♦Fluorouracil

(flure-oh-yoor’-a-seel)

5-FU, Adrucil

Pregnancy Category D

Mechanism of Action

Interferes with DNA synthesis and formation of RNA, which are essential for cell division and growth. Causes a thymine deficiency, which leads to unbalanced growth and death of the cell.

Indications

♦ Carcinoma of the colon, rectum, breast, stomach, and pancreas

♦ Orphan drug uses: In combination with interleukin-2a recombinant for esophageal and advanced colorectal carcinoma; with leucovorin for colorectal metastatic adeno-carcinoma.

Metabolism/Excretion

Primarily metabolized by the liver; excreted by the kidneys and lungs. Half-life: 8 to 20 minutes.

Dosage Range

Adult

Give 12 mg/kg for 4 consecutive days with a daily dose limit of 800 mg. If no toxicity occurs, give a 6-mg/kg dose on days 6, 8, 10, and 12. The drug is then discontinued even if there are no signs of toxicity. For high-risk patients or those who do not have adequate nutritional status, give 6 mg/kg for 3 consecutive days. If no toxicity is observed, give 3 mg/kg on days 5, 7, and 9 unless toxicity occurs. The daily dose should not exceed 400 mg.

For maintenance therapy, when toxicity is not a problem, follow the following dosing schedule:

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