Profiles of Aprindine, Cibenzoline, Pilsicainide and Pirmenol in the Framework of the Sicilian Gambit

Kodama, Itsuo; Ogawa, Satoshi; Inoue, Hiroshi; Kasanuki, Hiroshi; Kato, Takao; Mitamura, Hideo; Hiraoka, Masayasu; Sugimoto, Tsuneaki; Clinica, The Guideline Committee for

doi:10.1253/jcj.63.1

Cited by 50 publications

(23 citation statements)

References 97 publications

(241 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…1) is a class I-b antiarrhythmic agent for the treatment of atrial and ventricular tachyarrhythmias (33). In addition to blocking I Na , this drug inhibits I L-Ca , I K , I KACh , and I f in cardiac myocytes (34 -36).…”

Section: Aprindinementioning

confidence: 99%

Topics on the Na+/Ca2+ Exchanger: Pharmacological Characterization of Na+/Ca2+ Exchanger Inhibitors

2006

View full text Add to dashboard Cite

Abstract. Using the whole-cell voltage clamp, we examined acute effects of various agents on Na + / Ca 2+ exchange current (I NCX ) in guinea-pig cardiac ventricular cells and transfected cells. Among the antiarrhythmic drugs, amiodarone, bepridil, dronedarone, cibenzoline, azimilide, and aprindine inhibited I NCX in a concentration-dependent manner. We also investigated the effects on NCX of 2,3-buanedione monoxim (BDM) and selective NCX inhibitors such as KB-R7943, SEA0400, and SN-6. The presence of trypsin in the pipette solution attenuated the inhibitory effects on NCX of amiodarone, bepridil, and BDM, suggesting that these drugs inhibit NCX from the cytosolic side. In contrast, the trypsin-insensitive NCX inhibitors were aprindine, azimilide, dronedarone, cibenzoline, KB-R7943, SEA0400, and SN-6. KB-R7943, SEA0400, and SN-6 suppressed the uni-directional outward I NCX more potently than the uni-directional inward I NCX . The mechanism of this mode-dependency is unknown, but is suggested to be related to intracellular Na + concentration.

show abstract

Section: Aprindinementioning

confidence: 99%

Topics on the Na+/Ca2+ Exchanger: Pharmacological Characterization of Na+/Ca2+ Exchanger Inhibitors

2006

View full text Add to dashboard Cite

show abstract

“…T he class IC drug pilsicainide, a pure sodium channel blocker with slow recovery kinetics, 1 has often been used clinically in Japan to terminate paroxysmal atrial fibrillation (AF) and is known for its high conversion rate. 2 Although the mechanism is still unknown, its effects on electrophysiological parameters, such as the refractory period (RP), conduction velocity (CV), and wavelength (WL; the product of RP and CV), have been reported previously.…”

mentioning

confidence: 99%

Widening of the Excitable Gap and Enlargement of the Core of Reentry During Atrial Fibrillation With a Pure Sodium Channel Blocker in Canine Atria

et al. 2003

View full text Add to dashboard Cite

Background-This study aimed to assess the effects of pilsicainide, a pure sodium channel blocker, on electrophysiological action and wavefront dynamics during atrial fibrillation (AF). Methods and Results-In a newly developed model of isolated, perfused, and superfused canine atria (nϭ12), the right and left endocardia were mapped simultaneously by use of a computerized mapping system. AF was induced with 1 to 5 mol/L acetylcholine. The antifibrillatory actions of pilsicainide on AF cycle length (AFCL), refractory period (RP), conduction velocity (CV), excitable gap (EG), and the core of the mother rotor were studied. The RP was defined as the shortest coupling interval that could capture the fibrillating atrium. The EG was estimated as the difference between the AFCL and RP. At baseline, multiple wavefronts were observed. After 2.5 g/mL infusion of pilsicainide, all preparations showed irregular activity, and AF was terminated in 2 preparations. The AFCL and RP were prolonged, and CV was decreased significantly. The EG was widened (147%; PϽ0.01), and the core perimeter was increased (100%; PϽ0.01). Increasing the dosage either terminated AF (6 preparations) or converted to organized activity (ie, atypical atrial flutter) (4 preparations). On the maps, all "unorganized" AFs were terminated with the excitation of the core of the mother rotor by an outside wavefront, whereas in preparations with atrial flutter, pilsicainide did not terminate its activity. Conclusions-Widening

show abstract

“…On the other hand, bepridil is classified as a class IV antiarrhythmic drug because of its relatively strong calcium-channel blocking effect, but it has also shown sodium-and potassium-channel blocking effects, so this multi-ion channel blocker may work as a class I or III antiarrhythmic drug. 3,5,6 Interestingly, the results of the present study showed that bepridil was more effective in preventing PAF with a relatively shorter f-f interval on the ECG before drug administration, which suggests that the main antiarrhythmic action of bepridil for PAF prevention was not class I, but class III.…”

Section: Relationship Between the F-f Interval And The Effect Of Antimentioning

confidence: 57%

“…3,5,6 This suggests that class I drugs are more effective for relatively organized re-entrant arrhythmia, which consists of functional and anatomical block lines as the central obstacle. In contrast, class III drugs tend to be more effective for the re-entrant arrhythmia with a relatively small excitable gap; in other words, a smaller and functionally determined re-entrant circuit.…”

Section: Relationship Between the F-f Interval And The Effect Of Antimentioning

confidence: 99%

Evaluation of the Effect of Bepridil on Paroxysmal Atrial Fibrillation. Relationship Between Efficacy and the f-f Interval in Surface ECG Recordings.

Yoshida

Niwano

Inuo

et al. 2003

Circ J

View full text Add to dashboard Cite

Profiles of Aprindine, Cibenzoline, Pilsicainide and Pirmenol in the Framework of the Sicilian Gambit

Cited by 50 publications

References 97 publications

Topics on the Na+/Ca2+ Exchanger: Pharmacological Characterization of Na+/Ca2+ Exchanger Inhibitors

Topics on the Na+/Ca2+ Exchanger: Pharmacological Characterization of Na+/Ca2+ Exchanger Inhibitors

Widening of the Excitable Gap and Enlargement of the Core of Reentry During Atrial Fibrillation With a Pure Sodium Channel Blocker in Canine Atria

Evaluation of the Effect of Bepridil on Paroxysmal Atrial Fibrillation. Relationship Between Efficacy and the f-f Interval in Surface ECG Recordings.

Contact Info

Product

Resources

About