Therapeutic Classification: antineoplastics
Pharmacologic Classification: antimetabolites
Absorption: Minimal absorption (5–10%) after topical application.
Distribution: Widely distributed; concentrates and persists in tumors.
Metabolism/Excretion: Metabolized by dihydropyrimidine dehydrogenase to a less toxic compound; inactive metabolites are excreted primarily in urine.
Half-Life: 20 hr.
(IV = effects on blood counts, Top = dermatologic effects)
| ROUTE | ONSET | PEAK | DURATION |
|---|
| IV | 1–9 days | 9–21 days (nadir) | 30 days |
| Top | 2–3 days | 2–6 wk | 1–2 mo |
More likely to occur with systemic use than with topical use
CV: CARDIOTOXICITY
Derm: alopecia, maculopapular rash, local inflammatory reactions (topical only), melanosis of nails, nail loss, palmar-plantar erythrodysesthesia, phototoxicity
Endo: sterility
GI: diarrhea, nausea, stomatitis, vomiting
Hemat: anemia, leukopenia, thrombocytopenia
Local: thrombophlebitis
Neuro: acute cerebellar dysfunction
Misc: fever
- Doses may vary greatly, depending on tumor, patient condition, and protocol used
Advanced Colorectal Cancer
- IV (Adults ): In combination with leucovorin alone or leucovorin + oxaliplatin or irinotecan: 400 mg/m2 as IV bolus on Day 1, then 2400–3000 mg/m2 continuous infusion every 2 wk; In combination with leucovorin: 500 mg/m2 as IV bolus 1 hr after leucovorin on Days 1, 8, 15, 22, 29, and 36 every 8 wk.
Breast Cancer
- IV (Adults ): In combination with cyclophosphamide + epirubicin or cyclophosphamide + methotrexate: 500 mg/m2 or 600 mg/m2 on Days 1 and 28 every 28 days for 6 cycles.
Gastric Adenocarcinoma
- IV (Adults ): As part of platinum-containing regimen: 200–1000 mg/m2 as IV infusion (frequency of administration and number of cycles depends on specific regimen used).
Pancreatic Adenocarcinoma
- IV (Adults ): In combination with leucovorin or as part of multidrug regimen: 400 mg/m2 as IV bolus on Day 1, then 2400 mg/m2 continuous infusion every 2 wk.
Actinic (Solar) Keratoses
- (Adults ): Carac: Apply 0.5% cream to lesions once daily for up to 4 wk; Efudex: Apply 2% or 5% solution or cream to lesions twice daily for 2–4 wk.
Superficial Basal Cell Carcinomas
- (Adults ): Efudex: Apply 5% solution or cream to lesions twice daily for 3–6 wk (up to 12 wk).
