Cicloprolol is a partial β 1-adrenoceptor agonist .
Cicloprolol is a partial β1-adrenoceptor agonist considered for the treatment of patients with coronary artery disease and impaired left ventricular function[1]. The new β-adrenoceptor partial agonist Cicloprolol acts as a β-agonist at normal levels and as a β-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. Cicloprolol has a weak β1-agonistic effect at normal levels of adrenergic discharge and acts as an antagonist at high levels of discharge[2].
[1]. Weber S, et al. Pharmacodynamic without pharmacokinetic interaction between cicloprolol, a partial beta 1-adrenoceptor agonist, and digoxin in healthy subjects. Br J Clin Pharmacol. 1990 Sep;30(3):411-6 [2]. Cocco G, et al. An evaluation of the safety of the beta-modulator cicloprolol in chronic heart failure. Clin Cardiol. 1992 Jan;15(1):38-42.