替格瑞洛对PCI术后氯吡格雷抵抗患者血小板聚集率的影响

目的探讨对经皮冠状动脉介入(PCI)治疗术后氯吡格雷抵抗的患者以替格瑞洛替换氯吡格雷治疗后血小板聚集率的变化。方法用比浊法测定血小板聚集率,筛选出PCI术后氯吡格雷抵抗患者50例,将氯吡格雷(75 mg/d)替换为替格瑞洛(90 mg,2次/d),观察血小板聚集率变化及主要不良心血管事件和出血情况。结果所有患者在替格瑞洛服用后7、30、90 d与服用前相比,血小板聚集率均明显下降,差异有统计学意义(P<0.05)。治疗期间无主要不良心血管事件及严重出血事件发生。结论对于氯吡格雷抵抗患者,替格瑞洛能明显降低血小板聚集率,疗效确切,安全性好。     

分站式杂交冠状动脉血运重建术后替格瑞洛和氯吡格雷抗血小板聚集疗效与安全性的比较

目的比较分站式杂交冠状动脉血运重建术(HCR)后应用替格瑞洛或氯吡格雷抗血小板聚集的疗效与安全性。方法采用前瞻性随机对照研究方法, 根据术后抗血小板治疗方案将在我院接受分站式HCR治疗的冠状动脉多支病变患者分为替格瑞洛组(术后予阿司匹林肠溶片100 mg口服、1次/d, 替格瑞洛片90 mg口服、2次/d, 连续服用1年)与氯吡格雷组(术后予阿司匹林肠溶片100 mg口服、1次/d, 硫酸氢氯吡格雷片75 mg、1次/d, 连续服用1年)。分析比较2组患者一般情况、手术前后不同时点血小板聚集功能[血小板最大聚集率(MPAR)、P2Y12反应单位(PRU)], 术后血小板抑制率[阿司匹林抵抗(AA)、替格瑞洛或氯吡格雷抵抗(ADP)], 主要心血管不良事件(MACE)、出血事件和不良反应发生情况。结果纳入本研究的患者共124例, 替格瑞洛组和氯吡格雷组各62例, 2组患者基线资料(性别、年龄、纽约心脏病协会心功能分级、合并疾病等)的差异均无统计学意义(均P>0.05)。替格瑞洛组和氯吡格雷组术后24 h、7 d、1个月MPAR均低于术前[(50±9)%、(36±8)%、(29±6)...     

替格瑞洛对急性冠脉综合征经皮冠状动脉介入治疗围术期血小板聚集率的影响

目的 探讨替格瑞洛对急性冠脉综合征(ACS)经皮冠状动脉介入治疗(PCI)围术期血小板聚集率(MPAR)的影响.方法 80例确诊为ACS行PCI术患者为研究对象,术前采用随机数字表法分为替格瑞洛治疗组(观察组)和氯吡格雷治疗组(对照组),每组40例.所有研究对象入院前已连续服用氯吡格雷(泰嘉) 75 mg·d-1持续7 d以上者维持原剂量,未曾服用过氯吡格雷者予以300 mg负荷剂量后75 mg·d-1维持.观察组入院前已连续服用替格瑞洛每次90 mg,2次/天,持续7 d以上者维持原剂量,未曾服用过替格瑞洛者予以180 mg负荷剂量后改标准剂量替格瑞洛(每次90 mg,2次/天)治疗.分别于治疗前、术后5 d抽取空腹外周血标本进行MPAR的测定.结果 治疗前观察组和对照组患者MPAR比较,差异无统计学意义 (P>0.05);术后5 d外周血MPAR均明显低于治疗前(P<0.05);观察组MPAR明显低于对照组(P<0.05).结论 替格瑞洛较氯吡格雷能更好地抑制ACS血管病变患者PCI围术期MPAR,降低早中期不良心血管事件的发生率,对重度冠状动脉血管病变的患者具有更好抗血小板聚集的治疗效果.     

