β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists), β2-adrenergic receptor antagonists(Beta-2 adrenergic receptor antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Heart FailureHypertensionMyocardial Ischemia

Originator Organization

Sanofi

Active Organization-

Inactive Organization

SanofiSanofi-Synthelabo, Inc.

Drug Highest PhaseDiscontinuedNDA/BLA

First Approval Date-

Regulation-

Structure

Molecular FormulaC18H29NO4

InChIKeyJNDJPKHYZWRRIS-UHFFFAOYSA-N

CAS Registry94651-09-9

View All Structures (2)

100 Clinical Results associated with Cicloprolol Hydrochloride

100 Translational Medicine associated with Cicloprolol Hydrochloride

100 Patents (Medical) associated with Cicloprolol Hydrochloride

Literatures (Medical) associated with Cicloprolol Hydrochloride

01 Jan 2018·TalantaQ2 · CHEMISTRY

Structural characterization of electrochemically and in vivo generated potential metabolites of selected cardiovascular drugs by EC-UHPLC/ESI-MS using an experimental design approach

Q2 · CHEMISTRY

Article

Author: Baranowska, Irena ; Bajkacz, Sylwia ; Buszewski, Bogusław ; Szultka-Młyńska, Małgorzata

In the last few years, a number of studies were conducted which aimed at understanding the mechanisms of cardiovascular drug, metabolism, and there is still the need to determine the metabolites of cardiac drugs for the purpose of metabolism control. In this study, we employ a direct combination of electrochemical oxidation and mass spectrometric (EC-MS) identification for monitoring the oxidation pathway of ten cardiovascular drugs (metoprolol, propranolol, propafenone, mexiletine, oxprenolol, pirbuterol, pindolol, cicloprolol, acebutolol and atenolol). Oxidation was accomplished in an electrochemical thin-layer cell coupled on-line to electrospray ionization mass spectrometry (EC/ESI-MS). For further characterization of electrochemical products, the approach involving liquid chromatography linked to tandem mass spectrometry was used. Appropriate conditions for oxidation and identification processes with such parameters as the potential value, mobile phase (type and pH) and working electrode were optimized. Optimization was performed with the use of central composite design (CCD). Besides electrochemical oxidation of analytes (phase I of metabolic transformation), addition of glutathione (GSH) for follow-up reactions (phase II conjunction) was also investigated. The electrochemical results were compared to in-vivo experiments by analyzing plasma and urine samples from patients who had been administered selected cardiovascular drugs. These results show that electrochemistry coupled to mass spectrometry turned out to be an analytical tool suitable to procure a feasible analytical base for the envisioned in vivo experiments.

01 Oct 1992·Cardiovascular Drugs and TherapyQ3 · MEDICINE

Combined invasive and noninvasive study of left ventricular systolic and diastolic function following acute administration of cicloprolol to subjects with normal cardiac function

Q3 · MEDICINE

Article

Author: L. Niccoli ; S. Nodari ; F. Ettori ; L. Bonandi ; L. Dei Cas ; O. Visioli ; M. Metra

Cicloprolol is a new beta-blocking agent with high selectivity for beta 1 receptors and high intrinsic sympathomimetic activity. 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. All patients had normal coronary angiography and left ventriculography. Left ventricular pressure was determined throughout the cardiac cycle using a Millar 8Fr Minotip catheter; an echocardiogram, phonocardiogram, and ECG were simultaneously recorded to obtain left ventricular pressure-diameter loops. All the measurements were repeated before and after the intravenous administration of cicloprolol. Cicloprolol was administered at increasing doses of 0.05, 0.10, and 0.25 mg/kg until a cardiac output increase of at least 15% over basal values was achieved. A decrease of mean arterial pressure or cardiac output after cicloprolol was not observed in any patient. 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. No significant change in the echocardiographic parameters occurred. Among the indices of left ventricular diastolic function, the time constant of isovolumetric relaxation was significantly decreased (-43%) after cicloprolol; moreover, the left ventricular pressure-diameter loop in the protodiastolic phase was shifted to the left following cicloprolol infusion. This study confirms that in subjects with normal left ventricular function cicloprolol can improve resting left ventricular systolic function, and it shows that this action can also be attended by a more rapid isovolumetric relaxation, similar to what has been observed with other sympathomimetic amines.

01 Jan 1992·Clinical CardiologyQ3 · MEDICINE

An evaluation of the safety of the β‐modulator cicloprolol in chronic heart failure

Q3 · MEDICINE

ArticleOA

Author: G. Cocco ; R. Alfiero ; H. Pouleur

AbstractThe 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. 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.

100 Deals associated with Cicloprolol Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D03490	Cicloprolol Hydrochloride	-	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Heart Failure	NDA/BLA	FR	Sanofi-Synthelabo, Inc.	-
Heart Failure	NDA/BLA	-	Sanofi	-
Hypertension	NDA/BLA	-	Sanofi	-
Myocardial Ischemia	NDA/BLA	-	Sanofi	-

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