阿奇霉素与红霉素治疗急性细菌性感染的临床评价

目的：评价阿奇霉素注射液治疗急性呼吸道感染、泌尿道感染及皮肤软组织感染的安全性和有效性。方法：阿奇霉素注射液静脉滴注，每次250mg,qd，首次剂量加倍，疗程5d。对照药红霉素每日1—1．5g，分1—2次静脉滴注，疗程7—14d。结果：阿奇霉素注射液与红霉素随机对照治疗呼吸道、泌尿道及皮肤软组织感染32例，其中试验组17例，对照组15例。试验组与对照组的临床有效率分别为94．1％与86．7％，细菌清除率分别为100．0％与76．9％；不良反应发生率分别为10．53％与20．00％。以上结果经统计学处理差异无显著性。结论：阿奇霉素注射液静脉点滴，每次250mg，qd，首次剂量加倍，对敏感致病菌及支原体引起的轻、中度呼吸道感染，泌尿系感染及皮肤软组织感染均有很好临床疗效和细菌学疗效，不良反应低。     

阿奇霉素与乳糖酸红霉素随机对照及开放治疗急性下呼吸道感染70例临床验证

目的临床验证观察注射用阿奇霉素治疗急性下呼吸道感染的安全性和有效性。方法国产注射用阿奇霉素与乳糖酸红霉素随机对照开放治疗急性轻、中度下呼吸道感染70例,其中随机对照组40例,试验组20例应用阿奇霉素粉针剂,第1天,每次250mg,每日2次,以后每次250mg,每日1次,疗程5-7d;对照组20例应用乳糖酸红霉素粉针剂,每次600mg,每日2次,疗程7d。另用阿奇霉素进行开放试验治疗30例急性下呼吸道感染患者,阿奇霉素用法同前。结果试验组与对照组临床有效率分别为85％和80％,细菌清除率分别为100％和93．7％,不良反应发生率分别为10％和25％,以上结果经统计学处理差异无显著性。开放试验组临床有效率为86．7％,细菌清除率为95．7％,不良反应发生率为6．7％。结论阿奇霉素每次250mg,每日1次静脉滴注,首次剂量加倍,对于敏感致病茵所引起的急性轻、中度下呼吸道感染有较好的临床疗效和细菌学疗效。     

两种阿奇霉素制剂对下呼吸道感染的疗效比较

目的：评价注射用枸橼酸阿奇霉素(商品名：圣诺灵)治疗下呼吸道细菌感染的临床疗效及其安全性。方法：采用随机对照研究方法，将120例病人随机分成试验组和对照组，各60例。试验组使用注射用枸橼酸阿奇霉素500g，静滴，qd，疗程5天；对照组使用注射用乳糖酸阿奇霉素500g，与试验组同法给药。比较两种阿奇霉素制剂治疗下呼吸道感染的临床疗效、细菌学评价及不良反应。结果：试验组的痊愈率和总有效率分别为35．0％和100％，细菌清除率为96．5％，不良反应发生率为5．0％；对照组的痊愈率和总有效率分别为30．0％和96．7％，细菌清除率为94．7％，不良反应发生率为11．7％。结论：注射用枸橼酸阿奇霉素的临床疗效、细菌清除率与注射用乳糖酸阿奇霉素相当，不良反应发生率则相对较低。     

阿奇霉素注射液与注射用乳糖酸红霉素多中心随机对照治疗急性细菌性感染临床评价

目的评价阿奇霉素注射液治疗急性呼吸道感染、泌尿道感染及皮肤软组织感染的安全性和有效性。方法阿奇霉素注射液静脉滴注,每次250mg,每日1次,首次剂量加倍,疗程5d;对照药红霉素每日1g~1.5g,分1~2次静脉滴注,疗程7~14d。结果阿奇霉素注射液与红霉素随机对照治疗呼吸道、泌尿道及皮肤软组织感染134例,其中试验组69例,对照组65例。试验组与对照组的临床有效率(停药后1周)分别为94.2%与75.5%,细菌清除率分别91.9%与83.3%;不良反应发生率分别为8.45%与24.62%,以上结果经统计学处理有显著性差异(P<0.05)。结论阿奇霉素注射液静脉点滴,每次250mg,每日1次,首次剂量加倍,对敏感致病菌引起的轻、中度呼吸道感染,泌尿道感染及皮肤软组织感染均有很好临床疗效和细菌学疗效,不良反应发生率低。     

对照观察注射用阿奇霉素与红霉素治疗呼吸道感染的临床疗效

目的：评价注射用阿奇霉素治疗急性细菌性呼吸道感染的安全性和有效性。方法：采用区组随机、平行对照、多中心开放试验方法,设注射用阿奇霉素组为试验组,红霉素组为给药对照组,比较两组在治疗细菌性呼吸道感染的临床及细菌学疗效。结果：两药的临床和细菌学疗效相似,但试验药不良反应发生率更低、更具有安全性。结论：注射用阿奇霉素治疗急性细菌性呼吸道感当有效且不良反应更低。     

