3H-1,2-二氢-1-吡里酮衍生物的合成

发现3 H-1,2-二氢-1-吡咯里嗪酮具有明显的抗炎镇痛作用。用Friedel-Crafts酰化和Dieckmann缩合等反应制备了该酮的一些衍生物,其中五个未见于文献报道。药理实验证明,这些化合物均有不同程度的抗炎镇痛作用。     

Percutaneous transluminal angioplasty of the femoropopliteal artery: initial and long-term results

Patients with dilated stenoses and recanalized occlusions were evaluated to assess the initial and long-term results of percutaneous transluminal angioplasty (PTA) in the femoropopliteal artery. The follow-up period was at least 1 year. The initial success rate was 84% (128/164). The initial results were influenced by the radiologist's experience, catheter selection, and type of lesion. The 5- and 7-year cumulative patency rates were 70% and 60%. There was no difference in long-term patency between initially successful stenoses and short (less than 3 cm) occlusions. Both the morphology and location of the stenotic lesion influenced the long-term results. Although many factors influence the initial and long-term success rate, results of this study justify PTA in the femoropopliteal artery. Patients with localized stenoses and short occlusions are best suited for this treatment.     

The geometry of triple-balloon dilation

Triple-balloon dilation (TBD) of a variety of luminal structures has been successfully, though infrequently, used. A mathematical model is presented for the selection of balloon sizes, and equations and tables are derived that allow the user to estimate more accurately the size of balloons needed for TBD of structures with large lumina. With TBD, an approximately circular lumen can be formed. Also, TBD allows smaller, higher-pressure balloons to be used instead of single, low-pressure, large balloons. However, multiple puncture sites may be required for TBD.     

Early diagnosis and treatment of blunt diaphragmatic injury

Diaphragmatic rupture following blunt torso trauma is an infrequent injury often posing a considerable diagnostic challenge. Between June 1984 and July 1986, nine patients sustaining rupture of the diaphragm due to blunt trauma were treated. All were injured in high-speed motor-vehicle accidents. Six patients arrived in shock (SBP less than or equal to 95 mm Hg). All patients had multiple associated injuries; mean ISS = 41.5. Eight patients (89%) had associated intra-abdominal injuries, the spleen being injured most frequently (63%). Associated thoracic injuries occurred in six patients (67%). The admission CXR was abnormal in eight patients (89%) but diagnostic of diaphragmatic rupture in only four. DPL was positive in four of five patients (80%) and falsely negative in one. Seven ruptures were left-sided, one right-sided and one involved the central tendon. All injuries were diagnosed shortly after admission and successfully repaired via a transabdominal approach. One patient died as a result of a massive subdural hematoma. Blunt diaphragmatic rupture is an indication of a high-energy insult and is usually associated with other major organ system injuries. An aggressive approach to the management of the multiply injured patient can result in early recognition and successful treatment of this injury.     

Combined use of double- and single-contrast barium enema in the evaluation of suspected colonic disease

Although controversy has surrounded the use of single- and double-contrast barium enemas for many years, a growing opinion exists that these studies are complementary, each possessing advantages in different clinical settings. We have found that when interpretation of double-contrast studies is difficult because suspected abnormalities are subtle or because technical quality of examinations is less than ideal, single-contrast enemas can be helpful. We have been able to obtain high-quality single-contrast studies using low-viscosity, low-density barium suspensions administered immediately following evacuation after initial air contrast evaluation.     

Phase 2 trial of radiation plus high-dose tamoxifen for glioblastoma multiforme: RTOG protocol BR-0021

Preclinical studies support the concept that inhibition of protein kinase C (PKC) by tamoxifen (TAM) should provide both antineoplastic effects and radiosensitization. High-dose TAM (80 mg/m2 p.o. daily in divided doses) was given with and after conventional radiotherapy (XRT) to inhibit PKC-mediated signaling, which is known to be enhanced in glioblastoma (GBM). Seventy-seven patients were accrued between December 2000 and December 2001; two were ineligible and not included in the efficacy results. Pretreatment characteristics of the patients included the following: 52% were less than 60 years of age, 39% had a Zubrod score of 0, 70% had minor or no neurological symptoms, and 65% were Radiation Therapy Oncology Group-recursive partition analysis (RPA) class III and IV. Eighty-six percent of patients achieved acceptable dosing of TAM. Notable toxicity included late radiation grade 3 in two patients and thromboembolic events in 16 patients (two grade 2, 10 grade 3, three grade 4, and one grade 5), for an incidence of 20.8% (which is lower than expected, based on the literature for deep vein thrombophlebitis in GBM patients not receiving TAM). Median survival time (MST) was 9.7 months as compared (by three different statistical methodologies) to the historical GBM control database of 1457 RPA class III, IV, and V drug/XRT-treated patients. After controlling for RPA class IV, the MST was 11.3 months, which compares to the historical RPA control of 11.3 months (P = 0.37). The results obtained do not exhibit a substantial advance over those of previous studies with various XRT/drug doublets, including BCNU. However, as TAM does not have significant overlapping toxicities with most other drugs, its testing in a combined modality approach with other medications may be justified in future clinical trials. Historically, the incidence of thromboembolic events in GBM patients is approximately 30%. The lower-than-expected incidence seen here has also been observed in other high-dose TAM GBM studies. We speculate that TAM inhibited the PKC-mediated phosphorylation of coagulation factors.