Lack of pharmacokinetic interaction between pilsicainide and rifampicin in healthy volunteers

Tsuyoshi Shiga, Masayuki Hashiguchi, Koichi Nakamura, Mikiko Shimizu, Kaoru Shimizu, Atsushi Suzuki, Mayumi Mochizuki, Nobuhisa Hagiwara

研究成果: Article


Pilsicainide, a class Ic antiarrhythmic agent, is a cationic compound. It has been hypothesized that a P-glycoprotein(P-gp)-induced transport mechanism may mediate the intestinal absorption and the renal excretion of pilsicainide. We evaluated whether rifampicin, a known inducer of P-gp, affects the pharmacokinetics of pilsicainide after oral dosing in healthy subjects. A pharmacokinetic study was conducted on 8 healthy male subjects (aged 30 ±8 years: body weight 65.7 ±6.5 kg) and demonstrated that rifampicin (450 mg given orally once daily for 4 days) did not significantly affect the maximum plasma concentration (pilsicainide alone: 0.39 ± 0.15 versus pilsicainide + rifampicin: 0.36±0.06μg/mL), the time to maximum plasma concentration(1.38± 0.83 versus 1.06±0.18h), the area under the plasma concentration-time curve(2.81 ±0.91 versus 2.58±0.62 μg·h/mL), the renal clearance (198.46±85.93 versus 194.34±69.91 mL/min) or the net renal clearance by tubular secretion(128.75±73.56 versus 119.93 ±79.84 mL/min) of pilsicainide after a single oral dose(50 mg). In conclusion, our results indicated that rifampicin did not affect the pharmacokinetics of pilsicainide after oral dosing in humans.

ジャーナルJapanese Journal of Clinical Pharmacology and Therapeutics
出版物ステータスPublished - 2013 7 1


ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)