氨酚羟考酮片治疗癌痛疗效及安全性观察

目的:探讨氨酚羟考酮片(泰勒宁片)用于中重度癌痛的镇痛效果及其安全性.方法:选取102例中重度癌痛患者,口服氨酚羟考酮片,观察其疼痛缓解程度及其不良反应.结果:氨酚羟考酮片用于中度癌痛总有效率82.5%,用于重度癌痛者总有效率71.8%.有头晕、嗜睡、恶心、呕吐及便秘等不良反应,但发生率均较低.结论:氨酚羟考酮片用于治疗中重度癌痛疗效确切,不良反应小.     

氨酚羟考酮片治疗142例不同类型中重度癌性疼痛的疗效和不良反应

目的:观察氨酚羟考酮片在不同类型的中重度癌性疼痛中的治疗作用及不良反应.方法:采用多中心随机对照试验方法,将总共283例躯体痛、内脏痛、神经病理性疼痛的患者随机分为试验组(氨酚羟考酮片)和对照组(等效剂量吗啡片),观察其镇痛效果及不良反应.结果:对于躯体痛和内脏痛,试验组治疗前后疼痛强度差及镇痛有效率明显高于对照组;而对于神经病理性疼痛,两组之间无显著性差异.并且用药期间显示试验组胃肠道不良反应较对照组低.结论:氨酚羟考酮可作为治疗中重度肿瘤伤害性疼痛的首选药物之一.     

氨酚羟考酮控制中重度癌痛疗效观察

目的探讨氨酚羟考酮控制中重度癌痛的疗效。方法将入选病例94例随机分为氨酚羟考酮组和盐酸曲马朵组,氨酚羟考酮组口服氨酚羟考酮片1～2片/次,3/d;盐酸曲马朵组口服盐酸曲马朵片50～100mg/次,3/d,连服5d评价疗效。结果氨酚羟考酮在控制疼痛效果、作用起效时间及改善生活质量方面优于曲马朵,而作用持续时间及不良反应发生率比较,两药无显著差异。结论氨酚羟考酮是控制中重度癌痛的有效药物。     

氨酚羟考酮控制中重度癌痛疗效观察

目的探讨氨酚羟考酮控制中重度癌痛的疗效。方法将入选病例94例随机分为氨酚羟考酮组和盐酸曲马朵组,氨酚羟考酮组口服氨酚羟考酮片1～2片／次,3／d;盐酸曲马朵组VI服盐酸曲马朵片50～100mg／次,3／d,连服5d评价疗效。结果氨酚羟考酮在控制疼痛效果、作用起效时间及改善生活质量方面优于曲马朵,而作用持续时间及不良反应发生率比较,两药无显著差异。结论氨酚羟考酮是控制中重度癌痛的有效药物。     

氨酚羟考酮片联合放疗治疗中重度骨转移疼痛的疗效观察

目的：观察氨酚羟考酮片联合放疗治疗骨转移疼痛的疗效。方法：64例患者随机分为研究组（氨酚羟考酮口服联合放疗）及对照组（即释吗啡片口服联合放疗）。结果：研究组显效率87.50%,中度疼痛显效率93.33%,重度疼痛显效率82.35%,高于对照组,有统计学意义;不良反应包括恶心、呕吐、嗜睡、便秘等研究组均明显低于对照组,有统计学意义。结论：氨酚羟考酮片联合放疗治疗中重度骨转移疼痛安全有效,值得临床推广。     

氨酚羟考酮片与盐酸羟考酮缓释片在晚期癌痛治疗的药物经济学分析

目的:评价氨酚羟考酮片与盐酸羟考酮缓释片治疗晚期癌痛患者镇痛的成本-效果,为临床合理用药提供指导。方法:选取晚期癌痛患者148例,其中氨酚羟考酮组73例,羟考酮缓释片组75例,比较用药4周后的镇痛疗效、不良反应及治疗成本,并进行成本-效果分析。结果:氨酚羟考酮组和羟考酮缓释片组镇痛治疗总有效率分别为86.3%,和90.7%,2组间疗效差异无统计学意义(P>0.05),成本/效果比(C/E)分别为16.3和26.3,氨酚羟考酮组的不良反应发生率较羟考酮缓释片组低。结论:氨酚羟考酮片和盐酸羟考酮缓释片用于治疗晚期癌痛患者镇痛疗效相当,氨酚羟考酮片治疗成本较低,是晚期癌痛患者镇痛治疗的较佳方案。     

