Drug information of Floxuridine

Floxuridine is catabolized to fluorouracil after intra-arterial administration, resulting in activity similar to fluorouracil; inhibits thymidylate synthetase and disrupts DNA and RNA synthesis.

Metabolism

Hepatic; Active metabolites: Floxuridine monophosphate (FUDR-MP) and fluorouracil; Inactive metabolites: Urea, CO2, α-fluoro-β-alanine, α-fluoro-β-guanidopropionic acid, α-fluoro-β-ureidopropionic acid, and dihydrofluorouracil

Excretion

Urine: As fluorouracil, urea, α-fluoro-β-alanine, α-fluoro-β-guanidopropionic acid, α-fluoro-β-ureidopropionic acid, and dihydrofluorouracil; Respiratory (as exhaled gases [CO2])

Colorectal cancer, hepatic metastases: Palliative management of hepatic metastases of colorectal cancer (administered by continuous regional hepatic intra-arterial infusion) in select patients considered incurable by surgical resection or other means.

Usual Adult Dose for Liver Metastasis in Adenocarcinoma

Recommended dose: 0.1 to 0.6 mg/kg/day by continuous arterial infusion; the higher dosage ranges (0.4 mg to 0.6 mg) are usually used for hepatic artery infusion because the liver metabolizes the drug (thus reducing the potential for systemic toxicity)

1-Safety and efficacy have not been established in patients younger than 18 years.

2-Poor nutritional states; depressed bone marrow function; potentially serious infections

>10%:

Gastrointestinal: Diarrhea (may be dose limiting), stomatitis

Hematologic & oncologic: Anemia, bone marrow depression (nadir: 7-10 days; may be dose limiting), leukopenia, thrombocytopenia

1% to 10%:

Dermatologic: Alopecia, dermatitis, localized erythema, skin hyperpigmentation, skin photosensitivity

Gastrointestinal: Anorexia, biliary sclerosis, cholecystitis

Hepatic: Jaundice

1-Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

-Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

-Signs of bleeding like throwing up or coughing up blood; vomit that looks like coffee grounds; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a cause or that get bigger; or bleeding you cannot stop.

-Signs of infection like fever, chills, very bad sore throat, ear or sinus pain, cough, more sputum or change in color of sputum, pain with passing urine, mouth sores, or wound that will not heal.

-Feeling very tired or weak.

-Chest pain or pressure.

-Mouth irritation or mouth sores.

-Diarrhea.

-Very upset stomach or throwing up.

-Very bad belly pain.

-Dark urine or yellow skin or eyes.

2-Injection route (Powder for Solution)

All patients should be hospitalized for initiation of the first course of therapy with floxuridine because of the possibility of severe toxic reactions.

3-This drug is a highly toxic drug with a narrow margin of safety. Patients should be carefully supervised since therapeutic response is unlikely to occur without some evidence of toxicity.

1-You may have more chance of getting an infection. Wash hands often. Stay away from people with infections, colds, or flu.

2-You may bleed more easily. Be careful and avoid injury. Use a soft toothbrush and an electric razor.

3-If you have upset stomach, throwing up, diarrhea, or are not hungry, talk with your doctor. There may be ways to lower these side effects.

4-Talk with your doctor before getting any vaccines. Use of some vaccines with floxuridine may either raise the chance of an infection or make the vaccine not work as well.

5-Use birth control that you can trust to prevent pregnancy while taking floxuridine.

Storage

Store intact vials at 20°C to 25°C (68°F to 77°F). Reconstituted vials are stable for up to 2 weeks under refrigeration at 2°C to 8°C (36°F to 46°F). Follow USP 797 recommendations for beyond use dates based on the level of risk for preparation.