2005～2008年我院银杏叶注射液使用情况分析

银杏(Ginkgo biloba)属我国特产植物资源,在全球的天然药物中,银杏制剂是用量最大的品种之一.银杏叶注射液原研厂家为德国施瓦伯公司.银杏叶提取物注射液(Ginkgo Biloba kaf Extract Injection,EGb761)主要活性成分有银杏黄酮,银杏内酯A、B、C,白果内酯(BB)[1].银杏达莫(Ginkgo kaf Extract and Dipyridamole Injection)是由银杏黄酮和双嘧达莫组成的复方制剂.EGb761具有扩张血管、改善微循环、抗血小板激活因子、抗氧化及清除氧自由基等药理作用[2],因此在我国应用广泛.利用世界卫生组织推荐的"限定日剂量(DDD)"方法分析EGb761注射液的使用情况,能很好的分析其用量及其使用的合理性,现报道如下.     

银杏达莫注射液的主动及被动过敏性反应评价

目的：通过动物实验评价银杏达莫注射液引起过敏反应的风险。方法：通过腹腔注射银杏达莫注射液致敏豚鼠和大鼠,14 d后,静脉注射致敏豚鼠并收集血清皮内注射正常大鼠,做豚鼠的全身主动过敏和大鼠的皮肤被动过敏,评价银杏达莫注射液引起过敏反应的风险。结果：经银杏达莫注射液致敏和激发的豚鼠未出现全身主动过敏反应（n=6）;应用经银杏达莫注射液致敏大鼠的血清,被动致敏正常大鼠,经银杏达莫注射液激发后,亦未见皮肤被动过敏反应（n=6）。结论：动物实验显示银杏达莫注射液引起过敏反应的风险较小。     

银杏达莫注射液细菌内毒素检查法的研究

目的建立银杏达莫注射液的细菌内毒素检查法。方法按《中国药典》2005年版(二部)收载的细菌内毒素检查方法及指导原则进行实验。将银杏达莫注射液经64倍稀释,用标示灵敏度为0.5Eu.ml-1的鲎试剂检测其细菌内毒素。结果银杏达莫注射液稀释64倍对鲎试剂无干扰作用。结论可以用细菌内毒素检查法对银杏达莫注射液进行热原检查。     

银杏达莫注射液治疗冠心病心绞痛疗效分析

目的:分析银杏达莫注射液治疗冠心病心绞痛的疗效.方法:选择符合诊断标准的冠心病心绞痛患者120例,按入院编码随机分为两组,分别给予银杏达莫注射液与复方丹参注射液治疗两周,比较用药前后心绞痛发作次数以及心电图ST段的改变.结果:银杏达莫注射液治疗冠心病心绞痛发作次数和心电图指标以及硝酸甘油用量明显优于治疗前(P＜0.01),而且银杏达莫注射液总有效率明显优于复方丹参注射液组(P＜0.05).结论:银杏达莫注射液治疗冠心病心绞痛疗效显著.     

银杏达莫治疗急性脑梗死80例疗效观察

目的观察银杏达莫注射液治疗急性脑梗死的疗效。方法瘵160例急性脑梗死患者随机分为治疗组(80例)和对照组(80)例,治疗组应用银杏达莫注射液20ml静脉滴注,每日1次,连用14天,对照组应用维脑路通注射液500rag,静脉滴注,每日1次,连用14天。观察两组治疗前后神经功能缺损改善情况和血液流变学指标的变化。结果治疗组疗效显著高于对照组,尸<0.0I;血液流变学指标治疗前后比较有显著性差异(P<0.05或P<0.01),优于对照组。结论银杏达莫注射液治疗急性脑梗死具有良好的疗效。     

银杏达莫注射液治疗慢性脑供血不足的临床疗效分析

目的探讨银杏达莫注射液应用于临床治疗慢性脑供血不足(CCCI)的疗效。方法选取2010年3月至2014年3月间收治的慢性脑供血不足患者60例,按其入院时间分为银杏达莫组和对照组。银杏达莫组30例,应用银杏达莫注射液治疗;对照组30例,应用复方丹参注射液治疗。观察两组患者临床疗效及血流变指标。结果银杏达莫组临床症状改善情况明显优于对照组(P<0.05);两组患者在经临床治疗后,其各项脑血流变指标均较治疗前改善明显(P<0.05);且银杏达莫组患者各项脑血流变指标较对照组改善明显,有统计学意义。结论银杏达莫注射液可有效改善CCCI患者症状,促进血流变各项指标的恢复;具有较高的临床应用价值。     

银杏达莫注射液联合盐酸贝那普利治疗糖尿病肾病的疗效评价

目的探讨银杏达莫注射液联合盐酸贝那普利治疗糖尿病肾病(Diabeticnephropathy,DN)的疗效。方法选择在本院就诊的DN患者70例,分为观察组和对照组。对照组给予盐酸贝那普利片治疗;观察组给予银杏达莫注射液联合盐酸贝那普利片治疗。结果观察组总有效率为77.14%高于对照组总有效率48.57%,差异有统计学意义(P<0.05)。结论银杏达莫注射液联合盐酸贝那普利片治疗DN患者疗效佳,具有较高的临床应用价值。     