氨酚羟考酮片与洛芬待因片治疗中、重度癌性疼痛的疗效比较

目的：比较氨酚羟考酮片及洛芬待因片治疗中、重癌性疼痛效果及安全性。方法：随机抽取口服氨酚羟考酮片及洛芬待因片治疗中、重度癌性疼痛患者各30例,观察用药第24,48,72 h疼痛缓解程度及其不良反应。结果：氨酚羟考酮片组与洛芬待因片组在服药第24,48 h比较均P>0.05,第72 h比较P<0.05;服药后24,48,72 h与服药前比较均P<0.01;治疗重度疼痛氨酚羟考酮片组与洛芬待因片组第72 h镇痛效果,显效比较P<0.05,有效比较P>0.05;治疗中度疼痛氨酚羟考酮片组与洛芬待因片组第72 h镇痛效果,比较显效、有效均P>0.05;氨酚羟考酮片组与洛芬待因片组在服药第24,48,72 h比较不良反应,均P>0.05。结论：服药72 h疼痛强度(PI)评估氨酚羟考酮片优于洛芬待因片,24,48 h比较均无明显差异;服药72 h治疗重度疼痛氨酚羟考酮片组显效优于洛芬待因片组,有效无明显差异,治疗中度疼痛氨酚羟考酮片组与洛芬待因片组,显效、有效均无明显差异,治疗后副反应无明显差异。     

氨酚羟考酮片治疗带状疱疹后遗神经痛的临床研究

目的:探讨氨酚羟考酮片治疗带状疱疹后遗神经痛(PHN)的疗效.方法:72例PHN患者随机分为2组,治疗组36例,每次口服氨酚羟考酮片0.33 g,bid;对照组36例,每次口服布洛芬缓释胶囊,0.30 g,bid,治疗10 d后观察疗效及不良反应.结果:治疗组与对照组治疗有效率比较有显著性差异(P<0.01).结论:氨酚羟考酮片治疗PHN安全、有效.     

氨酚羟考酮用于经尿道前列腺激光气化电切术镇痛效果及护理

目的：探讨氨酚羟考酮用于经尿道前列腺激光气化电切术镇痛效果及护理。方法97例经尿道前列腺激光气化电切术患者,按随机数字表分为氨酚羟考酮组47例,氨酚羟考酮组手术前2h口服氨酚羟考酮1片,术后继续口服氨酚羟考酮1片,q8h,至停留置导尿;曲马多组手术前2h口服曲马多缓释片100mg,术后继续口服马多缓释片100mg,q12h,至停留置导尿。两组均使用视觉模拟评分法,进行术后1、6、24、48疼痛评分,并观察记录各种不良反应。结果氨酚羟考酮组术后1h、6h时间段VAS评分优于与曲马多组有显著差异（P＜0．05）,两组不良反应的发生率无显著性差异（ P＞0．05）。结论氨酚羟考酮用于经尿道前列腺激光气化电切术的镇痛效果满意,服用后不良反应轻微,同时密切的术前、术后护理配合,有力保障手术顺利完成。     

3种口服镇痛药控制中、重度癌症疼痛的疗效比较

目的观察比较氨酚羟考酮片、氨酚双氢可待因片、丙氧氨酚片3种口服镇痛药控制中、重度癌症疼痛的镇痛效果及其不良反应发生率。方法中、重度癌症疼痛患者512例分3组：氨酚羟考酮组216例,口服氨酚羟考酮片1次1~2片,1日4次;氨酚双氢可待因组93例,口服氨酚双氢可待因片1次1~2片,1日4次;丙氧氨酚组203例,口服丙氧氨酚片1次1~2片,1日4次,给药2周后,比较患者疼痛缓解程度以及不良反应发生情况。结果氨酚羟考酮组控制中、重度癌症疼痛有效率分别为92.6%、89.7%;氨酚双氢可待因组控制中、重度癌症疼痛有效率分别为90.6%、82.5%;丙氧氨酚组控制中、重度癌症疼痛有效率分别为91.3%、75.4%。所有病例不良反应均较少而轻微。结论通过观察发现3种药物在控制中、重度癌症疼痛上疗效确切,不良反应少,而氨酚羟考酮片在控制重度疼痛上具有较明显的优势。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.