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1.
The resolution of (±)-atenolol, (±)-propranolol and (±)-metoprolol into their enantiomers was achieved by TLC on silica-gel plates impregnated with optically pure

-lysine (0.5%) and

-arginine (0.5%) as the chiral selectors. In all cases, different combinations of acetonitrile–methanol solvent systems were found to be successful in resolving these compounds. Spots were detected using iodine vapour. The detection limit for both (±)-atenolol and (±)-propranolol was 2.6 μg and for (±)-metoprolol, it was 0.26 μg.  相似文献   
2.
The enantiomeric separation of metoprolol and its metabolites in human urine was undertaken using capillary electrophoresis (CE). Resolution of the enantiomers was achieved using carboxymethyl-β-cyclodextrin (CM-β-CD) as the chiral selector. A 100-mM acetate buffer (pH 4.0) containing 5% 2-propanol and 10 mM CM-β-CD resulted in the optimum separation of the metoprolol enantiomers and its acidic metabolite in human urine. Following a single metoprolol oral administration of 100 mg racemic metoprolol tartrate, stereoselective pharmacokinetic analysis showed that urinary acidic metabolite 3 of metoprolol accounted for 62.3% of the dose with an R/S ratio of 1.23 and urinary unchanged metoprolol 1 accounted for 6.3% of the dose with an R/S ratio of 0.72.  相似文献   
3.
目的:研究氯沙坦早期联合美托洛尔治疗高龄重症心力衰竭的临床疗效。方法:选取2010年1月至2013年1月本院住院治疗的60例高龄重症心力衰竭患者,采用随机数字表法随机分为氯沙坦联合美托洛尔治疗组、氯沙坦治疗组和对照组,每组患者20例;所有患者均采取常规治疗,对照组加用口服强心剂和利尿剂,氯沙坦治疗组在常规治疗的基础上加用氯沙坦,氯沙坦联合美托洛尔治疗组在常规治疗的基础上加用氯沙坦和美托洛尔,在治疗前及治疗后0.5a、1.0a检测所有患者的心功能、左室射血分数(LVEF)和血液中的B型脑钠肽(BNP),并观察治疗后1.0a的临床疗效。结果:治疗前三组患者的心功能、左室射血分数(LVEF)以及B型脑钠肽(BNP)间均无统计学差异(P0.05);氯沙坦治疗组、氯沙坦联合美托洛尔治疗组治疗后0.5a和1.0a的心功能和BNP均低于对照组(P0.05),而治疗后0.5a和1.0a的LVEF均高于对照组(P0.05);氯沙坦联合美托洛尔治疗组治疗后0.5a的心功能、LVEF以及BNP与氯沙坦治疗组无统计学差异(P0.05),而氯沙坦联合美托洛尔治疗组治疗后1.0a的心功能、LVEF以及BNP与氯沙坦治疗组均存在着统计学差异(P0.05);三组治疗后1.0a死亡率间存在统计学差异(P0.05);每年住院次数和平均住院日最少的是氯沙坦联合美托洛尔治疗组,其次为氯沙坦组。结论:氯沙坦与美托洛尔早期联合治疗高龄重症心力衰竭的疗效优于氯沙坦单独治疗。  相似文献   
4.
目的:观察美托洛尔联合硝酸甘油治疗老年高血压伴左心衰的临床疗效及其对血管内皮生长因子(VEGF),高敏C反应蛋白(hs-CRP)和脑钠素(BNP)的影响。方法:选取2009年6月至2010年12月入住我院的高血压伴急性左心衰患者150例,将其随机分为观察组和对照组,每组各75例。对照组在强心,利尿的基础上予以硝酸甘油治疗;观察组在对照组的基础上予以美托洛尔治疗。观察两组的疗效,血压,心率,血氧饱和度,血浆VEGF,hs-CRP和BNP的表达。结果:观察组的总有效率为94.67%,而对照组的总有效率为80.00%,观察组的总有效率明显高于对照组(P〈0.05)。两组治疗后,收缩压,舒张压,心率,VEGF,hs-CRP和BNP均较治疗前明显降低(P〈0.01),观察组的降低水平较对照组更为明显(P〈0.01);而两组治疗后的血氧饱和度较治疗前明显提高,观察组的提高水平更为明显(P〈0.01)。结论:美托洛尔联合硝酸甘油治疗老年高血压伴左心衰疗效显著,其机理可能与降低血浆中的VEGF,hs-CRP和BNP水平有关。  相似文献   
5.
Earlier studies from the authors' laboratory showed that malnourishment induces alterations in the cardiovascular homeostasis increasing the basal mean arterial pressure and heart rate. In this study, the authors evaluated whether the sympathetic and parasympathetic efferent activities contribute to changes in the cardiovascular homeostasis through altered modulation of the arterial baroreflex of malnourished rats. After weaning, male Fischer rats were given 15% (Normal Protein--NP) or 6% (Low Protein--LP) protein diet for 35 d. The baroreflex gain and latency were evaluated before and after selective autonomic blockades in control and malnourished rats. It was observed that malnourishment affected the baroreflex gain in response to activation and deactivation of the arterial baroreflex. Moreover, malnourished rats showed increased baroreflex latency as compared to that of control rats. Regarding the autonomic efferent activity directed to the heart, the data showed increased sympathetic and decreased parasympathetic efferent activities in malnourished rats, and such alterations could be related to the observed changes in the arterial baroreflex gain as well as in the basal mean arterial pressure and heart rate.  相似文献   
6.
