Reduction of plasma and urinary vasopressin during treatment of severe hypertension by captopril

Abstract. Plasma concentrations and urinary excretion rate of vasopressin (VP) were examined in ten cases of severe hypertension before and during short-term treatment by Captopril (SQ 14 225). Before Captopril, plasma and urinary VP were high (respectively 5.24 pmol/1 and 68 pmol/day) and positively correlated to plasma renin activity (PRA) and plasma aldosterone (PA). The decline in blood pressure (mean —15%) after Captopril was correlated not only to initial PRA and PA values, but also to plasma ( r = 0.89; P < 0.001) and urinary ( r = 0.78; P < 0.01) VP values. The initial dose of Captopril (1 mg/kg) induced a rapid decrease in blood pressure whereas plasma VP did not rise and aldosterone decreased. At the eighth day of Captopril treatment (mean daily dose 6±1.5 mg/kg) the drop in blood pressure (— 12%) and in aldosterone persisted together with a significant reduction in plasma (1.18 pmol/1; P <0.01) and urinary (25 pmol/day; P <0.01) VP. It is suggested that these sustained simultaneous reductions in the rates of secretion of vasopressin and aldosterone are both elements of the antihypertensive effect of Captopril.     

The effects of captopril (SQ 14,225) on bradykinin-induced bronchoconstriction in the anesthetized guinea pig.

The effect of captopril (SQ 14,225) a potent inhibitor of angiotensin converting enzyme (ACE: kininase II) on the bronchoconstrictor response to bradykinin was studied in the anesthetized guinea pig. The i.v. administration of captopril caused a profound long lasting hypotension without affecting pulmonary resistance or dynamic compliance. Similarly, the i.v. administration of bradykinin caused small increases in pulmonary resistance and decreases in dynamic compliance which were not altered by the administration of captopril. However, after beta-receptor blockade with propranolol, bradykinin-induced changes in resistance and compliance were enhanced; additional captopril administration further potentiated the bradykinin effects. The prostaglandin synthetase inhibitor indomethacin antagonized the bradykinin-induced bronchoconstriction in beta-blocked animals and its potentiation by captopril. In the isolated perfused guinea pig lung, bradykinin caused a dose dependent release of a prostaglandin-like substance which was significantly increased by captopril and antagonized by indomethacin. These results suggest that bradykinin causes a prostaglandin-mediated bronchoconstriction. Captopril, a potent inhibitor of ACE, prevents the degradation of bradykinin thus potentiating the bradykinin-induced bronchoconstriction, an effect observed in intact animals only in the absence of pulmonary beta-receptor activation.     

Relief from malignant hypertension by treatment with captopril in a patient on maintenance hemodialysis

Zusammenfassung Es wird ein Patient mit chronischem Nierenversagen auf dem Boden einer malignen Hypertonie beschrieben. Durch Dialysebehandlung konnte die Hypertonie nicht beherrscht werden. Der orale Angiotensin-converting Enzym Hemmstoff Captopril (SQ 14.255; 2-D-methyl-3-mercaptopropanoyl-L-prolin) erzielte eine dramatische Senkung des Blutdrucks sowohl unter ambulanten Bedingungen, als auch während der Dialyse. Nach 6 monatiger Behandlungsdauer wurden keine unerwünschten Wirkungen beobachtet. Die Wirkung von Captopril kann als biochemische Nephrektomie beschrieben werden.Supported by the Deutsche Forschungsgemeinschaft DFG Wi 548/1     

周围动脉内膜-中层增厚的诊断和药物干预的研究

目的 探讨颈动脉、股动脉、胸主动脉粥样硬化的超声诊断标准、自然演变及药物的干预作用。方法 研究对象包括259名正常人和102例动脉粥样硬化(AS)患者。在125名正常人及AS患者中进行了体表高频超声技术检查,在134名正常人中进行了经食管超声检查。将AS患者随机分为辛伐他汀组、普罗布考组、卡托普利组,测量颈动脉和股动脉后壁正常部位内膜-中层厚度(IMT)包括正常部位IMT值(IMTA),最大IMT(IMTB),4条动脉最大IMT平均值(IMTC),4条动脉中单个最大IMT(IMTD),分别服用辛伐他汀、普罗布考、卡托普利,3年后复查。结果 随年龄增加,胸主动脉、颈动脉及股动脉IMT呈增加趋势;正常人颈动脉、股动脉和胸主动脉IMT分别为0.63 mm±0.15 mm、0.68 mm±0.21 mm、1.02 mm±0.22 mm,上限分别为0.93 mm、1.10 mm、1.46 mm。IMTA的平均年增长速度为0.023 mm。各组治疗前后斑块部位IMT有增加趋势,但各治疗组IMT。增加的幅度显著低于对照组。结论 正常人颈动脉、股动脉及胸主动脉的IMT呈增龄性改变。建议颈动脉、股动脉和胸主动脉IMT增厚的超声诊断标准应分别为>0.93 mm,>1.10 mm和>1.46 mm。药物治疗具有延缓动脉粥样硬化进展的作用,高频超声技术能够可靠的观察颈动脉和股动脉动脉粥样硬化的消长改变。     

