胺碘酮联合小剂量氟伐他汀治疗阵发性房颤的临床观察

目的评价胺碘酮联合小剂量氟伐他汀治疗阵发性房颤的疗效和安全性。方法将78例阵发性心房颤动患者随机分为胺碘酮组(n=35)和胺碘酮 氟伐他汀组(n=43),治疗随访时间为6个月,研究的一级终点是房颤复发。比较两组治疗后的窦性心律维持率。结果治疗6个月后胺碘酮组有效率为71.4%,胺碘酮 氟伐他汀组有效率为78.4%(P<0.05),组间差异有统计学意义。结论胺碘酮联合小剂量氟伐他汀治疗阵发性房颤安全有效,还可能减少心脑血管病的发生。     

替米沙坦与胺碘酮联合治疗老年非瓣膜性阵发性心房颤动的临床观察

目的对比胺碘酮联合替米沙坦与胺碘酮单用治疗老年非瓣膜性阵发性心房颤动的长期疗效。方法对入选91例患者进行随机分组,通过短期(〈2个月)的观察,去除不适应继续长期观察者12例,分为单用胺碘酮组(N=30),胺碘酮联合替米沙坦组(N=49)。治疗观察2年。统计患者窦性心律维持率进行比较。结果二年观察后单用胺碘酮30例的窦性心律维持率为51.2%,胺碘酮联合应用替米沙坦49例的窦性心律维持率为82.4%,两组相比,有明显的统计学意义(P<0.01)。结论胺碘酮联合替米沙坦长期治疗老年非瓣膜性阵发性心房颤动,是一有效的方法。     

不同剂型胺碘酮的不良反应分析

目的分析胺碘酮片剂与注射剂的药物不良反应(ADRs)特点,为临床安全用药提供参考。方法收集2006年1月至2012年2月北京市药物不良反应监测中心收到的与胺碘酮肯定有关、很可能有关和可能有关的不良反应报告,比较2种剂型胺碘酮所致ADRs的临床表现、严重ADRs构成比及转归。结果共收集到胺碘酮相关ADRs报告180份,涉及180例患者、195例次ADRs。180例患者中男性119例,女性76例;年龄2个月～97岁,平均年龄64岁。21例患者既往有ADRs史。195例次ADRs中一般ADRs 151例次(77.4%),严重ADRs 44例次(22.6%)。胺碘酮片剂相关ADRs 46例次,其中严重ADRs 13例次(28.3%);胺碘酮注射剂相关ADRs 149例次,其中严重ADRs 31例次(20.8%)。胺碘酮片剂所致严重ADRs的比例稍高于注射剂,但差异无统计学意义(χ2=1.12,P=0.29)。胺碘酮片剂所致ADRs的主要临床表现为肝功能损伤(34.7%)、甲状腺功能亢进或减低(17.3%)、咳嗽、咳痰、呼吸困难(10.9%)、皮疹等(8.7%)、头痛头晕(4.3%)、横纹肌溶解(4.3%)、过敏(2.2%)等。胺碘酮注射剂所致ADRs的主要临床表现为肝功能损伤(25.5%)、静脉炎(27.5%)、皮疹(14.1%)、过敏(8.1%)、心律失常(6.0%)、头痛头晕(5.4%)、血压下降(4.7)等。2种剂型所致ADRs的转归差异无统计学意义(χ2=8.18,P=0.09)。结论胺碘酮片剂与注射剂所致ADRs有所不同,因此其ADR的监测应有所侧重。对使用胺碘酮片剂的患者尤应加强用药指导和相关指标监测。     

