Clinical Observation of Tirofiban Treatment on No-Flow Phenomenon in Patients with Acute ST-Elevation Myocardial Infarction during Percutaneous Coronary Intervention

目的:观察冠脉内注射替罗非班对急性ST段抬高型心肌梗死(STEMI)患者急诊经皮冠状动脉介入(PCI)治疗术中无复流的疗效.方法:将82例急性STEMI行急诊PCI术且术中出现无复流现象的患者分为2组,替罗非班组(48例)于冠脉内注入替罗非班10 μg· kg-1,5 min内注射完毕,继以0.15μg· kg-1·min-1静脉维持38 h;对照组(34例)于冠脉内注入维拉帕米200 μg,15 min内注射完毕.观察2组给药后20 min心肌梗死溶栓试验(TIMI)血流分级、TIMI心肌灌注分级(TMPG)和校正的TIMI帧数(CTFC).结果:给药后20 min,替罗非班组TIMI血流和TMPG心肌灌注3级获得率高于对照组,差异有统计学意义.给药前2组CTFC帧数差异无统计学意义,给药后20 min替罗非班组CTFC低于对照组,差异有统计学意义.结论:冠脉内注射替罗非班可以有效地改善STEMI急诊PCI术中无复流的现象.     

冠状动脉内注射替罗非班对急性冠状动脉综合征经皮冠状动脉介入术后炎性因子及冠状动脉血流的影响

目的了解冠状动脉内注射替罗非班对急性冠状动脉综合征(ACS)经皮冠状动脉介入术(PCI)后炎性因子及冠状动脉血流的影响。方法将38例ACS患者冠状动脉造影(CAG)术后随机分为A、B两组,A组(19例),冠状动脉内注射替罗非班10μg/kg,继之以0.15μg/(kg min)静脉滴注36h。B组(19例)ACS患者CAG术后即时,静脉注射替罗非班(10μg/kg),继之以0.15μg/(kg min)静滴36h。A、B两组ACS患者分别于CAG术后即时静脉血、PCI术后3d空腹静脉血查超敏C反应蛋白(hs-CRP)、血清基质金属蛋白酶2(MMP-2),并于PCI术后计算"罪犯血管"校正TIMI帧数(CTFC),并作对比。结果 A、B两组患者hs-CRP、MMP2对比差异无显著性(P>0.05),CTFC对比两组差异有显著性(P<0.05)。结论冠状动脉内注射替罗非班能明显改善冠状动脉血流,其抗炎效果与静脉内使用无差别。     

冠脉内使用替罗非班治疗ST段抬高型心肌梗死的临床观察

目的评价急诊行经皮冠状动脉介入治疗(PCI)的急性ST段抬高型心肌梗死(STEMI)患者冠脉内使用替罗非班的疗效及安全性。方法62例拟行急诊PCI术的STEMI患者随机进入对照组(未用替罗非班,20例)、替罗非班IV组(静脉内推注替罗非班,21例)和替罗非班IVIC组(静脉和冠脉内推注替罗非班,21例),观察患者PCI术后心肌梗死溶栓治疗(TIMI)血流分级、校正的TIMI帧数(CTFC)、肌酸激酶同工酶(CK-MB)水平、超声心动图主要不良心血管事件(MACE)和出血事件。结果与对照组相比,替罗非班IV组及替罗非班IVIC组患者术后CTFC、CK-MB水平和左室射血分数(LVEF)均有改善,且替罗非班IVIC组各项指标差异均有统计学意义;但TIMI血流分级、出血事件的发生率、住院期间MACE和住院天数等组间差异均无统计学意义。结论在STEMI患者急诊PCI术中,单纯静脉或静脉和冠脉内推注替罗非班疗效优于未接受替罗非班者,且静脉和冠脉内推注的近期疗效优于单纯静脉推注。     

替罗非班治疗冠状动脉介入中无复流的疗效观察

目的评价冠状动脉内注射国产盐酸替罗非班对急性冠状动脉综合征(acute coronary syn-drome,ACS)介入术后无复流患者冠状动脉TIMI血流的影响安全性及可行性。方法将ACS患者经皮冠状动脉介入治疗(percutaneous coronary intervention,PCI)术后判定无复流者67例,分为A组(冠状动脉内注射维拉帕米200μg及盐酸替罗非班10μg/kg)32例和B组(冠状动脉内注射维拉帕米200μg)35例。观察给药后10min TIMI血流分级及校正的TIMI计帧数(CTFC),出血并发症及30d内主要不良心血管事件(MACE)发生率。结果 A组介入术后无复流患者TIMIⅢ级血流获得率(65.6%)高于B组(42.9%)(P<0.05);CTFC显示替罗非班组血流快于维拉帕米组(P<0.01);出血并发症发生率和30d内MACE发生率与维拉帕米组差异均无统计学意义(P>0.05)。结论冠状动脉内注射国产盐酸替罗非班治疗ACS介入术后无复流患者是有效和安全可行的。     

