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31.
32.
RGD-based strategies for selective delivery of therapeutics and imaging agents to the tumour vasculature 总被引:12,自引:0,他引:12
Kai Temming Raymond M. Schiffelers Grietje Molema Robbert J. Kok 《Drug Resistance Updates》2005,8(6):381-402
During the past decade, RGD-peptides have become a popular tool for the targeting of drugs and imaging agents to alphavbeta3-integrin expressing tumour vasculature. RGD-peptides have been introduced by recombinant means into therapeutic proteins and viruses. Chemical means have been applied to couple RGD-peptides and RGD-mimetics to liposomes, polymers, peptides, small molecule drugs and radiotracers. Some of these products show impressive results in preclinical animal models and a RGD targeted radiotracer has already successfully been tested in humans for the visualization of alphavbeta3-integrin, which demonstrates the feasibility of this approach. This review will summarize the structural requirements for RGD-peptides and RGD-mimetics as ligands for alphavbeta3. We will show how they have been introduced in the various types of constructs by chemical and recombinant techniques. The importance of multivalent RGD-constructs for high affinity binding and internalization will be highlighted. Furthermore the in vitro and in vivo efficacy of RGD-targeted therapeutics and diagnostics reported in recent years will be reviewed. 相似文献
33.
A recent series of randomized prospective clinical trials that compared rate control with rhythm control in patients with atrial fibrillation (AF) found no significant difference in primary outcome between the two strategies. However, these trials lacked clear criteria for defining "successful" rate or rhythm control. Various measures have been used to gauge the success of antiarrhythmic drug therapy, including time to first recurrence of AF, any AF recurrence, AF burden, and a reduction in symptoms. Determining the success of antiarrhythmic therapy can be relatively straightforward by using how patients feel during therapy as a key endpoint. Most patients are satisfied with a major reduction in symptomatic AF episodes and can live comfortably with occasional episodes of AF. For those who are bothered by even infrequent, brief AF episodes, a treatment regimen that eliminates nearly all AF recurrences is required, although often hard to achieve. Catheter ablation may be necessary to achieve a successful outcome in these patients. Suppression of AF in a patient at high risk of stroke does not, however, remove the need for concomitant warfarin therapy. The endpoints of ventricular rate control are not clear, and the recently published rhythm versus rate control trials lacked standard criteria for judging acceptable rate control. One relatively simple method is to try and achieve a 24-hour heart rate that mimics expected normal sinus rhythm. It is important to achieve good rate control to minimize symptoms and the risk of tachycardia-mediated cardiomyopathy. 相似文献
34.
Although non-steroidal anti-inflammatory drug-induced colopathy is well described, colonic perforations complicating non-steroidal anti-inflammatory drug intake are rare. We report a patient with rheumatoid arthritis who was on long-term diclofenac and presented with early colonic stricture formation and a caecal perforation, which to the best of our knowledge, has only been reported once before. It is important to suspect this diagnosis in patients on non-steroidal anti-inflammatory drug therapy who present with an acute abdomen. 相似文献
35.
溃疡散预防消化性溃疡复发临床观察 总被引:4,自引:0,他引:4
冀慧鹏 《河南中医学院学报》2004,19(4):34-35
目的 :观察溃疡散对消化性溃疡的抗复发治疗的临床效果。方法 :随机将 80例患者分成溃疡散治疗组 (4 2例 )和雷尼替丁对照组 (38例 )并同时观察两组患者治疗前后溃疡复发情况。结果 :治疗后治疗组溃疡复发率明显低于对照组 ,P <0 .0 1,两组对比有非常显著性差异。结论 :治疗组能明显的改善患者临床症状和降低消化性溃疡复发率。 相似文献
36.
