Chaignon M, Lucsko M, Aubert P, Guédon J
Arch Mal Coeur Vaiss. 1982 Sep;75(9):963-9.
The acute effects of Metoprolol on blood pressure and heart rate were studied with reference to the plasma level of the betablocker in 10 patients (6 male and 4 female) with permanent moderate uncomplicated hypertension. Each patient was given a single oral dose of 200 mg Metoprolol: blood samples were taken over a 12 hour period at given times for Metoprolol estimation. The blood pressure was measured with a mercury manometer; heart rate was measured lying and during a stress test (glyceryl trinitrate). The antihypertensive effect of Metoprolol was significant from the 4th hour; at the 8th hour the systolic pressure was reduced by 15% and the diastolic pressure by 17% (p less than 0.001). The blood pressure then rose progressively. The heart rate in the recumbent position fell 10 to 15% during the study. The heart rate during the trinitrin test varied linearly with time (r = 0.991, p less than 0.001). The variation in systolic and diastolic blood pressure did not correlate with the plasma Metoprolol level (r = 0.03, and 0.19); no correlation was found between the fall in lying heart rate and the plasma betablocker level. On the other hand, the trinitrin heart rate (at the end of the test) correlated negatively with the logarithm of the plasma Metoprolol (n = 56, r = 0.688, p less than 0.001). These results confirm that the antihypertensive effect of Metoprolol is not directly related to the plasma level of the betablocker. On the other hand, the betablocker effect assessed by the trinitrin test, correlated with the plasma Metoprolol level. This relationship is similar to those previously observed with other betablockers; atenolol and oxprenolol.
在10例(6例男性,4例女性)持续性中度单纯性高血压患者中,参照β受体阻滞剂的血浆水平,研究了美托洛尔对血压和心率的急性影响。每位患者单次口服200mg美托洛尔:在12小时内于特定时间采集血样以测定美托洛尔。用汞柱血压计测量血压;分别在静息状态及应激试验(硝酸甘油)期间测量心率。美托洛尔的降压作用从第4小时起显著;在第8小时,收缩压降低15%,舒张压降低17%(p<0.001)。随后血压逐渐回升。在研究期间,卧位心率下降了10%至15%。硝酸甘油试验期间的心率随时间呈线性变化(r = 0.991,p<0.001)。收缩压和舒张压的变化与血浆美托洛尔水平无相关性(r = 0.03和0.19);卧位心率下降与血浆β受体阻滞剂水平之间未发现相关性。另一方面,硝酸甘油试验时的心率(试验结束时)与血浆美托洛尔的对数呈负相关(n = 56,r = 0.688,p<0.001)。这些结果证实,美托洛尔的降压作用与β受体阻滞剂的血浆水平无直接关系。另一方面,通过硝酸甘油试验评估的β受体阻滞剂作用与血浆美托洛尔水平相关。这种关系与先前观察到的其他β受体阻滞剂(阿替洛尔和氧烯洛尔)相似。