2012~2014年南京地区常用喹诺酮类抗菌药利用分析

摘 要 目的:了解南京地区喹诺酮类抗菌药的使用近况和发展趋势,为临床合理使用喹诺酮类抗菌药提供参考。方法：根据长江流域医药情报研究所提供的南京地区 2012~2014年喹诺酮类抗菌药的销售数据,采用限定日剂量法,对本地区34家医院近三年喹诺酮类抗菌药的销售金额、用药频度（DDDs）和限定日费用（DDC）等进行回顾性统计分析。结果：销售金额排名前三位的口服喹诺酮药是莫西沙星、左氧氟沙星、洛美沙星,喹诺酮类注射剂是莫西沙星、左氧氟沙星、加替沙星;DDDs排名前三位的口服喹诺酮类抗菌药是左氧氟沙星、莫西沙星、诺氟沙星,注射用喹诺酮类抗菌药是左氧氟沙星、莫西沙星、加替沙星,总销售金额和总DDDs均呈先降后升趋势,销售金额与DDDs的序号比值在0.5~2.0之间。结论：2012~2014年南京地区喹诺酮类抗菌药的临床应用品种受到了限制,口服药的比重增加,注射剂的使用减少,使用符合卫计委抗菌药应用管理的要求及安全、经济的用药原则。     

南京地区33家医院2014～2016年分子靶向抗肿瘤药应用分析

摘 要 目的：分析分子靶向抗肿瘤药的使用情况,为临床合理使用提供参考。方法：采用回顾性调查方法,对南京地区33家医院2014～2016年分子靶向抗肿瘤药物的用药金额、用药频度(DDDs)、限定日费用(DDC)及排序比(B/A)进行分析。结果：南京地区33家医院分子靶向抗肿瘤药销售金额由2014年的8 082.23万元增加至2016年的10 970.18万元,增长了35.73%。其中,单克隆抗体药的销售金额构成比逐年上升,酪氨酸激酶抑制药的销售金额构成比逐年下降。利妥昔单抗各年度销售金额均排名前列。吉非替尼连续3年DDDs排名第1,DDDs较高。大部分药物DDC相对稳定,B/A值大于1,销售金额与用药频度同步性总体较好。结论：2014～2016年南京地区分子靶向抗肿瘤药应用呈上升趋势,分子靶向药物越来越得到临床认可。     

2010～2012年南京地区34家医院抗抑郁药利用情况调查

摘 要 目的:了解南京地区抗抑郁药应用的情况及趋势。方法： 采用回顾性调查方法,对南京地区34家医院2010~2012年抗抑郁药的主要品种、销售金额、用量和生产厂家等情况进行统计分析。结果：3年中南京地区抗抑郁药的销售金额逐年上升,选择性5 羟色胺再摄取抑制药占销售金额比重最大,购药金额构成比例为70.62%、68.72%、69.07%。选择性5 羟色胺再摄取抑制药各年的用药频度（DDDs）构成比较高,分别为72.25%,70.74%,71.72%。2012年DDDs居于前3位的分别是帕罗西丁、舍曲林和文拉法辛。结论：抗抑郁药在临床治疗中发挥越来越重要的作用,南京地区使用抗抑郁药的结构和层次相对合理,基本符合我国目前抗抑郁药的发展现状。     

南京地区52家医院2014～2016年糖皮质激素用药情况分析

摘 要 目的：了解2014～2016年糖皮质激素类药物在南京52家医院中的应用情况,评估其现状和趋势。方法：利用Stata软件对南京市52家医院应用糖皮质激素类药物的销售金额、用量、用药频度（DDDs）等进行统计分析。结果：2014～2016年糖皮质激素类药物销售金额逐年上升,年增长率分别为11.6%和9.7%。连续3年销售金额排名前10位的短效糖皮质激素约占60%,中效糖皮质激素约占22%。所有药物中吸入剂销售金额最多,其次为注射剂、片剂和乳膏剂。醋酸泼尼松片、地塞米松磷酸钠注射液和甲泼尼龙片DDDs连续3年居首位,与2014年相比地塞米松磷酸钠注射液和甲泼尼龙片DDDs分别下降5.9%和6.3%。结论：糖皮质激素类药物在南京地区医院应用广泛,其中金额占比较大的是短效吸入用糖皮质激素,临床最常用的是醋酸泼尼松片,长效地塞米松使用下降,临床选择中效口服制剂时更倾向于选择醋酸泼尼松片。     