静脉应用胺碘酮治疗心房颤动复律的疗效观察

目的:观察静脉应用胺碘酮对心房颤动复律的临床疗效。方法:将172例心房颤动患者随机分为胺碘酮组和安慰剂组。胺碘酮组(n=87)静脉推注胺碘酮5mg·kg-1,再以胺碘酮10～20mg·kg-1·d-1加入0.9%氯化钠注射液中持续静脉滴注,维持直至恢复为窦性节律;安慰剂组(n=85)静脉推注和静脉滴注0.9%氯化钠注射液,并给予控制心室率治疗。观察2组复律成功率和复律时间。结果:胺碘酮组有74例(85.1%)恢复为窦性节律,安慰剂组有68例(80.0%)恢复为窦性节律,2组比较差异无统计学意义(P>0.05)。胺碘酮组心房颤动持续时间短于安慰剂组(P<0.01)。胺碘酮组1例患者出现窦性心动过缓,停药后恢复。结论:胺碘酮静脉应用不能提高复律率,但能缩短心房颤动持续时间。     

新生儿阵发性室上性心动过速28例临床分析

目的分析新生儿阵发性室上性心动过速(PSVT)的临床特点、治疗过程及临床预后情况,提高临床的诊治水平。方法对我院2010年1月~2015年6月28例新生儿PSVT的病历资料进行回顾性分析,分别采用冰敷(n=23)、ATP(n=10)、普罗帕酮(n=13)、胺碘酮(n=10)治疗,比较各种不同治疗方法的成功转复率、复发率及随访情况。结果在PSVT新生儿中,男多于女,于新生儿早期≤7d,发病的以早产儿为主,于新生儿后期7d发病的以足月儿为主。出现预激综合征的发生率较高67.9%。在新生儿PSVT治疗上,ATP、普罗帕酮、胺碘酮比较,以胺碘酮复律成功率最高,复发率最低,其中冰敷与ATP、普罗帕酮、胺碘酮比较,差异有统计学意义(χ~2=6.231,6.865,7.231,P0.05);胺碘酮与冰敷、ATP治比较,差异有统计学意义(χ~2=4.931,4.164,P0.05),胺碘酮与普罗帕酮比较,差异无统计学意义(χ~2=2.643,P0.05)。在随访中发现新生儿PSVT的复发率较高,达33.3%,感染为主要诱因,达78.9%。结论新生儿PSVT如及时处理,较少发生心力衰竭及心源性休克,预后良好。于新生儿PSVT发作时,胺碘酮可作为一线药物应用。感染为患儿出现PSVT后期复发的主要诱发因素。     

联合应用胺碘酮与琥珀酸美托洛尔减少阵发性心房颤动复发的疗效观察

目的比较胺碘酮与琥珀酸美托洛尔合用减少阵发性心房颤动复发的疗效。方法回顾分析42名阵发性心房颤动患者,根据心房颤动复律后维持用药的不同,分为3组:单用胺碘酮组(n=14);单用琥珀酸美托洛尔组(n=14);胺碘酮与琥珀酸美托洛尔合用组(n=14)。比较3组患者用药后12个月中房颤控制情况及心室率、心脏传导情况。结果单用胺碘酮组显效率35.7%,有效率35.7%,无效率28.6%;单用琥珀酸美托洛尔组显效率14.3%,有效率28.6%,无效率57.1%;胺碘酮与琥珀酸美托洛尔合用组显效率78.6%,有效率14.3%,无效率7.14%,其疗效明显优于单用胺碘酮(P<0.05)或单用琥珀酸美托洛尔(P<0.01)组,且未见明显副作用:3组间心室率未见显著差别。结论胺碘酮与琥珀酸美托洛尔合用可有效地控制阵发性心房颤动的发作。     

胺碘酮与普罗帕酮治疗阵发性室上性心动过速的疗效比较

目的 比较胺碘酮与普罗帕酮治疗阵发性室上性心动过速的临床疗效及不良反应.方法 97例阵发性室上性心动过速患者按入院先后顺序分为胺碘酮组和普罗帕酮组.比较两组用药后的心率、血压、转复率以及不良反应发生率.结果 普罗帕酮组用药后心率为(82.6±5.4)次/min,胺碘酮组为(83.9±6.8)次/min,两组用药前后心率变化差异均有统计学意义(t=0.743、0.185,P=0.011、0.017);普罗帕酮组用药后转复时间为(12.7±6.9)min,胺碘酮组为(27.9±10.7)min,两组转复时间差异有统计学意义(t=8.897,P=0.000);普罗帕酮组转复有效率为88.5％,胺碘酮组转复有效率为80.0％,两组差异无统计学意义(x2=2.115,P=0.107);普罗帕酮组用药后不良反应发生率为21.2％,胺碘酮组不良反应发生率为17.8％,差异无统计学意义(x2 =1.158,P=0.231).结论 胺碘酮与普罗帕酮治疗阵发性室上性心动过速疗效相当,且安全性好.但普罗帕酮起效更快,转复时间短于胺碘酮.     

