Journal of Korean Society for Clinical Pharmacology and Therapeutics (임상약리학회지)

Korean Society for Clinical Pharmacology and Therapeutics (대한임상약리학회)
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Tolerability and Pharmacokinetics Following a Single Dose of Vardenafil in Healthy Korean Volunteers

건강한 한국인 자원자에서 바데나필 단회 투여 후 내약성 및 약동학적 특성에 관한 연구

  • Kim, Seokuee (Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital) ;
  • Lee, SeungHwan (Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital) ;
  • Lim, Kyoung Soo (Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital) ;
  • Lim, Hyeong-Seok (Department of Clinical Pharmacology and Therapeutics, University of Ulsan and Asan Medical Center) ;
  • Shin, Sang-Goo (Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital) ;
  • Jang, In-Jin (Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital) ;
  • Yu, Kyung-Sang (Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital)
  • 김석의 (서울대학교 의과대학 임상약리학교실 및 서울대학교병원 임상약리학과) ;
  • 이승환 (서울대학교 의과대학 임상약리학교실 및 서울대학교병원 임상약리학과) ;
  • 임경수 (서울대학교 의과대학 임상약리학교실 및 서울대학교병원 임상약리학과) ;
  • 임형석 (울산대학교 의과대학 임상약리학교실 및 서울아산병원 임상약리학과) ;
  • 신상구 (서울대학교 의과대학 임상약리학교실 및 서울대학교병원 임상약리학과) ;
  • 장인진 (서울대학교 의과대학 임상약리학교실 및 서울대학교병원 임상약리학과) ;
  • 유경상 (서울대학교 의과대학 임상약리학교실 및 서울대학교병원 임상약리학과)
  • Received : 2012.06.21
  • Accepted : 2012.12.05
  • Published : 2012.12.31
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Abstract

Background: Vardenafil is a phosphodiesterase type 5 inhibitor, used in erectile dysfunction. This study aimed to evaluate the pharmacokinetics and tolerability of vardenafil following a single oral administration in healthy male subjects. Methods: A randomized, double-blind, placebo-controlled, single dosing, dose-escalation study was conducted in 30 healthy subjects. A single oral dose of vardenafil or placebo was given to 10 subjects (8 active + 2 placebo) in each dose group of 5, 10 and 20 mg. Serial blood and urine samples were obtained up to 48 hours for pharmacokinetic analysis. Vardenafil and its metabolite were detected by high performance liquid chromatography tandem mass spectrometry assay. Results: A total of 45 adverse events (AE) were reported in 22 subjects, including 5 AEs from placebo treatment, and all the AEs were mild, except one case of moderate nasal stuffiness. Vardenafil was absorbed after a single oral dose, with the $t_{max}$ of 0.5-1.0 hours. The $C_{max}$ and $AUC_{last}$ were $10.21{\pm}3.68$ ug/L($mean{\pm}SD$) and $18.08{\pm}7.44\;ug{\times}h/L$ in 5 mg dose group, $19.79{\pm}12.13$ ug/L and $38.61{\pm}21.04\;ug{\times}h/L$ in 10 mg dose group and $53.16{\pm}37.01$ ug/L and $110.05{\pm}69.65\;ug{\times}h/L$ in 20 mg dose group. Dose-linearity on $AUC_{last}$ and $C_{max}$ of vardenafil were observed in three dose groups. In all dose groups, the fraction excreted in urine was less than 1%. Conclusion: The vardenafil was tolerable over a single dose range of 5 - 20 mg. The pharmacokinetics of vardenfil after a single oral dose was explored and linear pharmacokinetic characteristics were observed over the dose range of 5 - 20 mg in healthy subjects.

Keywords

Acknowledgement

Supported by : 바이엘 코리아

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