脑活素对癫痫附加治疗的试验

部分性发作癫痫患１３例（男性７例，女性６例；年龄３６±ｓ１５ａ）在应用抗癫痫药同时，附加脑活素２０ｍＬ于１０％葡萄糖溶液５００ｍＬ，ｉｖｇｔｔ，ｑｄ，共１０－１４ｄ。结果发作频率由每月１７±３３次降为３±８次，总有效率７７％，单光子发射计算机断层摄影术摄取比值从８１±８上升至９５±８（Ｐ＜０．０１），提示脑活素对抗癫痫有支持作用。     

脑活素、丹参、能量合剂治疗突发性耳聋的相互比较

摘要目的：观察脑活素对突发性耳聋的治疗效果。方法：突发性耳聋病人１９７例（男性１２５例，女性７２例，年龄４５±ｓ８ａ（６～７５ａ），分３组。脑活素组６２例，丹参组６５例与能量合剂组７０例。脑活素组用脑活素１０ｍＬ，丹参组用丹参注射液１０ｍＬ，能量合剂组用三磷腺苷２０ｍｇ，辅酶Ａ１００Ｕ及细胞色素Ｃ３０ｍｇ，上述３组均加入５％葡萄糖盐水２５０ｍＬ或５００ｍＬ中静脉滴注，均以１０ｄ为一个疗程。结果：脑活素组，丹参组及能量合剂组有效率分别为９５％，４９％及２９％，脑活素组优于其他２组（Ｐ＜０．０１）。结论：脑活素治疗突发性耳聋效果满意。     

复方丹参与脑活素治疗新生儿缺氧缺血性脑病疗效比较

目的：比较复方丹参注射液与脑活素治疗新生儿缺氧缺血性脑病的疗效。方法：新生儿缺氧、缺血性脑病４６例，随机分为复方丹参组２３例（男性１３例，女性１０例；日龄＜３ｈ１６例，３～２４ｈ７例）给复方丹参注射液６～１０ｍＬ（１ｍＬ含丹参、降香各１ｇ）静脉滴注，ｑｄ，７ｄ为一个疗程。脑活素组２３例（男性１２例，女性１１例；日龄＜３ｈ１５例，３～２４ｈ８例）给脑活素４ｍＬ（１ｍＬ含浓缩脑活素２１５．２ｍｇ）静脉滴注，ｑｄ，７ｄ为一个疗程。结果：复方丹参组有效率８７％，脑活素组有效率９１％，Ｐ＞０．０５。结论：复方丹参注射液与脑活素治疗新生儿缺氧缺血性脑病疗效相似且安全。     

脑活素,丹参,能量合剂治疗突发性耳聋的相互比较

目的：观察脑活素对突发性耳聋的治疗效果。方法：突发性耳聋病１９７例（男性１２５例，女性７２例，年龄４５±ｓ８ａ（６－７５ａ），分３组。脑活素组６２例，丹参组６５例与能量合剂组７０例。脑活素组用脑活素１０ｍＬ丹参组用丹在注射液１０ｍＬ，能量合剂组用三磷腺苷２０ｍｇ，辅酶Ａ１００Ｕ及细胞色素Ｃ３０ｍｇ，上述３组均加入５％葡萄糖盐水２５０ｍＬ或５００ｍＬ中静脉滴注，均以１０ｄ为一个疗程。结果：脑活互组，     

脑活素治疗新生儿缺氧缺血性脑病

新生儿缺氧缺血性脑病３０例，２组采用相同的常规疗法（吸氧、限制液体入量、脱水疗法、止痉及能量合剂），其中１５例（男性９例，女性６例；入院时平均年龄为１．６±０．７ｄ）加用脑活素２ｍＬ，加入１０％葡萄糖液５０ｍＬ中静脉滴注，ｑｄ，共１０ｄ为脑活素组。另１５例（男性７例，女性８例，入院平均年龄为１．９±０．７ｄ）单采用常规疗法为对照组，疗程亦１０ｄ。结果：脑活素组总有效率９３％（１４／１５），对照组６０％（９／１５）（Ｐ＞０．０５）。     

脑蛋白水解物注射液与脑活素治疗脑血管疾病的比较

目的：比较新药脑蛋白水解物注射液与脑活素治疗脑血管疾病恢复期的疗效。方法：脑蛋白水解物组９０例（男性６７例，女性２３例，年龄６１±ｓ９ａ）其中脑梗死７２例，脑出血１８例，病程４．８±１．４ｍｏ；采用脑蛋白水解物注射液２０ｍＬ于０．９％氯化钠液２５０ｍＬ中静脉滴注，ｑｄ，２０ｄ为一疗程，脑活素组４５例（男性２９例，女性１６例，年龄６４±８ａ）其中脑梗死３５例，脑出血１０例，病程４．４±２．０ｍｏ，采     

脑蛋白水解物注射液与脑活素治疗脑血管疾病的比较

目的：比较新药脑蛋白水解物注射液与脑活素治疗脑血管疾病恢复期的疗效。方法：脑蛋白水解物组９０例（男性６７例，女性２３例；年龄６１±ｓ９ａ）其中脑梗死７２例，脑出血１８例；病程４．８±１．４ｍｏ；采用脑蛋白水解物注射液２０ｍＬ于０．９％氯化钠液２５０ｍＬ中静脉滴注，ｑｄ，２０ｄ为一个疗程。脑活素组４５例（男性２９例，女性１６例；年龄６４±８ａ），其中脑梗死３５例，脑出血１０例；病程４．４±２．０ｍｏ；采用脑活素治疗，剂量、用法及疗程同上。结果：脑蛋白水解物组的临床症状、体征及智能改善总有效率依次为９０％，６６％及６８％。脑活素组依次为９３％，６２％及４９％，２组无显著性差异，亦无显著不良反应。结论：２种药在改善脑血管疾病的神经功能障碍方面疗效均好，且安全可靠     

颅脑损伤后不同时期用脑活素治疗

重型颅脑损伤１５８例中，４８例（男性４０例。女性８例；年龄２６±ｓ８ａ）用常规治疗，１１０例（男性９６例，女性１４例；年龄２８±１１ａ）于伤后６－８ｈ，２４－３６ｈ和７２ｈ开始加用脑活素１０－２０ｍＬ于０．９％氯化钠溶液２５０ｍＬ静脉滴注，ｑｄ，分别２９±４．３０±６，２８±８次。结果：伤后６－８ｈ开始用脑活素组疗效最佳（Ｐ＜０．０１）。     

脑活素诱发癫痫发作1例

脑活素诱发癫痫发作１例马桂芳，张铭穷（中国人民解放军１７５医院漳州３６３０００）患者男性，５５岁，因头晕反复发作１０年，症状加重１周，于１９９４年４月１６日入院。既往有外伤性癫痫史，无药物过敏史。入院时查体：Ｔ３６℃，ＨＲ６２次／ｍｉｎ，Ｒ２０次／ｍ...     

颅脑损伤后不同时期用脑活素治疗

重型颅脑损伤１５８例中，４８例（男性４０例，女性８例；年龄２６±ｓ８ａ）用常规治疗，１１０例（男性９６例，女性１４例；年龄２８±１１ａ）于伤后６－８ｈ，２４－３６ｈ和７２ｈ开始加用脑活素１０－２０ｍＬ于０．９％氯化钠溶液２５０ｍＬ静脉滴注，ｑｄ，分别２９±４．０３±６，２８±８次。结果：伤后６－８ｈ开始用脑活素组疗效最佳（Ｐ〈０．０１）。     

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.