Therapeutic Classification: antineoplastics
Pharmacologic Classification: antimetabolites
Absorption: Well absorbed after oral administration.
Distribution: Unknown.
Metabolism/Excretion: Metabolized mostly in tissue and by the liver to 5-fluorouracil; 5-fluorouracil is metabolized by dihydropyrimidine dehydrogenase to a less toxic compound; inactive metabolites are excreted primarily in urine.
Half-life: 45 min.
(plasma concentrations)
†Onset of antineoplastic effect is 6 wk.
†Peak 5-fluorouracil concentrations occur at 2 hr.
CV: edema, arrhythmias, chest pain, HF, MYOCARDIAL ISCHEMIA/INFARCTION, SUDDEN CARDIAC DEATH.
Derm: dermatitis, hand-and-foot syndrome, nail disorder, alopecia, erythema, rash, STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS.
EENT: eye irritation, epistaxis, rhinorrhea.
F and E: dehydration.
GI: abdominal pain, anorexia, constipation, diarrhea, hyperbilirubinemia, ↑liver enzymes, nausea, stomatitis, vomiting, dyspepsia, NECROTIZING ENTEROCOLITIS, xerostomia.
GU: acute renal failure, ↓ fertility.
Hemat: anemia, neutropenia, thrombocytopenia.
MS: arthralgia, myalgia.
Neuro: dysgeusia, fatigue, headache, dizziness, insomnia, peripheral neuropathy.
Resp: cough, dyspnea.
Misc: fever.
Colorectal Cancer
Adjuvant Treatment of Colon Cancer- PO (Adults): Monotherapy: 1250 mg/m2 twice daily for the first 14 days of each 21-day cycle for a maximum of 8 cycles. In combination with oxaliplatin: 1000 mg/m2 twice daily for the first 14 days of each 21-day cycle for a maximum of 8 cycles.
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: ↓initial dose by 25%.
Perioperative Treatment of Rectal Cancer- PO (Adults): Without concomitant radiation: 1250 mg/m2 twice daily. With concomitant radiation: 825 mg/m2 twice daily.
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: ↓initial dose by 25%.
Unresectable or Metastatic Colorectal Cancer- PO (Adults): Monotherapy: 1250 mg/m2 twice daily for the first 14 days of each 21-day cycle; continue until disease progression or unacceptable toxicity. In combination with oxaliplatin: 1000 mg/m2 twice daily for the first 14 days of each 21-day cycle; continue until disease progression or unacceptable toxicity.
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: ↓initial dose by 25%.
Advanced or Metastatic Breast Cancer
- PO (Adults): Monotherapy or in combination with docetaxel: 1000 mg/m2 or 1250 mg/m2 twice daily for the first 14 days of each 21-day cycle; continue until disease progression or unacceptable toxicity.
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: ↓initial dose by 25%.
Gastric, Esophageal, or Gastroesophageal Junction Cancer
Unresectable or Metastatic Gastric, Esophageal, or Gastroesophageal Junction Cancer- PO (Adults): 625 mg/m2 twice daily on Days 1–21 of each 21-day cycle for a maximum of 8 cycles (in combination with platinum-containing chemotherapy) OR 850 mg/m2 or 1000 mg/m2 twice daily for the first 14 days of each 21-day cycle (in combination with oxaliplatin); continue until disease progression or unacceptable toxicity.
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: ↓initial dose by 25%.
HER-2 Overexpressing Metastatic Gastric or Gastroesophageal Junction Cancer- PO (Adults): In combination with cisplatin and trastuzumab: 1000 mg/m2 twice daily for the first 14 days of each 21-day cycle; continue until disease progression or unacceptable toxicity.
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: ↓initial dose by 25%.
Pancreatic Cancer
- PO (Adults): In combination with gemcitabine: 830 mg/m2 twice daily for the first 21 days of each 28-day cycle; continue until disease progression, unacceptable toxicity, or a maximum of 6 cycles.
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: ↓initial dose by 25%.
80 yr.