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

被引：16

作者：

Iwasaki, Hiroshi ^{[1
]}

Takahara, Akira ^{[1
]}

Nakamura, Yuji ^{[1
]}

Satoh, Yoshioki ^{[1
]}

Nagai, Takeshi ^{[2
]}

Shinkai, Norihiro ^{[2
]}

Sugiyama, Atsushi ^{[1
,3
]}

机构：

[1] Univ Yamanashi, Dept Pharmacol, Interdisciplinary Grad Sch Med & Engn, Chuo Ku, Yamanashi 4093898, Japan

[2] Nipro Patch Co Ltd, Dept Res & Dev, Kasukabe, Saitama 3440057, Japan

[3] Yamanashi Res Ctr Clin Pharmacol, Yamanashi 4060032, Japan

来源：

JOURNAL OF PHARMACOLOGICAL SCIENCES | 2009年 / 110卷 / 03期

关键词：

pilsicainide; transdermal delivery; atrial fibrillation; TORSADES-DE-POINTES; ANTIARRHYTHMIC DRUGS; CHANNEL BLOCKER; FIBRILLATION; MODELS; HEART;

D O I：

10.1254/jphs.09061SC

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 mu g/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.

引用

页码：410 / 414

页数：5

共 15 条

[1]

AISAKA K, 1988, ARZNEIMITTELFORSCH, V38-2, P1417

[2] Conversion of recent-onset atrial fibrillation by a single oral dose of pilsicainide (Pilsicainide Suppression Trial on Atrial Fibrillation) [J].