2014~2016年南京地区35家医院免疫调节药物利用分

摘 要 目的：了解南京地区免疫调节药物的最新应用情况和发展趋势,为临床合理使用免疫调节药物提供参考。方法：根据江苏省医药情报研究所提供的南京地区2014～2016年免疫调节药物的销售数据,采用金额排序法和用药频度分析法,对本地区35家医院近三年免疫调节药物的销售金额、用药频度（DDDs）、限定日费用（DDC）、序号比值等指标进行回顾性统计分析。结果：免疫抑制药销售金额排名前3位的药物是他克莫司、吗替麦考酚酯和环孢素,DDDs排名前3位的药物是雷公藤总苷、他克莫司和吗替麦考酚酯,总销售金额和总DDDs均呈增长趋势,销售金额与DDDs的序号比值在0.5～4.0之间;免疫增强药销售金额排名前3位的药物是白细胞介素、乌司他丁和匹多莫德,DDDs排名前3位的药物是白细胞介素、羧甲基淀粉钠和匹多莫德,总销售金额和总DDDs呈波动性,销售金额与DDDs的序号比值在0.3～2.0之间。结论：南京地区免疫调节药物的应用现状基本符合当前患者的用药需求。建议治疗时根据药物的特点和患者实际情况实施个体化给药,避免滥用,保证临床用药安全、有效、经济的基本原则。     

南京地区35家医院2009-2011年常用喹诺酮类药利用分析

目的:评价南京地区医院喹诺酮类药的应用情况。方法:对南京地区35家医院2009-2011年常用喹诺酮类药的销售金额、用药频度(DDDs)和日均费用(DDC)等进行回顾性统计、分析。结果:该地区医院喹诺酮类药的销售金额和DDDs整体呈逐年下降趋势,各年度的销售金额分别为83172965.10、76225513.46、62876382.09元,年均增长率为-13.05%;各年度的DDDs分别为2910542.73、2478391.70、2512051.15,年均增长率为-7.10%。左氧氟沙星的DDDs一直排在第1位,其DDDs分别为1102525.40、992019.80、1290872.60,占喹诺酮类药总DDDs的42.85%;莫西沙星注射剂的销售金额和DDDs逐年上升,各年度的销售金额分别为11781874.56、13120229.39、15527001.24元,各年度的DDDs分别为41092.00、45903.00、56016.00,各年度DDC分别为286.72、285.83、277.19元。除帕珠沙星注射剂外,其他品种的销售金额和DDDs皆呈下降趋势。2010年淘汰了3种药(吡哌酸、培氟沙星、妥舒沙星)并引进了1种新药(安妥沙星)。结论:该地区医院喹诺酮类药的应用逐年减少,但为延缓细菌耐药性的产生,仍应继续严格控制喹诺酮类药的应用,以确保临床用药安全、有效和经济。     

某部队医院军人病房2012~2014年口服抗高血压药应用调查

摘 要 目的：调查某部队医院军人病房口服抗高血压药使用情况,为提高用药合理性和药事管理水平提供参考。方法：采用回顾性分析方法,对2012~2014年某部队医院军人病房使用口服抗高血压药的品种、金额、用药频度（DDDs）、限定日费用（DDC）等进行统计分析。结果：2012~2014年某部队医院军人病房口服抗高血压药使用金额逐年增加,最低增幅达10.04%。2012~2014年金额排列前3位的均为钙通道阻滞药（CCB）、血管紧张素Ⅱ受体拮抗药（ARB）、血管紧张素转换酶抑制药（ACEI）,合计占口服抗高血压药销售总金额的87.74%以上,其中,CCB的销售金额占口服抗高血压药销售总金额的40.71%以上。3年中,单品种销售金额和DDDs排列首位的均为氨氯地平;2012年和2013年DDDs前3位的药品是氨氯地平、左旋氨氯地平和缬沙坦,2014年DDDs前3位是氨氯地平、左旋氨氯地平和美托洛尔;DDC最高的均为非洛地平。结论：某部队医院军人病房口服抗高血压药整体结构合理,符合《中国高血压防治指南》（2010年版）的用药原则。疗效好、使用方便、不良反应小的抗高血压药是患者选择的主要品种。     