注射用阿奇霉素治疗细菌性感染59例

目的：评价注射用阿奇霉素治疗细菌性感染的疗效与安全性。方法：采用随机对照多中心分组研究方法,将94例下呼吸道感染患者,随机分为两组（每组47例）。治疗组用阿奇霉素500mg加入5％葡萄糖注射液500mL,静脉灌注,qd,5-7d为1个疗程。对照组用乳糖酸红霉素500mg加入5％葡萄糖注射液500mL,静脉滴注,bid,5－7d为1个疗程。开放组12例（4例盆腔炎和8例下呼吸道感染）,以阿奇霉素治疗。结果：治疗组痊愈率61．7％、有效率91．5％及细菌清除率95．8％均极显著高于对照组（31．9％、70．2％76．6％）。阿奇霉素治疗的59例,总有效率93．2％,痊愈率62．7％。试验组不良反应率12．8％,显著低于对照组（34．0％）。结论：阿奇霉素是治疗院外获得性呼吸道与泌尿生殖道感染的有效和安全的药物。     

阿奇霉素乳糖酸盐与红霉素乳糖酸盐随机对照及开放治疗急性细菌性感染162例临床验证

目的　本项临床验证研究评价注射用阿奇霉素乳糖酸盐治疗急性呼吸道感染、泌尿道感染及皮肤软组织感染的安全性和有效性。方法　国产注射用阿奇霉素乳糖酸盐与红霉素乳糖酸盐随机对照开放治疗呼吸道、泌尿道及皮肤软组织感染 162例 ,其中随机对照组 12 9例 ,试验组 65例使用阿奇霉素乳糖酸盐粉针剂 ,治疗第 1天 ,每次 2 5 0mg ,每日二次 ;第 2～ 5天 ,每次 2 5 0mg ,每日一次 ,疗程 5d。对照组 64例使用红霉素乳糖酸盐粉针剂 ,剂量每日 1～ 2g ,分 1～ 2次静脉滴注 ,疗程 7～ 14d。另用阿奇霉素乳糖酸盐进行开放试验治疗3 3例感染病人 ,阿奇霉素乳糖酸盐用法同前。结果　试验组与对照组的临床有效率分别为 96.8%与 82 .8%,细菌清除率分别 84.9%与 88.5 %,不良反应发生率分别为 12 .1%与 2 1.7%,以上结果经统计学处理无显著性差异。开放试验组临床有效率为 87.9%,细菌清除率为 95 .7%,不良反应发生率为 6.7%。结论　阿奇霉素乳糖酸盐静脉点滴 ,每次 2 5 0mg ,每日 1次 ,首次剂量加倍 ,对敏感致病菌及支原体引起的轻、中度呼吸道感染 ,泌尿系感染及皮肤软组织感染均有很好临床疗效和细菌学疗效     

阿奇霉素注射用灭菌粉末治疗呼吸系统中重度感染30例

目的评价阿奇霉素注射用灭菌粉末(派奇)对呼吸系统中、重度感染的疗效与安全性。方法采用随机对照研究方法，将60例中、重度呼吸系统感染患者随机分为两组。治疗组30例，用阿奇霉素注射用灭菌粉末250 mg加入5 %葡萄糖注射液500 mL，静脉滴注，qd，疗程5 d。对照组用红霉素注射用灭菌粉末1.5 g加入5 %葡萄糖注射液500 mL，静脉滴注，qd，疗程5 d。结果治疗组有效率和痊愈率分别为93.3 %和83.3 %，对照组为86.7 %和66.7 %(均P＞0.05)。治疗组不良反应发生率为16.7 %，显著低于对照组的36.7 %（P＜0.05）。结论阿奇霉素注射用灭菌粉末对呼吸系统中、重度感染疗效好且不良反应低。     

注射用阿奇霉素治疗非淋菌性尿道炎和宫颈炎随机对照多中心临床研究

为了评价注射用阿奇霉素治疗衣原体和地原体引起的非淋菌性尿道炎和宫颈炎的疗效和安全性，采用多中心、随机、对照试验，并与口服阿奇霉素胶囊进行比较。共纳入临床试验病例243例，可供疗效评价的病例241例，可进行安全性评价病例242例。其中试验组172例，静脉滴注阿齐霉素500mg，每天一次，连续2d。肌注阿齐霉素500mg，每天一次，连续2d，对照组69例，阿奇霉素胶囊1000mg，单剂量口服一次。总治愈率为74．42％（对照组60．87％）,总有效率为87．21％（对照组73．0％）；病原学清除率为88．44％（对照组81．01％）；不良反应发生率为6．94％（对照组为4．35％）。注射用阿奇霉素与对照药口服奇霉素胶囊相比较，在统计学上总治愈率与总有效率有显著性差异（P＜0．05），病原学疗效无显著性差异（P＞0．05），不良反应发生率无显著性差异（P＞0．05）。结果表明注射用阿奇霉素治疗由衣原体和支原体引起的非淋菌笥尿道炎和宫颈炎疗效确切、安全性好。     

注射用阿奇霉素与红霉素治疗小儿肺炎支原体肺炎的疗效比较

目的 评价注射用阿奇霉素治疗小儿肺炎支原体肺炎的安全性和有效性。方法 将确诊为肺炎支原体肺炎100例患儿随机分为甲组（50例）和乙组（50例），甲、乙组分别静脉滴注阿奇霉素10mg／（kg·d），一日一次，疗程3～5d；静脉滴注红霉素20-35mg／（kg·d），一日二次，疗程7～14d，观察疗效及不良反应。比较两组有效率和不良反应发生率。结果 甲组有效率为92.0％，不良反应发生率为12．0％；乙组有效率72．0％，不良反应发生率为32．0％，有显著性差异。结论 静脉滴注阿奇霉素治疗小儿肺炎支原体肺炎较静脉滴注红霉素有较高的疗效和较低的不良反应发生率。     

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.     

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.