Heart failure: Effects of beta receptor antagonists on left ventricular function in patients with clinical evidence of heart failure after myocardial infarction. A double-blind comparison of metoprolol and xamoterol Echocardiographic results from the Metoprolol and Xamoterol Infarction Study (MEXIS)

Two hundred and ten patients with clinical evidence of heartfailure, developing after an acute myocardial infarction, wererandomized to treatment with the ß₁ antagonist metoprolol50–100mg b.i.d. (n=106) or the ß₁ partial agonistxamoterol 100–200 mg bid. (n=104). Left ventricular systolicand diastolic function were assessed with echocardiography andtransmitral Doppler cardiography before and after 3 and 12 monthsof double-blind treatment. E-point septal separation and percent left ventricular fractional shortening were used as indicesof systolic function. The ratio between peak early and latemitral diastolic flow (E/A ratio) and isovolumic relaxationtime were used as indices of diastolic function. In the xamoterol group, there was a deterioration in E-pointseptal separation (P<0·05). A difference between thetreatment groups was present both at 3 months (E-point septalseparation 11·4 vs 13·0 mm, P<0·0l,fractional short ening 271 vs 252%, P<005) and 12 months(E-point septal separation Ill vs 13·2 mm, P<0·05fractional shortening 26·9 vs 25·0%, P<0·05).E/A ratio increased in the metoprolol group (P<0·05)but not in the xamoterol group. At 3 months there was a significantdifference (0·85 vs 0·67, P<0·005 betweenthe groups but not at 12 months. In comparison with the ß₁-receptor antagonist metoprolol,the ß₁ partial agonist xamoterol impaired left ventricularsystolic function in patients with clinical evidence of heartfailure after an acute myocardial infarction.     

乌苯美司的药物动力学及对实验性肿瘤转移的治疗作用

目的：探讨乌苯美司对小鼠药物动力学及与实验性肿瘤转移治疗活性间的关系。方法：用放射免疫法测定小鼠在不同给药途径下的乌苯美司血清药物动力学及观察乌苯美司对黑色素瘤肺转移模型的治疗活性。结果：乌苯美司ｉｖ的Ｔ１２较短，初始血药浓度较高。ｉｖ和ｉｍ给药后的曲线下面积较大；ｐｏ及ｉｐ则较小。不同给药途径对实验性肿瘤转移均有治疗作用。结论：乌苯美司的血清Ｔ１２较短，其治疗活性取决于冲击和高剂量的给药方式。     

7β-(6-取代-2-喹诺酮-3-乙酰氨基)头孢菌素的合成

以6-取代-2-喹诺酮-3-乙酸为侧链,用CDI法和潘化酯法与7-ADCA,7-ACA,7-ACT,和7-ACD缩合,合成了16个新的7β-(6-取代-2-喹诺酮-3-乙酰氨基)头孢菌素类化合物,通过溶媒转提,葡聚糖凝胶(Sephadex LH-20)柱层析及离心薄层层析分离精制,得到纯品。初步体外抑菌试验表明:新化合物对革兰氏阳性及某些阴性菌具有高度敏感性。大多数化合物对所试试验菌的抗菌活性与头孢唑啉和青霉素G钠相当,有些比它们还强。     

抗癌药物对心脏毒性反应(附五例报告)

本文报道五例肿瘤患者在用抗癌药的治疗过程中,出现对心脏不同程度的毒性反应,并就有关几种抗癌药物的毒性作用机理及防治进行了讨论。     

抗真菌剂三氮唑含硫化合物的合成

合成了１３个三氮唑含硫化合物，均为未见文献报道的新化合物，对所合成的化合物，选择三种常见真菌进行体外最低抑菌浓度（ＭＩＣ）的测定，结果表明它们均有较好的抗真菌活性，有些化合物抑菌活性极高，有进一步研究和开发前景。     

Topographical analysis of the EEG effects of a subconvulsive dose of lidocaine in healthy volunteers