胺碘酮剂量调整对华法林维持剂量的影响

目的分析胺碘酮剂量调整对华法林维持剂量的影响,为预测华法林的维持剂量提供参考。方法选取2017年1～12月,我院收治长期合用胺碘酮和华法林的房颤患者71例,随访6个月,收集患者完整的临床资料,观察华法林和胺碘酮的剂量调整情况,记录处于稳定期的胺碘酮和华法林的维持剂量,比较胺碘酮剂量调整前后的华法林维持剂量的差异是否有统计学意义;采用简单线性回归方法分析胺碘酮与华法林的剂量关系。结果胺碘酮剂量调整前后华法林的维持剂量比较,差异有统计学意义(t=-5.654,P 0.05);胺碘酮和华法林的维持剂量之间线性关系差(R2=0.055/0.06,60%,远小于1;P=0.048/0.039,接近0.05),但胺碘酮维持剂量的改变量与华法林维持剂量的变化幅度呈良好的线性关系:Y3=22.783-0.100X3,R2=0.975,P=0.000。结论胺碘酮剂量调整对华法林的维持剂量有影响,华法林维持剂量的变化与胺碘酮的调整剂量呈良好的负相关,华法林的维持剂量可根据胺碘酮剂量的改变量进行相应的调整。     

胺碘酮与普罗帕酮治疗阵发性快速心房颤动的临床疗效对比观察

目的:对比观察静脉应用胺碘酮与普罗帕酮治疗阵发性快速心房颤动的疗效。方法:选择32例患者,按就诊顺序随机分成胺碘酮和普罗帕酮两组,胺碘酮组16例:胺碘酮(可达龙)300mg微泵持续匀速1小时静脉输入,未转复窦性心律者以胺碘酮1mg/分持续静脉滴注5小时;普罗帕酮组16例:普罗帕酮70mg加生理盐水20ml,10分钟注射完毕,观察20分钟,未转复窦性心律者重复静脉注射普罗帕酮70mg,观察20分钟仍未转复者以普罗帕酮0.5mg/分持续静脉滴注,滴注时间不超过2小时。结果:转复率:胺碘酮组81.25%(13/16),普罗帕酮组75%(12/16),两组转复率比较差异无统计学意义(χ2=0.080,P=0.777)。转复时间:胺碘酮组(209±133)分钟,普罗帕酮组(166±128)分钟,两组转复时间比较差异有统计学意义(t=2.524,P=0.019)。转复后心室率比较:胺碘酮组(69.8±12.2)次/分,普罗帕酮组(83.5±19.7)次/分,两组转复后心室率比较差异有统计学意义(t=-2.794,P=0.010)。结论:胺碘酮和普罗帕酮对阵发性快速心房颤动均有较高的转复率,转复时间普罗帕酮短于胺碘酮,转复后心室率胺碘酮较普罗帕酮慢。     

胺碘酮治疗快速性心律失常的临床效果研究

目的探讨胺碘酮应用于治疗快速性心律失常患者的临床效果。方法 71例快速性心律失常患者被随机分为实验组(n=36)和对照组(n=35),对照组给予普罗帕酮治疗,实验组给予胺碘酮治疗。结果实验组总有效率为97.2%,显效率为88.9%,无严重的不良反应,临床效果显著优于对照组(P<0.05)。结论胺碘酮应用于冠状动脉粥样硬化性心脏病的康复,能显著提高临床效果,改善患者生活质量,值得在临床上应用和推广。     

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.