Silas J H, Freestone S, Lennard M S, Ramsay L E
Br J Clin Pharmacol. 1985 Oct;20(4):387-91. doi: 10.1111/j.1365-2125.1985.tb05082.x.
We have compared the beta-adrenoceptor blocking and antihypertensive effects of chronic once daily treatment with conventional metoprolol 200 mg, two 'long-acting' formulations of metoprolol 200 mg and atenolol 100 mg in a cross-over study in 12 hypertensive patients concurrently receiving diuretic therapy. The peak effects of all compounds were similar, with significant reductions in exercise heart rate and blood pressure. Twenty-four hours after dosing only atenolol treatment was consistently associated with a reduction in both exercise heart rate (P less than 0.001) and blood pressure (P less than 0.02) when compared with placebo. Once daily treatment of hypertension with metoprolol, even in 'long-acting' formulations, cannot be recommended because of waning antihypertensive effect which would be missed at routine clinic attendance. Metoprolol should be prescribed twice daily in hypertension. So-called long-acting formulations do not always confer benefits over conventional dose forms.
在一项针对12名同时接受利尿剂治疗的高血压患者的交叉研究中,我们比较了常规美托洛尔200毫克每日一次慢性治疗、两种美托洛尔200毫克“长效”制剂以及阿替洛尔100毫克的β-肾上腺素能受体阻断和降压效果。所有化合物的峰值效应相似,运动心率和血压均显著降低。给药24小时后,与安慰剂相比,仅阿替洛尔治疗始终与运动心率降低(P<0.001)和血压降低(P<0.02)相关。由于降压效果逐渐减弱,在常规门诊就诊时可能会错过,因此不建议使用美托洛尔每日一次治疗高血压。高血压患者应每日服用美托洛尔两次。所谓的长效制剂并不总是比常规剂型更具优势。