妥泰单药治疗小儿癫痫86例临床疗效观察

目的观察托吡酯（妥泰）（Topiramate,TPM）单药治疗小儿癫痫的长期疗效、剂量及安全性。方法妥泰单药治疗癫痫,逐渐加量,发作明显控制后停止加量,所有病例均治疗并随访12个月。结果总有效率94.6%（无发作17.1%,显效46.0%,有效31.5%）。76例患儿无因妥泰的不良反应而停药。结论妥泰单药治疗小儿癫痫疗效较好且较安全,副作用较轻微,是一种值得推广的抗癫痫新药。     

西比灵合用妥泰预防偏头痛发作的临床研究

目的：观察西比灵合用妥泰对偏头痛发作的预防作用。方法：将126例偏头痛患者随机分为西比灵合用妥泰组（42例）、西比灵组（44例）及心得安组（40例），疗程1月，观察3月，观察上述三组治疗前后头痛指数和一月内头痛总天数的变化。结果：西比灵合用妥泰组和西比灵组头痛指数及一月内头痛总天数皆较心得安组显著降低，而西比灵合用妥泰组较西比灵组明显降低。结论：西比灵合用妥泰对偏头痛发作具有更好的预防作用。     

妥泰治疗小儿癫痫36例临床分析

目的观察妥泰添加或单一治疗小儿癫痫,尤其是常规治疗效果较差的难治性癫痫的疗效及不良反应。方法对我院符合病例,添加或单独应用妥泰治疗,进行自身治疗前后的开放性评价。结果经妥泰治疗3个月以上,平均疗程6个月,无发作15例,占41.7%;发作减少50%以上13例,占36.1%,无效8例,占22.2%;总有效率77.8%。结论妥泰是治疗小儿癫痫,尤其是难治性癫痫较安全有效的新型抗癫痫药物,但剂量个体差异较大,需要灵活制订个体给药方案。     

托吡酯添加治疗儿科难治性癫痫18例报告

目的 为验证托吡酯（商品名：妥泰）治疗儿科难治性癫痫的疗效和安全性。方法 对18例诊断为难治性癫痫患儿，添加妥泰至治疗量，以疗效前后发作频率来评价疗效。随访病例时间长1年余。结果 添加妥泰后，完全控制1例，明显好转15例，好转2例，无变化0例，总有效率100%。结论 妥泰对各种类型发作均有效。辐 作用小，为添加治疗控制难治性癫痫带来福音。     

妥泰治疗各类癫痫的临床开放性研究

目的：观察妥泰单一治疗各类癫痫的疗效及副作用。方法：采用开放性、自身对照性研究方法对87例各类癫痫的患者(成人65例，儿童22例)进行妥泰单一治疗观察疗效。结果：总有效率：成人组73．8％，儿童组72．72％，副作用主要为头晕，记忆力下降，体重减轻及肾结石。发生程度较轻．经对症治疗均好转。结论：妥泰单用可治疗备类型癫痫，对难治性癫痫效果更好。     

妥泰治疗小儿癫痫36例分析

目的对应用妥泰对患有癫痫的患儿实施治疗的临床效果进行研究。方法抽取72例患有癫痫的患儿,随机分为对照组和治疗组,平均每组36例。采用苯巴比妥对对照组患儿实施治疗;采用妥泰对治疗组患儿实施治疗。结果治疗组患儿癫痫病情控制效果明显优于对照组;症状表现控制时间和用药治疗总时间明显短于对照组;两组患儿未出现任何药物不良反应。结论应用妥泰对患有癫痫的患儿实施治疗的临床效果非常明显。     

妥泰与丙戊酸钠治疗小儿癫痫疗效对比分析

目的:比较妥泰与丙戊酸钠治疗儿童癫痫的疗效。方法:将182例癫痫患儿完全随机分为妥泰组108例,丙戊酸钠组74例。妥泰组应用妥泰单药治疗,从小剂量开始逐渐增量,发作明显控制后停止加量维持治疗;丙戊酸钠组应用丙戊酸钠单药治疗,5 mg.kg-1.d-1起始,逐渐增量至20~30 mg.kg-1.d-1,发作明显控制后维持治疗。治疗6个月后评定疗效,包括发作情况、痫样放电情况及不良反应。结果:108例癫痫患儿经妥泰单药治疗完全控制16例,显效34例,有效43例,无效15例,总有效率86.11%,不良反应28例,占25.93%。74例癫痫患儿经丙戊酸钠单药治疗完全控制8例,显效21例,有效24例,无效21例,总有效率71.62%,不良反应31例,占41.89%。两组比较痫样放电改善情况妥泰组与丙戊酸钠组差异无显著性。结论:妥泰对各种类型癫痫均有良好效果,是一种相对安全、有效的小儿抗癫痫治疗药物,妥泰单药治疗亦可用于初发的癫痫患儿。     

妥泰治疗儿童癫痫临床疗效观察

目的观察妥泰治疗儿童癫痫的临床疗效。方法癫痫患儿26例,其中部分性发作9例,全身强直-阵挛发作15例,失神2例,给予妥泰治疗。结果 26例癫痫患儿治疗12周后取得了良好的疗效,无发作的患儿超过1/3,无患儿因不良反应退出治疗。结论妥泰对部分性发作、全身强直-阵挛及失神癫痫患儿的治疗安全有效,副作用轻。     

硫喷妥钠治疗小儿癫痫持续状态的临床研究

目的：探讨硫喷妥钠治疗小儿癫痫持续状态的临床疗效。方法：将40例癫痫持续状态患儿随机分为对照组（20例）和治疗组（20例）,治疗组20例给予硫喷妥钠每次15mg/kg,加入5%葡萄糖液配制成1.5%溶液,先按5mg/kg静脉缓注,余者使用静脉滴注泵按2mg/min的剂量静滴,惊厥控制后递减滴速。对照组给地西泮0.3mg/kg静脉注射,最大剂量不超过10mg,惊厥未停止或又出现另一次惊厥发作者,15min后再次注射等剂量地西泮,同时使用苯巴比妥20mg/kg静脉注射。结果：硫喷妥钠治疗组在30min内时癫痫持续状态的控制率为100%,对照组为70%,治疗组控制率明显高于对照组,两组比较差异有统计学意义（P〈0.005）。结论：硫喷妥钠控制小儿癫痫持续状态快速、高效,可作为治疗小儿癫痫持续状态的首选药物。     

托吡酯治疗小儿偏头痛临床观察

近年来国内外有报道用托吡酯托吡酯(妥泰)治疗小儿偏头痛.为探讨妥泰的治疗效果,本文收集因偏头痛一直在我院儿科门诊接受西比灵或妥泰治疗的患儿各20例进行疗效比较,以期观察妥泰在小儿偏头痛中治疗效果.     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.