Different Influences on Tacrolimus Pharmacokinetics by Coadministrations of Zhi Ke and Zhi Shi in Rats
Joint Authors
Lin, Shiuan-Pey
Chao, Pei-Dawn Lee
Tsai, Shang-Yuan
Hou, Yu-Chi
Fang, Shih-Hua
Wang, Meng-Ju
Wu, Ping-Ping
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-6, 6 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-01-20
Country of Publication
Egypt
No. of Pages
6
Main Subjects
Abstract EN
Tacrolimus, an immunosuppressant with narrow therapeutic window, has been used widely in transplant patients.
Grapefruit juice and pomelo have been reported to increase the blood levels of tacrolimus.
Zhi Ke and Zhi Shi, the ripe peels and unripe fruits of Citrus aurantium which is chemotaxonomically related to grapefruit and pomelo, are in wide use in clinical Chinese medicine.
To investigate the possible interaction of these two Citrus herbs with tacrolimus, male Sprague-Dawley rats were orally given tacrolimus (1.5 mg/kg) with and without Zhi Ke and Zhi Shi decoctions in a cross-over design.
Blood samples were withdrawn via cardiopuncture at specific time and quantitated by a microparticle enzyme immunoassay.
In addition, to explore the mechanism of interaction, LS 180 cell line was used for the transport study of rhodamine 123, a typical substrate of P-glycoprotein (P-gp).
The results showed that Zhi Shi significantly decreased the Cmax and AUC0-t of tacrolimus by 72.4% and 72.0%, respectively, whereas Zhi Ke did not affect tacrolimus pharmacokinetics.
LS 180 cell line study indicated that Zhi Shi increased the efflux activity of P-gp, enabling us to explain the decreased oral bioavailability of tacrolimus caused by Zhi Shi.
Hence, we suggest that Zhi Shi be contraindicated for transplant patients treated with tacrolimus to reduce the risk of allograft rejection.
American Psychological Association (APA)
Lin, Shiuan-Pey& Wu, Ping-Ping& Hou, Yu-Chi& Tsai, Shang-Yuan& Wang, Meng-Ju& Fang, Shih-Hua…[et al.]. 2011. Different Influences on Tacrolimus Pharmacokinetics by Coadministrations of Zhi Ke and Zhi Shi in Rats. Evidence-Based Complementary and Alternative Medicine،Vol. 2011, no. 2011, pp.1-6.
https://search.emarefa.net/detail/BIM-495874
Modern Language Association (MLA)
Lin, Shiuan-Pey…[et al.]. Different Influences on Tacrolimus Pharmacokinetics by Coadministrations of Zhi Ke and Zhi Shi in Rats. Evidence-Based Complementary and Alternative Medicine No. 2011 (2011), pp.1-6.
https://search.emarefa.net/detail/BIM-495874
American Medical Association (AMA)
Lin, Shiuan-Pey& Wu, Ping-Ping& Hou, Yu-Chi& Tsai, Shang-Yuan& Wang, Meng-Ju& Fang, Shih-Hua…[et al.]. Different Influences on Tacrolimus Pharmacokinetics by Coadministrations of Zhi Ke and Zhi Shi in Rats. Evidence-Based Complementary and Alternative Medicine. 2011. Vol. 2011, no. 2011, pp.1-6.
https://search.emarefa.net/detail/BIM-495874
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-495874