Pharmacokinetics of levosimendan and its active metabolite OR-1896 in rapid and slow acetylators.

OBJECTIVE: The purpose of this study was to investigate the pharmacokinetics of levosimendan and to determine the primary pharmacokinetic parameters of the pharmacologically active metabolite OR-1896 in rapid and slow acetylators. METHODS: Levosimendan was administered as a constant rate (0.1 microg/(kg min)) i.v. infusion for 24h in six rapid and six slow acetylators based on N-acetyltransferase 2 genotyping. At the end of the infusion, a small amount (2.5 microg/kg) of (13)C-labeled OR-1896 was administered by i.v. infusion for 10 min. Blood samples were taken at predefined sampling points 14 days post-infusion and levosimendan and its metabolite concentrations were determined by LC-MS/MS. RESULTS: Steady-state concentrations of levosimendan were achieved within 4-8h and no differences were found in the pharmacokinetics of the parent compound between the rapid and slow acetylators. The maximum concentrations of amino phenylpyridazinone metabolite OR-1855 and N-acetylated conjugate OR-1896 were observed approximately 24h after terminating the infusion. AUC of OR-1896 was approximately 3.5 times higher in the rapid acetylators compared to the slow acetylators (P = 0.002, 95% confidence interval for group ratio from 2.0 to 8.2). The mean +/- S.D. fraction of levosimendan metabolized to OR-1896 was 6.8 +/- 2.8% in the rapid and 4.3 +/- 2.4% in the slow acetylators (P = 0.12). (13)C-OR-1855 concentrations were detected in plasma after administration of (13)C-OR-1896 indicating deacetylation from OR-1896 to OR-1855. CONCLUSIONS: Plasma OR-1896 levels during and after levosimendan treatment are dependent on the acetylation status of the subject-rapid acetylators having 3.5 times higher concentrations than slow acetylators.     

丹皮酚的抗炎作用研究

目的：观察二氧化碳（CO2）超临界提取的丹皮酚的抗炎作用。方法：用醋酸导致小鼠腹腔毛细血管通透性增加;用角叉菜胶导致大鼠足跖肿胀。结果：丹皮酚50．0、25．0、12．5mg,／kg灌胃给药,可明显降低小鼠腹腔毛细血管通透性;丹皮酚32.0、16．0、8．0mg,／kg灌胃给药,能显著抑制角叉菜胶所引起的大鼠足肿胀。结论：经CO2超临界提取的丹皮酚具有明显的抗炎作用。     

紫花高乌头总碱对实验性吗啡戒断症状的影响

目的:观察紫花高乌头总碱对吗啡戒断症状的影响。方法:采用剂量递增法复制吗啡依赖小鼠和大鼠模型,注射纳洛酮催促产生戒断症状。结果:紫花高乌头总碱可减少小鼠的跳跃反应,降低大鼠的戒断反应症状分值,不同程度的控制小鼠和大鼠的体重下降。结论:紫花高乌头总碱可抑制吗啡依赖动物的戒断症状。     

分化好的胃肠胰神经内分泌瘤G3的诊治新进展

神经内分泌肿瘤属于少见肿瘤,发病率低,异质性强,可发生于全身多个器官.在中国,胃肠胰是神经内分泌肿瘤发病率最高的部位,自2017年世界卫生组织(World Health Organization,WHO)消化系统肿瘤病理学分类关于胃肠胰神经内分泌肿瘤提出分化好的神经内分泌瘤G3(neuroendocrine tumor...     

慢性阻塞性肺疾病合并Ⅱ型呼吸衰竭并发上消化道出血的诱发因素分析

目的探讨慢性阻塞性肺疾病（COPD）合并Ⅱ型呼吸衰竭并发上消化道出血的诱发因素,分析总结其临床特征。方法选择2008年2月至2011年10月收治的43例COP]）合并Ⅱ型呼吸衰竭并发上消化道出血患者作为观察组,另同期随机选择40例未并发上消化道出血的COPD合并Ⅱ型呼吸衰竭患者作为对照组。观察比较两组患者血气分析结果及诱发因素,分析其并发上消化道出血的原因。结果观察组pH值和动脉血氧分压明显低于对照组,动脉血二氧化碳分压明显高于对照组,差异均有统计学意义（P〈0．05）;观察组因肝肾功能损害、重症感染、全身激素使用而发生上消化道出血的发生率均高于对照组．差异均有统计学意义（P〈0．05）。结论COPD合并Ⅱ型呼吸衰竭并发上消化道出血与低氧血症、高碳酸血症、重症感染及应用损害胃肠黏膜药物等因素有密切关系,且以低氧血症、高碳酸血症为主要因素,需尽早干预。     