硫酸氢氯吡格雷与替格瑞洛治疗急性冠状动脉综合征患者的临床研究

目的 观察硫酸氢氯吡格雷与替格瑞洛治疗急性冠状动脉综合征的临床疗效及对患者血脂的影响。方法 经皮冠状动脉介入术的急性冠状动脉综合征患者按照抗血小板聚集药物的不同,将其分为氯吡格雷组和替格瑞洛组。氯吡格雷组给予硫酸氢氯吡格雷片75 mg,阿托伐他汀钙片20 mg,阿司匹林肠溶片100 mg,每日1次,口服;替格瑞洛组给予阿托伐他汀钙片20 mg,每日1次,阿司匹林肠溶片100 mg,每日1次,替格瑞洛片90 mg,每日2次,口服。2组均连续治疗1个月。比较2组患者的临床疗效、中性粒细胞/淋巴细胞比(NLR)、低密度脂蛋白胆固醇(LDL-C)、血小板最大聚集率以及药物不良反应发生情况。结果 氯吡格雷组144例和替格瑞洛组145例。替格瑞洛组治疗后总有效率为86.90%,高于氯吡格雷组的75.00%,差异有统计学意义(P<0.05)。治疗后,氯吡格雷组和替格瑞洛组的NLR水平分别为3.26±0.15和3.10±0.11;LDL-C水平分别为(2.24±0.14)和(1.77±0.16)mmol·L^-1,差异有统计学意义(P<0.05)。氯吡格雷组患者在术后2...     

替格瑞洛用于氯吡格雷抵抗急性心肌梗死患者PCI术后抗血小板治疗中的效果分析

目的:探讨替格瑞洛用于氯吡格雷抵抗急性心肌梗死(AMI)患者PCI术后抗血小板治疗的效果.方法:选取2015年1月~2016年1月收治的氯吡格雷抵抗AMI患者88例,随机分为两组各44例,均行PCI手术,对照组同时服用氯吡格雷,观察组给予替格瑞洛.结果:观察组术后2h、1d、7d各时间点血小板聚集率(49.78±6.82,45.53±6.25,39.85±5.82)均低于对照组(57.77±6.72,54.82±5.92,49.64±7.52)(P<0.05);观察组术后谷草转氨酶(27.63±4.82IU/L)、血肌酐(122.94±6.35μmol/L)高于对照组(24.24±4.76IU/L,110.53±6.83μmol/L)(P<0.05);观察组不良反应发生率(15.91%)高于对照组(4.55%)(P<0.05);观察组不良心脑血管事件发生率(4.55%)低于对照组(18.18%)(P<0.05).结论:替格瑞洛用于氯吡格雷抵抗AMI患者PCI术后抗血小板治疗效果显著,但对肝肾功能有一定影响.     

氯吡格雷抵抗患者应用替格瑞洛治疗的血小板凝集状况分析

目的：对氯吡格雷抵抗患者应用替格瑞洛治疗的血小板凝集状况研究分析。方法：对2015年1月～2016年12月在我院行经皮冠状动脉介入治疗术的540例患者进行血小板聚集率的测定,筛选出氯吡格雷抵抗患者97例,随机分为对照组（48例）、观察组（49例）,观察组改用替格瑞洛进行治疗,对照组继续进行氯吡格雷治疗,对比分析两组治疗前后的血小板聚集率。结果：观察组经替格瑞洛治疗后血小板聚集率降低值高于对照组（P<0.05）,观察组的血小板聚集率达标率（83.7%）高于对照组（4.2%,P<0.05）。结论：用替格瑞洛治疗PCI术后氯吡格雷抵抗,可增加血小板抑制率,降低血小板聚集率,出血事件并未显著增加,所以,替格瑞洛是氯吡格雷抵抗患者进行抗血小板治疗的选择之一。     

