新型合成毒品4-甲基乙卡西酮对大鼠空间学习与记忆能力的远期影响

目的:探讨卡西酮类新型合成毒品4-甲基乙卡西酮(4-MEC)的慢性使用对大鼠空间学习记忆能力的远期影响。方法:将50只♂SD大鼠随机分成4-MEC给药组(3 mg·kg-1、10 mg·kg-1和30 mg·kg-1)、甲基苯丙胺阳性对照组(3 mg·kg-1)和生理盐水对照组,每组10只,连续一周腹腔注射给药后进入为期两周的戒断。用Morris水迷宫实验比较各组在戒断2周后的空间学习与记忆能力、以及同等剂量药物再暴露后的空间记忆能力。结果:连续注射4-MEC的各组大鼠经过2周戒断后,在连续5 d的逃生习得训练过程中,逃生潜伏期与生理盐水对照组之间均无显著性差异。然而,与慢性生理盐水对照组接受4-MEC(10 mg·kg-1)注射后的空间记忆功能的指标相比,4-MEC戒断的大鼠再次给予4-MEC后,目标象限内滞留时间比、目标象限内移动距离比、虚拟平台穿越次数等反映空间位置记忆能力的指标发生明显的降低。结论:与没有4-MEC使用经验的动物相比,具有慢性使用经验的大鼠在长期戒断后,药物再暴露可造成空间记忆能力的显著下降。该结果揭示慢性卡西酮类毒品的使用对认知功能具有远期的损害作用。     

HPLC-MS/MS检测尿液中甲卡西酮及其代谢物卡西酮

目的:建立尿液中甲卡西酮及其代谢物卡西酮的高效液相色谱-串联质谱(HPLC-MS/MS)检测方法。方法:用含内标双苯戊二氨酯(SKF_525A)的乙腈提取含有甲卡西酮及卡西酮的尿液,经0.22μm微孔有机滤膜过滤,HPLC-MS/MS检测。采用ZORBAX SB-C₁₈色谱柱(50 mm×4.6 mm, 1.8μm),以0.2%甲酸乙腈液和0.2%甲酸水溶液为流动相进行梯度洗脱,流速0.3 mL·min^-1,柱温23℃,电喷雾离子源(ESI),正离子多反应监测模式(MRM)检测。结果:甲卡西酮质量浓度在0.2～3 000 ng·mL^-1范围内线性关系良好,线性方程为Y=0.000 688X+0.000 51(r~2=0.999 1),检测限为0.1 ng·mL^-1,定量限为0.2 ng·mL^-1;卡西酮质量浓度在0.5～3 000 ng·mL^-1范围内线性关系良好,线性方程为Y=0.000 687X+0.000 175(r~2=0.99...     

4-甲基甲卡西酮列入精神药品管理

近期,一些国家出现了4-甲基甲卡西酮的滥用问题。为防止该品种的滥用问题蔓延至我国境内,引发社会和公共卫生问题,2010年8月2日,国家食品药品监督管理局、公安部、卫生部联合发布公告,自2010年9月1日起,4-甲基甲卡西酮列入第一类精神药品管理,未经批准,     

新型策划药4-甲基甲卡西酮的流行与管制

<正>药物设计(drug design)是应用分子模拟技术,通过对已知有活性化合物的改良衍化,得到具有更高活性的新化合物的药物开发方法[1]。他克林(tacrine)是最早应用于老年痴呆治疗的乙酰胆碱酯酶抑制剂,但其对乙酰胆碱酯酶抑制活性较低,且肝毒性明显。通过改造他克林分子结构,获得的双     

新型毒品卡西酮类策划药“浴盐”

浴盐是近期在国际范围内出现的一类新型毒品,主要成分包括4-甲基甲卡西酮(Mephedrone)和/或者亚甲基二氧吡咯戊酮(Methylenedioxypyrovalerone,简称MDPV)。本文对该毒品的理化性质、毒副作用、检验方法及管制情况等进行了介绍,希望能帮助法庭科学人员对该毒品有进一步的了解。     

SPE-GC/MS法检测尿中的甲卡西酮

采用ProElut PLS柱萃取尿样中的甲卡西酮,以气质联用(GC/MS)测定,检测限为0.025μg/mL,并试验了pH值对回收率的影响.结果表明,样品流速为0.5mL/min,以二氯甲烷为洗脱剂,回收率较好.其回收率在85.3%~90.3%之间.并通过实际案件验证了本方法的可靠性.     

