奈替米星与阿米卡星治疗下呼吸道感染的疗效比较

目的：比较奈替米星（Ｎｅｔ）与阿米卡星（Ａｍｉ）在下呼吸道细菌性感染疾病中的疗效及不良反应。方法：对痰细菌培养有致病菌生长的１６０例患者随机分成２组,分别用Ｎｅｔ３００ｍｇ或Ａｍｉ４００ｍｇ,ｉｖｇｔｔ,ｑｄ,疗程７～１０ｄ结果：Ｎｅｔ组有效率（８７．５％）明显高于Ａｍｉ组（６６．２％）。辅助检查中白细胞及分类恢复正常率、胸片恢复正常率和痰菌转阴率,前组均高于后组,而不良反应发生率前组低于后组。结论：Ｎｅｔ治疗下呼吸道感染的疗效优于Ａｍｉ,且不良反应也较少。     

阿米洛利与氨苯蝶啶治疗原发性高血压545例的比较

对545例轻、中型高血压患者,其中Ⅰ组134例(男88例,女46例;年龄50±9a)采用阿米洛利片5mg/d;Ⅱ组139例(男90例,女49例;年龄51±10a)采用氨苯喋啶片50mg/d;复Ⅰ组159例(男103例,女56例;年龄51±8a)采用复方阿米洛利片1片/d;复Ⅱ组113例(男69例,女44例;年龄51±9a)采用复方氨苯喋啶片1片/d;疗程均2mo。结果:总有效率Ⅰ组优于Ⅱ组(67.2％对49.6％);复Ⅰ组优于复Ⅱ组(83.0％对69.9％);P值均<0.01。     

特布他林加赛庚啶与氨茶碱治疗婴儿气喘和咳嗽的比较

目的：探讨特布他林加赛庚啶对婴儿气喘和咳嗽的疗效，并与氨茶碱作比较。方法：治疗组３１例（男性２１例，女性１０例，年龄１５±ｓ６ｍｏ）采用特布他林０．０６５ｍｇ／（ｋｇ·ｄ），赛庚啶０．２５ｍｇ／（ｋｇ·ｄ），均分为３次口服。对照组２８例（男性１６例，女性１２例，年龄１６±６ｍｏ）用氨茶碱３～５ｍｇ／（ｋｇ·ｄ），分３次口服。２组综合治疗（地塞米松、镇咳药、抗生素、吸氧）大致相仿。结果：２组总显效率分别是５５％和２５％，治疗组止咳平喘作用显著优于对照组（Ｐ＜０．０５）。结论：特布他林加赛庚啶治疗婴儿气喘和咳嗽的安全性强、疗效较好。     

Modification of spatial recognition memory and object discrimination after chronic administration of haloperidol, amitriptyline, sodium valproate or olanzapine in normal and anhedonic rats

In the present study we have investigated the effects of a chronic administration of olanzapine (Ola) on visual and spatial memory in normal and anhedonic rats. The effects of Ola have been compared to those of the typical antipsychotic Hal, the tricyclic antidepressant amitriptyline (Ami), and the mood stabilizer VPA. Anhedonia (assessed by reduction of sucrose preference) was induced by administration of a chronic mild stress (CMS) protocol, in which rats were exposed sequentially, over a period of 4 wk, to a variety of unpredictable mild stressors. The spatial memory was evaluated by testing the ability of the rats to discriminate a familiar vs. a novel environment, while the visual memory was assessed by testing the ability of the rats to discriminate familiar vs. novel objects. In CMS-free rats, VPA (5 or 30 mg/kg.d), Ola (0.02 or 0.1 mg/kg.d), Ami (2 mg/kg.d) and Hal (0.2 mg/kg.d) caused no detectable modifications of visual memory, whereas VPA (5 mg/kg.d), Ami (2 mg/kg.d) and Ola (0.02 mg/kg.d) did not modify spatial memory performance. In our experimental conditions, the administration of the CMS protocol caused an impairment of both visual and spatial memory. The chronic treatment of anhedonic rats with Ola (0.02 mg/kg.d) or Ami (2 mg/kg.d) prevented, at least in part, the stress-induced impairment of visuospatial performance. In conclusion, the results of the present preclinical study seem to indicate that the chronic administration of low doses of Ola or Ami has the potential to lead to substantial cognitive benefits in depressed patients.     

Effects of chronic administration of olanzapine, amitriptyline, haloperidol or sodium valproate in naive and anhedonic rats

Although in bipolar patients the main therapeutic indication of atypical antipsychotics is the management of acute mania, several observations suggest that these agents may exert antidepressant as well as anti-manic effects. The main goal of the present work was to evaluate the putative antidepressant effect of chronic olanzapine (Ola) (0.02-0.1 or 0.5 mg/kg.d), in comparison to haloperidol (Hal) (0.2 mg/kg.d) and sodium valproate (VPA) (5 or 30 mg/kg.d), in rats exposed to a protocol of chronic mild stress. The tricyclic compound amitriptyline (Ami) (5 mg/kg.d) was used as reference drug. The results indicate that Ola, in a rodent model of depression, has protective effects against the stress-induced anhedonia. Compared to Hal and VPA, Ola shows a greater antidepressant activity and is as effective as Ami in preventing the anhedonic state. The effects of Ola and Ami, however, have a different time-course. A full reversion of the anhedonia by Ami appears after a latency of 4 wk, whereas the effect of Ola is already evident 1 wk after the beginning of the chronic treatment. Moreover, the recovery from anhedonia at the end of the stress protocol and after drug cessation was more rapid in groups of rats pretreated with Ola or VPA than in the group of saline-pretreated rats. In conclusion, the results indicate that 0.02 mg/kg.d Ola causes a rapid and sustained antidepressant-like effect, while all other anti-manic treatments show loss of efficacy at 3 wk. Taken together, these observations support the hypothesis that Ola has a broader pharmacotherapeutic profile than solely as an antipsychotic or anti-manic agent.     

