Pharmacokinetics and Pharmacodynamics of Entacapone and Tolcapone after Acute and Repeated Administration: A Comparative Study in the Rat

@article{Forsberg2003PharmacokineticsAP,
  title={Pharmacokinetics and Pharmacodynamics of Entacapone and Tolcapone after Acute and Repeated Administration: A Comparative Study in the Rat},
  author={M. Forsberg and M. Lehtonen and M. Heikkinen and J. Savolainen and T. J{\"a}rvinen and P. M{\"a}nnist{\"o}},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2003},
  volume={304},
  pages={498 - 506}
}
Two catechol-O-methyltransferase (COMT) inhibitors, entacapone and tolcapone, were compared in the rat to elucidate the actual differences between their pharmacokinetics and pharmacodynamics after single and repeated administration. Their inhibitory potencies were also compared in vitro. After intravenous administration (3 mg/kg), the elimination half-life (t 1/2β) of entacapone (0.8 h) was clearly shorter than that of tolcapone (2.9 h). The striatum/serum ratio of tolcapone was 3-fold higher… Expand

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