We studied the cardiac electrophysiological effects of falipamil, a specific bradycardic agent, in conscious dogs, in comparison with those of alinidine. Sinus rate, corrected sinus recovery time, and Wenckebach point were measured in six intact dogs. Atrial rate, ventricular rate, and atrial effective refractory period were measured in six atrioventricular-blocked dogs. In both groups, blood pressure was also monitored. Each dog received, with at least a three-day interval, falipamil (hydrochloride) and alinidine (hydrobromide) in four successive intravenous injections, 30 min apart, at 0.5, 0.5, 1, and 2 mg kg-1. Falipamil increased sinus rate and atrial rate, but decreased ventricular rate, whereas alinidine decreased sinus rate and ventricular rate, but increased atrial rate. Falipamil shortened corrected sinus recovery time and increased Wenckebach point, whereas alinidine lengthened corrected sinus recovery time and decreased Wenckebach point. Falipamil and alinidine increased atrial effective refractory period. Neither falipamil nor alinidine modified mean blood pressure in either group. Overall, these results show that (a) falipamil exhibits effects on the electrical activity of the heart, reflecting the predominant direct vagolytic effect of this drug, (b) alinidine exhibits effects reflecting the marked antiarrhythmic potential of this agent, and (c) thus indicate that two drugs with almost identical specific bradycardic properties can produce quite different electrophysiological effects in the conscious dog.

01 Apr 1994·Journal of Cardiovascular PharmacologyQ4 · MEDICINE

Chronotropic Cardiac Effects of Falipamil in Conscious Dogs: Interactions with the Autonomic Nervous System and Various Ionic Conductances

Q4 · MEDICINE

Article

Author: Boucher, Michel ; Duchene-Marullaz, Pierre ; Chapuy, Eric ; Chassaing, Claude

The chronotropic cardiac effects of falipamil were studied in conscious dogs with chronic atrioventricular (AV) block. Falipamil (0.5-2 mg/kg) initially increased atrial rate dose dependently. After atropine and atropine-pindolol, falipamil (2 mg/kg) decreased atrial rate, but after pindolol, it did not modify atrial rate. After atropine-pindolol-phenoxybenzamine, atropine-pindolol-yohimbine, atropine-pindolol-verapamil, and atropine-pindolol-quinidine pretreatment, falipamil produced atrial bradycardia. Falipamil dose-relatedly decreased ventricular rate. Falipamil (2 mg/kg) decreased ventricular rate after atropine, pindolol, and atropine-pindolol more than under basal conditions. After the other four pretreatments, it also produced ventricular bradycardia. Falipamil did not affect mean blood pressure (MBP) at any dose. These results (a) show that the initial atrial cardio-acceleration produced by falipamil results from its direct vagolytic action; (b) show that absence of atrial bradycardia results from buffering by the vagolytic effect and/or a relatively low basal atrial rate; (c) suggest that the falipamil ventricular bradycardia is partly buffered by the vagolytic effect, norepinephrine (NE) release, and involvement of alpha 2-adrenoceptors; (d) exclude involvement of postsynaptic muscarinic, alpha- and beta-adrenoceptors, and of the slow calcium current in the mechanism(s) by which falipamil decreases cardiac automaticity; and (e) suggest possible involvement of a quinidine-sensitive current in this (these) mechanism(s).

01 Nov 1993·Arzneimittel-Forschung

Pattern of interaction between dihydropyridine calcium antagonists and cationic amphiphilic drugs in isolated guinea-pig left atria.

Article

Author: Herzig, S ; Schröder, F

The pharmacodynamic interaction between dihydropyridine calcium antagonists and several cationic amphiphilic agents with respect to their negative inotropic action has been studied in isolated guinea-pig left atria. (+/-)-Bepridil (CAS 64706-54-3), (+/-)-cis-diltiazem (CAS 33286-22-5), falipamil (CAS 77862-92-1), (+/-)-gallopamil (CAS 16662-47-2), lidocaine (CAS 6108-05-0), procainamide (CAS 614-39-1), or quinidine (CAS 50-54-4) were added at fixed concentrations. Afterwards, concentration-response curves for nifedipine (CAS 21829-25-4), the S-enantiomer niguldipine.HCl and its R-enantiomer dexniguldipine.HCl (CAS 113165-32-5), (+/-)-nimodipine (CAS 66085-59-4) (+/-)-nitrendipine (CAS 39562-70-4), or (+/-)-isradipine (CAS 75695-93-1) were obtained. In most cases, a left-ward shift in the concentration-response curve of the dihydropyridine was observed. The extent of this shift varied between dihydropyridines, and it depended on the catamphiphilic compound present. A high correlation was found between the different dihydropyridines, when comparing the extent of displacement of their concentration-response curves by the various catamphiphilic test compounds. Although quantitative differences exist between the different dihydropyridines, they are affected in potency by other compounds with a rather similar pattern. Accordingly, some general predictions about the interactions of a given dihydropyridine might be possible using limited datasets.

100 Deals associated with Falipamil

External Link

KEGG	Wiki	ATC	Drug Bank
-	Falipamil	-	-

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Myocardial Ischemia	Phase 2	DE	Boehringer Ingelheim Pharma GmbH & Co., KG	-
Myocardial Ischemia	Phase 2	-	C.H. Boehringer Sohn AG & Co. KG	-
Tachycardia, Sinus	Phase 2	-	C.H. Boehringer Sohn AG & Co. KG	-
Tachycardia, Sinus	Phase 2	DE	Boehringer Ingelheim Pharma GmbH & Co., KG	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis