精神病专科医院住院患者抗精神病药使用分析

目的：了解本院长期住院精神疾病患者抗精神病药使用特点。方法：对2014年10月20日住院时间超过1个月的精神疾病患者处方进行调查分析。结果：1196例精神疾病患者,单一用药352例（29.4%）,其中利培酮142例（40.3%）、氯氮平68例（19.3%）;联合用药844例（70.6%）,常用联合方案为氯氮平+新型非典型抗精神病药、利培酮+丙戊酸盐、氯氮平+新型非典型抗精神病药+丙戊酸盐;氯氮平与其它精神药物联用时剂量低于单用,有显著性差异。结论：住院精神疾病患者使用利培酮比率最高,药物治疗以联合用药为主,联合用药方案基本合理。     

非典型抗精神病药治疗700例精神分裂症住院患者的应用分析

目的：了解我院精神分裂症住院患者非典型抗精神病药的应用现状,探讨临床使用非典型抗精神病药的特点。方法：随机抽查本院2008年住院的700例诊断为精神分裂症患者应用非典型抗精神病药,采用WHO药物统计合作中心设定的限定日剂量（DDD）计算我院非典型抗精神病药的用药频度（DDDs）、药物利用指数（DUI）及联合用药情况。结果：非典型抗精神病药的DDDs排序为：喹硫平、利培酮、氯氮平、阿立哌唑、齐拉西酮、奥氮平。单一药物治疗496例,占70.86%;二联或三联用药204例,占29.14%。DUI≤1。结论：我院非典型抗精神病药用药结构倾向合理。对于精神分裂症的临床治疗应以单一药物治疗为主。     

我院2013年707例住院患者抗精神病药应用现状分析

目的了解我院抗精神病药的使用现状,为临床合理用药提供依据。方法对我院2013年7月22日住院和新入院的精神病患者的用药情况进行分析。结果在707例患者中,使用1种抗精神病药治疗的患者有421例(59.97%),奥氮平位居首位(91例,12.87%),其余依次为喹硫平(64例,9.05%)、利培酮(58例,8.20%)、氯氮平(45例,6.37%);联合2种药物治疗的有207例(29.28%),以氯氮平+阿立哌唑、氯氮平+利培酮、奥氮平+利培酮多见。结论非典型抗精神病药占临床用药主导地位,两种抗精神病药物联合用药比例较2008年有所增加。     

精神分裂症患者用药合理性的调查与研究

目的：调查成年精神分裂症住院患者抗精神病药的临床使用现状。方法：结合患者的病历资料,对2017年12月期间某院603例精神分裂症患者的用药情况进行回顾性分析。结果：入组的603例患者中,接受单一抗精神病药物治疗（单一组）的患者260例（43.12%）,采用联合2种及以上抗精神病药治疗的患者245例（40.63%）,其中联用情感稳定剂例数为117（19.40%）。第2代抗精神病药使用比例明显高于第一代抗精神病药。使用频率居前的5种药物依次是：奥氮平213例（35.32%）,利培酮191例（31.67%）,氯氮平153例（25.37%）,阿立哌唑93例（15.42%）,丙戊酸钠93例（15.42%）。结论：精神分裂症住院患者的药物使用基本合理,但少部分病例存在3种及以上抗精神病药联合的情况,缺少循证医学证据支持,需进一步研究,以确保患者用药的安全、有效。     

625例精神病住院患者精神药物使用时点调查

目的：了解住院精神疾病患者精神药物的应用情况及其用药规律。方法：选取2009年8月5日河南省精神病医院住院精神疾病患者的精神药物用药资料进行分析,将其结果与2004年的调查结果相比较。结果：抗精神病药用药频度居前5位的依次为氯氮平、喹硫平、利培酮、阿立哌唑和奥氮平。抗抑郁药用药频度居前3位的依次为舍曲林、帕罗西汀和曲唑酮。苯二氮类药物应用频率有所下降。结论：非典型抗精神病药和新型抗抑郁药已成为临床一线用药,用药方案基本合理。     

