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Floxuridine

Drug Nomenclature

FloxuridineSynonyms: 5-Fluorouracil Deoxyriboside; FUDR; Floxuridina; NSC-27640; WR-138720
USAN: Floxuridine
INN: Floxuridine [rINN (en)]
INN: Floxuridina [rINN (es)]
INN: Floxuridine [rINN (fr)]
INN: Floxuridinum [rINN (la)]
INN: Флоксуридин [rINN (ru)]
Chemical name: 2´-Deoxy-5-fluorouridine; 5-Fluoro-2´-deoxyuridine; 1-(2-Deoxy-β-d-ribofuranosyl)-5-fluoropyrimidine-2,4(1H,3H)-dione
Molecular formula: C9H11FN2O5 =246.2
CAS: 50-91-9

Pharmacopoeias. In US.

The United States Pharmacopeia 31, 2008 (Floxuridine). Store in airtight containers at a temperature of 25°, excursions permitted between 15° and 30°. Protect from light.

Adverse Effects, Treatment, and Precautions

As for Fluorouracil. Adverse reactions after intra-arterial infusion often include local reactions, thromboembolic complications, and infection or bleeding at the catheter site, or blockage of the catheter. Erythema, stomatitis, and gastrointestinal disturbances are relatively common. There have also been signs of liver dysfunction.

Effects on the liver

Serious biliary toxicity has been reported in over half of all patients receiving hepatic arterial infusions of floxuridine, usually manifesting as sclerosing cholangitis or acalculous cholecystitis; as a result some surgeons routinely remove the gallbladder at the time of infusion pump implantation. Extrahepatic biliary stenosis with jaundice and cholestasis has also been described; the authors suggest that this could lead to intra-hepatic biliary damage from bile stasis and infection, recurrent cholangitis, and biliary sclerosis. Floxuridine infusions have also been associated with a case of fatal progressive cirrhosis of the liver in the absence of overt cholestasis. Pseudoaneurysms of the hepatic artery, leading to serious retroperitoneal or gastrointestinal bleeding, have also been described.

Interactions

As for Fluorouracil.

Pharmacokinetics

Floxuridine is poorly absorbed from the gastrointestinal tract and it is usually given by injection. Floxuridine is metabolised mainly in the liver to fluorouracil after rapid injection. When given by slow intra-arterial infusion, more of the drug is metabolised to floxuridine monophosphate (F-dUMP). It is excreted as carbon dioxide via the lungs; some is excreted, as unchanged drug and metabolites, in urine. Floxuridine crosses the blood-brain barrier to some extent and is found in CSF.

Uses and Administration

Floxuridine is an antineoplastic which acts as an antimetabolite, either by conversion to fluorouracil (after rapid injection), or, when given by slow intra-arterial infusion, partly via floxuridine monophosphate (F-dUMP), which produces greater inhibition of DNA synthesis.

Floxuridine is used in the palliative treatment of hepatic metastases of colorectal cancer — see Malignant Neoplasms of the Liver. It has been tried in some other solid neoplasms. Doses of 100 to 600 micrograms/kg daily are given by continuous hepatic arterial infusion, usually with the aid of an infusion pump, until toxicity occurs.

White cell and platelet counts should be carried out regularly during therapy and treatment should be stopped if the white cell count falls rapidly or if the white cell or platelet count falls below acceptable levels (see also Bone-marrow Depression), or if major adverse effects occur.

Preparations

The United States Pharmacopeia 31, 2008: Floxuridine for Injection.

Proprietary Preparations

USA: FUDR.

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