珠江三角洲地区药物滥用者应用三唑仑调查

目的:调查珠江三角洲地区药物滥用者应用三唑仑情况。方法:采用国家药物滥用监测中心编制《药物滥用监测调查表》和自拟调查表,对2005年8月至10月珠江三角洲地区的深圳、东莞、广州、佛山和珠海等地戒毒所收治的5737例药物滥用者进行流行病学调查。结果:珠江三角洲地区的药物滥用者曾经应用三唑仑的行为386例发生率为6.73%,目前主要使用和滥用三唑仑者分别为2.25%和1.57%。应用方式包括口服、烫吸和香烟掺入。零售药店和私人诊所是三唑仑主要的流弊渠道,即使出于治疗目的,多数药物滥用者仍是通过非法渠道获取三唑仑。结论:珠江三角洲地区存在三唑仑流弊和滥用现象,加强对零售药店和私人诊所供、销渠道的监管,是预防本地区三唑仑非法流弊的重要措施之一。戒毒机构应加强对药物滥用者使用三唑仑的指导,防止多药滥用。     

2017-2020年南京医科大学附属脑科医院第二类精神药品使用情况分析

目的 探讨2017—2020年南京医科大学附属脑科医院第二类精神药品的使用情况与发展趋势。方法 采用回顾性研究方法,对南京医科大学附属脑科医院2017—2020年第二类精神药品的销售金额、用药频度（DDDs）、日均费用（DDC）、排序比（B/A）等进行统计分析。结果 将使用的第二类精神药品品种按化学结构分类,各分类金额构成比基本稳定。巴比妥类占比最低,苯二氮类和非苯二氮类的销售金额呈逐年上升趋势。非苯二氮类的DDDs构成比呈微增长趋势,苯二氮类和巴比妥类的DDDs构成比呈微下降趋势。第二类精神药品销售金额的前3位保持稳定,分别为唑吡坦、劳拉西泮、佐匹克隆。唑吡坦、佐匹克隆、劳拉西泮的DDDs始终位于前3。2017—2020年第二类精神药品的DDC保持基本稳定,略有上涨。大部分药品的B/A在0.8～1.2,比较明显的是奥沙西泮的B/A<0.8,艾司唑仑、阿普唑仑、硝西泮的B/A>1.2。结论 南京医科大学附属脑科医院第二类精神药品结构合理,非苯二氮类药物使用逐渐增多。     

我院门诊2007年第二类精神药品应用分析

目的:评价我院门诊第二类精神药品的应用情况。方法:采用回顾性分析方法,对我院门诊2007年第二类精神药品的应用情况进行统计、分析。结果:我院应用的第二类精神药品有2种剂型11种药品,用药频度排序列前5位的是氯硝西泮片、唑吡坦片、劳拉西泮片、阿普唑仑片和艾司唑仑片;销售金额排序列前5位的是唑吡坦片、劳拉西泮片、氯硝西泮片、咪达唑仑注射液和阿普唑仑片。结论:我院第二类精神药品应用基本合理,但部分药品存在滥用现象。     

医疗机构药物滥用监测模式下药物成瘾性特征分析

目的： 了解医疗机构就诊患者麻醉、精神药品滥用/依赖情况和特征，为加强麻醉、精神药品管理提供依据。方法： 利用Excel表统计分析2018-2019年某院确诊为药物滥用或药物依赖患者的麻醉、精神药品使用情况，对确诊为麻醉、精神药品滥用/依赖者的人口学特征、药物使用情况进行描述性分析。结果： 该院就诊患者确诊药物依赖237例，未发现药物滥用患者。237例药物依赖者中，男性84例，占35.44%，女性153例，占64.56%；>60岁的药物依赖者161例，占67.93%；平均年龄（66.83±13.97）岁；依赖年限分布集中在1~3年，占56.119%，平均年限为（4.75±6.96）年；初中及以下文化程度者190例，占79.76%；已婚158例，占66.67%；离/退休人员140例，占59.07%。依赖的药物主要为苯二氮类，145例，占61.19%；药物获得渠道来自医疗机构占99.58%；使用药物原因为控制疾患的患者216例，占91.14%；监测上报人群中以医师、药师为主，占85.23%。结论： 在医疗机构药物滥用监测模式下能关注老年人麻醉、精神药品的合理使用，挖掘潜在的用药风险信号，提前预警与干预，降低药物成瘾性损害事件的发生。     

