Drug Interactions between rifampin and selumetinib

Selumetinib should be taken on an empty stomach, at least one hour before or two hours after a meal. Do not consume grapefruit, grapefruit juice, or any supplements that contain grapefruit extract during treatment with selumetinib unless directed otherwise by your doctor. Grapefruit juice can increase the blood levels of selumetinib. This may increase the risk and/or severity of serious side effects such as diarrhea; colitis (inflammation of the colon); skin rashes; cardiomyopathy (a condition that affects the heart muscle and its ability to pump blood); rhabdomyolysis (a rare condition involving the breakdown of skeletal muscle tissue that can cause kidney damage and death); and eye problems that can lead to blindness. Talk to your doctor if you have any questions or concerns. You should seek prompt medical attention if you experience severe diarrhea; severe skin reactions (rash over a large area of the body, peeling skin, blisters); signs and symptoms of heart trouble (persistent coughing or wheezing, shortness of breath, swelling of ankles and feet, fatigue, increased heart rate); muscle problems (unexplained muscle pain, tenderness or weakness, especially with fever and/or dark colored urine); or vision problems (blurred vision, light sensitivity, dark spots or floaters, vision loss). It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

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GENERALLY AVOID: Concurrent use of rifampin in patients who ingest alcohol daily may result in an increased incidence of hepatotoxicity. The increase in hepatotoxicity may be due to an additive risk as both alcohol and rifampin are individually associated with this adverse reaction. However, the exact mechanism has not been established.

ADJUST DOSING INTERVAL: Administration with food may reduce oral rifampin absorption, increasing the risk of therapeutic failure or resistance. In a randomized, four-period crossover phase I study of 14 healthy male and female volunteers, the pharmacokinetics of single dose rifampin 600 mg were evaluated under fasting conditions and with a high-fat meal. Researchers observed that administration of rifampin with a high-fat meal reduced rifampin peak plasma concentration (Cmax) by 36%, nearly doubled the time to reach peak plasma concentration (Tmax) but reduced overall exposure (AUC) by only 6%.

MANAGEMENT: The manufacturer of oral forms of rifampin recommends administration on an empty stomach, 30 minutes before or 2 hours after meals. Patients should be encouraged to avoid alcohol or strictly limit their intake. Patients who use alcohol and rifampin concurrently or have a history of alcohol use disorder may require additional monitoring of their liver function during treatment with rifampin.