Electrophysiologic effects, antiarrhythmic activity and pharmacokinetics of cibenzoline studied with programmed stimulation of the heart in patients with supraventricular reentrant tachycardias.
Cibenzoline, an imidazoline derivative is a new antiarrhythmic agent. Its electrophysiological effects and antiarrhythmic properties were studied with programmed electrical stimulation of the heart in 12 patients with recurrent episodes of reentrant supraventricular tachycardia; atrionodal (5 cases), circus movement tachycardia involving an accessory pathway (6 cases), intraatrial reentry (one case). Cibenzoline was infused intravenously at a dose of 1 mg kg-1 to 1.75 mg kg-1 during sustained episodes of tachycardia and over 9 to 15 min. Cibenzoline shortened the sinus cycle length, moderately increased the transnodal conduction time and markedly lengthened the HV interval. The refractory periods of the atrioventricular (A-V) node, the atrium and the ventricle did not change. The effects of cibenzoline on accessory pathways used in the anterograde direction were measurable in 4 cases. Complete blockade of the bypass was seen in every case. In the retrograde direction the refractory period of the bypass could be evaluated; in 5 patients it lengthened systematically. Infused intravenously during epidoses of tachycardia, the drug terminated the rhythm disorder in 9 out of 12 cases. Tachycardia could still be initiated in 8 patients after i.v. cibenzoline (2 out of 5 A-V nodal tachycardias, 6 out of 6 circus movement tachycardias). The distribution of the drug followed a bicompartment pharmacokinetic model. The plasma levels at the end of infusion ranged from 1.34 to 3.19 microgram ml-1. Cibenzoline, primarily has class I antiarrhythmic properties and its well-understood pharmacokinetics should be of help in tailoring the treatment to the individual needs of the patient.
D000293:Adolescent; D000328:Adult; D000889:Anti-Arrhythmia Agents / Q000378:metabolism / Q000627:therapeutic use*; D002304:Cardiac Pacing, Artificial; D004594:Electrophysiology; D005260:Female; D006329:Heart Conduction System / Q000187:drug effects* / Q000503:physiopathology; D006801:Humans; D007093:Imidazoles / Q000378:metabolism / Q000627:therapeutic use*; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D013610:Tachycardia / Q000188:drug therapy* / Q000503:physiopathology
D000889:Anti-Arrhythmia Agents; D007093:Imidazoles; C032151:cifenline