精神分裂症患者住院期间精神药物使用情况分析

目的了解精神分裂症患者住院期间精神药物使用情况。方法采用自编量表通过我院病案室出院登记系统,对我院2010年1月至2010年12月出院的精神分裂症患者住院期间使用精神药物的品种、剂量及合并用药情况进行调查。结果全院精神科总住院人数1940人,调查登记精神分裂症1350人,占总住院人数的69.6%。单一服用抗精神病药物者980例(72.6%),按使用率顺序为氯氮平(25.9%)、利培酮(17.8%)、氯丙嗪(15.6%)、氟哌啶醇(4.4%)、奥氮平(4.4%)、奋乃静(2.96%)、舒必利(1.5%)。两种精神药物合并者为360例(26.6%)。其中以氯氮平、利培酮、奥氮平再合并其他一种抗精神病药为多见。按使用率顺序主要为氯氮平+舒必利、利培酮+氯氮平、利培酮+舒必利、氯氮平+氟哌啶醇、氯氮平+哌泊噻嗪、氯氮平合并癸氟奋乃静、奥氮平合并氟哌啶醇等。三种抗精神病药合用者10例。另外,合并安坦220例(16.3%);异丙嗪60例(4.4%);苯二氮卓类药150例(11.1%);心得安260例(19.3%)。60例(4.4%)合用抗抑郁剂。合并ECT者210例(15.6%)。结论住院精神分裂症的治疗以单一应用抗精神病药为主,非典型抗精神病药的应用逐年增加,且居首位。新型非典型抗精神病药如利培酮等药物的应用增多,已经被广大医生及患者所接受。     

精神科住院患者用药时点调查分析

目的：了解中山市第三人民医院住院精神障碍患者的药物应用情况及其用药规律。方法采用一日法,以2013年5月14日为时间节点,对住院患者的用药情况进行分析,总结其用药规律。结果住院患者抗精神病药用药频度居前5位的依次为利培酮、氯氮平、奥氮平、阿立哌唑和喹硫平。心境稳定剂用药频度居前3位的是丙戊酸钠、奥卡西平和丙戊酸镁。结论非典型抗精神病药和新型抗抑郁药已成为临床一线用药,临床治疗总体用药比较规范,但仍需要注意苯海索和苯二氮类（BDZ）的合理使用。     

儿童精神分裂症住院患者不同年代用药比较

目的探讨儿童精神分裂症住院患儿不同年代使用精神药物的变化趋势.方法回顾性分析相隔15年,1年内住院的儿童精神分裂症患儿病例资料共306例,比较两组使用精神药物情况、疗效和不良反应.结果15年前组用药前三位为氯丙嗪、奋乃静、舒必利,以典型抗精神病药为主;15年后组用药前三位为利培酮、氯氮平、奎硫平,以非典型抗精神病药为主.结论儿童精神分裂症住院患儿临床用药由典型抗精神病药转向非典型抗精神病药,利培酮、氯氮平等非典型抗精神病药可作为儿童精神分裂症的首选药物.     

2007—2011年盐城市第四人民医院抗精神病药应用分析

目的：了解2007—2011年我院抗精神病药使用情况,以促进临床合理用药。方法：采用回顾性分析法,对2007—2011年我院抗精神病药销售金额、用药频度（DDDs）和限定日费用（DDC）等进行统计、分析。结果：新型非典型抗精神病药的用量逐年上升,5年销售金额增长了2.84倍,DDDs上升了2.53倍;而典型抗精神病药及非典型抗精神病药氯氮平的用量则逐年下降,5年DDDs下降了33.00%。利培酮、阿立哌唑、喹硫平、奥氮平的销售金额及DDDs排序均居前列。2011年抗精神病药的平均DDC比2007年增长了2.26倍,DDC呈现快速增长趋势。结论：我院抗精神病药应用合理,新型非典型抗精神病药的用量呈现增长态势,典型抗精神病药及非典型抗精神病药氯氮平仍是部分患者特别是经济承受能力较低患者的首选药,选用国产和普通剂型的药物有利于降低药物治疗成本。     

住院精神疾病患者抗精神病药使用情况调查

目的:了解住院精神疾病患者抗精神病药的使用情况。方法:采用回顾性调查方法,对中山市第三人民医院2013年1月1日—12月31日出院的精神疾病患者的用药情况进行统计、分析。结果:在住院精神疾病患者的疾病构成中,以精神分裂症和心境障碍所占比例最多;抗精神病药使用最多的是利培酮;合并用药的治疗方式在住院患者中非常普遍;抗精神病药的使用剂量基本都在推荐的安全剂量范围之内。结论:该院抗精神病药以使用非典型抗精神药为主;各种抗精神病药临床用药多样化,用药安全不容忽视。     

Theophylline kinetics in peripheral tissues in vivo in humans

Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (c_max, t_max, AUC) were calculated for plasma and tissue time courses. The mean AUC_tissue /AUC_plasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA Fluorescence polarisation immuno assay - AUC Area under the curve - t_max Time to peak concentration - c_max Peak concentration     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg.kg) or i.p. (50 mg.kg) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) l.h. kg in the male rat and 10.6 (95% CI: 7.5, 15.0) l.h. kg in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p 0.001) in plasma obtained from the male (8.8 2.0%) compared with the female rat (11.7 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

