Fluorouracil

— THERAPEUTIC CATEGORIES —
  • Breast cancer
  • Colorectal and other GI cancers
  • Pancreatic, thyroid, and other endocrine cancers

Fluorouracil Generic Name & Formulations

General Description

Fluorouracil 50mg/mL; soln for IV inj or infusion.

Pharmacological Class

Antimetabolite.

How Supplied

Contact supplier.

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 Indications

Indications

Adenocarcinoma of the breast.

Fluorouracil Dosage and Administration

Adult

Give by IV bolus or IV infusion. Individualize. As a component of a cyclophosphamide-based multidrug regimen: 500mg/m2 or 600mg/m2 on Days 1 and 8 every 28 days for 6 cycles.

Children

Not established.

Fluorouracil Contraindications

Not Applicable

Fluorouracil Boxed Warnings

Not Applicable

Fluorouracil Warnings/Precautions

Warnings/Precautions

Increased risk of serious, including fatal, adverse reactions in patients with certain homozygous or compound heterozygous DPYD variants: not recommended. Withhold or permanently discontinue if evidence of acute early-onset or unusually severe reactions occur. Consider testing for genetic DYPD variants prior to initiation. Hyperammonemic encephalopathy may occur within 72hrs after initiating therapy; withhold and initiate ammonia-lowering therapy if occurs. Withhold if cardiotoxicity, neurologic toxicity, Grade 3/4 diarrhea, Grade 2/3 palmar-plantar erythrodysesthesia (hand-foot syndrome), Grade 4 myelosuppression, or Grade 3/4 mucositis occurs. Monitor CBCs prior to each treatment cycle, weekly if administered on a weekly or similar schedule, and as needed. Embryo-fetal toxicity. Advise females of reproductive potential and males w. female partners to use effective contraception during and for 3 months after the last dose. Pregnancy (Cat. D): may cause fetal harm. Nursing mothers: not recommended. 

 

Fluorouracil Pharmacokinetics

Metabolism

Hepatic.

Elimination

Renal. Half-life: 8 to 20 minutes.

Fluorouracil Interactions

Interactions

Potentiated by leucovorin. Monitor closely for INR or prothrombin time with concomitant coumarin-derivative anticoagulants (eg, warfarin).

Fluorouracil Adverse Reactions

Adverse Reactions

Stomatitis, esophagopharyngitis, GI upset, anorexia, leukopenia, alopecia, dermatitis, hand-foot syndrome; others.

Fluorouracil Clinical Trials

See Literature

Fluorouracil Note

Notes

Testing considerations: TS (thymidylate synthase), MSI (microsatellite instability), DPD (dihydropyrimidine dehydrogenase). Formerly known under the brand name Adrucil.

Fluorouracil Patient Counseling

See Literature

Fluorouracil Generic Name & Formulations

General Description

Fluorouracil 50mg/mL; soln for IV inj or infusion.

Pharmacological Class

Antimetabolite.

How Supplied

Contact supplier.

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 Indications

Indications

Adenocarcinoma of the colon, rectum, and stomach.

Fluorouracil Dosage and Administration

Adult

Give by IV bolus or IV infusion. Individualize. Colon or rectum adenocarcinoma: infusional regimen: (in combination with leucovorin alone or with leucovorin and oxaliplatin or irinotecan): 400mg/m2 via IV bolus on Day 1, then 2400mg/m2 to 3000mg/m2 via continuous infusion over 46 hours every 2 weeks. Bolus dosing regimen: 500mg/m2 via IV bolus on Days 1, 8, 15, 22, 29, and 36 in 8-week cycles. Gastric adenocarcinoma: as a component of a platinum-containing multidrug chemotherapy regimen: 200mg/m2 to 1000mg/m2 via continuous infusion over 24hrs.

Children

Not established.

