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Research ArticleArticle

Carbamazepine Inhibition of Neuronal Na+ Currents: Quantitative Distinction from Phenytoin and Possible Therapeutic Implications

Chung-Chin Kuo, Ren-Shiang Chen, Lu Lu and Rong-Chi Chen
Molecular Pharmacology June 1997, 51 (6) 1077-1083; DOI: https://doi.org/10.1124/mol.51.6.1077
Chung-Chin Kuo
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Ren-Shiang Chen
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Lu Lu
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Rong-Chi Chen
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Abstract

Carbamazepine and phenytoin, two of the most commonly prescribed antiepileptic drugs, have been proposed to share a similar mechanism of action by use-dependent inhibition of Na+ channels. The proposed similar mechanism of action, however, cannot explain the common clinical experiences that the two drugs are different; in some patients, one drug may be more effective than the other. This may occur even when optimal therapeutic concentrations are reached with both medications in plasma or the cerebrospinal fluid. In this study, we show that the action of the two drugs on Na+ channels are quantitatively very different. The affinity between inactivated Na+ channels and carbamazepine (apparent dissociation constant ∼25 μm) is ∼3 times lower than that of phenytoin, yet the binding rate constant of carbamazepine onto the inactivated Na+ channels is ∼38,000m − 1/sec− 1, or ∼5 times faster than that of phenytoin. It is speculated that carbamazepine may be more effective than phenytoin in treating seizures whose ictal depolarization shift is relatively short, whereas a better response to phenytoin may imply abnormal discharges characterized by more prolonged depolarization.

Footnotes

    • Received October 22, 1996.
    • Accepted February 4, 1997.
  • Send reprint requests to: Chung-Chin Kuo, Department of Physiology, National Taiwan University College of Medicine, No. 1 Jen-Ai Rd., 1st Section, Taipei, 100, Taiwan, Republic of China. E-mail: cckuo{at}ntumcl.mc.ntu.edu.tw

  • This work was supported by Grant NSC-85–2331-B-002–195-M10 from the National Science Council, Taiwan, Republic of China.

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 51 (6)
Molecular Pharmacology
Vol. 51, Issue 6
1 Jun 1997
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Research ArticleArticle

Carbamazepine Inhibition of Neuronal Na+ Currents: Quantitative Distinction from Phenytoin and Possible Therapeutic Implications

Chung-Chin Kuo, Ren-Shiang Chen, Lu Lu and Rong-Chi Chen
Molecular Pharmacology June 1, 1997, 51 (6) 1077-1083; DOI: https://doi.org/10.1124/mol.51.6.1077

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Research ArticleArticle

Carbamazepine Inhibition of Neuronal Na+ Currents: Quantitative Distinction from Phenytoin and Possible Therapeutic Implications

Chung-Chin Kuo, Ren-Shiang Chen, Lu Lu and Rong-Chi Chen
Molecular Pharmacology June 1, 1997, 51 (6) 1077-1083; DOI: https://doi.org/10.1124/mol.51.6.1077
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