Background: The purpose of the present study was to assess the effects of intravenous lidocaine on spatial changes of electroen-cephalographic power and on psychomotoric status in conscious volunteers.
Methods: In 11 healthy volunteers lidocaine (2-min bolus, 100 mg; 15-min infusion, 40 μg kg^-1 min^-1) or placebo were given intravenously in a randomized, single-blinded, two-way crossover study. Haemodynamics and lidocaine plasma concentrations were measured at baseline and within a period of 30 min following bolus injection. Vigilance and emotional status were tested using visual analogue scales (VAS). Toxic CNS effects were evaluated by a questionnaire. The raw EEG (17 leads, reference C_z) and computed power spectra were continuously recorded.
Results: The chosen lidocaine dosage led to nearly constant plasma concentrations (unbound lidocaine 2.5 min and 15 min after bolus 0.36±0.14 μg/ml and 0.30±0.06 μg/ml, respectively [mean±SD]). The placebo caused no symptoms, changes in VAS-scores or EEG-parameters. Lidocaine induced pronounced subjective symptoms and significant increases in delta activity for 15 min, most dominant at the frontotemporal and occipital leads (max. +219% O₁). Frontal and occipital beta1 and beta2 power (max. +131% and +124% at O₁, respectively) was immediately increased after the bolus injection. No EEG changes occurred at central region C_z, and no interhemispheric EEG differences were noted. Theta, alphal, and alpha2 power remained unchanged.
Conclusion: The current data demonstrate simultaneous changes in psychomotoric status as well as delta and beta spectral power during lidocaine infusion. These data could be an indication that the pronounced frontotemporal and occipital EEG changes are the electroencephalographic expression of subjective sensations.     

The use of the rat facial nerve model to assess the effect of differing nerve anastomotic agents on the facial nerve

There are relatively few papers which prove that one nerve anastomotic agent for the facial nerve is superior to any other. Previous experiments on the division and anastomosis of the facial nerve have failed to consider the indeterminate variables involved, i.e. operator variability, controls and the reaction of the materials on normal nerve tissue. In this experiment, a variety of anastomotic agents were tested to see if the anastomotic agents themselves affected the extra-temporal facial nerve function. The absorbable suture, non-absorbable suture, glue and tube wrap used had no effect on normal nerve tissue or on the anastomosis of the sectioned facial nerve of the rat compared with simple laying together of the divided ends of the divided nerve.     

芪月降脂片中黄芪甲苷的含量测定

[目的 ]研究芪月降脂片中黄芪甲苷的含量测定方法 .[方法 ]用甲醇提取、水饱和正丁醇萃取、大孔吸附树脂处理供试品后 ,以双波长薄层扫描法测定黄芪甲苷的含量 .[结果 ]黄芪甲苷的平均回收率为 10 4 18% ,RSD为 3 2 5% .[结论 ]双波长薄层扫描法较为简便、经济且重现性较好 ,可用于制剂中黄芪甲苷的质量控制     

新型络合剂对肾镉促排作用及对微量元素影响的观察

为观察新型络合剂Ｇ－Ｃｙｓ－ＤＴＣ、Ｇ－Ｔｈｒ－ＤＴＣ对染毒大鼠肾内蓄积镉的络合促排作用及对肾皮质元素分布的影响，比较促排治疗对肾皮质铁、铜、锌等含量的影响，利用北京正负电子对撞机提供的硬Ｘ射线对肾皮质冰冻切片扫描及原子吸收分光光度法、Ｘ射线荧光测定染毒鼠肾皮质镉及其他元素含量。结果，新型络合剂Ｇ－Ｃｙｓ－ＤＴＣ、Ｇ－Ｔｈｒ－ＤＴＣ能大幅度降低肾内镉负荷。染毒肾皮质中Ｃｄ与Ｓｅ密切相关，而Ｚｎ和Ｓｅ的相关性下降。提示新型络合剂对肾内蓄积镉有较好驱排效果；硒和锌在镉中毒作用机制中可能起一定的保护作用。