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Int J Med Sci 2011; 8(5):406-412. doi:10.7150/ijms.8.406

Research Paper

Effects of Bolus Injection of 5-Fluorouracil on Steady-State Plasma Concentrations of 5-Fluorouracil in Japanese Patients with Advanced Colorectal Cancer

Takao Tamura 1,2, Akiko Kuwahara2,3, Kaori Kadoyama 2,4, Motohiro Yamamori2,3, Kohshi Nishiguchi 2,5, Tsubasa Inokuma 4, Yoshiji Takemoto 4, Naoko Chayahara 2, Tatsuya Okuno 2, Ikuya Miki 2, Yoshimi Fujishima2, Toshiyuki Sakaeda 2,4 ✉

1. Kinki University Nara Hospital, Nara 630-0293, Japan
2. Kobe University Graduate School of Medicine, Kobe 650-0017, Japan
3. School of Pharmacy and Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya 663-8179, Japan
4. Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto 606-8501, Japan
5. Department of Clinical Pharmacy, Kyoto Pharmaceutical University, Kyoto 607-8414, Japan


Objectives: The irinotecan (CPT-11) + 5-fluorouracil (5-FU)/leucovorin (LV) + UFT/LV chemotherapy, in which repetitive oral administration of UFT/LV replaces the infusion of 5-FU/LV in the FOLFIRI regimen, has been proposed previously. In this study, five of 10 patients were injected with a bolus of 5-FU and the other were not injected with it in order to examine the effect of omitting it in terms of pharmacokinetics of 5-FU.

Methods: The treatment consisted of the intravenous infusions of CPT-11 at 100 mg/m2 and l-LV at 15 mg/m2, and the injection of a bolus of 5-FU at 500 mg/m2 on day 1, and the repetitive oral administration of UFT/LV (300 mg/m2/day as tegafur + 75 mg/day of LV) on days 1-5. A total of 13 measurements of the plasma concentrations of uracil, 5-FU and tegafur were made per patient within 48 hr after the start of chemotherapy and the value of area under the concentration-time curve (AUC0-48) was evaluated. The plasma concentration was also determined at 2 weeks to assess long-term exposure to 5-FU.

Results: The plasma concentrations of 5-FU at 24 hr after the start of treatment were 27.4 ng/mL and 9.4 ng/mL in the patients with and without the bolus injection, respectively. At 48 hr, they were 31.3 ng/mL and 10.4 ng/mL with the AUC0-48 values of 22.16 mg*h/L and 0.65 mg*h/L, respectively. The 5-FU was detected in the plasma at 226 hr after the last administration of UFT/LV for the patients with the bolus injection, but not for those without.

Conclusion: A bolus of 5-FU on day 1 provided long-term exposure to 5-FU.

Keywords: 5-fluorouracil, UFT, bolus injection, constant infusion, pharmacokinetics

This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) License. See for full terms and conditions.
How to cite this article:
Tamura T, Kuwahara A, Kadoyama K, Yamamori M, Nishiguchi K, Inokuma T, Takemoto Y, Chayahara N, Okuno T, Miki I, Fujishima Y, Sakaeda T. Effects of Bolus Injection of 5-Fluorouracil on Steady-State Plasma Concentrations of 5-Fluorouracil in Japanese Patients with Advanced Colorectal Cancer. Int J Med Sci 2011; 8(5):406-412. doi:10.7150/ijms.8.406. Available from