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Updated: Aug 23, 2026

High-throughput Identification of Synergistic Drug Combinations by the Overlap2 Method
Published on: May 21, 2018
Potential interaction between telithromycin and warfarin
Likurgos Kolilekas1, George K Anagnostopoulos, Ioannis Lampaditis
1Department of Pulmonary Medicine, Hellenic Air Force and Veterans General Hospital, Athens, Greece. lykol@yahoo.gr
Objective:
To report a case of warfarin-telithromycin interaction resulting in an elevated international normalized ratio (INR) and hemoptysis.
Case Summary:
A 73-year-old white man developed an elevated INR and mild hemoptysis as a result of an interaction between warfarin and telithromycin 800 mg/day. The INR increased from 3.1 before telithromycin was started to 11 after 5 days of telithromycin therapy. The INR returned to the therapeutic range 4 days after telithromycin was discontinued.
Discussion:
Telithromycin is the first member of the macrolide subclass of ketolides and offers potential advantages over traditional macrolides/azalides for community-acquired respiratory tract infections caused by macrolide-resistant pathogens. As of July 16, 2004, bleeding complications and an increased INR as a result of an interaction between warfarin and telithromycin have not been described. Although the mechanism for this interaction remains unknown, it is suspected that it is a result of the inhibition of the metabolism of the R-isomer of warfarin, which is metabolized predominantly by CYP1A2 and less by CYP3A4. Further research is required to elucidate this issue. An objective causality assessment revealed that this adverse drug event as a result of the warfarin and telithromycin interaction was probable.
Conclusions:
We recommend close monitoring of INR levels in patients on warfarin who receive telithromycin therapy in an effort to control and prevent bleeding complications.
Insights
A case report highlights a significant drug interaction between warfarin and telithromycin, leading to elevated international normalized ratio (INR) and bleeding. Close monitoring of INR is crucial for patients on warfarin receiving telithromycin to prevent complications.
Area of Science:
- Pharmacology
- Clinical Medicine
- Drug Interactions
Background:
- Warfarin is a common anticoagulant requiring regular monitoring of the international normalized ratio (INR).
- Telithromycin, a ketolide antibiotic, is used for respiratory tract infections.
- Drug interactions can alter the efficacy and safety of anticoagulant therapy.
Observation:
- A 73-year-old male patient experienced elevated INR and hemoptysis while on warfarin therapy.
- The patient was concurrently treated with telithromycin 800 mg/day.
- INR levels rose from 3.1 to 11 within 5 days of telithromycin initiation.
Findings:
- Discontinuation of telithromycin led to INR normalization within 4 days.
- This interaction between warfarin and telithromycin has not been previously described.
- The mechanism is suspected to involve inhibition of warfarin metabolism, possibly via CYP1A2 or CYP3A4 pathways.
Implications:
- Healthcare providers should be aware of the potential for warfarin-telithromycin interactions.
- Close INR monitoring is recommended for patients on warfarin who are prescribed telithromycin.
- This case underscores the importance of vigilance in managing polypharmacy and preventing adverse drug events.
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