血栓弹力图评价替格瑞洛对氯吡格雷低反应患者血小板抑制的影响

目的探讨经皮冠状动脉介入(PCI)术后,经血栓弹力图(TEG)检测的氯吡格雷药物低反应患者,换用替格瑞洛治疗后的血小板抑制情况。方法因冠心病不稳定型心绞痛行PCI术的患者常规氯吡格雷联合阿司匹林抗栓,经TEG筛选出53例氯吡格雷抑制不敏感、阿司匹林抑制正常的患者,换用替格瑞洛联合阿司匹林治疗。使用TEG比较换药前后花生四烯酸(AA)诱导的血小板抑制率及二磷酸腺苷(ADP)诱导的血小板抑制率。结果经TEG检测的氯吡格雷药物低反应患者,在换用替格瑞洛后,由ADP诱导的血小板抑制率明显升高[(41±8)%与(70±11)%],差异有统计学意义(P<0.01)。换用替格瑞洛前后由AA诱导的血小板抑制率变化差异无统计学意义(P>0.05)。结论对于血小板高反应性的患者,每天75mg氯吡格雷不能满足血小板抑制效果,换用替格瑞洛能够有效减低药物低反应的发生率,明显改善血小板抑制效果。     

冠状动脉支架术后氯吡格雷抵抗患者抗血小板治疗的效果

目的探讨冠状动脉支架术后氯吡格雷抵抗患者抗血小板治疗的效果。方法对92例实施冠状动脉支架术患者进行分析,其经血栓弹力图检查确诊为氯吡格雷抵抗;随机抛掷硬币将患者分为对照组(n=46)与观察组(n=46);对照组采用氯吡格雷+阿司匹林治疗、观察组采用替格瑞洛+阿司匹林治疗,分析两组的临床效果。结果术后1、3、6、8个月两组患者的血小板聚集率均在下降且观察组术后各阶段的血小板聚集率均低于对照组(P <0.05);观察组的不良事件发生率为4.3%,对照组的不良事件发生率为21.7%(P <0.05)。结论在冠状动脉支架术后氯吡格雷抵抗患者的治疗中采用替格瑞洛来替代氯吡格雷,具有降低血小板聚集率与将心脏不良事件发生率的作用。     

服用氯吡格雷或替格瑞洛患者的血小板最大聚集率差异研究

摘 要 目的：研究经皮冠脉介入术（PCI）后服用氯吡格雷的患者与服用替格瑞洛的患者血小板最大聚集率（MAR）的差异和出血情况,为临床使用抗血小板药物提供参考。方法: 选取因急性冠状动脉综合征(ACS)入院行PCI后服用氯吡格雷或者替格瑞洛的患者,在出院前对其MAR值进行检测,随访3个月内出血事件的发生情况,并比较两组患者MAR值以及随访结果的差异。结果: 服用氯吡格雷的患者出院时MAR为（51.1±13.7）%（n=76）,服用替格瑞洛的患者MAR为（32.6±15.7）%（n=76）,两组差异有统计学意义（P<0.001）。随访结果显示氯吡格雷组出血事件低于替格瑞洛组（P<0.05）。结论: 服用替格瑞洛的患者出院后出血的倾向可能比服用氯吡格雷的患者更大。     

急性冠状动脉综合征患者PCI术后抗血小板治疗的药物经济学评价

摘要：目的:从医疗服务角度,对急性冠状动脉综合征(ACS)患者行经皮冠状动脉介入治疗(PCI)术后两种抗血小板药物治疗方案进行经济学评价。方法:两种治疗方案为在使用阿司匹林基础上,经验性给予国产氯吡格雷,或经验性给予替格瑞洛,由此建立决策树及Markov模型并进行成本-效果分析,评价中国ACS患者PCI术后使用氯吡格雷和替格瑞洛的成本-效果。结果:经验性给予国产氯吡格雷联合阿司匹林治疗方案为成本最低方案,但直接给予替格瑞洛联合阿司匹林治疗方案具有较好的成本-效果。结论:对于PCI术后的ACS患者抗血小板治疗,最推荐直接采用替格瑞洛联合阿司匹林的治疗方案。     

