氮唑取代苯基醚类衍生物的合成及其抗真菌活性

通过取代溴苄与１－（２，４－二取代苯基）－２－（１Ｈ－吲哚和苯并咪唑－１－基）乙醇反应，合成了一系列１－｛２－「（取代苯基）甲基」－２－（取代苯基）乙基－１－吲哚和苯并咪唑类新化合物，并用二倍体稀释法对化合物进行了体外抗真菌试验。     

Antiepileptic drug toxicity: Definition and mechanism of action

A detailed review of the adverse reactions of anticonvulsants is given, focusing on the definitions of drug toxicity, sources of information, patterns of durg utilization, pharmacokinetic variables and different mechanisms of action. The information available in the literature provides a wide spectrum of drug toxicity with no attempt at a practical definition of the reported events. This favors uncertainty among practising physicians, who are led to use the individual items with different attitudes. Suggestions are given for the evaluation, prevention and treatment of anticonvulsant drug toxicity.

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Sommario La presente è una revisione critica dei diversi aspetti della tossicità dei farmaci antiepilettici. L'analisi della letteratura è condotta con particolare riferimento alle diverse fonti di informazione, ai pattern di utilizzo dei singoli principi attivi, ai dati farmacocinetici ed ai meccanismi di azione farmacologica sottostanti. L'ampio panorama che ne deriva non consente una definizione pratica degli effetti indesiderati degli anticonvulsivanti. Ciò determina incertezza e confusione nella pratica medica, con conseguente diversità di comportamenti. La rassegna si conclude con la presentazione di alcuni suggerimenti pratici per la valutazione, la prevenzione ed il trattamento della tossicità da anticonvulsivanti.

     

抗真菌剂三氮唑含硫化合物的合成

合成了１３个三氮唑含硫化合物，均为未见文献报道的新化合物，对所合成的化合物，选择三种常见真菌进行体外最低抑菌浓度（ＭＩＣ）的测定，结果表明它们均有较好的抗真菌活性，有些化合物抑菌活性极高，有进一步研究和开发前景。     

磺胺噻二嗪硫酮衍生物的合成及其抑菌活性

利用药物化学骈合原理设计并合成了一系列新的３，５－二取代１，３，５－噻二嗪－２－硫酮类化合物，其结构经红外光谱，紫外光谱及元素分析证实，抑菌活性试验显示了良好的抑菌活性。     

Surgical treatment of patients with psychiatric disorders: A review of 21 patients

Between January 1985 and September 1994, 21 patients with psychiatric disorders underwent various forms of surgery at our hospital. There were 12 men and 9 women with an average age of 57.6 years. The coexisting psychiatric disorders were schizophrenia in 15 patients, depression in 2, dementia in 2, mental retardation with epilepsy in 1, and Parkinson's disease in 1. All the patients had been receiving neuroleptic medications for a long period. The indications for surgery were: cholelithiasis in 6 patients, acute appendicitis in 4, perforation of the small intestine in 3, incarceration of an inguinal hernia in 2, and esophageal cancer, stomach cancer, bleeding from a gastric ulcer, perforation of a duodenal ulcer, strangulating ileus, and burns in 1 patient each, respectively. All of the patients who underwent elective surgery were given epidural anesthesia with or without general anesthesia. Antipsychotic medications were given until just prior to surgery and recommenced concurrent with the first meal. Abnormal behavior was observed in 11 patients (52.4%) postoperatively, but all the patients were discharged in accordance with recovery from their surgical disorder. Intra- and postoperative hypotension resistant to intravenous catecholamine administration was recognized in 9 patients (42.9%), and this peculiar complication should be borne in mind when patients with psychiatric disorders require surgical management. Presented at the 94th annual meeting of the Japanese Surgical Society, held in Tokyo in March, 1994     

Anti-inflammatory,analgesic, antipyretic and related properties of meloxicam,a new non-steroidal anti-inflammatory agent with favourable gastrointestinal tolerance

The anti-inflammatory, analgesic and antipyretic properties of the new non-steroidal anti-inflammatory agent, meloxicam, were investigated in a variety of animal models and compared with the properties of piroxicam, diclofenac, indomethacin and several other NSAIDs.With respect to the total effect of a single oral dose, the anti-exudative effect of meloxicam on carrageenaninduced oedema in the rat exceeded that of all the NSAIDs included in the comparison. Additionally, meloxicam showed the greatest potency of all the compounds examined with respect to adjuvant-induced arthritis in the rat, the granuloma pouch model and the cotton pellet test in the rat. Unlike indomethacin, in the carrageenan pleurisy model in the rat, meloxicam caused both a dose-dependent reduction in exudate volume and also inhibition of leucocyte migration.Meloxicam showed a strong and lasting effect on inflammatory pain in the rat. Like other NSAIDs, but unlike dipyrone, meloxicam had no effect in the hot plate and tail clamp tests, which are used to identify weak central analgesic effects. Unlike dipyrone and like indomethacin, meloxicam had no effect in a model of visceral distention pain.In common with other NSAIDs, meloxicam had no influence on the body temperature of normothermic rats in the anti-inflammatory dose range, but did reduce yeastinduced fever in the rat in a dose-dependent manner. Like piroxicam, meloxicam had a uricosuric effect on rats treated with oxonic acid.Low-dose meloxicam inhibited both bradykinin-induced and PAF-induced bronchospasm in the guinea-pig, but had no effect on acetylcholine-induced bronchospasm.Piroxicam had greater ulcerogenic effects in the rat stomach than meloxicam.The therapeutic range of meloxicam in the rat, with regard to inhibition of adjuvant arthritis, was several times greater than that of piroxicam, indomethacin, diclofenac and naproxen.     

从脾论治磺脲类降糖药继发性失效

对 64例 2型糖尿病继发磺脲类降糖药失效患者 ,在继续口服磺脲类药的基础上加用健脾中药 ,结果显效 1 5例 ,有效 3 6例 ,无效 1 3例 ,总有效率 85 .2 4% ;治疗前后血糖明显下降 ,有显著性差异 ( P<0 .0 0 1 )     

Antimicrobial properties of heartwood,bark/sapwood and leaves of Juniperus species

Hexane and methanol extracts of heartwood, bark/sapwood and leaves of twelve taxa of Juniperus from the United States were assayed for antifungal and antibacterial activities. The hexane extract of the heartwood of several junipers appeared comparable in antibacterial activity to streptomycin. Antibacterial activity of the hexane extracts from the bark/sapwood of J. monosperma and J. californica were comparable to streptomycin. No appreciable antibacterial activities were found in the leaf extracts from any species examined. No antifungal activities comparable to amphotericin B were found in either hexane or methanol extracts of the heartwood nor from the bark/sapwood. Antifungal activity against Cryptococcus neoformans comparable to amphotericin B was found in the hexane extract of the leaves of J. occidentalis var. australis. The methanol extracts from the leaves of J. osteosperma and J. californica had antifungal activities comparable to amphotericin B against Trichophyton mentagrophytes.