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Indications ⬇

High Alert


Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

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

Interactions ⬆ ⬇

Drug-drug:

Availability ⬆ ⬇

(Generic available)

Route/Dosage ⬆ ⬇

Advanced Colorectal Cancer

Breast Cancer

Gastric Adenocarcinoma

Pancreatic Adenocarcinoma

Actinic (Solar) Keratoses

Superficial Basal Cell Carcinomas

US Brand Names ⬆ ⬇

Carac, Efudex, Tolak

Action ⬆ ⬇

  • Inhibits DNA and RNA synthesis by preventing thymidine production (cell-cycle S-phase-specific).
Therapeutic effects:
  • Death of rapidly replicating cells, particularly malignant ones.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: antimetabolites

Pharmacokinetics ⬆ ⬇

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.

Time/Action Profile ⬆ ⬇

(IV = effects on blood counts, Top = dermatologic effects)

ROUTEONSETPEAKDURATION
IV1–9 days9–21 days (nadir)30 days
Top2–3 days2–6 wk1–2 mo

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

flure-oh-YOOR-a-sill

Code ⬆

NDC Code