替罗非班在急性心肌梗死患者PCI中的应用

目的观察替罗非班冠脉内注射及/或静脉注射对ST段抬高性急性心肌梗死(AMI)患者冠状动脉介入治疗(PCI)预后的影响。方法将113例STEMI患者随机分为常规治疗组(对照组)60例和替罗非班组(治疗组)53例。2组均给予常规药物治疗和PCI治疗;在此基础上替罗非班组在PCI时,冠脉内注射替罗非班10μg/kg,术后以维持量0.1μg·kg-1·min-1由静脉微泵维持泵入24~48 h;用心肌梗死溶栓试验(TIMI)和校正的TIMI计帧数(CTFC)测量法,评估PCI术后即刻结果、临床疗效、心肌损伤标志物水平、心血管事件和不良反应。结果 PCI后,TIMI血流3级获得率,替罗非班组高于常规治疗组(P=0.046)。结论替罗非班冠脉内注射治疗急性心肌梗死患者安全有效。     

硝普纳联合替罗非班治疗急诊冠脉介入中无复流现象的疗效观察

目的观察硝普钠联合替罗非班对急性前壁心肌梗死急诊冠状动脉介入治疗中无复流患者冠脉TIMI血流分级、TIMI心肌灌注分级、左心室功能和收缩同步性的影响。方法 59例明确诊断为首次急性前壁心肌梗死行急诊冠状动脉介入治疗无复流的患者被随机分为治疗组(30例)和对照组(29)例,对照组于无复流即刻经导引导管给予硝酸甘油200μg,治疗组于无复流即刻经微导管选择性冠脉内给予硝普钠200μg及替罗非班500μg均于2min内注射,两组患者均于冠脉介入术后给予替罗非班6μg/(kg·h)的速度静脉泵入,持续24h。观察2组患者给药5min后冠脉TIMI血流分级、TIMI心肌灌注分级,治疗后6个月用平衡法核素心室显像及相位分析自动获得左室收缩、舒张功能和收缩同步性参数。结果治疗组给药5min后TIMI血流分级、TIMI心肌灌注分级显效率均高于对照组,术后第6个月治疗组左室收缩功能参数、舒张功能参数及心室收缩同步性参数明显优于对照组。结论经微导管选择性联合给予硝普钠及替罗非班可明显改善急性心肌梗死冠脉介入中无复流患者梗死相关动脉TI-MI血流分级、TIMI心肌灌注分级、左室收缩和舒张功能,增加左室收缩同步性。     

术前与术中使用替罗非班对急性ST段抬高心肌梗死急诊介入治疗慢血流的比较及安全性

目的:探讨术前与术中应用替罗非班对急性ST段抬高心肌梗死经皮冠状动脉介入(PCI)治疗中慢血流的比较及安全性。方法:将90例急性ST段抬高心肌梗死患者随机分为替罗非班术前组(30例)、替罗非班术中组(30例)和对照组(30例)。比较三组患者梗死相关血管PCI治后即刻TIMI血流、校正TIMI帧数计数(CTFC)、90min ST段回落百分比、出血和血小板减少的发生率。结果:与对照组相比,替罗非班术前组及替罗非班术中组PCI后慢血流发生率显著降低(P<0.05),90min内ST段回落百分比提高;与替罗非班术中组相比,替罗非班术前组PCI后慢血流发生率降低更加显著(P<0.05);两组患者均未出现住院期间死亡及急性血栓形成,出血并发症比较差异无统计学意义(P>0.05)。结论:PCI术前早期应用替罗非班能更好地改善急性ST段抬高心肌梗死患者PCI后梗死相关血管的慢血流的发生,临床应用安全有效。     

