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Anticoagulants: In vitro studies have shown bicalutamide can displace coumarin anticoagulants, such as warfarin, from their protein-binding sites. It is recommended that if bicalutamide is started in patients already receiving coumarin anticoagulants, closely monitor prothrombin times and adjust the anticoagulant dose if necessary.
Cytochrome P-450 system: R-bicalutamide is an inhibitor of CYP3A4. Coadministration with midazolam has shown mean midazolam levels increased 1.5-fold (for maximum plasma concentration) and 1.9-fold (for area under the curve). Exercise caution when bicalutamide is coadministered with CYP3A4 substrates.
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