Fluorouracil (7 brand names, 3 dosage forms, 3 routes)
Available dosage forms: INJECTABLE, CREAM, SOLUTION.
Routes of administration: INJECTION, TOPICAL, INTRAVENOUS.
Brand Names
- ADRUCIL
- CARAC
- EFUDEX
- FAVLYXA
- FLUOROPLEX
- FLUOROURACIL
- TOLAK
Boxed Warning
Increased Risk of Serious Adverse Reactions or Death in Patients with Complete DPD Deficiency Test patients for genetic variants of DPYD prior to initiating fluorouracil unless immediate treatment is necessary. Avoid use of fluorouracil in patients with certain homozygous or compound heterozygous DPYD variants that result in complete DPD deficiency [see Warnings and Precautions (5.1)].
Indications and Usage
Fluorouracil is indicated for the treatment of patients with:
Contraindications
None.
Adverse Reactions
The following adverse reactions are discussed in more detail in other sections of the labeling: •Serious Adverse Reactions or Death from Dihydropyrimidine Dehydrogenase (DPD) Deficiency [see Warnings and Precautions (5.1)] •Cardiotoxicity [see Warnings and Precautions (5.2)] •Hyperammonemic encephalopathy [see Warnings and Precautions (5.3)] •Neurologic toxicity [see Warnings and Precautions (5.4)] •Diarrhea [see Warnings and Precautions (5.5)] •Palmar-plantar erythrodysesthesia (hand-foot syndrome) [see Warnings and Precautions (5.6)] •Myelosuppression [see Warnings and Precautions (5.7)] •Mucositis [see Warnings and Precautions (5.8)] •Increased risk of elevated INR when administered with warfarin [see Warnings and Precautions (5.9)]
Mechanism of Action
Fluorouracil is a nucleoside metabolic inhibitor that interferes with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibits the formation of ribonucleic acid (RNA); these affect rapidly growing cells and may lead to cell death. Fluorouracil is converted to three main active metabolites: 5-fluoro-2′-deoxyuridine-5′-monophosphate (FdUMP), 5-fluorouridine-5′- triphosphate (FUTP) and 5-fluoro-2′-deoxyuridine-5′-triphosphate (FdUTP). These metabolites have several effects including the inhibition of thymidylate synthase by FdUMP, incorporation of FUTP into RNA and incorporation of FdUTP into DNA.
Overdosage
Administer uridine triacetate within 96 hours following the end of fluorouracil infusion for management of fluorouracil overdose.