休克时血中氧自由基的变化

本实验测定10名休克患者血浆和红细胞的丙二醛(MDA)、血浆总抗的氧化活性(AOA)的含量。结果表明:休克病人红细胞膜和血浆 MDA 含量(4.298±0.722;5.348±0.834)与对照组(3.235±0.682;4.356±1.081)比较明显增高(P<0.05);血浆 AOA(39.65±7.858)与对照组(48.21±10.81)比较明显降低(P<0.01)。提示:休克时,患者机体内自由基反应增强是引起组织细胞损伤的原因之一。     

Interindividual variability in metabolic activation in humans in vivo

In assessing interindividual variability in metabolic activation, the toxic metabolite is often too unstable for conventional analysis. Possible alternatives include a stable product of the reactive metabolite e.g. cysteinyl derivatives of N-acetyl-4-benzoquinoneimine, the toxic metabolite of paracetamol, adducts with DNA or protein, and indirect measurement of the activity of the enzyme(s) producing the active metabolite. An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. The extent of inhibition, determined from levels of unchanged amine in urine, is an indirect measure of the activity of the activation pathway. Further refinement of this approach, allied to improved measures of the biological process of interest should prove of value in evaluating interindividual variability and its role in the risk assessment process.     

Polymorphisms in genes involved in neurotransmission in relation to smoking

Smoking behavior is influenced by both genetic and environmental factors. The genetic contribution to smoking behavior is at least as great as its contribution to alcoholism. Much progress has been achieved in genomic research related to cigarette-smoking within recent years. Linkage studies indicate that there are several loci linked to smoking, and candidate genes that are related to neurotransmission have been examined. Possible associated genes include cytochrome P450 subfamily polypeptide 6 (CYP2A6), dopamine D₁, D₂, and D₄ receptors, dopamine transporter, and serotonin transporter genes. There are other important candidate genes but studies evaluating the link with smoking have not been reported. These include genes encoding the dopamine D₃ and D₅ receptors, serotonin receptors, tyrosine hydroxylase, trytophan 2,3-dioxygenase, opioid receptors, and cannabinoid receptors. Since smoking-related factors are extremely complex, studies of diverse populations and of many aspects of smoking behavior including initiation, maintenance, cessation, relapse, and influence of environmental factors are needed to identify smoking-associated genes. We now review genetic polymorphisms reported to be involved in neurotransmission in relation to smoking.     

Genotoxic effects of chlorophenoxy herbicide diclofop-methyl in mice in vivo and in human lymphocytes in vitro

Diclofop-methyl (DM) is a chlorophenoxy derivative used in large quantities for the control of annual grasses in grain and vegetable crops. In this study, the genotoxic effects of DM were investigated by measuring chromosomal aberrations (CAs) in mouse bone-marrow cells and CA and the comet assay in human peripheral lymphocytes. Mice were treated with 15.63, 31.25, 62.5, and 125?mg/kg body weight of DM intraperitoneally for 24 hours, and 15.63-, 31.25-, 62.5-, 125-, and 250-µg/mL concentrations were applied to human lymphocytes for both 24 and 48 hours. In in vivo treatments, DM significantly, but not dose dependently, increased the total chromosome aberrations, compared to both negative and solvent controls. Cell proliferation was significantly, but not dose dependently, affected by all doses. In in vitro treatments, DM (except 15.63 µg/mL) significantly and dose dependently increased the frequency of chromosome aberrations. Also, 250 µg/mL of 48-hour treatment was found to be toxic. Cell proliferation was significantly and dose dependently affected by DM applications, when compared to negative control. In in vitro treatments, DM significantly decreased the mitotic index only at the highest concentration for 24 hours, and 62.5- and 125-µg/mL concentrations for 48 hours. In the comet assay, a significant and dose-dependent increase in comet-tail intensity was observed at 62.5-, 125-, and 250-µg/mL concentrations. The mean comet-tail length was significantly increased in all concentrations. Our results demonstrate that DM is genotoxic in mammalian cells in vivo and in vitro.     

Tramadol concentrations in blood and in cerebrospinal fluid in a neonate

Based on blood and cerebrospinal fluid samples collected in a full-term neonate, the penetration of tramadol in the central nervous system is described. Following intravenous administration of tramadol, a lag time of about 4 h was observed until full blood–brain equilibration was achieved. This pharmacokinetic observation is in line with a recent pharmacodynamic evaluation of the central opioid effects of tramadol in adults.     

2010调脂治疗领域进展

2010年在调脂治疗领域针对他汀治疗心血管病的防治又进行了许多探索。本文通过综述他汀类药物的国际大规模临床试验结果,重新评价了他汀类药物在冠心病一级预防和冠心病二级预防中的地位,阐明了强化他汀治疗的意义;对他汀的心肾保护作用和安全性新证据进行了说明。