南京地区肿瘤治疗辅助药的利用分析

目的：探讨南京地区肿瘤治疗辅助药的临床使用情况。方法：采用回顾性调查方法,对南京地区医院2012-2014年肿瘤治疗辅助药的用药金额、用药频度（DDDs）、日均费用（DDC）及排序比（B/A）进行分析。结果：2012-2014年,该地区医院肿瘤治疗辅助药的用药金额呈上升趋势。用药金额排名靠前的康莱特、消癌平、康艾注射液、艾迪注射液等用药金额与用药人次同步性较差,临床使用不合理。结论：肿瘤治疗辅助药在抗肿瘤治疗中占据重要地位,应进一步规范其临床应用,提高用药安全性和经济性。     

2012~2014年武汉地区32家医院中药注射剂应用分析

摘 要 目的：探讨武汉地区中药注射剂的应用特点和趋势,为临床合理使用中药注射剂提供参考。方法: 采用限定日剂量（DDD）为指标的分析方法,对武汉地区32家医院2012~2014年中药注射剂的用药金额、用药频度（DDDs）、限定日费用（DDC）等进行统计分析。结果: 武汉地区32家医院中药注射剂用药金额仍逐年上升,但上升趋势趋缓。心脑血管类中药注射剂用药金额和DDDs仍居第一,但占比小幅下降。肿瘤辅助用中药注射剂占比逐年小幅增长,DDC普遍较高。抗感染类中药注射剂喜炎平销售金额连续3年居首位。结论:中药注射剂临床应用仍呈现增长趋势,为了保障该类药物的临床应用安全,应加强用药管理和监控。     

2013~2015年武汉市34家医院抗高血压药使用情况分析

摘 要 目的：探讨抗高血压药在武汉市的利用情况与发展趋势。方法: 对武汉市34家医院2013~2015年抗高血压药的种类、销售金额和用药频度（DDDs）等进行统计和分析。结果:2013~2015年抗高血压药的年度销售总金额逐年增长,分别为20 896.67,23 527.19,24 033.44万元,其中不同类别药物构成比变化不大,钙通道阻滞药（CCB）、血管紧张素Ⅱ受体拮抗药（ARB）、肾上腺素受体阻断药和血管紧张素转化酶抑制药（ACEI）在3年中均居前4位,新型复方制剂的销售金额和DDDs逐年增加。单药品种销售金额和DDDs排名前2位的分别是左旋氨氯地平和氨氯地平。结论:在武汉市, CCB、ARB、ACEI、肾上腺素受体阻断药和利尿药最常用,符合目前高血压治疗用药的指南推荐。     

Role of glutathione in reduction of arsenate and of gamma-glutamyltranspeptidase in disposition of arsenite in rats

Arsenate (AsV), the environmentally prevalent form of arsenic, is converted sequentially in the body to arsenite (AsIII), monomethylarsonic acid (MMAsV), monomethylarsonous acid (MMAsIII), and dimethylarsinic acid (DMAsV) and some trimethylated metabolites. Although the biliary excretion of arsenic in rats is known to be glutathione (GSH)-dependent, involving transport of arsenic-GSH conjugates, the role of GSH in the reduction of AsV to the more toxic AsIII in vivo has not been defined. Therefore, we studied how the fate of AsV is influenced by buthionine sulfoximine (BSO), which depletes GSH in tissues. Control and BSO-treated rats were given AsV (50 micromol/kg, i.v.) and arsenic metabolites in bile, urine, blood and tissues were analysed by HPLC-HG-AFS. BSO increased retention of AsV in blood and tissues and decreased appearance of AsIII in blood, bile (by 96%) and urine (by 63%). The biliary excretion of MMAsIII was also nearly abolished, the appearance of MMAsIII and MMAsV in the blood was delayed and the renal concentrations of these monomethylated arsenicals were decreased by BSO. Interestingly, appearance of DMAsV in blood and urine remained unchanged and the concentrations of this metabolite in the kidneys and muscle were even increased in response to BSO. To test the role of gamma-glutamyltranspeptidase (GGT) in arsenic disposition, the effect of the of the GGT inhibitor acivicin was investigated in rats injected with AsIII (50 micromol/kg, i.v.). Acivicin lowered the hepatic and renal GGT activities and increased the biliary as well as urinary excretion of GSH, but failed to alter the disposition (i.e. blood and tissue concentrations, biliary and urinary excretion) of AsIII and its metabolites. In conclusion, shortage of GSH decreases not only the hepatobiliary transport of arsenic, but also reduction of AsV and the formation of monomethylated arsenic, while not hindering the production of dimethylated arsenic. While GSH plays an important role in the disposition and toxicity of arsenic, GGT, which hydrolyses GSH and GSH conjugates, apparently does not influence the fate of the GSH-reactive trivalent arsenicals in rats.     

