比索洛尔改善充血性心衰心功能及心肌重塑的疗效观察

目的　观察比索洛尔 (bisoprolol)对充血性心衰心功能及心肌重塑的临床疗效 .方法　 2 12例患者随机分为比索洛尔组和常规药物组 ,比索洛尔剂量起始量 0 .6 2 5 mg～1.2 5 0 mg,1次· d- 1 ,逐渐增加至最大剂量为 2 .5 mg～ 5 .0mg,1次· d- 1 .观察心功能、临床疗效、左室舒张末内径(L VEDD)、左室收缩末内径 (L VESD)、射血分数 (EF)、舒张早期 E峰流速 /舒张晚期 A峰流速 (VE/ VA) .结果　比索洛尔组与常规药物组比较 ,比索洛尔治疗 3m o后有效者(87.7% )高于常规药物组 (6 6 .0 % ) ,P <0 .0 5 ;冠心病(87.9% )和扩张型心肌病心衰 (91.9% )疗效明显好于常规药物组 (分别为 6 6 .7% ,6 7.4 % ) ;治疗 6 mo后重度心衰者疗效(90 .0 % )明显好于常规药物组 (6 5 .4 % ,P <0 .0 5 ) .治疗后比索洛尔组 L VESD[(44 .8± 3.9) m m vs(48.8± 4 .6 ) mm],EF[(40 .7± 7.5 ) % vs (35 .7± 5 .2 ) % ]优于常规药物组 (P<0 .0 1) ;L VEDD,VE/ VA也较治疗前有明显改善 .结论　比索洛尔改善充血性心力衰竭临床症状 ,促进心脏收缩、舒张功能恢复 ,部分逆转心肌重塑 .     

比索洛尔对冠心病心力衰竭患者心室重塑和心功能的影响

目的 :探讨比索洛尔对冠心病心力衰竭患者心室重塑及心功能的影响。方法 :冠心病心力衰竭患者 12 0例 ,左室射血分数≤ 45 % ,心功能 (NYHA)Ⅱ -Ⅳ级 ,常规治疗基础上随机分为比索洛尔治疗组和对照组。治疗 6个月 ,观察比索洛尔对心室重塑、心功能的影响。应用心脏彩色超声仪测定基线值及 1个月、3个月、6个月左室结构及功能指标变化。结果 :比索洛尔平均用量为 (7 5 0± 2 5 0 )mg/d ,经过 6个月治疗 ,比索洛尔治疗组症状和心功能改善 ,与对照组比较左室射血分数上升 [(4 9 2± 2 8) %VS(3 9 6± 3 6) % ,P <0 0 5 ] ,左室收缩末容积下降[(15 7 7± 42 6)mlVS(180 9± 3 9 6)ml] ;与基线比较左室舒张末容积下降 (P <0 0 5 )。结论 :在强心、利尿、血管紧张素转化酶抑制剂基础上 ,应用比索洛尔能显著改善冠心病心力衰竭患者的心功能 ,改善心室重塑。长期应用可改善衰竭心脏心肌细胞的生物学效应 ,这种有益的作用在不同心功能级别间无显著性差异     

Effects of single oral doses of bisoprolol and atenolol on airway function in nonasthmatic chronic obstructive lung disease and angina pectoris

Summary A randomized, placebo-controlled, double-blind crossover investigation in 12 patients with non-asthmatic chronic obstructive lung disease and co-existing stable angina pectoris was done to compare two ₁-selective adrenoceptor blocking agents, atenolol 100 mg and bisoprolol 20 mg. Systolic and diastolic blood pressures (SBP, DBP), heart rate (HR) as well as airway resistance (AWR, and less frequently forced expiratory volume in 1 s (FEV₁) and intrathoracic gas volume (ITGV) were measured in the sitting position before and at various times up to 24 h after drug intake.During the first 4 h both beta-blockers produced a significant reduction in HR in comparison to placebo (p<0.01). Atenolol 100 mg significantly increased AWR relative to placebo and bisoprolol (p<0.05). After 24 h, a significant reduction in HR (p<0.01) could only be demonstrated after bisoprolol, whereas atenolol alone led to a significant elevation in AWR relative to placebo and bisoprolol (p<0.05) at that time.It is concluded that bisoprolol appears to have a high degree of beta₁-selectivity, thus providing a wide split between beta₁- and beta₂-adrenoceptor blockade. Bisoprolol in its therapeutic dose range is expected to be relatively safe as regards bronchoconstriction in patients suffering both from hypertension and/or angina pectoris and chronic obstructive lung disease.     