替罗非班治疗比伐卢定抗凝下急性ST段抬高性心肌梗死经皮冠状动脉介入术中无复流或慢血流

目的观察替罗非班对急性ST段抬高性心肌梗死(STEMI)患者在比伐卢定抗凝下直接经皮冠状动脉介入治疗(PCI)中出现无复流或慢血流的疗效。方法 87例STEMI患者在比伐卢定抗凝下直接PCI术中出现无复流或慢血流,均给予硝酸甘油冠脉内推注,仍无复流或慢血流的患者随机冠脉内给予替罗非班10μg·kg-1(治疗组,n=44)或肝素盐水20 m L(8 U·m L-1,对照组,n=43),于给药后5 min时复查造影,观察两组梗塞相关血管的TIMI血流分级(TFG)和校正的TIMI血流帧数计数(CTFC)、出血并发症和30 d主要心血管事件(MACE)。结果给药后5 min两组TFG、CTFC比给药前显著好转(P<0.05),治疗组优于对照组(P<0.05)。两组术后出血并发症和30 d MACE发生率无显著差异(P>0.05)。结论对于STEMI患者在比伐卢定抗凝下直接PCI术中出现无复流或慢血流,冠脉内给予替罗非班效果明显且安全。     

血栓抽吸联合冠脉内注射替罗非班治疗急性ST段抬高型心肌梗死的疗效观察

目的：评价在急性ST段抬高型心肌梗死（STEMI）患者直接经皮冠状动脉介入治疗（PCI）中联合应用血栓抽吸和经指引导管梗死相关动脉内注射替罗非班的有效性和安全性。方法选取100例STEMI患者,观察组为血栓抽吸＋替罗非班组（50例）,血栓抽吸后3 min内经指引导管梗死相关动脉内注射替罗非班500μg并植入支架,后静脉滴入替罗非班[0.1μg/（kg·min）]12 h;对照组为单纯血栓抽吸组（50例）。观察两组术前TIMI血流分级、MBG分级,术后TIMI血流分级及MBG分级增加值、手术时间以及ST段完全回落率、CK-MB和TnT峰值、左心室射血分数、临床终点事件和出血事件。结果治疗后观察组TIMI血流分级及MBG分级增加值较对照组明显改善（P＜0.05）;术后心电图ST段完全回落率、PCI治疗后16 h及3个月超声心动图LVEF值显著高于对照组（P＜0.05）;CK-MB和TNT峰值明显低于对照组（P＜0.05）。观察组在临床终点事件总发生率方面明显低于对照组（P＜0.05）,而两组在出血并发症方面差异无统计学意义。结论PCI联合应用血栓抽吸和经指引导管在梗死相关动脉内应用替罗非班可以改善心肌灌注,安全有效。     

急性冠脉综合征患者介入应用替罗非班对冠脉血流和心肌灌注的影响

目的观察急性冠脉综合征患者介入治疗中应用替罗非班对冠脉血流的影响。方法接受经皮冠状动脉介入治疗(PCI)急性冠脉综合征患者共82例,分为替罗非班组42例(替罗非班+介入治疗),对照组40例(介入治疗),观察两组患者冠状动脉血流指标如TIMI血流分级、校正的TIMI计帧数(CTFC)、TIMI心肌灌注分级(TMPG)的差别。结果替罗非班组TIMI血流分级、TIMI计帧、TIMI灌注分级均明显优于对照组(P<0.05)。结论急性冠脉综合征患者介入治疗中应用替罗非班可以改善冠脉血流及心肌灌注。     

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。     

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。     

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.     

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。     

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.     

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.     

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.     

Chondroprotective Effects of Wogonin in Experimental Models of Osteoarthritis in vitro and in vivo

We evaluated the chondroprotective effects of wogonin by investigating its effects on the gene expression and production of matrix metalloproteinase-3 (MMP-3) in primary cultured rabbit articular chondrocytes, as well as on production of MMP-3 in the rat knee. Rabbit articular chondrocytes were cultured in a monolayer, and RT-PCR was used to measure interleukin-1β (IL-1β)-induced expression of MMP-3, MMP-1, MMP-13, a disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4), and type II collagen. In rabbit articular chondrocytes, the effects of wogonin on IL-1β-induced production and proteolytic activity of MMP-3 were investigated using western blot analysis and casein zymography, respectively. The effect of wogonin on MMP-3 protein production was also examined in vivo. In rabbit articular chondrocytes, wogonin inhibited the expression of MMP-3, MMP-1, MMP-13, and ADAMTS-4, but increased expression of type II collagen. Furthermore, wogonin inhibited the production and proteolytic activity of MMP-3 in vitro, and inhibited production of MMP-3 protein in vivo. These results suggest that wogonin can regulate the gene expression and production of MMP-3, by directly acting on articular chondrocytes.