Related Experiment Video
Updated: Nov 18, 2025

Author Spotlight: Genetic Profiling for Fluorouracil Response in Gastric Cancer
Published on: May 10, 2024
Genetic Polymorphism Effect on Warfarin-Rifampin Interaction: A Case Report and Review of Literature
Muhammad Salem1, Islam Eljilany2, Ahmed El-Bardissy1
1Department of Pharmacy, Hamad General Hospital, Doha, Qatar.
Abstract:
Warfarin-rifampin interaction has been reported since the 1970s. Due to rifampin's strong induction of CYP2C9, most cases could not attain the target international normalized ratio (INR) despite warfarin dose escalation. Genetic polymorphisms determine up to 50% of warfarin dose variability. A 38-year-old woman was started on warfarin and rifampin for cerebral venous sinus thrombosis and pulmonary tuberculosis. Over six weeks, the daily warfarin dose was increased from 3 to 10 mg to attain three consecutive in-clinic therapeutic INRs. She completed three complications-free months of warfarin treatment with time in therapeutic range (TTR) of 46%. We performed retrospective genetic testing to determine the patient's CYP2C9, CYP4F2, and VKORC1 genotypes and whether they had affected the interaction outcome. The analysis revealed that the subject carries CYP2C9*3*3 and VKORC1-1639 (GA) mutations, classifying her as a slow metabolizer and, hence, highly warfarin-sensitive. This was reflected on how the case responded to a relatively lower dose than previously reported cases that did not achieve the target on warfarin daily doses up to 35 mg. This is the first report addressing the genotype effect on this interaction. Patients with genetic variants requiring low warfarin doses are more likely to respond at a feasible dose while on rifampin. Future studies to evaluate warfarin-rifampin-gene interaction are warranted.
Insights
Genetic factors influence warfarin dosing during rifampin treatment. A patient with specific gene variants achieved therapeutic international normalized ratio (INR) levels on a lower warfarin dose, suggesting genotype impacts this drug interaction.
Area of Science:
- Pharmacogenomics
- Drug Interactions
- Internal Medicine
Background:
- The interaction between warfarin and rifampin is well-documented, with rifampin's induction of CYP2C9 often necessitating high warfarin doses.
- Genetic polymorphisms in warfarin-metabolizing enzymes and targets significantly affect individual dose requirements, accounting for up to 50% of variability.
Related Concept Videos
Effect of Hepatic Disease on Pharmacokinetics: Dose Adjustments Due to Hepatic Impairment
Pharmacokinetics: Drug–Drug Interactions
Effect of Hepatic Disease on Pharmacokinetics: Active Drug, Metabolite and Fraction of Metabolized Drug
Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Metabolism
Pharmacokinetics: Drug–Food and Drug–Viral Interactions
Factors Affecting Protein-Drug Binding: Drug Interactions
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...