应用卡维地洛、比索洛尔和常规方法治疗慢性心力衰竭临床疗效比较

目的比较应用卡维地洛、比索洛尔和常规方法治疗慢性心力衰竭(CHF)的疗效。方法92例CHF患者分为卡维地洛组(34例)、比索洛尔组(38例)和常规组(20例)。常规组应用血管紧张素转换酶抑制剂、利尿剂和洋地黄制剂,卡维地洛组和比索洛尔组在常规治疗基础上分别加用卡维地洛和比索洛尔。随访半年,分别测量治疗前后心率、血压6、min步行试验距离,并用超声心动图测定心功能进行疗效观察。结果1)卡维地洛组和比索洛尔组心率、血压和心肌耗氧量均较常规组明显降低,6min步行试验距离增加,但差异无统计学意义。2)卡维地洛组和比索洛尔组左心室舒张末径(LVEDD)和左心室收缩末径(LVESD)显著低于常规组,左心室射血分数(LVEF)显著高于常规组,且卡维地洛组LVESD较比索洛尔组明显减小。结论卡维地洛和比索洛尔通过β1受体阻滞等作用,逆转左心室重构,在改善CHF患者心功能方面作用相似。     

Clinical improvement in patients with orthostatic intolerance after treatment with bisoprolol and fludrocortisone

Orthostatic intolerance is the development of disabling symptoms upon assuming an upright posture that are relieved partially by resuming the supine position. Postural tachycardia syndrome (POTS) is an orthostatic intolerance syndrome characterized by palpitations because of excessive orthostatic sinus tachycardia, lightheadedness, tremor, and near-syncope. Patients usually undergo extensive medical, cardiac, endocrine, neurologic, and psychiatric evaluation, which usually fails to identify a specific abnormality. The authors investigated the autonomic and hemodynamic profile of patients with POTS and the effectiveness of bisoprolol and fludrocortisone. The authors evaluated 11 female patients with POTS before and after medical treatment with a cardioselective bisoprolol -blocker or fludrocortisone, or both, and 11 age-matched control patients. Variability of heart rate and systolic blood pressure was assessed by fast Fourier transform, and spontaneous baroreceptor gain was assessed by use of the temporal sequences slope and index. Modelflow was used to quantify hemodynamics. Symptoms in all patients improved greatly after medication. The autonomic and hemodynamic impairment observed in patients with POTS, particularly after orthostatic stress, is treated effectively with bisoprolol or fludrocortisone or both. These results need further confirmation in a controlled double-blind study. Proper medical treatment improves dramatically the clinical and autonomic-hemodynamic disturbances observed in patients with POTS. The data support the hypothesis that POTS is the result of a hyperadrenergic activation or hypovolemia during orthostasis.     

