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Floxuridine

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Ongondi Timothy
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24 views10 pages

Floxuridine

Uploaded by

Ongondi Timothy
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PDF, TXT or read online on Scribd
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Floxuridine

Beryl Gesare Achei


GMOP/M/3834/09/24
Floxuridine
• Drug name: Floxuridine /Fluorodeoxyuridine FUdR
• Drug class: Antimetabolite, Pyrimidine Analog
• Mechanism of action: Floxuridine is catabolized to fluorouracil after
intra-arterial administration, resulting in activity similar to
fluorouracil; inhibits thymidylate synthetase and disrupts DNA and
RNA synthesis.
• Cell-cycle specific for the S-Phase
Pharmacokinetics
Administration: Intra-arterial; continuous infusion into the hepatic
artery using an infusion pump.
The response rate is about 40-50% or double that which is achieved by
intravenous infusions.
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 10%,; Respiratory 60% (as exhaled gases CO2)
Pharmacokinetics…Cont’d
Hepatic artery infusion pump
Indications
• Treatment of unresectable intrahepatic metastases in
cholangiocarcinoma and colorectal cancer

Hepatic artery infusion: 0.1-0.6 mg/kg/day (with dexamethasone and


heparin) as a continuous infusion for 14 days plus IV chemotherapy on
Day 1 & 15.
Intrahepatic arterial infusion for 14-21 days causes minimal systemic
toxicity.
Dose limiting ADR
• Hepatotoxicity - Floxuridine can cause both parenchymal and
cholestatic injury
Parenchymal injury – increased levels of transaminases AST, ALT
Cholestatic- biliary sclerosis, biliary strictures, permanent jaundice,
cholangitis
ADR Management
Hepatotoxicity; Biliary sclerosis, Moninor ALP, AST, bilirubin levels
cholecystitis, jaundice, increased Dose reductions
transaminase levels
Gastroenteritis/Diarrhea/ GI ulceration Monitor for symptoms
and bleeding/ Intractable Discontinue treatment
vomiting/Stomatitis/Esophagopharyngitis Supportive care

Bone marrow toxicity; leukopenia Withhold treatment until recovery


(WBC<3.5x10^9), thrombocytopenia
<100,000
Myocardial ischaemia,
Dermatologic: Alopecia, dermatitis, Moisturizers, Sunscreens
localized erythema, skin
hyperpigmentation, skin photosensitivity
ADR…Cont’d
Serum bilirubin, transaminases, or alkaline phosphatase
Parameter Dose Modification
Serum bilirubin ≥1.2 × ULN to <1.5 × ULN Administer 80% of the floxuridine dose.
Alkaline phosphatase ≥1.2 × ULN to <1.5 × ULN
Serum bilirubin ≥1.5 × ULN to <2 × ULN, Administer 50% of the floxuridine dose
Transaminases 3 × baseline
Alkaline phosphatase ≥1.5 × ULN to <2 × ULN
Serum bilirubin ≥2 × ULN, Withhold until recovery to normal levels
Transaminases >3 × baseline, or
Alkaline phosphatase ≥2 × ULN
Monitoring Parameters
• Monitor CBC with differential
• Liver function (bilirubin, alkaline phosphatase, and transaminases);
• ADR monitor for signs/symptoms of stomatitis/esophagopharyngitis,
gastrointestinal ulceration/bleeding, hemorrhage, vomiting, and/or
diarrhea.
Storage
• Floxuridine for Injection, USP, 500 mg, lyophilized, in a 5 mL vial
• The sterile powder should be stored at 20° to 25°

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