FUDR
FUDR - General Information
An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract. [PubChem]
Pharmacology of FUDR
FUDR is a pyrimidine analog that acts as an inhibitor of the S-phase of cell division. This selectively kills rapidly dividing cells. FUDR is an anti-metabolite. Anti-metabolites masquerade as pyramidine-like molecules which prevents normal pyrimidines from being incorporated into DNA during the S phase of the cell cycle. Flurouracil (the end-product of catabolism of floxuridine) blacks an enzyme which converts cytosine nucleosides into the deoxy derivative. In addition, DNA synthesis is further inhibited because fluoruracil blocks the incorporation of the thymdine nucleotide into the DNA strand.
FUDR for patients
Patients should be informed of expected toxic effects, particularly oral manifestations. Patients should be alerted to the possibility of alopecia as a result of therapy and should be informed that it is usually a transient effect.
FUDR Interactions
Combination Therapy: Any form of therapy which adds to the stress of the patient, interferes with nutrition or depresses bone marrow function will increase the toxicity of Floxuridine.
FUDR Contraindications
FUDR therapy is contraindicated for patients in a poor nutritional state, those with depressed bone marrow function or those with potentially serious infections.
Additional information about FUDR
FUDR Indication: For palliative management of gastrointestinal adenocarcinoma metastatic to the liver, when given by continuous regional intra-arterial infusion in carefully selected patients who are considered incurable by surgery or other means.
Mechanism Of Action: FUDR is rapidly catabolized to 5-fluorouracil which is the active form of the drug. Fluorouracil inhibits thymydilate synthase leading to inhibition of DNA synthesis, RNA synthesis and cell death.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Floxuridine
Synonyms: 5 Fluorodeoxyuridine; 5FDU; Deoxyfluorouridine; FDUR; FDURD; Floxiridina [Inn-Spanish]; Floxuridinum [Inn-Latin]; Floxuridin; Fluorodeoxyuridine; Fluoruridine Deoxyribose
Drug Category: Antineoplastics; Antimetabolites
Drug Type: Small Molecule; Approved
Other Brand Names containing Floxuridine: FUDR;
Absorption: Not Available
Toxicity (Overdose): Oral, rat LD50: 215 mg/kg. Signs of overdose include nausea, vomiting, diarrhea, gastrointestinal ulceration and bleeding, and bone marrow depression (including thrombocytopenia, leukopenia and agranulocytosis).
Protein Binding: Not Available
Biotransformation: Hepatic.
Half Life: Not Available
Dosage Forms of FUDR: Powder, for solution Intra-arterial
Chemical IUPAC Name: 5-fluoro-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
Chemical Formula: C9H11FN2O5
Floxuridine on Wikipedia: https://en.wikipedia.org/wiki/Floxuridine
Organisms Affected: Humans and other mammals