G蛋白β3亚单位C825T基因多态性与富马酸比索洛尔降压疗效的相关性

 目的 探讨G蛋白β₃亚单位C825T基因多态性与富马酸比索洛尔降压疗效的相关性。方法 选择2018-10至2020-10在解放军总医院第一医学中心心内科住院或门诊就诊的轻、中度原发性高血压患者,均口服5 mg/d比索洛尔,进行GNβ₃-C825T基因型测定,依据基因型分为3组:CC组、CT组、TT组,每组150例,在3组受试者治疗7 d,1、3、6个月后进行随访,测定患者的富马酸比索洛尔药物代谢血药浓度;治疗前、治疗7 d,1、3、6个月后进行24 h动态血压监测,比较患者静息状态下收缩压及舒张压(SBP、DBP),24 h收缩压均数(24 h SBP)、24 h舒张压均数(24 h DBP)、白天收缩压均数(d SBP)、白天舒张压均数(d DBP)、夜间收缩压均数(n SBP)、夜间舒张压均数(n DBP)的组间差异;进行24 h动态心电图监测,比较24 h平均心率、窦性心律震荡水平。结果 治疗7 d,随访1、3、6个月TT组富马酸比索洛尔血药浓度均高于CC组及CT组,差异均有统计学意义(P＜0.05),CC组与CT组无统计学差异,3组组内不同时间血药浓度变化均无统计学差异;应用富马酸比索洛尔后,3组患者血压均有下降趋势,其中TT组降压效果＞CT组＞CC组,3组间血压下降水平有统计学差异(P＜0.05);治疗7 d后,动态心电图显示:3组患者心率有下降趋势,TT组＞CT组＞CC组,其中TT组与CT组、CC组比较有统计学差异(P＜0.05),CT组与CC组心率下降无统计学差异;TT组窦性心律震荡水平优于CT组、CC组。结论 G蛋白β₃亚单位C825T基因多态性与富马酸比索洛尔降压疗效之间具有相关性。     

比索洛尔、拉西地平和赖诺普利对高血压病患者24小时血压的影响

目的比较比索洛尔、拉西地平和赖诺普利对２９例高血压病患者的降压疗效。方法采用随机、单盲和交叉的方法，运用２４小时动态血压监测。结果三药均能显著降低血压，彼此间降低偶测血压的幅度无显著差异。比索洛尔和拉西地平降低２４小时平均和白天平均血压的幅度大于赖诺普利。三药均能有效控制清晨血压高峰期的血压，它们的降压谷／峰比值都超过６５％。结论比索洛尔、拉西地平和赖诺普利均可每日服用１次，前二药控制２４小时血压及清晨醒后的高峰期血压较后者为佳。     

富马酸比索洛尔的合成工艺改进

目的改进富马酸比索洛尔的合成方法。方法以3-(异丙基氨基)丙烷-1,2-二醇为起始原料,经成环、对甲苯磺酰化、偶合、开环及成盐5步反应制得富马酸比索洛尔。结果与结论目标化合物及中间体的结构经1H-NMR、MS谱等确证。新合成路线操作简便,反应条件温和,总收率为36%,适合工业化生产。目标物经HPLC法检测纯度达99.4%,单个杂质含量小于千分之一,符合中华人民共和国药典标准。     

比索洛尔和低分子肝素治疗老年不稳定心绞痛的疗效比较

目的 比较比索洛尔和低分子肝素治疗老年不稳定心绞痛的临床疗效和安全性。方法 选取2011年9月-2013年4月在延安市中医医院就诊的不稳定心绞痛患者186例,随机分为比索洛尔组、低分子肝素组和对照组,每组62例。对照组给予吸氧、阿司匹林、硝酸甘油治疗,比索洛尔组在对照组的基础上口服比索洛尔片,5 mg/次,1次/d;低分子肝素组在对照组的基础上加用低分子肝素注射液,皮下注射,0.6 mL/次,2次/d。3组均连续治疗2个月。治疗后,比较3组患者的临床疗效和心血管事件发生率。结果 比索洛尔组、低分子肝素组的临床疗效有效率及心电图改善优良率均较对照组高,均具有统计学意义（P<0.05）;比索洛尔组的临床疗效有效率和心电图改善优良率均高于低分子肝素组,两组比较差异均有统计学意义（P<0.05）。比索洛尔组、低分子肝素组的心绞痛、心律失常、急性心肌梗死发生率均低于对照组,差异有统计学意义（P<0.05）;比索洛尔组和低分子肝素组心绞痛、心律失常、急性心肌梗死的发生率差异没有统计学意义。3组不良反应发生率比较,差异均不具有统计学意义。结论 在常规治疗基础上给予比索洛尔治疗不稳定心绞痛具有确切的临床疗效,不良反应较少,值得临床推广应用。