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Chemical Compound Review

Pilsicainida     N-(2,6-dimethylphenyl)-2- (1,2,3,5,6,7...

Synonyms: Pilsicainide, Pilzicainide, Pilsicainidum, CHEMBL163238, SureCN142244, ...
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Disease relevance of Pilsicainide

  • OBJECTIVES: The purposes of this study were to measure the atrial refractory period and the conduction velocity (CV) during atrial fibrillation (AF) and to explore the antiarrhythmic mechanism of a sodium channel blocker, pilsicainide, during AF [1].
  • RESULTS: Ventricular arrhythmia was not induced by administration of pilsicainide in 55 patients (no-VA group) [2].
  • Administration of pilsicainide-induced VA in 10 patients (Pil-VA group) and polymorphic ventricular tachycardia in four patients [2].
  • Ischemia enhances use-dependent sodium channel blockade by pilsicainide, a class IC antiarrhythmic agent [3].
  • The aim of this study was to elucidate whether the electrophysiologic properties of pilsicainide, a novel class IC drug with slow kinetic properties, could be altered in the presence of acute myocardial ischemia [3].

High impact information on Pilsicainide


Chemical compound and disease context of Pilsicainide


Biological context of Pilsicainide


Anatomical context of Pilsicainide


Associations of Pilsicainide with other chemical compounds


Gene context of Pilsicainide

  • Pilsicainide significantly decreased AP amplitude (APA) and Max dV/dt in both control and T4-treated rat atrial cells [7].
  • Conduction delay was increased (total QRS: 112.2 +/- 6.3 msec to 131.7 +/- 6.3 msec; under 40 microV: 42.0 +/- 8.5 msec to 52.7 +/- 12.7 msec; last 40 msec: 17.4 +/- 5.9 microV to 10.4 +/- 6.1 microV) on SAECG by pilsicainide [21].
  • Effects of Na+ channel blocker, pilsicainide, on HERG current expressed in HEK-293 cells [22].
  • These results suggest C/D is increased in patients with high CRP levels because of binding of pilsicainide to protein, resulting decreased clearance [13].
  • Images in cardiology: Successful treatment of atrial tachycardia-induced cardiomyopathy with pilsicainide [23].

