Disease relevance of Cicloprolol

• Haemodynamic dose-response actions of cicloprolol in left ventricular dysfunction due to ischaemic heart disease [1].
• All doses of cicloprolol above 2.5 mg reduced an exercise tachycardia but there was no increase in effect above a dose of 50 mg [2].
• Comparative effects of atenolol and cicloprolol on cardiac performance in coronary heart disease [3].
• We studied the acute hemodynamic effects of cicloprolol in nine subjects with no evidence of left ventricular dysfunction who underwent cardiac catheterization for the evaluation of chest pain [4].

High impact information on Cicloprolol

• In this in vivo preparation, xamoterol and pindolol were more potent beta-1 adrenoceptor antagonists than cicloprolol; however, cicloprolol and xamoterol, in contrast to pindolol, were selective for beta-1 adrenoceptors [5].
• Pharmacokinetics and safety of cicloprolol in uraemic patients [6].
• Pharmacodynamic without pharmacokinetic interaction between cicloprolol, a partial beta 1-adrenoceptor agonist, and digoxin in healthy subjects [7].
• Digoxin was given alone during the first period to reach steady state; then digoxin was given with cicloprolol or placebo during the second and third periods, according to a cross-over design [7].
• Effect of cicloprolol in intraocular pressure in healthy volunteers [8].

Biological context of Cicloprolol

• 1. Cicloprolol is a partial beta 1-adrenoceptor agonist considered for the treatment of patients with coronary artery disease and impaired left ventricular function [7].
• Cicloprolol caused a dose dependent increase in sleeping heart rate up to 200 mg [2].
• Cicloprolol increased resting supine heart rate, systolic blood pressure, forearm blood flow and finger tremor [2].
• A decrease of mean arterial pressure or cardiac output after cicloprolol was not observed in any patient [4].
• Cicloprolol increased left ventricular ejection fraction, reduced its end-diastolic volume, and tended to reduce filling pressure without change in other variables [3].

Anatomical context of Cicloprolol

• Cicloprolol administration significantly increased cardiac output (24%), stroke volume (22%), and peak positive dP/dt (25%); no significant changes in heart rate, systemic blood pressure, right atrial pressure, or pulmonary artery pressures were observed [4].

Gene context of Cicloprolol

• Cicloprolol has significant partial agonist activity at the beta 1-adrenoceptor as indicated by increases in heart rate and systolic blood pressure [2].
• The increases in finger tremor and forearm blood flow suggest that cicloprolol has some partial agonist activity at the beta 2-adrenoceptor [2].

Analytical, diagnostic and therapeutic context of Cicloprolol

• Routine monitoring of cicloprolol can be done easily with the HPLC method, whereas the time-consuming GC method may be reserved for pharmacokinetic studies where late-sampled tubes, with low concentrations, must be analysed [9].
• Two methods, one based on high-performance liquid chromatography (HPLC) and the other on gas chromatography (GC), were developed for the quantification of the partial adrenergic receptor antagonist cicloprolol [9].
• Following a 20 min stable control period, the effects of four doses of cicloprolol (0.025, 0.025, 0.05 and 0.1 mg/kg at 10 min intervals) were measured at rest 5-10 min after each intravenous injection [1].

References