Pazopanib Hydrochloride and Food

Do not consume grapefruit or grapefruit juice during treatment with PAZOPanib unless directed otherwise by your doctor. Grapefruit juice can increase the blood levels of PAZOPanib, which may lead to an increased risk of serious side effects such as liver damage, irregular heart rhythm, bleeding, high blood pressure, heart attack, and stroke. Taking PAZOPanib with food can also significantly increase its absorption and levels in the blood. Therefore, you should take PAZOPanib on an empty stomach, at least one hour before or two hours after eating. Call your doctor immediately if you develop fever, chills, joint pain or swelling, unusual bleeding or bruising, skin rash, itching, loss of appetite, fatigue, nausea, vomiting, dark colored urine, and/or yellowing of the skin or eyes, as these may be signs and symptoms of liver damage. You should also seek immediate medical attention if you experience signs and symptoms that could indicate cardiovascular problems such as sudden dizziness; lightheadedness; fainting; fast or pounding heartbeats; chest pain or tightness; pain in your arms, back, neck, or jaw; shortness of breath; numbness or weakness on one side of your body; and slurred speech or difficulty speaking. 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.

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of pazopanib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. Although not studied, the interaction may increase the risk of QT interval prolongation and torsade de pointes arrhythmia as well as severe and fatal hepatotoxicity associated with the use of pazopanib.

ADJUST DOSING INTERVAL: Food increases the oral bioavailability of pazopanib. The mechanism of interaction is unknown. Administration of pazopanib with a high-fat or low-fat meal results in an approximately 2-fold increase in peak plasma concentration (Cmax) and systemic exposure (AUC).

MANAGEMENT: Patients treated with pazopanib should avoid consumption of grapefruit, grapefruit juice, and any supplement containing grapefruit extract. Pazopanib should be administered at least one hour before or two hours after a meal.