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Updated: Aug 13, 2026

High-throughput Identification of Synergistic Drug Combinations by the Overlap2 Method
Published on: May 21, 2018
An adverse interaction between warfarin and fluoropyrimidines revisited
1Division of Hematology/Oncology and Department of Clinical Pharmacology/Toxicology, Comprehensive Cancer Center, University of Alabama at Birmingham 35294-3300, USA. wasif.saif@ccc.uab.edu
Patients taking capecitabine or 5-fluorouracil with warfarin may experience dangerous bleeding due to altered coagulation. Frequent monitoring of anticoagulant response is crucial for dose adjustment.
Area of Science:
- Oncology
- Pharmacology
- Hematology
Background:
- Fluoropyrimidines like 5-fluorouracil (5-FU) and capecitabine are standard chemotherapy for various cancers.
- Warfarin is a widely prescribed oral anticoagulant.
- Concomitant use of capecitabine/5-FU and warfarin can lead to altered coagulation and bleeding events.
Purpose of the Study:
- To review the literature on the interaction between capecitabine/5-FU and warfarin.
- To describe the clinical presentation and mechanism of altered coagulation.
- To provide monitoring guidelines for patients receiving both agents.
Main Methods:
- Literature review of reported cases and studies.
- Analysis of clinical presentations and coagulation parameter changes (INR, PTT).
- Comparison of interactions between 5-FU and capecitabine, including other agents like uracil/tegafur.
Main Results:
- Capecitabine/5-FU can significantly increase INR and PTT in patients stabilized on warfarin.
- Altered coagulation can occur days to months after starting or even stopping chemotherapy.
- Events observed in patients with and without liver metastases; mechanism under investigation.
Conclusions:
- The interaction between capecitabine/5-FU and warfarin necessitates frequent monitoring of anticoagulant response (INR/PTT).
- Dose adjustments of anticoagulants are critical to manage altered coagulation and prevent bleeding.
- FDA and manufacturers have issued warnings regarding this drug interaction.
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