吡喹酮对日本血吸虫雄虫的Ca~(2 ),Mg~(2 ),K~ 与Na~ 的含量及~(45)Ca~(2 )在虫体内分布的影响

日本血吸虫雄虫在4℃或37℃的HBS及无~(45)Ca~(2α)的HBS中经吡喹酮1或30μg/ml作用0.5～2h后,未见虫的Ca~(2 ),Mg~(2 )含量有明显变化,但除4℃的HBS组外,余2组虫的K~ 含量明显减少,而虫的Na~ 含量的增加则不明显。在含30 mM Mg~(2 )的HBS中,雄虫经吡喹酮作用1h后,虫的Mg~(2 )含量明显增加。在37℃的HBS中,血吸虫雄虫经吡喹酮1μg/ml作用5～60min后,虫的皮层胞质中的~(45)Ca~(2α)含量的百分比较各相应对照组的明显减少,而虫体肌肉的则相反。在4℃的HBS或无~(45)Ca~(2α)的HBS中,吡喹酮对~(45)Ca~(2α)在虫体内的分布无明显影响。     

Theoretical π-π* absorption and circular dichroic spectra of cyclic dipeptides

The dipole interaction model, treated by the partially dispersive normal mode method, is used to calculate circular dichroic spectra of cyclo(Gly-Gly), cyclo (Ala-Gly), cyclo(Ala-Ala), cyclo(Pro-Gly), cyclo(Pro-Ala), cyclo(Pro-Val), cyclo (Pro-D-Val), and cyclo(Pro-Pro) in the amide π-π* absorption band near 190 nm. Assuming a standard backbone geometry, spectra which are in fair to good agreement wth experiment are obtained for these molecules. The spectra are predicted to be sensitive to conformations of Pro and Val side chains. The effects of dipeptide ring folding on calculated CD spectra are mostly consistent with those found by other workers, except that it is found that a planar ring conformation of cyclo (Ala-Ala) and cyclo (Ala-Gly) gives predicted spectra comparable to experiment. The same model gives theoretical absorption spectra consistent with available experimental data.     

Dinoflagellate polyether within the yessotoxin, pectenotoxin and okadaic acid toxin groups: Characterization, analysis and human health implications

Diarrhetic Shellfish Poisoning (DSP) is a specific type of food poisoning, characterized by severe gastrointestinal illness due to the ingestion of filter feeding bivalves contaminated with a specific suite of toxins. It is known that the problem is worldwide and three chemically different groups of toxins have been historically associated with DSP syndrome: okadaic acid (OA) and dinophysistoxins (DTXs), pectenotoxins (PTXs) and yessotoxins (YTXs). PTXs and YTXs have been considered as DSP toxins because they can be detected with the bioassays used for the toxins of the okadaic acid group, but diarrhegenic effects have only been proven for OA and DTXs. Whereas, some PTXs causes liver necrosis and YTXs damages cardiac muscle after intraperitoneal injection into mice. On the other hand, azaspiracids (AZAs) have never been included in the DSP group, but they cause diarrhoea in humans. This review summarizes the origin, characterization, structure, activity, mechanism of action, clinical symptoms, method for analysis, potential risk, regulation and perspectives of DSP and associated toxins produced by marine dinoflagellates.     

联合检测血清Hcy和Lp (a)与UA对冠心病患者预后评估的价值探讨

目的 探讨血清同型半胱氨酸(Hcy)、脂蛋白a[Lp(a)]和尿酸(UA)联合检测对冠状动脉粥样硬化性心脏病(CHD)的病情及预后的评估价值.方法 选取CHD患者96例(疾病组)和体检健康者50例(正常组),采集清晨空腹静脉血,检测血清Hcy、Lp(a)和UA.观察组(疾病组)随访1年,91例病情缓解或无进展,5例发展为急性心肌梗死(AMI).采用受试者工作特征曲线分析血清Hcy、Lp(a)和UA单独及联合检测对CHD患者预后的诊断价值.结果 疾病组血清Hcy、Lp(a)和UA水平均高于正常组(均P＜ 0.05);随访发展为AMI患者入院时血清Hcy、Lp(a)和UA水平均高于病情缓解或无进展者(均P＜ 0.01).Hcy、Lp(a)和UA联合检测对CHD患者预后评估的AUC为0.855、敏感性为89.4％、特异性为80.2％、阳性预测值86.4％,均高于3项单独检测.结论 冠状动脉粥样硬化性心脏病患者血清Hcy、Lp (a)和UA水平均升高,其水平变化可反映冠状动脉粥样硬化性心脏病病情,三者联合检测可提高对患者预后的判断价值.     

