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The new beta-adrenoceptor partial agonist cicloprolol acts as a beta-agonist at normal levels and as a beta-antagonist at high levels of adrenergic discharge. Treatment with cicloprolol should protect the heart against excessive stimulation, while providing a baseline level of sympathetic drive. The clinical interest of such a profile is, however, not yet established in heart failure. Accordingly this study examined the safety of oral cicloprolol, a step necessary before undertaking efficacy comparison with other compounds recently proposed to treat heart failure. Twenty-five patients were studied. Cicloprolol was given once a day for 2 weeks in a crossover double-blind placebo-controlled design. Follow-ups were obtained at baseline and at the end of each period. At baseline all patients had clear evidence of heart failure. Cicloprolol did not affect resting heart rate and blood pressure, but it reduced significantly peak exercise heart rate and peak rate-pressure product. The effect was especially significant in patients with sinus rhythm. The drug did not induce bradycardia or arrhythmias. Resting and exercise ejection rate were not affected. Cicloprolol improved the quality of life and the work capacity of 5 of 12 patients with congestive failure due to ischemic etiology. Side effects were few and similar with placebo and cicloprolol. Thus, short-term administration of cicloprolol is safe in moderate heart failure.

The antihypertensive and anti-ischaemic effects of methyldopa and captopril were compared in 12 hypertensive patients with coronary artery disease. The antihypertensive effect of alpha-methyldopa (A) and captopril (C) were significant and similar. On the other hand, while methyldopa did not increase the product of systolic pressure and heart rate and did decrease the effort-induced S-T segment depression, C increased the double product (DP) and decreased the ischaemic S-T changes. Captopril might be useful in the treatment of hypertensive patients with coronary artery disease.

Twelve normotensive patients with coronary artery disease and stable effort-induced angina pectoris were selected: the antiischemic effect of captopril was studied. A maximal cycloergometer effort test was obtained before (base) and after administration of placebo or captopril (50 mg p.o.). The following parameters were measured: heart rate (HR), blood pressure (BP), maximal rate/pressure product (MRPP), maximal workload sustained, (MWS), maximal working time (MWT), and S-T depression at MRPP. The base and placebo were similar. Compared to them captopril augmented the MWT, increased the MWS, reduced S-T depression at MRPP, and decreased the number of patients with effort-induced angina pectoris. The antiischemic effect of captopril seems related both to its effect on HR and BP, and to a local enhancement of coronary blood flow.