银杏达莫注射液治疗椎基底动脉供血不足性眩晕疗效观察

银杏达莫注射液是以银杏提取物(GBE)为基础的复合制剂,在临床上常用于心脑血管病及外周循环障碍性疾病的治疗,我科于2004年3月~2006年3月应用银杏达莫注射液治疗椎基底动脉供血不足(VBI)性眩晕,并与复方丹参注射液进行对比研究,获得较好效果。     

银杏达莫注射液治疗糖尿病下肢血管病变的临床疗效

目的分析在糖尿病下肢血管病变的药物治疗中使用银杏达莫注射液的效果。方法对2011年6月～2012年1月48例糖尿病下肢血管病变患者进行分组用药,前期用药的24例为单一组,使用银杏达莫注射液;后期用药的24例为联合组,在使用银杏达莫注射液的基础上口服西洛他唑,两组持续用药周期均为2周,分析疗效和下肢供血情况。结果两组下肢供血情况均得到改善,联合组改善更显著(P<0.05);两组疗效均良好,联合组更理想(P<0.05)。结论在糖尿病下肢血管病变的药物治疗中使用银杏达莫注射液可较好改善下肢供血情况,若同期口服西洛他唑可协同增效。     

银杏达莫注射液对慢性肺源性心脏病急性加重期35例的疗效观察

目的观察银杏达莫注射液对慢性肺源性心脏病急性加重期的治疗效果。方法将70例患者随机分为治疗组(n=35)和对照组(n=35)两组均给予一般治疗如吸氧、控制感染、改善通气、适当强心、利尿等。治疗组在一般治疗上加用银杏达莫注射液20mL+5%葡萄糖注射液250mL静脉滴注1次/d,疗程14d。结果治疗组临床疗效总有效率91.4%,对照组65.7%。差异具有高度显著性(P<0.01)。结论银杏达莫注射液可提高慢性肺源性心脏病的临床治疗效果。     

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.

     

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.     

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.     

2-(Acetoxyphenyl)-(Z)-styryl sulfides as cyclooxygenase inhibitors

2-(Acetoxyphenyl)-(Z)-styryl sulfides are described as selective cyclooxygenase-2 (COX-2) inhibitors, useful for treating inflammation and COX-2-mediated disorders including neoplasia. 2-(Acetoxyphenyl)-(Z)-styryl sulfide is claimed to be the most potent COX inhibitor in the series with a COX-2 selectivity ratio of 33. This compound is also claimed to be superior to celecoxib (Celebrex^®, Pfizer) in inhibiting cell growth of colorectal carcinoma cells. In this evaluation, the COX inhibitory activity of this compound is compared to that previously disclosed for diarylheterocycles and 2-(acetoxyphenyl)alkyl sulfides. The validity of the DLD-1 cell line in the growth inhibition studies is questioned based on recent literature reports indicating the lack of COX-2 expression in this cell line.     

Sleep-disordered breathing with chronic opioid use

Chronic opioid use for pain relief or as substitution therapy for illicit drug abuse is prevalent in our societies. In the US, retail distribution of methadone and oxycodone has increased by 824 and 660%, respectively, between 1997 and 2003. μ-Opioids depress respiration and deaths related to illicit and non illicit chronic opioid use are not uncommon. Since 2001 there has been an emerging literature that suggests that chronic opioid use is related to central sleep apnoea of both periodic and non-periodic breathing types, and occurs in ～ 30% of these subjects. The clinical significance of these sleep-related abnormalities are unknown. This review addresses the present knowledge of control of ventilation mechanisms during wakefulness and sleep, the effects of opioids on ventilatory control mechanisms, the sleep-disordered breathing found with chronic opioid use and a discussion regarding the future research directions in this area.     

Drug targets for cognitive enhancement in neuropsychiatric disorders

The investigation of novel drug targets for treating cognitive impairments associated with neurological and psychiatric disorders remains a primary focus of study in central nervous system (CNS) research. Many promising new therapies are progressing through preclinical and clinical development, and offer the potential of improved treatment options for neurodegenerative diseases such as Alzheimer's disease (AD) as well as other disorders that have not been particularly well treated to date like the cognitive impairments associated with schizophrenia (CIAS). Among targets under investigation, cholinergic receptors have received much attention with several nicotinic agonists (α7 and α4β2) actively in clinical trials for the treatment of AD, CIAS and attention deficit hyperactivity disorder (ADHD). Both glutamatergic and serotonergic (5-HT) agonists and antagonists have profound effects on neurotransmission and improve cognitive function in preclinical experiments with animals; some of these compounds are now in proof-of-concept studies in humans. Several histamine H3 receptor antagonists are in clinical development not only for cognitive enhancement, but also for the treatment of narcolepsy and cognitive deficits due to sleep deprivation because of their expression in brain sleep centers. Compounds that dampen inhibitory tone (e.g., GABA_A α5 inverse agonists) or elevate excitatory tone (e.g., glycine transporter inhibitors) offer novel approaches for treating diseases such as schizophrenia, AD and Down syndrome. In addition to cell surface receptors, intracellular drug targets such as the phosphodiesterases (PDEs) are known to impact signaling pathways that affect long-term memory formation and working memory. Overall, there is a genuine need to treat cognitive deficits associated with many neuropsychiatric conditions as well as an increasingly aging population.