The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing metoprolol tartrate (MT) as a model drug by the optimization technique. A 23 factorial design was employed in formulating the GFDDS with total polymer content-to-drug ratio (X1), polymer-to-polymer ratio (X2), and different viscosity grades of hydroxypropyl methyl cellulose (HPMC) (X3) as independent variables. Four dependent variables were considered: percentage of MT release at 8 hours, T50%, diffusion coefficient, and floating time. The main effect and interaction terms were quantitatively evaluated using a mathematical model. The results indicate that X1 and X2 significantly affected the floating time and release properties, but the effect of different viscosity grades of HPMC (K4M and K10M) was nonsignificant. Regression analysis and numerical optimization were performed to identify the best formulation. Fickian release transport was confirmed as the release mechanism from the optimized formulation. The predicted values agreed well with the experimental values, and the results demonstrate the feasibility of the model in the development of GFDDS.  相似文献   
7.
This study investigated (i) blood pressure (BP), heart rate (HR), and their relation to urinary NOx and eNOS protein expression in male and female spontaneously hypertensive rats (SHR), as well as (ii) gender‐dependent cardiovascular effects of nebivolol (NEB) in comparison to metoprolol (MET) in SHR. BP and HR were measured telemetrically after a single intraperitoneal application of NEB or MET at 07.00 and 19.00 h in male rats and at 19.00 h in proestrus female rats. The two β‐blockers varied in time of decreasing BP and HR and also in duration. In males, MET decreased BP and HR for few hours exclusively when applied at the onset of the activity phase (i.e., at 19.00 h), while after its application at 07.00 h, BP and HR were unchanged. In females, MET also caused a short‐lasting BP and HR reduction, with the effect being more pronounced than in males. In males, NEB at either dosing time decreased HR and BP to a greater extent than did MET. This effect was evident both during the activity and rest periods and persisted for at least five days. In females, NEB provoked a similar, but more pronounced, effect on BP and HR in comparison to males. These findings demonstrate that significant gender‐dependent differences in the circadian profile of BP and HR exist. BP and urinary NOx as well as eNOS expression are inversely correlated, and the cardiovascular effects of NEB and MET vary, depending on the time of application as well as gender.  相似文献   
8.
目的:研究早期足量应用美托洛尔对急性心肌梗死的疗效及安全性.方法:将40例AMI患者随机分为治疗组和对照组.治疗组静脉缓慢注射美托洛尔15mg后予关托洛尔150-200mg/d口服;对照组按常规剂量给予美托洛尔25-50mg/d口服.其它治疗相同,两组治疗4周.比较两组治疗后QTcd、心律失常发生的种类、心肌耗氧指数、梗死后心绞痛、梗死延展的发生率和心功能的变化.结果:治疗组QTcd、室性心律失常发生率、心肌耗氧指数、梗死后心绞痛和梗死延展的发生率均低于对照组(P<0.05).心功能两组无显著性差异.结论,AMI患者早期足量使用美托洛尔可以从多方面获益,安全性高.  相似文献   
9.
目的:观察氨氯地平联合美托洛尔治疗高血压的临床效果及安全性。方法:对2012年4月至2012年11月期间在我科住院治疗的102例患者随机分成两组,对照组接受氨氯地平治疗,治疗组在对照组的基础上使用美托洛尔治疗,分析比较两组的疗效。结果:治疗组和对照组的血压以及心率较治疗前明显降低,差异有统计学意义(P〈0.01);治疗组治疗后的舒张压与对照组治疗后的舒张压相比,差异有统计学意思(P〈0.01);治疗组的总有效率高于对照组(P〈0.05);治疗组的副反应低于对照组(P〈0.05)。结论:氨氯地平联合美托洛尔治疗高血压效果显著,优于单纯应用氨氯地平。  相似文献   
10.
胡玉海 《蛇志》2016,(4):428-429
目的分析普罗帕酮联合美托洛尔治疗小儿心律失常的临床疗效。方法将2014年5月~2015年4月我院收治的160例小儿心律失常患儿为研究对象,按照住院顺序分为对照组和观察组各80例,对照组患儿给予普罗帕酮治疗,观察组患儿在对照组治疗的基础上加美托洛尔治疗,比较两组患儿的临床治疗效果和不良反应情况。结果对照组患儿的临床总有效率为85%明显低于观察组的97.5%,两组比较差异有统计学意义(P0.05);观察组患儿的不良反应发生率为12.5%明显低于对照组的27.5%,差异有统计学意义(P0.05)。结论普罗帕酮联合美托洛尔治疗小儿心律失常的效果满意,安全性较高,值得临床推广。  相似文献   
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