Rosiglitazone treatment alleviates inflammation and improves liver function in overweight women with polycystic ovary syndrome: a randomized placebo-controlled study

In a randomized, placebo-controlled study, we studied the effects of 4 months' treatment with rosiglitazone on low-grade inflammation, liver function, lipid levels, and blood pressure in 30 overweight women with polycystic ovary syndrome. Rosiglitazone significantly decreased serum C-reactive protein levels, white blood cell count, and alanine aminotransferase enzyme activity but did not affect lipid or blood pressure levels. Placebo had no effect on any parameters.     

如何做好腹腔镜下胃癌根治手术：iFIST理念

腹腔镜胃癌根治手术自开创至今已经历20余年的发展,随着微创外科理念的不断深入及腹腔镜器械的不断革新,腹腔镜胃癌手术在世界范围已广泛开展。我国虽起步较晚,也取得了长足进步,但腹腔镜胃癌手术的技术水平仍良莠不齐,严重影响临床疗效。笔者就如何做好腹腔镜下胃癌根治术作一概述。提出iFIST理念,即：严格适应证、干净无血术野、腹腔充分灌洗、标本完整、全腹腔镜下手术。     

Osteoarthritis of finger joints in Finns aged 30 or over: prevalence,determinants, and association with mortality

BACKGROUND: Prevalence and risk factors of osteoarthritis (OA) in finger joints have been amply explored in previous studies. However, no study has focused on finger joint OA as a predictor of mortality. OBJECTIVE: To investigate finger joint OA for its associations with alleged risk factors and with life expectancy in an extensive health survey. METHODS: From 1978 to 1980 a representative population sample of 8000 Finns aged 30 years or over was invited to participate in a comprehensive health examination; 90% accepted. Hand radiographs were taken from 3595 subjects. By the end of 1994, 897 of these had died. RESULTS: The prevalence of OA of Kellgren's grade 2 to 4 in any finger joint and in at least two symmetrical pairs of distal interphalangeal joints (DIPs) was 44.8% and 16.0%, respectively. Age and body mass index were significant determinants for OA both in any finger joint and in symmetrical DIP OA. The history of physical workload in women showed a positive association with OA in any finger joint. Smoking in men seemed to protect against symmetrical DIP OA. As adjusted for the determinants above, symmetrical DIP OA predicted mortality in women (relative risk (RR), 1.23; 95% confidence interval (95% CI) 1.01 to 1.51), but not in men (RR 0.89; 95% CI 0.68 to 1.16). In men, however, OA in any finger joint significantly predicted cardiovascular deaths (RR 1.42; 95% CI 1.05 to 1.92). CONCLUSION: OA in any finger joint and symmetrical DIP OA have different risk factor profiles and predict mortality in different patterns between men and women.     

Homocysteine and major coronary events: a prospective population study amongst women

OBJECTIVES: To study serum homocysteine concentration for its prediction of major coronary heart disease events amongst women. DESIGN: A case-control study nested within a follow-up study. Subjects. A total of 74 and 75 major coronary events (coronary deaths or nonfatal myocardial infarction) which occurred in women with and without known heart disease, respectively, during a 13-year follow-up and two individually matched controls per case. Main outcome measure. Major coronary event. RESULTS: Amongst women with baseline heart disease, the relative risk (95% CI) of such events, adjusted for age, smoking, hypertension, diabetes, serum cholesterol and body mass index, was 3.32 (1.05-10.5) in the highest homocysteine quintile compared with the lowest quintile. Amongst women free of heart disease at baseline, the corresponding relative risk value was 0.77 (0.24-2.45). CONCLUSIONS: This prospective study support the hypothesis that homocysteine is a risk factor for coronary events in women with heart disease.