Floxuridine: Difference between revisions

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{{intro}}Floxuridine (FUDR) is a pyrimidine analogue used as an antineoplastic agent, usually as a continuous hepatic arterial infusion to treat hepatic metastases from colon cancer. 
== Floxuridine ==


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[[File:Floxuridine_Biosynthesis.png|thumb|right|Biosynthesis of Floxuridine]]
Intraarterial floxuridine is associated with a very high rate of serum enzyme and [[bilirubin]] elevations during therapy, and with frequent biliary damage that can result in a secondary sclerosing cholangitis, which can be severe and lead to cirrhosis. 


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'''Floxuridine''' is a chemotherapeutic agent used primarily in the treatment of [[cancer]]. It is an antimetabolite that interferes with the synthesis of [[DNA]], thereby inhibiting the growth of rapidly dividing cancer cells. Floxuridine is particularly effective in the treatment of [[gastrointestinal cancer]]s, especially those that have metastasized to the [[liver]].
Floxuridine (flox ure' i deen) is a fluoropyrimidine (fluorodeoxyuridine; FUDR) that has antineoplastic action against several solid tumors including liver, gastrointestinal adenocarcinoma and colorectal cancers.  Floxuridine, like fluorouracil, requires conversion to monophosphate and possibly the triphosphate.  It appears to act by inhibition of production or direct competition with thymidine triphosphate, which is necessary for [[DNA]] synthesis. 


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== Mechanism of Action ==
Floxuridine was approved for use as an [[anticancer]] agent in the United States in 1970 and is given predominantly by continuous infusion into the hepatic artery to treat metastatic carcinoma of the colon or following resection of colon cancer metastases. 


{{dose}}
Floxuridine is a fluorinated pyrimidine analog. It is converted into 5-fluorouracil (5-FU) in the body, which is then metabolized into active metabolites that disrupt the synthesis of DNA and [[RNA]]. The primary mechanism involves the inhibition of the enzyme [[thymidylate synthase]], which is crucial for the synthesis of thymidine, a nucleotide necessary for DNA replication. By inhibiting this enzyme, floxuridine effectively halts the proliferation of cancer cells.
Floxuridine is available as a powder for reconstitution in 500 mg vials (5 mL, 100 mg/mL) in several generic forms.  Floxuridine is typically given by infusion pump into the hepatic artery in a dose of 0.1 to 0.6 mg/kg/day.  Because the liver metabolizes floxuridine, administration by direct infusion into the hepatic artery deceases the systemic [[side effects]] which can be severe. 


{{se}}
== Administration ==
Common [[side effects]] of intraarterial therapy include [[bone marrow suppression]], [[fatigue]], weakness, [[headache]], [[dizziness]], insomnia, paresthesias, abdominal pain, constipation, [[diarrhea]], dyspepsia, [[nausea]], stomatitis, and rash.


{{cancer drugs}}  
Floxuridine is typically administered via continuous [[intravenous infusion]] directly into the [[hepatic artery]]. This method allows for high concentrations of the drug to be delivered directly to liver tumors, maximizing its efficacy while minimizing systemic exposure and side effects.
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== Side Effects ==
 
The side effects of floxuridine are similar to those of other antimetabolites and include [[nausea]], [[vomiting]], [[diarrhea]], and [[myelosuppression]]. Myelosuppression can lead to decreased production of blood cells, resulting in [[anemia]], increased risk of [[infection]], and [[bleeding]].
 
== Biosynthesis ==
 
The biosynthesis of floxuridine involves the incorporation of a fluorine atom into the pyrimidine ring, creating a compound that can mimic the natural nucleoside [[uridine]]. This modification allows floxuridine to be incorporated into RNA and DNA, disrupting their normal function and leading to cell death.
 
== Related Pages ==
 
* [[Chemotherapy]]
* [[Antimetabolite]]
* [[Thymidylate synthase]]
* [[5-Fluorouracil]]
* [[Cancer treatment]]
 
[[Category:Chemotherapy]]
[[Category:Antimetabolites]]
[[Category:Cancer treatments]]

Latest revision as of 11:08, 15 February 2025

Floxuridine[edit]

Biosynthesis of Floxuridine

Floxuridine is a chemotherapeutic agent used primarily in the treatment of cancer. It is an antimetabolite that interferes with the synthesis of DNA, thereby inhibiting the growth of rapidly dividing cancer cells. Floxuridine is particularly effective in the treatment of gastrointestinal cancers, especially those that have metastasized to the liver.

Mechanism of Action[edit]

Floxuridine is a fluorinated pyrimidine analog. It is converted into 5-fluorouracil (5-FU) in the body, which is then metabolized into active metabolites that disrupt the synthesis of DNA and RNA. The primary mechanism involves the inhibition of the enzyme thymidylate synthase, which is crucial for the synthesis of thymidine, a nucleotide necessary for DNA replication. By inhibiting this enzyme, floxuridine effectively halts the proliferation of cancer cells.

Administration[edit]

Floxuridine is typically administered via continuous intravenous infusion directly into the hepatic artery. This method allows for high concentrations of the drug to be delivered directly to liver tumors, maximizing its efficacy while minimizing systemic exposure and side effects.

Side Effects[edit]

The side effects of floxuridine are similar to those of other antimetabolites and include nausea, vomiting, diarrhea, and myelosuppression. Myelosuppression can lead to decreased production of blood cells, resulting in anemia, increased risk of infection, and bleeding.

Biosynthesis[edit]

The biosynthesis of floxuridine involves the incorporation of a fluorine atom into the pyrimidine ring, creating a compound that can mimic the natural nucleoside uridine. This modification allows floxuridine to be incorporated into RNA and DNA, disrupting their normal function and leading to cell death.

Related Pages[edit]