国产利福昔明治疗急性细菌感染性腹泻115例

目的评价国产利福昔明治疗急性细菌感染性腹泻的疗效与安全性。方法急性细菌感染性腹泻患者224例，随机分为治疗组和对照组，治疗组115例给予国产利福昔明片口服，第1天3次，每次0.4 g，第2天起每天两次，每次0.4 g;对照组109例给予左氧氟沙星片口服，第1天3次，每次0.2 g，第2天起每天2次，每次0.2 g。疗程均为3～5 d。结果治疗组与对照组临床有效率分别为93.9%和90.8%，细菌清除率分别为97.62%和100.00%，不良反应发生率分别为2.61%和1.83%，两组各对应指标均差异无显著性(均P＞0.05)。结论国产利福昔明片治疗急性细菌感染性腹泻安全、有效。     

利福昔明胶囊治疗急性细菌感染性腹泻的临床疗效观察

目的:评价利福昔明胶囊治疗急性细菌感染性腹泻的疗效和安全性。方法:采用随机双盲平行对照研究。利福昔明胶囊组,每次口服利福昔明胶囊0.4 g,首日t.i.d,以后b.i.d;对照环丙沙星胶囊组,每次口服环丙沙星0.2 g,首日t.i.d,以后b.i.d,疗程均为3-5 d。治疗前后查血、尿、大便常规、肝肾功能、心电图用于安全性评价。结果:利福昔明胶囊组治疗感染性腹泻16例,有效率93.8%,对照环丙沙星胶囊组治疗感染性腹泻19例,有效率89.5%,两组间疗效差异无显著性(P >0.05)。35例中有11例治疗前粪便细菌培养阳性,阳性率31.4%,治疗后细菌清除率为100%。利福昔明胶囊组未观察到不良反应和严重不良事件发生。结论:对治疗急性细菌感染性腹泻利福昔明胶囊具有与环丙沙星胶囊同等的疗效和安全性。     

利福昔明治疗感染性腹泻50例的随机双盲对照试验

目的 :评价利福昔明治疗感染性腹泻的疗效及安全性。方法 :采用随机、双盲对照临床试验设计 ,选用 18～ 6 5a病人共 12 6例 ,分为A ,B两组。分别用利福昔明与环丙沙星 2种药物治疗 ,用法一致 ,d 1,2粒 ,tid ,以后 2粒 ,bid ,疗程皆为 3～ 5d。结果 :利福昔明与环丙沙星临床疗效评价病例数分别为 5 0例和 5 7例 ,有效率分别为 94 %与 95 % ,细菌阳性率分别为 4 4%与 4 6 % ,细菌清除率分别为95 %与 92 % ,不良反应发生率分别为 2 %与 5 % (均P >0 .0 5 )。结论 :利福昔明是治疗成人肠道细菌感染的有效和安全的药物 ,与环丙沙星相当     

利福昔明治疗急性细菌感染性腹泻94例的随机双盲多中心临床试验

目的:评价国产新药利福昔明胶囊治疗细菌感染性腹泻的有效性与安全性。方法:采用多中心随机双盲对照试验设计,分成2组。试验组(n=94)给利福昔明400 mg,对照组(n=109)给环丙沙星200 mg,均po,d 1,tid,d 2~5,bid。疗程均3~5d。结果:利福昔明与环丙沙星在症状及体征复常率、止泻率、止泻时间、粪便常规、粪便性状复常率和细菌清除率均无显著性差异;试验组与对照组总痊愈率分别为79%和88.1%(P>0.05),总有效率分别为94%和94.5%(P>0.05);试验组不良反应发生率为1.8%,对照组为5.0%(P>0.05),未发生严重不良反应。2组疗效与安全性的差异均无显著意义。结论:国产利福昔明胶囊治疗急性细菌感染性腹泻安全、有效,与环丙沙星胶囊相似。     

利福昔明片治疗急性感染性腹泻的多中心临床研究

目的评价利福昔明片治疗急性感染性腹泻的临床疗效及安全性。方法采用多中心、随机、双盲双模拟、阳性药物平行对照研究。227例急性感染性腹泻患者被随机分成试验组(111例)和对照组(116例)。试验组给利福昔明片第1天为0.3g Po,tid,第2天起改为0.3g,Po,bid。对照组给氧氟沙星片,第1天为0.3g Po,tid,第2天起改为0.3g,Po,bid。疗程3~5d。观察两组疗效和不良反应。结果利福昔明组痊愈率和有效率分别为84.7%和100%,氧氟沙星组痊愈率和有效率分为77.6%和100%;两组疗效无统计学差异(P>0.05)。利福昔明组和氧氟沙星组细菌清除率分别为100%和99%,两组均未出现不良反应。结论利福昔明片是治疗急性感染性腹泻具有明显疗效且安全的口服制剂。     