甲卡西酮滥用人群的冲动性和攻击性特征及其影响因素分析

目的探讨甲卡西酮滥用人群冲动性和攻击性特征及其影响因素。方法采用自制的甲卡西酮滥用情况调查问卷及中文版Barratt冲动量表(Barratt Impulsivity Scale, BIS-11)和中文版Buss&Perry攻击量表(Buss&Perry Aggression Questionnaire, BP-AQ),对山西省某强制隔离戒毒所内566例主要滥用物质为甲卡西酮的滥用人群进行调查。评估甲卡西酮滥用人群的冲动性和攻击性,并运用多重线性回归方法分析冲动性和攻击性的影响因素。结果甲卡西酮滥用人群BIS-11冲动性量表评分为37.57±16.83,BP-AQ攻击性量表评分为25.70±18.12,均显著高于正常人(冲动性:31.70±13.20,攻击性:21.01±12.71);甲卡西酮滥用时间长(≥12个月,β=4.11,P=0.004)、滥用后有渴求感(β=5.15,P<0.001)、伴随抑郁症状(β=7.57,P<0.001)或精神病性症状(β=6.05,P=0.002)可显著增加该人群冲动性水平;甲卡西酮滥用剂量大(≥0.5g/次,β=4.11,P=0.032)、同时滥用其他毒品(β=8.12,P=0.002)、滥用后有渴求感(β=4.73,P=0.002)、伴随抑郁症状(β=9.29,P<0.001)或精神病性症状(β=4.42,P=0.032)、有高冲动性(β=5.14,P=0.001)可显著增加该人群攻击性水平。结论甲卡西酮滥用者具有较高的冲动性和攻击性,甲卡西酮滥用程度越严重的人群其冲动性攻击性越强,且伴随抑郁、精神病性症状者其冲动性攻击行为也越多。研究表明,应进一步强化宣传教育,预防干预甲卡西酮滥用,并积极治疗毒品使用后出现的精神症状以减少和预防该人群冲动攻击行为的发生,减少其社会危害。     

甲卡西酮使用人群中焦虑及抑郁症状特征及危险因素分析

目的 了解甲卡西酮滥用人群的流行病学特征及该人群中焦虑/抑郁症状的特征。方法 对来自山西省某强制隔离戒毒所中主要滥用物质为甲卡西酮的人群进行横断面调查,并对该人群中焦虑及抑郁症状患病率及其影响因素进行分析。本研究分别采用汉密尔顿焦虑量表(HAMA)和BECK抑郁自评量表(BDI)评估调查对象的焦虑及抑郁症状。结果 本次研究共纳入767名研究对象,以已婚、低学历男性为主;12.6%的调查对象有多药滥用经历,且有48.4%的调查对象有甲卡西酮依赖;分别有15.3%和49.2%的甲卡西酮滥用者存在焦虑及抑郁症状。多因素logistic回归分析显示曾使用过2种及以上的合成毒品(aOR=2.13, 95%CI:1.26-3.61)、甲卡西酮依赖(1.77, 1.13～2.78)及抑郁症状(1.67, 1.10-2.54)是焦虑症状的危险因素,而参加过戒毒治疗(0.42, 0.27-0.64)是焦虑症状的保护因素;甲卡西酮的累计使用时间(>24个月)(1.41, 1.01-1.96)及焦虑症状(1.71, 1.14-2.55)是抑郁症状的危险因素。结论 甲卡西酮滥用后可导致焦虑及抑郁等精神症...     

4-甲基甲卡西酮列入第一类精神药品管理

近期,一些国家出现了4-甲基甲卡西酮（Mephedrone）的滥用问题。为防止该品种的滥用问题蔓延至我国境内,引发社会和公共卫生问题,2010年8月2日,国家食品药品监督管理局、公安部、卫生部联合发布公告,自2010年9月1日起,4-甲基甲卡西酮列入第一类精神药品管理,未经批准,任何单位和个人不得进行4-甲基甲卡西酮的实验研究、生产、经营、使用、存储、运输和进出口等活动。     

4-甲氧甲基芬太尼类似物的合成及其镇痛作用

本文报道了某些N-[1-(2-苯乙基)-4-甲氧甲基-4-哌啶基]-N-丙酰苯胺(4-甲氧甲基芬太尼)类似物的合成及其镇痛活性。小白鼠热板试验的结果表明,该类化合物有很强的吗啡样镇痛活性,但活性弱于相应的4-甲氧羰基芬太尼类化合物;4-N-酰基上羰基的存在对产生强效镇痛活性有重要作用。     

Experiences with mephedrone pre- and post-legislative controls: perceptions of safety and sources of supply

Background

Drug scenes within several countries have changed in recent years to incorporate a range of licit psychoactive products, collectively known as “legal highs.” Hundreds of different legal high products have been described in the literature. Many of these products contain synthetic stimulants that allegedly “mirror” the effects of some illicit drugs. In 2009-2010, growing concern by the UK and Irish governments focused on mephedrone, a synthetic stimulant that had become embedded within several drug scenes in Britain and Ireland. In April 2010, mephedrone and related cathinone derivatives were banned under the UK's Misuse of Drugs Act 1971. Setting aside “worse case scenarios” that have been portrayed by UK and Irish media, little is known about mephedrone use from the consumer's perspective. The purpose of this paper was to (1) explore respondents’ experiences with mephedrone, (2) examine users’ perceptions about the safety of mephedrone, and primarily to (3) examine sources of mephedrone supply during the pre- and post-ban periods.

