SummaryNebivolol is a racemic adrenergic i3-blocker, with i3-blocking activity that is essentially due to its d-enantiomer.The anti-ischaemic activity of nebivolol was investigated in 16 patients with stable angina of effort, with a fixed ischaemic threshold (variations < ± 15%).After a IO-day washout period, patients were randomised to treatment with either nebivolol 5mg daily or placebo for 14 days. Patients underwent maximal symptom-limited exercise tests (10 W/min on a bicycle) during washout (twice), and after the completion of each treatment period. Patients were studied by ECG and systolic blood pressure measurement (cuff method). After nebivolol treatment, ischaemic and anginal thresholds were increased for at least 8 hours compared with placebo (ischaemic threshold: nebivolol 637.5 ± 47sec; placebo 534.3 ± 38sec; p < 0.01; anginal threshold: nebivolol 754.6 ± 59sec; placebo 674 ± 4lsec; p < 0.05). Rate pressure product was significantly decreased at rest and during exercise.In conclusion, nebivolol possesses an anti-ischaemic and antianginal activity lasting at least 8 hours. This activity is mainly due to the reduction in myocardial oxygen consumption.Nebivolol, a racemic mixture of the d and I isomers, is a novel selective adrenergic fJ-blocker with distinctive characteristics. In contrast to other fJblockers, the adrenergic fJl-antagonism of nebivo-101 is essentially due to its d-enantiomer, with the l-enantiomer having minimal fJ-blocking activity. Studies in vitro showed that nebivolol possesses a strong affinity for adrenergic fJl-receptors, less for Ih-receptors, and is devoid of adrenergic C¥I-, C¥2-, dopamine D I and D2 receptor-blocking activities.
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