利福昔明片治疗急性感染性腹泻的多中心临床研究

目的:观察利福昔明片治疗急性感染性腹泻的临床疗效和安全性.方法:采用多中心随机双盲双模拟平行对照方法,以环丙沙星片作为对照.253例急性感染性腹泻患者被随机分成试验组(127例)和对照组(126例).试验组给利福昔明片,d1为0.4g,po,tid,d2起改为0.4g,bid.对照组给环丙沙星片,d1为0.5g,po,tid,d2起改为0.5g,bid.疗程3～7d.结果:试验组和对照组疗效分别为90.40%和93.55%;无显著性差异(P>0.05).试验组发生不良反应1例1次,发生率为0.79%;对照组5例7次,发生率为3.79% (其中1例因不良事件导致脱落).结论:利福昔明片是治疗急性感染性腹泻有效且安全的口服制剂,不良反应发生率低于环丙沙星片.     

利福昔明治疗急性感染性腹泻111例临床疗效及安全性

目的:评价利福昔明治疗急性感染性腹泻的临床疗效及安全性。方法:采用多中心、随机、双盲双模拟、阳性药物平行对照研究。入选急性感染性腹泻240例,完成227例,其中利福昔明组111例,男性52例,女性49例,年龄(30±s11)a,入组d1,服用利福昔明300mg和左氧氟沙星安慰剂1片,po,tid,d2~5,利福昔明400mg和左氧氟沙星安慰剂1片,po,bid;左氧氟沙星组116例,男性57例,女性59例,年龄(30±11)a,入组d1,服用左氧氟沙星100mg和利福昔明安慰剂3片,po,tid,d2~5,左氧氟沙星100mg和利福昔明安慰剂4片,po,bid。2组疗程均为3~5d。观察2组疗效和不良反应。结果:利福昔明组痊愈率和有效率分别为84.7%和100%,左氧氟沙星组痊愈率和有效率分别为77.6%和100%。2组疗效无统计学差异(P>0.05)。利福昔明组和左氧氟沙星组细菌清除率分别为100%和99%,2组无统计学差异(P>0.05)。2组均未出现不良反应。结论:利福昔明治疗急性感染性腹泻具有明显疗效,未见不良反应。     

利福昔明治疗急性细菌性肠道感染107例

目的　评价利福昔明治疗急性细菌性肠道感染疾病的疗效和安全性。方法　采用多中心随机双盲双模拟平行对照试验。急性细菌性肠道感染患者 211例,随机分为两组,治疗组 107例,每次给予利福昔明 0. 2g,po,q6h,同时给予环丙沙星模拟安慰药片 1片,bid,疗程 5d;对照组 104例每次给予环丙沙星 0 .25g,po,bid,同时给予利福昔明模拟安慰药片 2片,po,q6h,疗程 5d。评价两药的疗效及不良反应。结果　治疗组肠道感染的治愈率和显效率分别是 75 7%和 18 .7%,总有效率为 94 .4%;对照组分别是 84 .6%和 13 .5%,总有效率为 98 .1%。利福昔明和环丙沙星的细菌清除率分别是 96. 2%和 96 3%,不良反应发生率为 2. 8%和 2. 9%。各项结果的差异均无显著性 (P>0 .05)。结论　利福昔明治疗急性细菌性肠道感染具有较好的疗效,不良反应发生率低,与环丙沙星的疗效相仿。     

两种药物治疗急性感染性腹泻的临床研究

目的评估利福昔明片治疗急性感染性腹泻的临床疗效及安全性。方法采用随机、双盲双模拟、阳性药物平行对照的方法,入选120例患者,实验组60例服用利福昔明片,第1天300mg,3次/d;第2~5天400mg,2次/d;对照组60例服用左氧氟沙星片,第1天100mg,3次/d;第2~5天100mg,2次/d,疗程为3~5d。结果实验组治疗3~5d后,腹痛、腹泻及大便检查恢复正常或明显好转,痊愈率84.68%,显效率15.31%,总有效率为100.00%,细菌清除率为100.00%,与对照组比较P>0.05,两组均未见严重不良反应(P>0.05)。结论利福昔明片是治疗急性感染性腹泻安全有效的药物。     

利福昔明胶囊对急性感染性腹泻的疗效和安全性及其血药浓度测定

目的评价利福昔明胶囊（抗结核病药）治疗急性感染性腹泻的疗效、安全性及口服后吸收情况。方法用随机对照前瞻性试验方法，共入选病例70例，利福昔明胶囊（试验组33例）每次200mg，每6h1次；左氧氟沙星胶囊（对照组35例）每次200mg，每12h1次，疗程均3天。试验组有10例患者接受了血药浓度分析。结果从开始服药至最后1次排不成型便的时间，试验组和对照组平均分别为33．56，31．13h，2组相比无明显差异（P〉0．05）；2者的临床疗效比较也无明显差异（P〉0．05）；利福昔明口服后血药浓度极低或测不出。结论利福昔明口服后基本不吸收，是治疗急性感染性腹泻的安全有效药物。     

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.     

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.     

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.