Although cardiac arrhythmias remain a serious clinical problem in many patients with heart disease, the exact role of antiarrhythmic drug therapy is currently under intense evaluation. Within the last several years it has become clear that there are significant risks as well as potential benefits associated with existing agents. Ongoing studies in large patient populations should help determine the benefit/risk ratio of traditional therapy. Regardless of the outcome of these trials, current electrophysiological dogma will have to be re-evaluated and newer concepts evolve for drug development to make further progress. The goal of this symposium is to exchange information among basic and clinical investigators so as to facilitate the emergence of novel electrophysiological concepts that will form the basis for future generations of antiarrhythmic drugs. 相似文献
37.
Rosen Raymond C. Kostis John B. Jekelis Albert Taska Lynn S. 《Archives of sexual behavior》1994,23(2):135-152
Antihypertensive drugs are commonly associated with adverse side effects in both clinical and laboratory studies. We investigated the sexual sequelae of several major classes of antihypertensive drugs (e.g., beta blockers, central alpha agonists, diuretics) in normal males and in hypertensive patients. We compared the effects of four widely used agents (methyldopa, propranolol, atenolol, hydrochlorothiazide-triamterene) and placebo, in a selected sample of 21 sexually dysfunctional male hypertensives, 13 of whom completed all five phases of the study. Each study drug was administered for a 1-month treatment period, followed by a 2-week, single-blind washout phase, according to a randomized, Latin square crossover design. Dependent variables for the study included a broad range of hormonal, NPT, and self-report measures of sexual response. Results indicated a lack of consistent drug effects on measures of sexual response, although more frequent sexual and nonsexual side effects were observed with methyldopa and propranolol. As in our previous studies, age was negatively correlated with both hormonal and NPT measures, whereas changes in blood pressure were not significantly related to sexual function scores. Results do not support the hypothesis that sexually dysfunctional males are at greater risk for adverse sexual sequelae when treated with centrally active agents or diuretics. 相似文献
38.
Allan J. Flach Bernard J. Dolan 《Documenta ophthalmologica. Advances in ophthalmology》1993,83(4):323-329
Amiodarone hydrochloride is a potent antiarrhythmic agent recently approved for use by the Food and Drug Administration. Anterior subcapsular lens opacities were observed in seven of fourteen patients treated with moderate to high doses of amiodarone at the Veterans Administration Medical Center in San Francisco in 1982. The present report summarizes the present status of these same fourteen patients ten years later. Anterior subcapsular lens opacities developed or progressed in all patients continuing treatment with this antiarrhythmic agent during the following ten year interval. Although Snellen visual acuities are not decreased, subtle visual impairment is present as measured by contrast sensitivity measurements with and without glare. This decrease in visual acuity is not a contraindication for therapy with this potentially life saving drug. 相似文献
39.
初步分析了11例外伤性截瘫合并耳聋患者,指出外伤性截瘫多有慢性肾功能不全、肾性贫血等并发症。这些并发症对耳聋的发生有一定的影响,但长时间或反复使用耳毒性药物是一个不可忽视的重要因素。作者对此提出了预防耳聋的一些具体措施,可供临床参考或借鉴。 相似文献
40.
本实验以荷 Lewis 肺癌的 NIH 小鼠为模型,以肿瘤平均直径倍增时间(MDDT)为终点,进行加温合并抗癌药物的研究。结果表明:①43℃加温25分钟,对 Lewis 肺癌有明显的治疗效果(P<0.05);②喜树碱16mg/kg合并加温25分钟,对 Lewis 肺癌的抑制作用随加热温度升高而加强,在43℃时出现相加作用(P<0.001);③斑蝥素0.45mg/kg,高三尖杉酯碱1.2mg/kg 或消瘤芥0.75mg/kg 合并加温25分钟,对Lewis 肺癌的抑制作用随加热温度升高而增强,其中斑蝥素和消瘤芥在43℃时出现协同作用(P<0.001);①去甲斑蝥酸钠3mg/kg 对 Lewis 肺癌无治疗作用,但合并43℃加温25分钟时有协同作用;⑤鸦胆子油口服乳液8ml/kg,间隔27小时合并43℃加温25分钟,对 Lewis 肺癌的治疗有相加作用,并明显延长了荷瘤动物的生存时间。 相似文献