抗焦虑药物和催眠镇静剂的滥用问题

<正> 抗焦虑药物和催眠镇静剂是当前国内应用最为广泛的药物类别。这类药物使用不当极易形成滥用并产生药物依赖性,危及人类健康。这一类的药物滥用,统称为镇静剂型的药物依赖,加之这一类型的药物属于处方用药,无论在历史和当前,国外均已在人群中流行,构成毒害人民健康的精神药品影响着群体的健康与社会安全。为此,在我国社会主义精神文明建设中,应宣传合理使用此类精神药物,积极防止滥用,及时识别形成依赖者并予以治疗。一、抗焦虑药物和催眠镇静剂的使用状况 (一)催眠镇静药物:常以巴比妥类为代表。巴比妥类催眠镇静剂最早由巴比妥酸衍     

2007年深圳市药物滥用调查监测分析

目的：了解深圳地区2007年药物滥用流行情况,为药物滥用防治工作提供科学依据。方法：对2007年深圳地区4家戒毒机构、3家美沙酮药物维持治疗门诊和1家司法劳教所收集到的8662例戒毒者资料进行分析。结果：深圳市药物滥用者以流动人口为主;滥用的精神活性物质种类较多;吸毒者以无业人员为主;药物滥用者的文化程度较低;药物滥用方式以烫吸和静脉注射为主;毒品主要来源是同伴提供和来自黑市;精神药品、新型毒品滥用比例正在迅速上升,对个人和家庭造成了一定的危害。结论：建立预防机制,采取干预措施,加大禁毒知识宣传教育,加强对私人诊所、药店的监督管理,建立药物滥用和特殊药品安全管理突发事件应急处理机制,才能更好地控制药物滥用情况,维护社会稳定。     

2007N2010年我院第二类口服精神药品应用分析

对我院2007～2010年第二类口服精神药品的用药总量、使用频度（DDDs）进行分析。结果医院第二类口服精神药品的用量比较平稳,最常用的药品是：艾司唑仑、氯硝西泮、盐酸曲马多和阿普唑仑。我院精神药品使用基本合理。     

2007～2010年我院第二类口服精神药品应用分析

对我院2007～2010年第二类口服精神药品的用药总量、使用频度(DDDs)进行分析.结果医院第二类口服精神药品的用量比较平稳,最常用的药品是:艾司唑仑、氯硝西泮、盐酸曲马多和阿普唑仑.我院精神药品使用基本合理.     

2006-2008年我院第二类精神药品应用分析

目的：了解我院第二类口服精神药品的使用情况。方法：对我院2006-2008年第二类口服精神药品的用药总量、使用频度（DDDs）和药物利用指数（DUI）进行分析。结果：医院第二类口服精神药品的用量比较平稳。最常用的药品是阿普唑仑、氯硝西泮、艾司唑仑。结论：我院精神药品使用基本合理。     

第二类精神药品的使用管理

第二类精神药品是临床广泛使用的特殊管理药品,如镇静、催眠药和抗焦虑药巴比妥类和苯二氮卓类,中枢兴奋剂咖啡因等。该类药品可直接作用于中枢神经系统,使之兴奋或抑制,具有潜在的依赖性和耐受性。过去,相关法规对第二类精神药品的具体规定较少,其管理的特殊性并未充分体现,个别地区滥用现象时有发生。一些地区第二类精神药品购销、储存管理、处方使用存在疏漏犤1犦。为此,国家食品药品监督管理局曾专门发出通知,加强第二类精神药品的监管。2005年,国务院发布的《麻醉药品和精神药品管理条例》和卫生部发布的《麻醉药品、精神药品处方管理…     

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.