微透析取样技术在中药体内分析中的应用研究进展

本文综述了微透析取样技术在中药体内分析中的应用,介绍微透析取样技术的原理、组成、探针类型、特点,重点阐述了微透析取样技术在测定脑、血液、皮肤等组织器官中中药有效成分浓度的应用实例。表明微透析取样技术在中药药效研究中具有广阔的前景。     

应用PASS系统分析我院2010年住院医嘱

目的:了解我院2010年住院患者的合理用药情况,探讨如何利用合理用药监测系统( PASS)提高合理用药水平.方法:利用PASS对我院2010年15 966例住院患者的1 184 997条用药医嘱进行监测,以黑色警示医嘱为依据,收集不合理用药信息,并对监测结果进行统计、分析.结果:不合理用药医嘱50 261条,发生率为4.24％.绝对禁止黑色医嘱5441条,主要为药物相互作用(66.54％)、注射液体外配伍(17.86％)、用法用量(15.46％)、儿童警告(1.14％).结论:应用PASS系统能有效监测医嘱中的不合理用药情况,有利于提高临床合理用药水平,但PASS系统尚存在局限性,有待进一步完善.     

Changes in levels of dependency and predictors of mortality in elderly people in institutional care in Dunedin

The 1983 study of dependency of subjects in institutional care in Dunedin was repeated two years later. A significant increase in levels of dependency in residential homes, particularly in the Religious and Welfare sector was found. In 1983 there were 29 high dependency residents and 73 medium dependency residents in residential homes. In 1985 these numbers had increased to 55 and 86 respectively. There was no change in the number of low dependency residents. In 1983, 6 high dependency residents had been admitted to residential home care in the year prior to the study. In 1985 the number of high dependency residents recently admitted had increased to 23. There had also been a significant increase in the dependency of patients in Religious and Welfare continuing care hospitals. Of the 933 subjects in institutional care in 1983 who were able to be followed, 354 (37.9%) died in the following 2 years. Mortality rate was higher for those in hospital care (48.1%) than for those in residential home care (29.6%). Mortality rates were higher in more dependent subjects and this was evident for each measure of dependency.     

应用PASS系统对我院2008年住院医嘱的分析

目的监测分析2008年我院住院患者用药情况。方法将PASS系统嵌入医生工作站、临床药学工作站等子系统,构建合理用药计算机网络系统,对住院医嘱进行及时监测,将监测结果向医生反馈,并对其进行统计、分析。结果2008年共监测医嘱3 620 241条,不合理医嘱908条,占0.02%。不合理医嘱中,配伍禁忌(381条)占41.96%,用法用量(381条)占41.96%,药物相互作用(108条)占11.89%,儿童用药(38条)占4.19%。经与医生沟通后,更改不合理医嘱856条,占94.27%。结论PASS系统可有效监测医嘱中的不合理用药,通过与医生交流,大大减少药物不良事件的发生,值得临床推广应用,也为临床药师开展工作带来了极大的便利。但PASS系统尚存在局限性,有待进一步完善。     

Role of desacetylation in the detoxification of cephalothin in renal cells in culture

