Classifications: antineoplastic; antimetabolite, pyrimidine; Therapeutic: antineoplastic; antimetabolite
Prototype: 5-Fluorouracil (5-FU)
Pregnancy Category: D
150 mg, 500 mg tablets
Pyrimidine antagonist and cell cycle-specific antimetabolite. Prodrug of 5-FU. Blocks actions of enzymes essential to normal
DNa and RNA synthesis. May become incorporated into RNA molecules of tumor cells, thereby interfering with RNA and protein
Reduces or stabilizes tumor size in metastatic breast cancer.
Metastatic breast cancer refractory to other treatments, colorectal cancer, single-agent adjuvant therapy for colon cancer
Hypersensitivity to capecitabine, doxifluridine, 5-FU; myelosuppression; dihydropyrimidine dehydrogenase (DPD) deficiency;
females of childbearing age; active infection; jaundice; severe renal failure or impairment; pregnancy (category D); lactation,
children <18 y.
Mild to moderate renal or hepatic dysfunction; bacterial or viral infection; coronary artery disease, angina, cardiac arrhythmias;
history of varicella zoster or other herpes infections; older adults.
Route & Dosage
|Breast Cancer, Colorectal Cancer
Adult: PO 2500 mg/m2/d in 2 divided doses x 2 wk, then 1 wk off. Repeat.
Clcr 3050 mL/min: reduce dose by 25%; <30 mL/min: do not use
- Morning and evening doses (about 12 h apart) should be given within 30 min of the end of a meal. Water is the preferred
liquid for taking this drug.
Adverse Effects (≥1%)Body as a Whole: Fatigue,
pyrexia, pain, myalgia. CV:
Edema. GI: Severe diarrhea, nausea, vomiting, stomatitis,
abdominal pain, constipation
, dyspepsia, anorexia. Hematologic: Neutropenia, thrombocytopenia, anemia, lymphopenia. Metabolic:
Dehydration, hyperbilirubinemia. CNS:
Paresthesias, headache, dizziness, insomnia
. Skin: Hand-and-foot syndrome, dermatitis,
nail disorder. Special Senses:
increases concentration and toxicity of 5-FU,
altered coagulation and/or bleeding reported with warfarin. Food:
Food decreases extent of absorption.
Absorption significantly reduced by food. Peak:
1.52 h. Distribution:
Approx 35% protein bound. Metabolism:
Extensively metabolized to 5-FU. Elimination:
In urine. Half-Life:
Assessment & Drug Effects
- Lab tests: Monitor periodically CBC with differential and liver functions including bilirubin, transaminases, alkaline phosphatase.
- Monitor carefully for S&S of grade 2 or greater toxicity: diarrhea >4 BMs/day or at night; vomiting >1 time/24 h; significant
loss of appetite or anorexia; stomatitis; hand-and-foot syndrome (pain, swelling, erythema, desquamation, blistering); temperature
= 100.5° F; and S&S of infection.
- Withhold drug and immediately report S&S of grade 2 or greater toxicity.
- Monitor for dehydration and replace fluids as needed.
- Monitor carefully patients with coronary artery disease for S&S of cardiotoxicity (e.g., increasing angina).
Patient & Family Education
- Report immediately significant nausea, loss of appetite, diarrhea, soreness of tongue, fever of 100.5° F or more, or
signs of infection. Review patient drug package insert carefully for more detail.
- Inform physician immediately if you become pregnant.