Methods

Semi-structured interviews were conducted with 23 adults who had used mephedrone during 2009-2010. Data collection occurred in May and June 2010, following the ban on mephedrone. A total of 20/23 respondents had used mephedrone during the post-ban period, and the vast majority had prior experience with ecstasy or cocaine. Respondents’ ages ranged from 19 to 51, approximately half of the sample were female and the majority (19 of 23) were employed in full- or part-time work.

Results

Most respondents reported positive experiences with mephedrone, and for some, the substance emerged as a drug of choice. None of the respondents reported that the once-legal status of mephedrone implied that it was safe to use. Very few respondents reported purchasing mephedrone from street-based or on-line headshops during the pre-ban period, and these decisions were guided in part by respondents’ attempts to avoid “drug user” identities. Most respondents purchased or obtained mephedrone from friends or dealers, and mephedrone was widely available during the 10-week period following the ban. Respondents reported a greater reliance on dealers and a change in mephedrone packaging following the criminalisation of mephedrone.

Conclusion

The findings are discussed in the context of what appears to be a rapidly changing mephedrone market. We discuss the possible implications of criminalising mephedrone, including the potential displacement effects and the development of an illicit market.     

Mephedrone (4-methylmethcathinone), a principal constituent of psychoactive bath salts,produces behavioral sensitization in rats

Background

The present study tested the hypothesis that mephedrone (MEPH) produces behavioral sensitization (i.e., a progressive increase in motor response during repeated psychostimulant exposure) in rats.

Methods

MEPH was administered in two paradigms: (1) a 7-day variable-dosing paradigm (15 mg/kg on the first day, 30 mg/kg for 5 days, 15 mg/kg on the last day) and (2) a 5-day constant-dosing paradigm (15 mg/kg for 5 days). Following 10 days of drug absence, rats were challenged with MEPH (15 mg/kg).

Results

MEPH challenge produced enhancement of repetitive movement compared to acute MEPH exposure in both paradigms. Sensitization of repetitive movements to MEPH was also detected following a shorter (2-day) absence interval, before initiation of an absence interval (i.e., following repeated daily exposure), and across context-independent and -dependent dosing schedules. A lower dose of MEPH (5 mg/kg) did not produce sensitization of repetitive movement. Sensitization of ambulatory activity was not detected in any experimental paradigm.

Conclusion

These results suggest that repeated MEPH exposure produces preferential sensitization to repetitive movement produced by acute MEPH challenge. Our findings suggest that MEPH is a unique stimulant displaying weak sensitizing properties with overlapping, but distinctive, features relative to established psychostimulant drugs.     

Synthesis, full chemical characterisation and development of validated methods for the quantification of (±)-4'-methylmethcathinone (mephedrone): a new "legal high"

The recent global increase in the abuse of 4′-methylmethcathinone and related compounds has developed a requirement for full chemical characterisation of these products. In this work we present full synthetic and chemical characterisation data and supplemental information for mephedrone synthesised as both the hydrobromide and hydrochloride salt. Additionally we report the first fully validated chromatographic methods for the detection and quantitative analysis of the substance both in its pure form and in the presence of a number of common adulterants used in illicit drug manufacture.     

Drugs for youth via Internet and the example of mephedrone

Recently a new class of “designer drugs” has emerged on the drugs abuse market, known as “legal highs”. Such drugs are legal to use and possess, and legal to supply. Mephedrone, a central nervous system stimulant, is the most widely experienced “legal high”.This review presents any available information about psychoactive properties, safety profile, clinical data, and legislation of the new “legal high” and emphasizes the role of Internet with mephedrone's expansion. Available data were collected by various literature search engines and World Wide Web. All valuable information about psychoactive properties, safety profile and clinical data for mephedrone and its use as “legal high” were managed to spot and summarise.Internet plays a significant role for the distribution of “legal highs”, becoming one of the major “drug market”. Adolescents and young adults who are curious about drugs may search on the Internet and thereby become exposed to thousands of sites that expound upon the positive effects of drugs and downplay or deny any negative effects. Use of mephedrone is mainly a youth phenomenon. The hazardous side-effects are strong desire to re-dose, uncomfortable changes in body temperature and heart rate, hallucinations and psychosis.     

