Archives of Pharmacal Research

, Volume 37, Issue 12, pp 1617–1623

Effect of Sophora flavescens on the pharmacokinetics of carbamazepine in rats

Authors

  • Lei Shi
    • Department of Pharmacy, Tangdu HospitalFourth Military Medical University
  • Xue-Liang Dang
    • Department of Pharmacy, Tangdu HospitalFourth Military Medical University
  • Xin-You Liu
    • Department of Pharmacy, Tangdu HospitalFourth Military Medical University
  • Hua-Mei Wei
    • Department of Pharmacy, Tangdu HospitalFourth Military Medical University
  • Meng-Meng Yang
    • Department of Pharmacy, Tangdu HospitalFourth Military Medical University
    • Department of Pharmacy, Tangdu HospitalFourth Military Medical University
Research Article

DOI: 10.1007/s12272-014-0375-8

Cite this article as:
Shi, L., Dang, X., Liu, X. et al. Arch. Pharm. Res. (2014) 37: 1617. doi:10.1007/s12272-014-0375-8

Abstract

Carbamazepine (CBZ), an antiepileptic with narrow therapeutic window, is a substrate of CYP 3A4 which metabolizes CBZ to carbamazepine-10,11-epoxide (CBZE). CBZE is an active and toxicity metabolite, and it is a substrate of MRP-2. Using CBZ for a long time can cause hepatic injury. Sophora flavescens (SF) is a medicinal herb used for the protected hepatic injury. This study investigated the acute and chronic effects of SF on the pharmacokinetics of CBZ in rats. The concentrations of CBZ and CBZE in plasma and tissues were determined by HPLC method. The results showed that SF which significantly decreased the AUC0-t of CBZ, increased CBZE conversely. Tissue analysis showed that the concentrations of CBZ and CBZE in brain and liver were decreased by SF. In addition, the distribution of CBZE in kidney was reduced significantly, which influenced the CBZE excretion and increased the drug toxic potentially. Results in the current study suggest that patients using CBZ might be cautioned in the use of SF extract or Sophora-derived products. Meanwhile, patients receiving drugs which are substrates of CYP 3A4 and/or MRP-2 should be advised of the potential herb–drug interaction to reduce the risk of therapeutic failure or increased toxicity of conventional drug therapy.

Keywords

Sophora flavescensCarbamazepineCarbamazepine-10,11-epoxidePharmacokineticsHerb–drug interaction

Copyright information

© The Pharmaceutical Society of Korea 2014