Protective role of exogenous α-lipoic acid (ALA) on hippocampal antioxidant status and memory function in rat pups exposed to sodium arsenite during the early post-natal period

The present work focussed on the effect of exogenous α-lipoic acid (ALA) administration on retention memory and oxidative stress markers in the hippocampus subsequent to early post-natal exposure of rat pups to sodium arsenite (NaAsO₂). Wistar rat pups were divided into the control groups receiving either no treatment (Ia) or distilled water by intraperitoneal route (i.p.) (Ib) and the experimental groups receiving either NaAsO₂ alone (1.5 and 2.0?mg/kg body wt.) (IIa, IIb) or NaAsO₂ (1.5 and 2.0?mg/kg body wt.) followed by ALA (70?mg/kg body wt.) (IIIa, IIIb) (i.p.) from post-natal day (PND) 4–15. The initial and retention transfer latency (ITL and RTL) was determined on PND 14 and 15 using elevated plus maze. The animals were sacrificed by cervical decapitation (PND 16) and the brains were obtained. The dissected out hippocampus was processed for estimation of oxidative stress markers, glutathione (GSH), and superoxide dismutase (SOD). NaAsO₂ exposure resulted in longer RTL in animal groups IIa and IIb, thereby suggestive of arsenic-induced impairment in retention memory. RTL was significantly shorter in animal groups (IIIa, IIIb) receiving ALA following NaAsO₂, thereby suggestive of improvement in retention memory. GSH and SOD levels were significantly decreased in animals receiving NaAsO₂ alone as against group Ib and administration of ALA following NaAsO₂ increased the levels of hippocampal GSH and SOD. These observations are suggestive of the role of exogenous ALA in ameliorating the adverse effects induced by NaAsO₂ exposure of rat pups on retention memory and oxidative stress markers.     

商陆皂甙甲抑制大鼠腹腔巨噬细胞释放血小板活化因子

卡西霉素(A_(23187))刺激大鼠腹腔巨噬细胞释放血小板活化因子(PAF),用洗涤血小板聚集的方法测定,证明商陆皂甙甲在0.1～100μmol/L浓度范围内及所试的时间范围内,呈剂量及时间依赖性抑制大鼠腹腔巨噬细胞释放PAF:商陆皂甙甲可能就是通过抑制体内PAF生成而起抗炎作用的。     

反相高效液相色谱法测定藿香正气胶囊中厚朴酚及和厚朴酚的含量

目的 建立藿香正气胶囊中厚朴酚及和厚朴酚的含量测定方法。方法 反相高效液相色谱法测定藿香正气胶囊中厚朴酚及和厚朴酚的含量。选用ODS hypersil C—18反相色谱柱：以甲醇-乙腈-水（5：2：4）为流动相;检测波长294nm。结果 此方法线性关系良好（r=1．000）,平均回收率99．95％。结论 此方法简便,快速,准确,可用于藿香正气胶囊中厚朴酚及和厚朴酚的含量测定。     

Pharmacology of (S)-homoquisqualic acid and (S)-2-amino-5-phosphonopentanoic acid [(S)-AP5] at cloned metabotropic glutamate receptors