The toxicity of three cephalosporin antibiotics to rabbit kidney cells in culture was compared to their known nephrotoxic potential in vivo (cephaloridine greater than cefazolin greater than cephalothin). While cephalothin is considered to be a relatively nonnephrotoxic cephalosporin when administered to many species including humans and rabbits, in several in vitro systems involving rabbit renal tissue, cephalothin was comparatively more toxic than anticipated based on in vivo data. Cephalothin is extensively desacetylated in rabbits to a less microbiologically active metabolite, desacetylcephalothin. When a microsomal S9 fraction from rabbit kidney was added to the in vitro assay in cultured rabbit renal cells, cephalothin was desacetylated and its toxicity to kidney cells was reduced. The addition of S9 in vitro provided a toxicity ranking of the cephalosporins that correlated with their known in vivo nephrotoxic potentials (cephaloridine greater than cefazolin greater than cephalothin). The in vitro detoxification of cephalothin by S9 was blocked by the coadministration of the esterase inhibitor, aminocarb. Desacetylcephalothin was relatively nontoxic to rabbit renal tissue in vitro. These results suggest that the desacetylation of cephalothin in vivo represents a previously unrecognized mechanism of detoxification of this cephalosporin antibiotic. Furthermore, this mechanism of detoxification may be applicable to other acetylated cephalosporins.     

2009年某院住院患者抗真菌药用药调查

目的:分析讨论某院抗真菌药使用的合理性,为临床安全有效地使用抗真菌药提供参考。方法:回顾性统计分析某院2009年住院患者抗真菌药用药信息。结果:2009年某院住院患者抗真菌药DDDs排名前3名分别为:氟康唑、制霉菌素和伊曲康唑;使用金额排名前3名分别为:氟康唑、米卡芬净及卡泊芬净;更换一种抗真菌药进行治疗的患者数为176人,在全部患者中占13.4%。结论:应进一步强化用药指征的意识,提高标本送检率,同时改善某些抗真菌用药不合理更换的现象,以避免耐药性发生,从而更好更长远地体现抗真菌药的治疗价值。     

Kinetics of in vitro metabolism of methoxyphenamine in rats

1. Methoxyphenamine (MP) was metabolized in vitro by rat liver preparations to O-desmethylmethoxyphenamine (O-desmethyl-MP), N-desmethylmethoxyphenamine (N-desmethyl-MP) and 5-hydroxymethoxyphenamine (5-hydroxy-MP). These metabolic pathways were inhibited by SKF 525-A and carbon monoxide, which indicates that these reactions were mediated at least partly by an NADPH-dependent cytochrome P-450 system. 2. Strain differences in the metabolism of this drug in vitro were observed in female Lewis and Dark Agouti (DA) rats, which are proposed models for human debrisoquine phenotypes. Methoxyphenamine O-demethylase and 5-hydroxylase activity in DA rats were lower than those in Lewis rats. 3. The metabolic transformation of methoxyphenamine in vitro to O-desmethyl-MP was inhibited competitively by debrisoquine and sparteine. This indicates that the cytochrome P-450 isoenzyme mediating the metabolism of MP to O-desmethyl-MP is similar to that mediating metabolism of debrisoquine and sparteine. However, no inhibition was observed with methenytoin.     

Comparison of in vitro cell models in predicting in vivo brain entry of drugs

Although several in vitro models have been reported to predict the ability of drug candidates to cross the blood-brain barrier, their real in vivo relevance has rarely been evaluated. The present study demonstrates the in vivo relevance of simple unidirectional permeability coefficient (P(app)) determined in three in vitro cell models (BBMEC, Caco-2 and MDCKII-MDR1) for nine model drugs (alprenolol, atenolol, metoprolol, pindolol, entacapone, tolcapone, baclofen, midazolam and ondansetron) by using dual probe microdialysis in the rat brain and blood as an in vivo measure. There was a clear correlation between the P(app) and the unbound brain/blood ratios determined by in vivo microdialysis (BBMEC r=0.99, Caco-2 r=0.91 and MDCKII-MDR1 r=0.85). Despite of the substantial differences in the absolute in vitro P(app) values and regardless of the method used (side-by-side vs. filter insert system), the capability of the in vitro models to rank order drugs was similar. By this approach, thus, the additional value offered by the true endothelial cell model (BBMEC) remains obscure. The present results also highlight the need of both in vitro as well as in vivo methods in characterization of blood-brain barrier passage of new drug candidates.