Determination of certain drugs in binary mixtures formulations by second derivative ratio spectrophotometry and LC

Spectrophotometric and high-performance liquid chromatographic (HPLC) methods are developed for simultaneous determination of three binary mixtures with overlapping spectra. The spectrophotometric method is based on the use of second derivative of the ratio spectra (2DD) for resolution of three binary mixtures of indapamide with captopril (mixture 1), cinnarizine with heptaminol acefylline (mixture 2) and amoxycillin trihydrate with flucloxacillin sodium (mixture 3). The HPLC method depends on the separation of components of binary mixtures using ODS column with mobile phase consisting of acetonitrile and 5 mM aqueous heptane sulphonic acid sodium salt in ratios of (60:40, v/v, pH 5.5) for mixture 1, (50:50, v/v, pH 3.0) for mixture 2 and (35:65, v/v, pH 4.2) for mixture 3. The proposed methods are accurate, non-destructive and successfully applied for the determination of the three binary combinations in synthetic mixtures and commercial pharmaceutical products.     

氯沙坦钾片与卡托普利片治疗高血压病的临床疗效

目的 比较氯沙坦钾片与卡托普利片治疗高血压痛的临床疗效.方法 选择轻、中度高血压患者158例,其中96例(男性66例,女性30例,平均年龄52.3岁)用氯沙坦钾50mg,口服,一日一次,连续用药4周.其余62例(男性46例,女性16例,平均年龄51.0岁)用卡托普利50mg,口服,一日三次,连续用药4周.结果 氯沙坦钾组总有效率94.8%,与卡托普利组80.6%相比,差别有统计学意义(P<0.05).不良反应发生率氯沙坦钾组14.65,与卡托普利组20.9%比较,差别有统计学意义(P<0.05).结论 氯沙坦钾片对高血压的疗效显著而又安全,优于卡托普利片.     

三种普利类药物治疗原发性高血压的成本-效果分析

目的：探讨培哚普利，贝拉普利与卡托普利三种普利类药物治疗高血压的经济效果。方法：运用药物经济学的成本-效果分析方法。从成本与效果的比值（C/E），增加的成本与效果的比值（△C/△E），以及安全性和有效性对患所用三种药物进行综合分析评价。结果：贝拉普利的费用最低，培哚普利费用略高于贝拉普利，二的疗效相近。结论：本认为贝拉普利为三种普利类中最佳药物。     

卡托普利和尼群地平小量联用治疗高血压病

目的　观察卡托普利和尼群地平小量联合用药治疗高血压病的疗效。方法　卡托普利和尼群地平小量联合用药。结果　卡托普利和尼群地平小量联和 ,治疗高血压病总有效率 90 .9% ,单用卡托普利总有效率 63.6% ,单用尼群地平总有效率 62 .5%。卡方检验 ,单一用药与联合用药相比 ,χ2 分别为 4 .59和 4 .16,P<0 .0 5。结论　两药联合用药疗效确切 ,副作用减小 ,可推广使用     

卡托普利对家兔动脉粥样硬化内皮依赖舒张反应的影响

目的研究卡托普利对家兔动脉粥样硬化（ＡＳ）动脉内皮依赖舒张反应的影响。方法２７只家兔随机分成正常对照组，ＡＳ组及卡托普利（２５ｍｇｋｇ－１ｄ－１）组，饲养１２周。取一段（０．５ｃｍ）靠近升主动脉起始部的动脉做常规病理切片，一近端腹主动脉（３ｃｍ～４ｃｍ）做血管功能测定，观察对不同浓度乙酰胆缄及硝普钠的舒张反应。结果与ＡＳ组比较，卡托普利组血浆总胆固醇浓度无显著改变，但病理形态学发现卡托普利组脂纹数量减少，平均最大脂纹厚度明显降低，示卡托普利有抗ＡＳ作用。腹主动脉乙酰胆缄引起的平均最大舒张百分数３组分别为６２．３±２．５％、３．７±３．２％、３５．９±１１．４％，表明卡托普利能改善内皮依赖的舒张反应，而非内皮依赖的舒张反应（硝普钠引起者）３组间无差异。结论改善内皮功能不全可能是卡托普利抗动脉粥样硬化的重要机制