1. In this study we have determined the pharmacological profile of (S)-quisqualic acid, (S)-2-amino-4-phosphonobutyric acid ((S)-AP4) and their higher homologues (S)-homoquisqualic acid, (S)-2-amino-5-phosphonopentanoic acid ((S)-AP5), respectively, and (R)-AP5 at subtypes of metabotropic (S)-glutamic acid (mGlu) receptors expressed in Chinese hamster ovary cells.
2. (S)-Quisqualic acid was a potent mGlu₁/mGlu₅ agonist (EC₅₀ values of 1.1 μM and 0.055 μM, respectively) showing no activity at mGlu₂ and weak agonism at mGlu₄ (EC₅₀∼1000 μM).
3. (S)-Homoquisqualic acid displayed competitive antagonism at mGlu₁ (K_B=184 μM) and full agonism at mGlu₅ (EC₅₀=36 μM) and mGlu₂ (EC₅₀=23 μM), but was inactive at mGlu₄.
4. (S)-AP4 was a potent and selective mGlu₄ agonist (EC₅₀=0.91 μM) being inactive at mGlu₁, mGlu₂ and mGlu₅ both as agonist and antagonist.
5. (S)-AP5 displayed very weak agonist activity at mGlu₄. At the mGlu₂ receptor subtype (S)-AP5 acted as a competitive antagonist (K_B=205 μM), whereas the compound was inactive at mGlu₁ and mGlu₅. (R)-AP5 was inactive at all mGlu receptor subtypes tested both as agonist and antagonist.
6. These studies demonstrate that incorporation of an additional carbon atom into the backbone of (S)-glutamic acid and its analogues, to give the corresponding homologues, and replacement of the terminal carboxyl groups by isosteric acidic groups have profound effects on the pharmacological profiles at mGlu receptor subtypes. Furthermore, (S)-homoquisqualic acid has been shown to be a potentially useful tool for differentiating mGlu₁ and mGlu₅.

     

扇贝裙边糖胺聚糖对OX-LDL致血管内皮细胞损伤的保护作用

目的　研究扇贝裙边提取物糖胺聚糖 (SS GAG)对血管内皮细胞的保护作用 ,进而探讨其抗动脉粥样硬化 (AS)作用机制。方法　本研究采用氧化低密度脂蛋白 (OX LDL)建立体外培养的人脐静脉血管内皮细胞株 (HUVEC ,CRL 2 4 80 )损伤模型 ,用MTT法和化学方法分别从细胞和分子水平观察SS GAG对血管内皮细胞增殖活性及细胞内一氧化氮 (NO)水平和内皮型一氧化氮合酶 (eNOS)活性的影响。结果　OX LDL能明显抑制血管内皮细胞的增殖活性 (P <0 0 1) ,降低血管内皮细胞内NO水平及eNOS的活性 (P <0 0 1) ;用SS GAG(终浓度为 5 0 ,10 0 ,2 0 0mg·L-1)预处理后 ,能逆转上述效应 (P <0 0 1)。结论　OX LDL抑制血管内皮细胞的增殖 ,降低内皮型eNOS的活性 ,减少细胞内NO的生成 ;SS GAG对血管内皮细胞的脂质过氧化物损伤有保护作用。     

油茶皂苷抗心肌缺血大鼠氧自由基和脂质过氧化作用

目的　以皮下注射异丙肾上腺素 (ISO)诱发大鼠心肌损伤为模型 ,观察油茶皂苷 (SQS)对心肌线粒体MDA含量、SOD、GSH Px活性的影响。方法　实验分生理盐水组 (NS组 )、ISO诱发损伤组 (I/R组 )、SQSⅠ组 (I/R +SQS 0 1mg·kg-1)和SQSⅡ组 (I/R +SQS 0 2mg·kg-1)。从阴茎静脉注射各被试药物或NS ,每天 1次 ,连续 3d。末次给药后取心肌组织行上述指标的测定。结果　I/R组MDA含量明显升高、SOD及GSH Px活性显著降低 ;SQS能对抗ISO所致上述指标的改变 ,且呈剂量依赖关系。结论　SQS具有抗ISO所致大鼠心肌缺血时氧自由基和脂质过氧化作用