Simultaneous Assessment of Pharmacokinetics of Pilsicainide Transdermal Patch and Its Electropharmacological Effects on Atria of Chronic Atrioventricular Block Dogs

Journal of Pharmacological Sciences

Takeshi Nagai¹  Norihiro Shinkai¹  Yuji Nakamura²  Akira Takahara²  Atsushi Sugiyama²  Yoshioki Satoh²  Hiroshi Iwasaki² 

[1] Research & Development Department, Nipro Patch Co., Ltd., Japan;Department of Pharmacology, Interdisciplinary Graduate School of Medicine and Engineering, University of Yamanashi, Japan

关键词: pilsicainide;    transdermal delivery;    atrial fibrillation;   

DOI  :  10.1254/jphs.09061SC

学科分类：药学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(15)Cited-By(7)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 Cmax of 0.49 ± 0.13 μg/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.

【 授权许可】

Unknown