强化基本药物政策法律地位,提高合理用药水平

目的:提高合理用药水平。方法:从基本药物政策的法律地位入手,分析我国现行基本药物政策在提高合理用药水平方面的重要作用。结果与结论:基本药物政策推行不力,是制约我国提高合理用药水平的重要原因之一。应从立法、执法、普法方面加强基本药物政策法律地位,推动合理用药水平的提高。     

A web-based survey on mephedrone

Background

This study sought to collect information on the former legal-high ‘mephedrone’ using a web-based survey targeted at mephedrone users.

Methods

The survey was advertised on websites frequented by drug users. Individuals were invited to complete the survey if they had taken mephedrone on at least one occasion in the past.

Results

One thousand and six completed forms were received from declared users, making this the largest survey on mephedrone to date.

Conclusion

Results showed that mephedrone users consider its effects to compare best with those of MDMA, and while MDMA was considered marginally safer and its effects more pleasurable, mephedrone's appeal lay in its availability, low price and reliable purity.     

The Toxicology of Bath Salts: A Review of Synthetic Cathinones

Synthetic cathinones have recently emerged and grown to be popular drugs of abuse. Their dramatic increase has resulted in part from sensationalized media attention as well as widespread availability on the Internet. They are often considered "legal highs" and sold as "bath salts" or "plant food" and labeled "not for human consumption" to circumvent drug abuse legislation. Cathinone is a naturally occurring beta-ketone amphetamine analogue found in the leaves of the Catha edulis plant. Synthetic cathinones are derivatives of this compound. Those that are being used as drugs of abuse include butylone, dimethylcathinone, ethcathinone, ethylone, 3- and 4-fluoromethcathinone, mephedrone, methedrone, methylenedioxypyrovalerone (MDPV), methylone, and pyrovalerone. Synthetic cathinones are phenylalkylamines derivatives, and are often termed "bk-amphetamines" for the beta-ketone moiety. They may possess both amphetamine-like properties and the ability to modulate serotonin, causing distinct psychoactive effects. Desired effects reported by users of synthetic cathinones include increased energy, empathy, openness, and increased libido. Cardiac, psychiatric, and neurological signs and symptoms are the most common adverse effects reported in synthetic cathinone users who require medical care. Deaths associated with use of these compounds have been reported. Exposure to and use of synthetic cathinones are becoming increasingly popular despite a lack of scientific research and understanding of the potential harms of these substances. The clinical similarities to amphetamines and MDMA specifically are predictable based on the chemical structure of this class of agents. More work is necessary to understand the mechanisms of action, toxicokinetics, toxicodynamics, metabolism, clinical and psychological effects as well as the potential for addiction and withdrawal of these agents.     

不合理用药分析并典型案例点评

目的：分析处方点评工作中暴露的问题,促进临床合理用药。方法以随机抽样法抽取该院每月门诊处方100张,共计1200张,临床药师对处方逐一进行审查,对不合理用药处方进行统计分析,并对其中的部分典型不合理处方进行点评。结果不合理处方122张,占总抽查处方数的10．17％,不合理处方类型主要包括临床诊断不明确、药物用法、用量不合理、溶媒选择或合用不合理、无指征使用抗生素、药物配伍不当等。结论医院用药基本合理,但仍有小部分处方用药不合理,需大力改进;处方点评是了解临床用药水平的重要手段,通过定期进行处方点评,剖析临床用药存在的问题,及时发现,合理干预,将有利于提高临床医师合理用药水平。     

处方点评实践工作中典型案例分析

目的:分析处方点评工作中暴露的问题,促进临床合理用药。方法:以随机抽样法抽取每月门诊处方100张,共计1 400张,对其进行分析、点评。结果:不合理用药主要表现在用药与临床诊断不相符、用法与用量不适宜、违反《抗菌药物临床应用指导原则》、抗菌药物使用疗程过长、联合用药不适宜、有配伍禁忌或潜在不良相互作用、溶剂使用不当等。门诊不合格处方161张,占总抽查处方数的11.5%。其中适应证不适宜处方所占比例最大,共49张,占不合格处方数的30.4%;其次是用法、用量不适宜的处方较多,共31张,占不合格处方数的19.3%。结论:处方点评是了解临床用药水平的重要手段,通过定期进行处方点评,剖析临床用药存在的问题,及时发现,合理干预,将有利于提高临床医生合理用药水平。     

有机化学复习课上的归纳与总结

归纳与总结是教师引导学生复习已学课程、掌握并灵活应用有机化学知识的重要手段。