poor operative risk: clinical, uroflowmetric and ultrasonographic patterns.

The prostatic UroLume Wallstent was positioned in 30 poor operative risk patients with bladder outlet obstruction due to benign prostatic hyperplasia. Preoperatively, 12 patients (40%) could still void spontaneously (group 1), while 18 (60%) had an indwelling catheter (group 2). Preoperative and postoperative assessment included scoring of subjective symptoms, physical examination, uroflowmetry with maximum flow nomogram, transrectal ultrasonography of the prostate, determination of residual urine volume and cystourethroscopy. All but 1 patient could void spontaneously after insertion of the stent. In group 1 preoperative and 1-year followup mean (plus or minus standard error) peak flow rates were 8.0 +/- 0.7 ml. per second and 15.8 +/- 1.8 ml. per second, respectively (p < 0.01), the mean residual urine volumes were 127 +/- 27 ml. and 38 +/- 11 ml. (p < 0.05), respectively, and the mean maximum flow nomograms (plus or minus standard deviation) were -2.6 +/- 0.1 and -1.4 +/- 0.4, respectively. In group 2 the 1-year followup mean peak flow rate, residual urine volume and maximum flow nomogram were 13.2 +/- 0.8 ml. per second (standard error), 32 +/- 14 ml. (standard error) and -1.5 +/- 0.1 (standard deviation), respectively. According to the maximum flow nomogram values all patients were nonobstructed postoperatively. At 1 year the stent was completely covered by prostatic epithelium in 90% of the patients, while in the remainder it was still partially visible at urethroscopy. Transrectal ultrasonography had an essential role in patient followup by accurately assessing the position of the stent. Placement of this prostatic stent is safe and effective for selected benign prostatic hyperplasia patients who cannot undergo surgical treatment due to poor operative risk.

Prostatic spiral versus prostatic urolume wallstent for urinary retention due to benign prostatic hyperplasia. A long-term comparative study.

Thirty-eight high-risk surgical patients with urinary retention due to benign prostatic hyperplasia (BPH) were treated by placement of a prostatic spiral under local anesthesia (group 1: 20 patients) or a prostatic stent under intravenous sedation (group 2: 18 patients). At the 1-year follow-up, mean peak flow rate, residual urine volume and subjective symptoms scale were significantly better in the stent group (p < 0.01). The rate of postoperative urinary incontinence and dislocation of the device was greater in the spiral group. Cystoscopic manipulation and removal of the device were definitely easier with the spiral. Both the prostatic spiral and stent have specific roles in the treatment of urinary retention in the unfit BPH patient. The selection of the most suitable device depends on accurate patient assessment.

[Chronic granulomatous prostatitis: echographic features in patients submitted to immunoprophylaxis/therapy with BCG]. / Prostatite cronica granulomatosa: aspetti ecografici in pz. sottoposti ad immunoprofilassi/terapia con BCG.

48 consecutive male patients with T.C.C. Ta-T1 and C.I.S. underwent local therapy with BCG. 4 patients presented with perineal pain and dysuria. T.R.U.S. showed hypoechoic areas with capsular infiltration. Transperineal echo-guided biopsy was taken and histology showed specific chronic granulomatous prostatitis.

Open surgical revision of laparoscopic pelvic lymphadenectomy for staging of prostate cancer: the impact of laparoscopic learning curve.

We attempt to clarify the impact of the learning curve on the first 30 laparoscopic pelvic lymphadenectomies performed at our institute. Open surgical revision of the area of laparoscopic dissection was performed at radical retropubic prostatectomy. The mean number of obturator and iliac lymph nodes removed laparoscopically was 8.7 and 8.8 from the right and left sides, respectively. The mean number of residual obturator and iliac lymph nodes removed at open operation was 3.2 and 3 from the right and left sides, respectively. The amount of residual lymph node tissue after laparoscopic lymphadenectomy progressively decreased with time, especially after the first 20 cases. A microscopic pelvic lymph node metastasis was found at open operation in patients 6, 14 and 15, who had false-negative results at laparoscopy. Due to the learning curve effect, the first 30 patients who undergo laparoscopic pelvic lymphadenectomy should be assessed again by an open operation at radical retropubic prostatectomy.