Analytical, diagnostic and therapeutic context of Pilsicainide


  1. Determination of refractory periods and conduction velocity during atrial fibrillation using atrial capture in dogs: direct assessment of the wavelength and its modulation by a sodium channel blocker, pilsicainide. Shinagawa, K., Mitamura, H., Takeshita, A., Sato, T., Kanki, H., Takatsuki, S., Ogawa, S. J. Am. Coll. Cardiol. (2000) [Pubmed]
  2. Ventricular arrhythmia induced by sodium channel blocker in patients with Brugada syndrome. Morita, H., Morita, S.T., Nagase, S., Banba, K., Nishii, N., Tani, Y., Watanabe, A., Nakamura, K., Kusano, K.F., Emori, T., Matsubara, H., Hina, K., Kita, T., Ohe, T. J. Am. Coll. Cardiol. (2003) [Pubmed]
  3. Ischemia enhances use-dependent sodium channel blockade by pilsicainide, a class IC antiarrhythmic agent. Sadanaga, T., Ogawa, S. J. Am. Coll. Cardiol. (1994) [Pubmed]
  4. Severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency: first case presentation showing competition for excretion via renal multidrug resistance protein 1 and organic cation transporter 2. Tsuruoka, S., Ioka, T., Wakaumi, M., Sakamoto, K., Ookami, H., Fujimura, A. Clin. Pharmacol. Ther. (2006) [Pubmed]
  5. Effect of cimetidine and probenecid on pilsicainide renal clearance in humans. Shiga, T., Hashiguchi, M., Urae, A., Kasanuki, H., Rikihisa, T. Clin. Pharmacol. Ther. (2000) [Pubmed]
  6. Class IC antiarrhythmic drugs, flecainide and pilsicainide, produce ST segment elevation simulating inferior myocardial ischemia. Nakamura, W., Segawa, K., Ito, H., Tanaka, S., Yoshimoto, N. J. Cardiovasc. Electrophysiol. (1998) [Pubmed]
  7. Effect of sodium channel blocker, pilsicainide hydrochloride, on net inward current of atrial myocytes in thyroid hormone toxicosis rats. Yamakawa, M., Sunagawa, M., Shimabukuro, M., Higa, N., Takasu, N., Kosugi, T. Thyroid (2005) [Pubmed]
  8. Effects of pilsicainide and propafenone on vagally induced atrial fibrillation: role of suppressant effect in conductivity. Iwasa, A., Okumura, K., Tabuchi, T., Tsuchiya, T., Tsunoda, R., Matsunaga, T., Tayama, S., Yasue, H. Eur. J. Pharmacol. (1998) [Pubmed]
  9. Slow abnormal conduction in the low right atrium: its anatomic basis and relevance to atrial reentry. Yamashita, T., Oikawa, N., Inoue, H., Murakawa, Y., Nakajima, T., Usui, M., Ajiki, K., Ohkawa, S., Sugimoto, T. Am. Heart J. (1994) [Pubmed]
  10. Pilsicainide-induced verapamil sensitive idiopathic left ventricular tachycardia. Nagai, T., Suyama, K., Shimizu, W., Noda, T., Satomi, K., Kurita, T., Aihara, N., Kamakura, S. Pacing and clinical electrophysiology : PACE. (2006) [Pubmed]
  11. Modes of the Na channel blocking action of pilsicainide, a new antiarrhythmic agent, in cardiac cells. Hattori, Y., Inomata, N. Jpn. J. Pharmacol. (1992) [Pubmed]
  12. Electrophysiologic and hemodynamic effects of a single oral dose of pilsicainide hydrochloride, a new class 1c antiarrhythmic agent. Ino, T., Atarashi, H., Kuruma, A., Onodera, T., Saitoh, H., Hayakawa, H. J. Cardiovasc. Pharmacol. (1998) [Pubmed]
  13. Effect of protein binding of pilsicainide on the pharmacokinetics. Fukumoto, K., Tanemura, M., Tsuchishita, Y., Kusumoto, M., Matsumoto, K., Kamakura, S., Ueno, K. Drug Metab. Pharmacokinet. (2005) [Pubmed]
  14. Pilsicainide for atrial fibrillation. Kumagai, K., Nakashima, H., Tojo, H., Yasuda, T., Noguchi, H., Matsumoto, N., Ogawa, M., Saku, K. Drugs (2006) [Pubmed]
  15. T wave alternans in an in vitro canine tissue model of Brugada syndrome. Morita, H., Zipes, D.P., Lopshire, J., Morita, S.T., Wu, J. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  16. Differentiation of the electrophysiological effects on the atrial myocardium between the pure na channel blocker, pilsicainide, and flecainide. Kanemoto, M., Shimizu, A., Yamagata, T., Esato, M., Ueyama, T., Yoshiga, Y., Kakugawa, H., Kametani, R., Inoue, N., Sawa, A., Matsuzaki, M. Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy. (2004) [Pubmed]
  17. Inhibitory effects of antiarrhythmic drugs on phenacetin O-deethylation catalysed by human CYP1A2. Kobayashi, K., Nakajima, M., Chiba, K., Yamamoto, T., Tani, M., Ishizaki, T., Kuroiwa, Y. British journal of clinical pharmacology. (1998) [Pubmed]
  18. Enhancement of J-ST-segment elevation by the glucose and insulin test in Brugada syndrome. Nogami, A., Nakao, M., Kubota, S., Sugiyasu, A., Doi, H., Yokoyama, K., Yumoto, K., Tamaki, T., Kato, K., Hosokawa, N., Sagai, H., Nakamura, H., Nitta, J., Yamauchi, Y., Aonuma, K. Pacing and clinical electrophysiology : PACE. (2003) [Pubmed]
  19. Effects of pilsicainide on systemic hemodynamics and cardiac function of anesthetized dogs. Sakanashi, M., Noguchi, K., Matsuzaki, T., Ojiri, Y., Nakasone, J., Itomine, T., Higuchi, M., Shiroma, N. Cardioscience. (1993) [Pubmed]
  20. Effects of antiarrhythmic drugs on apoptotic pathways in H9c2 cardiac cells. Isomoto, S., Kawakami, A., Arakaki, T., Yamashita, S., Yano, K., Ono, K. J. Pharmacol. Sci. (2006) [Pubmed]
  21. Relatively benign clinical course in asymptomatic patients with brugada-type electrocardiogram without family history of sudden death. Takenaka, S., Kusano, K.F., Hisamatsu, K., Nagase, S., Nakamura, K., Morita, H., Matsubara, H., Emori, T., Ohe, T. J. Cardiovasc. Electrophysiol. (2001) [Pubmed]
  22. Effects of Na+ channel blocker, pilsicainide, on HERG current expressed in HEK-293 cells. Wu, L.M., Orikabe, M., Hirano, Y., Kawano, S., Hiraoka, M. J. Cardiovasc. Pharmacol. (2003) [Pubmed]
  23. Images in cardiology: Successful treatment of atrial tachycardia-induced cardiomyopathy with pilsicainide. Nakazato, Y., Nakata, Y. Heart (2001) [Pubmed]
  24. Dispersion of signal-averaged P wave duration on precordial body surface in patients with paroxysmal atrial fibrillation. Yamada, T., Fukunami, M., Shimonagata, T., Kumagai, K., Sanada, S., Ogita, H., Asano, Y., Hori, M., Hoki, N. Eur. Heart J. (1999) [Pubmed]
  25. Pilsicainide for conversion and maintenance of sinus rhythm in chronic atrial fibrillation: a placebo-controlled, multicenter study. Okishige, K., Nishizaki, M., Azegami, K., Igawa, M., Yamawaki, N., Aonuma, K. Am. Heart J. (2000) [Pubmed]
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