title: Simultaneous assessment of pharmacokinetics of pilsicainide transdermal patch and its electropharmacological effects on atria of chronic atrioventricular block dogs.
abstract: Pharmacokinetics of pilsicainide transdermal patch and its electropharmacological effects were simultaneously assessed using chronic atrioventricular block dogs. After application of the patch (9.8 mg/kg), pilsicainide was continuously absorbed through the skin with a C(max) of 0.49 +/- 0.13 microg/ml, while its plasma concentration was kept above the clinically reported minimum effective plasma concentration for 2 - 8 h. Inter-atrial conduction time was significantly prolonged, whereas statistically significant prolongation was not detected in the atrial effective refractory period. Prolongation of the cycle length of atrial fibrillation and anti-fibrillatory action were confirmed. Thus, pilsicainide can be absorbed transdermally to exert long-lasting electropharmacological effects leading to anti-atrial fibrillatory action.
authors: Department of Pharmacology, Interdisciplinary Graduate School of Medicine and Engineering, University of Yamanashi, Yamanashi, Japan.
authors: Hiroshi
authors: H
authors: Iwasaki
authors: Akira
authors: A
authors: Takahara
authors: Yuji
authors: Y
authors: Nakamura
authors: Yoshioki
authors: Y
authors: Satoh
authors: Takeshi
authors: T
authors: Nagai
authors: Norihiro
authors: N
authors: Shinkai
authors: Atsushi
authors: A
authors: Sugiyama
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000494:pharmacology*; D001281:Atrial Fibrillation / Q000517:prevention & control; D054537:Atrioventricular Block / Q000503:physiopathology*; D004285:Dogs; D005260:Female; D006325:Heart Atria / Q000187:drug effects*; D008012:Lidocaine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008297:Male
chemical_list: D000889:Anti-Arrhythmia Agents; D008012:Lidocaine; C042288:pilsicainide