Fluorouracil

GoodRx

Fluorouracil 50 mg/mL · injectable solution

Misc., Injections & Implants

OFF-LABELNot in the FDA label for this product

Bleb needling after trabeculectomy

Subconjunctival 5-fluorouracil at the needling site, dose and concentration varying by protocol

NMA · no difference shown

A systematic review with network meta-analysis of needling revision compared mitomycin C, 5-fluorouracil and no antimetabolite at all. It found no significant difference between them in intraocular pressure at 12 months or latest follow-up, complication rates, qualified or complete success, or the number of re-needling cases. Six studies met inclusion and only one was randomised, and the authors attribute an overall low quality of evidence to that design mix and call for further research. So this is no difference SHOWN, not a difference ruled out.

Halili A, Kessel L, Subhi Y, Bach-Holm D. Needling after trabeculectomy - does augmentation by anti-metabolites provide better outcomes and is Mitomycin C better than 5-Fluoruracil? A systematic review with network meta-analyses. Acta Ophthalmol. 2020;98(7):643-653

Contraindications

None.

Available Forms

500 mg/10 mL vial, 50 mg/mL vial, 1 g/20 mL, 50 mg/mL vials, 10 mL vials, 20 mL vials

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.

Warnings & Precautions

Cardiotoxicity: Fluorouracil can cause cardiotoxicity, including angina, myocardial infarction/ischemia, arrhythmia, and heart failure. Withhold fluorouracil for cardiac toxicity.
Hyperammonemic Encephalopathy: Altered mental status, confusion, disorientation, coma, or ataxia with elevated serum ammonia level can occur within 72 hours of initiation of fluorouracil. Withhold fluorouracil and initiate ammonia-lowering therapy.
Neurologic Toxicity: Fluorouracil can cause acute cerebellar syndrome, confusion, disorientation, ataxia, or visual disturbances. Withhold fluorouracil for neurologic toxicity.
Diarrhea: Fluorouracil can cause severe diarrhea. Withhold fluorouracil for severe diarrhea until resolved.
Palmar-Plantar Erythrodysesthesia (Hand-Foot Syndrome): Fluorouracil can cause hand-foot syndrome. If severe, discontinue fluorouracil until resolved or decreased to Grade 1, then resume at a reduced dose.
Myelosuppression: Fluorouracil can cause severe and fatal myelosuppression. Withhold fluorouracil until severe myelosuppression resolves, then resume at a reduced dose.

Common Side Effects

Reported adverse reactions include cardiotoxicity, hyperammonemic encephalopathy, neurologic toxicity, diarrhea, palmar-plantar erythrodysesthesia (hand-foot syndrome), myelosuppression, mucositis, and increased risk of elevated INR when administrated with warfarin. Ophthalmic reactions include lacrimal duct stenosis, visual changes, lacrimation, photophobia.

Pregnancy & Lactation

Pregnancy: There are no adequate and well-controlled studies with fluorouracil in pregnant women. Based on its mechanism of action, fluorouracil can cause fetal harm when administered to a pregnant woman.

Lactation: It is not known whether fluorouracil or its metabolites are present in human milk.

Pediatric Use

The safety and effectiveness in pediatric patients have not been established.