Fluorouracil Contraindications

Not Applicable

Fluorouracil Boxed Warnings

Not Applicable

Fluorouracil Warnings/Precautions

Warnings/Precautions

Increased risk of serious, including fatal, adverse reactions in patients with certain homozygous or compound heterozygous DPYD variants: not recommended. Withhold or permanently discontinue if evidence of acute early-onset or unusually severe reactions occur. Consider testing for genetic DYPD variants prior to initiation. Hyperammonemic encephalopathy may occur within 72hrs after initiating therapy; withhold and initiate ammonia-lowering therapy if occurs. Withhold if cardiotoxicity, neurologic toxicity, Grade 3/4 diarrhea, Grade 2/3 palmar-plantar erythrodysesthesia (hand-foot syndrome), Grade 4 myelosuppression, or Grade 3/4 mucositis occurs. Monitor CBCs prior to each treatment cycle, weekly if administered on a weekly or similar schedule, and as needed. Embryo-fetal toxicity. Advise females of reproductive potential and males w. female partners to use effective contraception during and for 3 months after the last dose. Pregnancy (Cat. D): may cause fetal harm. Nursing mothers: not recommended. 

 

Fluorouracil Pharmacokinetics

Metabolism

Hepatic.

Elimination

Renal. Half-life: 8 to 20 minutes.

Fluorouracil Interactions

Interactions

Potentiated by leucovorin. Monitor closely for INR or prothrombin time with concomitant coumarin-derivative anticoagulants (eg, warfarin).

Fluorouracil Adverse Reactions

Adverse Reactions

Stomatitis, esophagopharyngitis, GI upset, anorexia, leukopenia, alopecia, dermatitis, hand-foot syndrome; others.

Fluorouracil Clinical Trials

See Literature

Fluorouracil Note

Notes

Testing considerations: TS (thymidylate synthase), MSI (microsatellite instability), DPD (dihydropyrimidine dehydrogenase). Formerly known under the brand name Adrucil.

Fluorouracil Patient Counseling

See Literature

Fluorouracil Generic Name & Formulations

General Description

Fluorouracil 50mg/mL; soln for IV inj or infusion.

Pharmacological Class

Antimetabolite.

How Supplied

Contact supplier.

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 Indications

Indications

Adenocarcinoma of the pancreas.

Fluorouracil Dosage and Administration

Adult

Give by IV bolus or IV infusion. Individualize. In combination with leucovorin or as a component of a multidrug chemotherapy regimen: 400mg/m2 via IV bolus on Day 1, followed by 2400mg/m2 via continuous infusion over 46hrs every 2 weeks.

Children

Not established.

Fluorouracil Contraindications

Not Applicable

Fluorouracil Boxed Warnings

Not Applicable

Fluorouracil Warnings/Precautions

Warnings/Precautions

Increased risk of serious, including fatal, adverse reactions in patients with certain homozygous or compound heterozygous DPYD variants: not recommended. Withhold or permanently discontinue if evidence of acute early-onset or unusually severe reactions occur. Consider testing for genetic DYPD variants prior to initiation. Hyperammonemic encephalopathy may occur within 72hrs after initiating therapy; withhold and initiate ammonia-lowering therapy if occurs. Withhold if cardiotoxicity, neurologic toxicity, Grade 3/4 diarrhea, Grade 2/3 palmar-plantar erythrodysesthesia (hand-foot syndrome), Grade 4 myelosuppression, or Grade 3/4 mucositis occurs. Monitor CBCs prior to each treatment cycle, weekly if administered on a weekly or similar schedule, and as needed. Embryo-fetal toxicity. Advise females of reproductive potential and males w. female partners to use effective contraception during and for 3 months after the last dose. Pregnancy (Cat. D): may cause fetal harm. Nursing mothers: not recommended. 

 

Fluorouracil Pharmacokinetics

Metabolism

Hepatic.

Elimination

Renal. Half-life: 8 to 20 minutes.

Fluorouracil Interactions

Interactions

Potentiated by leucovorin. Monitor closely for INR or prothrombin time with concomitant coumarin-derivative anticoagulants (eg, warfarin).

Fluorouracil Adverse Reactions

Adverse Reactions

Stomatitis, esophagopharyngitis, GI upset, anorexia, leukopenia, alopecia, dermatitis, hand-foot syndrome; others.

Fluorouracil Clinical Trials

See Literature

Fluorouracil Note

Notes

Testing considerations: TS (thymidylate synthase), MSI (microsatellite instability), DPD (dihydropyrimidine dehydrogenase). Formerly known under the brand name Adrucil.

Fluorouracil Patient Counseling

See Literature