Determination of amitriptyline and nortriptyline in human liver microsomes with reversed-phase HPLC in vitro

ＤｅｔｅｒｍｉｎａｔｉｏｎｏｆａｍｉｔｒｉｐｔｙｌｉｎｅａｎｄｎｏｒｔｒｉｐｔｙｌｉｎｅｉｎｈｕｍａｎｌｉｖｅｒｍｉｃｒｏｓｏｍｅｓｗｉｔｈｒｅｖｅｒｓｅｄｐｈａｓｅＨＰＬＣｉｎｖｉｔｒｏ１ＳＨＵＹａｎ，ＺＨＵＲｏｎｇＨｕａ２，ＸＵＺｈｅｎＨｕ...     

反相高压液相色谱法测定体外人肝微粒体孵育液中阿米替林及其代谢 …

AIM: To develop a method for simultaneous determinations of amitriptyline (Ami) and its metabolite nortriptyline (Nor) in human liver microsomes. METHODS: An incubation buffer containing microsomes, NADPH-generating system, and Ami, after termination of enzyme reaction and desipramine (Des) as internal standard (IS), was extracted with diethy ether and separated on a reversed-phase ODS column. Detection was achieved at 242 nm by ultraviolet detector. RESULTS: No potential interfering peaks were found. Ami and Nor gave rapid elution and baseline resolution. The linear curves of both analyses ranged 0.02-10 nmol and the limit of detection was 0.01 nmol. The recovery (94%-101%) had good precision with relative s of < 8.3%. CONCLUSION: This method is rapid, sensitive, and simple for studying the metabolism of Ami and Nor.     

Cytotoxic effects of changrolin, lidocaine and amiodarone on ultrastructure of cultured rat beating cardiac myocytes

Ultrastructural and morphological alterations of cultured rat beating cardiac myocytes treated with changrolin (CRL), lidocaine (Lid), and amiodarone (Ami) were studied. After the cultures were treated with CRL 100 micrograms/ml for 24 h, the beating of the myocytes stopped, the configuration and fine structure were destroyed, while the nuclei showed pyknotic deformation and reduced in size. The membrane and structures of mitochondria were disrupted and myofibrils fragmented and disrupted. In addition, a lot of vacuoles with characteristic dense particles were found in the cytoplasm. Similar alterations were seen when Lid 1000 micrograms/ml and Ami 50 micrograms/ml were added to the cultures. Normal beating networks of myocytes were examined under inverted microscopy after the cultured cells were treated with CRL 25 micrograms/ml, Lid 250 micrograms/ml or Ami 6.25 micrograms/ml. The ultrastructure of some regions of the myocytes showed very slight damage. The results indicated that the dosage of CRL and Lid generally used in anti-arrhythmic therapy basically exerted no harm to myocytes. However, caution should be taken when Ami was given intravenously, since its effective serum concentration was close to the dosage which could cause slight damage to the ultrastructure of cultured cells.     

胺碘铜对快速右心室起搏致心力衰竭犬心室电生理特性的影响

AIM: To study the effects of amiodarone (Ami) on cardiac electrophysiologic properties and ventricular fibrillation threshold (VFT) in right ventricular rapid pacing-induced congestive heart failure (CHF) dogs. METHODS: Dogs (n = 25) were randomly allocated into 3 groups: A) control group; B) CHF group induced by right ventricular rapid pacing (4 pulses.s-1) for 4-5 wk; C) CHF models p Ami 300 mg.d-1 for 4-5 wk. The electrophysiologic parameters and VFT were evaluated by electric stimulation and monophasic action potential (MAP) recording. RESULTS: In CHF models, ventricular MAP duration (MAPD90), ventricular late repolarization duration (VLRD), and intra-ventricular conduction time (IVCT) were prolonged by 43%, 318%, and 19%, respectively; the ratio of ventricular effective refractory period (VERP) to MAPD90 (VERP/ MAPD90) and VFT were decreased by 13% and 48% respectively; the dispersion of ventricular recovery time (RT-D) was increased by 185%. In CHF models, Ami had no effects on ventricular MAPD90, but increased VERP/ MAPD90, IVCT, and VFT by 15%, 10%, and 67%, respectively, shortened VLRD by 87%; and decreased RT-D by 87%. Ami had no significant influences on the hemodynamic parameters of the CHF dogs. CONCLUSION: Ami normalizes the cardiac electrophysiologic properties in CHF dogs.     

胺碘酮对离体心肌的负性肌力作用

对离体左,右心房肌,胺碘酮(Ami)1～100μmol·L~(-1)均有负性肌力作用,30μmol·L~1明显抑制心肌静息后收缩,正阶梯和成对刺激效应,1～10μmol·L~1使苯福林,异丙肾上腺素,组胺和CaCl_2正性肌力作用的量效曲线呈非竞争性拮抗作用,心肌动作电位和收缩力同步记录发现,Ami 30μmol·L~1减弱心肌收缩,延长APD,但对平台期和V_(max)无影响.故Ami的负性肌力作用可能是抑制心肌细胞外Ca~(2+)内流和细胞内Ca~(2+)释放所致,并非选择性阻滞心肌α,β和H_2受体以及电压依赖性钙通道引起 .