295例葛根素注射液不良反应分析

目的：总结葛根素注射液不良反应发生的类型及特点.方法：对2005～2009年浙江省药品不良反应监测中心接收到的295例葛根素注射液不良反应报告进行分析和总结.结果：葛根素注射液的不良反应临床表现主要为药物热、药疹、溶血及休克等症状,在高剂最（≥400mg/d）及连续用药时更易发生.结论：葛根素注射液不良反应的发生与多种因素有关,应用时应高警惕.     

169例葛根素注射液不良反应分析

目的分析葛根素注射液不良反应的发生特点,为临床用药提供参考。方法对葛根素注射液不良反应169例进行归纳分析。结果葛根素注射液不良反应的表现主要为发热、药疹及溶血等症状,不良反应多发生在用药7~10 d,有过敏史的患者,再次使用症状加重。结论应注意葛根素注射液的使用疗程及过敏史,以减少不良反应的发生。     

葛根素注射液不良反应分析

目的:探讨葛根素注射液所致不良反应的一般规律和特点,为临床合理用药提供参考。方法:检索《中国生物医学期刊引文数据库》1994年～2006年报道的葛根素注射液所致不良反应文献及另手工检索到1994年以前2篇,共计51篇,并进行统计、分析。结果与结论:药物热是葛根素注射液最常见的不良反应,其与用药量、用药时间有密切关系,其次为药疹、溶血反应;最严重的不良反应为溶血反应和休克,使用时应格外关注。     

葛根素注射液29例不良反应分析

目的 分析葛根素注射液不良反应的特点,指导临床合理用药.方法 对1997年～2006年8月近10年间我院报告的29例葛根素注射液不良反应报告进行回顾性分析.结果 29例不良反应中,以皮肤及附件损害(9例)和过敏样反应(8例)为主,溶血3例其中死亡1例,肾功能异常1例,腰痛2例,其他反应6例.结论 寻找葛根素注射液过敏原将成为葛根素的研究方向之一,反复用药可能成为刺激肌体产生抗体的原因,葛根素注射液应在严密监测下使用.     

135例患者应用葛根素注射剂安全性分析

目的 :了解葛根素注射剂在临床应用中的安全性。方法 :对2002年10月～2003年2月我院所有使用葛根素注射剂的住院患者用药情况及出现的不良反应进行调查。结果 :按照药品说明书规定的剂量 ,以0 9 %氯化钠注射液和5 %葡萄糖注射液作为溶媒 ,单独配制且单独输注 ,输注速度40～60滴/min时较为安全 ,不良反应少 ;超剂量用药 ,不良反应显著增加。结论 :应严格按照药品说明书的规定用药。     

葛根素注射液致急性溶血性贫血反应35例文献分析

目的:分析葛根素注射液致急性溶血性贫血的特点.方法:检索1994年1月-2007年3月国内医药学期刊,收集葛根素注射液致急性溶血性贫血反应35例病例,应用文献计量学方法对病例进行整理与归纳.结果:35例病例中男性22例,女性13例,≥60岁者27例(占77.14%);患者用药剂量200-600 mg,1次/d,皆为静脉滴注;不良反应多发生于用药6-10 d.结论:葛根素注射液致急性溶血性贫血反应多发于中老年人,且与多种因素有关,在使用时应注意观察用药后反应.     

葛根素注射液治疗脑梗死的临床观察及不良反应监测

目的观察葛根素注射液治疗急性脑梗死(ACI)患者的临床疗效,并观察葛根素注射液发生的药品不良反应现象。方法观察我院92例经头颅CT或MRI证实的脑梗死患者。随机分为治疗组(48例)和对照组(44例)。治疗组静脉滴注葛根素注射液0.6g,1次/d,共14d;对照组静脉滴注注射用丹参600mg,1次/d,共15d。两组均给予阿司匹林、辛伐他汀、胞二磷胆碱等基础治疗。观察两组患者治疗前后的症状及神经功能缺损的变化。同时监测二者药品不良反应的种类和数量。结果根素注射液治疗组用药总有效率为91%,对照组为72%,两组比较差异有统计学意义(P<0.05)。在药品不良反应监测过程中,葛根素总体不良反应发生率为8.33%,但未发生严重不良反应。结论葛根素注射液治疗急性脑梗死是安全有效。     

葛根素注射液致溶血反应16例文献调查

目的:分析葛根素注射液致溶血反应发生的特点。方法:对1999-2003年国内文献报道的葛根素致溶血反应16例病例进行分析。结果:16例中男性12例,女性4例,≥60岁者10例(2例未报道年龄)。患者用药量200～600mg,1次/d。溶血反应多发生于首次用药3～10d,仅有3例(18.75%)是再次用药发生,既往有无药物过敏史均有可能发生溶血反应。临床以急性溶血性贫血为主要表现,如腰腿关节及全身疼痛,寒战发热,肉眼血尿或尿呈酱油色、浓茶色,实验室检查阳性指标有血RBC、Hb降低,尿中出现血红蛋白(尿潜血阳性)及红细胞。血免疫学检查可见葛根素特异性抗体。结论:葛根素注射液致溶血反应发生与多种因素有关,使用时应高度重视。     

葛根素注射剂不良反应分析和处理对策

目的 探讨葛根素注射剂的不良反应及特点,以指导临床合理用药.方法 通过检索2000-2009年国内医学期刊,收集葛根素注射剂致不良反应病例190例,对病例的流行病学资料进行统计分析.结果 葛根素注射剂不良反应包括发热、药疹及溶血等症状,其出现时间多发生在用药1周左右,男性多于女性,46～55岁较多.结论 加强了解葛根素注射剂所导致的不良反应的规律和特点,设计个体化给药,以减少或避免不良反应的发生.     

葛根素注射液致急性血管内溶血的临床特征和发病机制及其安全应用

葛根素是从豆科植物野葛或甘葛藤干燥根中提出的一种异黄酮类化合物,其注射液用于心脑血管疾病的治疗。近年来葛根素注射液引起急性血管内溶血的报道增多,经检索国内相关文献,自1993年至2005年间应用葛根素注射液引起血管内溶血的患者共32例,男21例,女11例,平均年龄（69±9）岁;其中有10例死亡,平均年龄为（72±5）岁。在资料完整的25例患者中,21例单用葛根素注射液,4例为联合用药;葛根素100～700mg溶于0.9%氯化钠或5%葡萄糖注射液中静脉滴注;用药时间22例为5～10d,3例〉10d。血管内溶血的临床表现主要为腰、背痛,血尿、尿少、血红蛋白尿,网织红细胞升高（0.05～0.30）,高胆红素血症（29.1～123.2μmol/L）。22例患者经停药并给予糖皮质激素或抗组胺药物以及血液透析治疗后,多于6～7d症状消失或病情稳定。葛根素注射液致血管内溶血的可能因素为葛根素注射液的质量、患者过敏体质、年龄、用药时间或联合用药等。其发生机制可能与葛根素注射液引起的免疫性或非免疫性反应及其促氧化作用等有关。预防措施为：有过敏史者不宜应用;高龄及肝肾功能不全者用药应调整剂量;与可能致溶血的药物联用应谨慎。     

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.     

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.     

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.