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Fluorouracil
(5-Fluorouracil, 5-FU)
Fluorouracil (Adrucil)
5-Fluorouracil (Adrucil)
5-FU (Adrucil)
Fluorouracil
(flew-roh-
YOUR-ah-sill)
Pregnancy Category: X
Adrucil
Efudex
Fluoroplex (Abbreviation: 5-FU)
(Rx)
Classification:
Antineoplastic, antimetabolite
See Also:
See also
Antineoplastic Agents
[.
]
Action/Kinetics:
Pyrimidine antagonist that inhibits the methylation reaction of deoxyuridylic acid to thymidylic acid. Thus, synthesis of DNA and, to a lesser extent, RNA is inhibited. Cell-cycle specific for the S phase of cell division.
t
1/2, initial: 5-20 min;
final: 20 hr. From 60% to 80% eliminated as respiratory CO
2 (8-12 hr); small amount (15%) excreted unchanged in urine (1-6 hr). Highly toxic; initiate use in hospital. When used topically, the following response occurs:
- Early inflammation: erythema for several days (minimal reaction)
- Severe inflammation: burning, stinging, vesiculation
- Disintegration: erosion, ulceration, necrosis, pain, crusting, reepithelialization
- Healing: within 1-2 weeks with some residual erythema and temporary hyperpigmentation
Uses:
Systemic: Palliative management of certain cancers of the rectum, stomach, colon, pancreas, and breast. In combination with levamisole for Dukes' stage C colon cancer after surgical resection. In combination with leucovorin for metastatic colorectal cancer.
Investigational: Cancer of the bladder, ovaries, prostate, cervix, endometrium, lung, liver, head, and neck. Also, malignant pleural, peritoneal, and pericardial effusions.
Topical (as solution or cream): Multiple actinic or solar keratoses. Superficial basal cell carcinoma.
Investigational: Condylomata acuminata (1% solution in 70% ethanol or the 5% cream).
Additional Contraindications:
Systemic: Clients in poor nutritional state, with severe bone marrow depression, severe infection, or recent (4-week-old) surgical intervention. Lactation. To be used with caution in clients with hepatic or liver dysfunction.
Special Concerns:
Safety and efficacy of topical products have not been established in children. Occlusive dressings may result in increased inflammation in adjacent normal skin when topical products are used.
Additional Side Effects:
Systemic: Esophagopharyngitis, myocardial ischemia, angina, acute cerebellar syndrome, photophobia, lacrimation, decreased vision. Also, arterial thrombosis, arterial ischemia, arterial aneurysm, bleeding or infection at site of catheter, thrombophlebitis, embolism, fibromyositis, abscesses.
Topical: D
ermatologic: Pain, pruritus, hyperpigmentation, irritation, inflammation, burning at site of application, scarring, soreness, allergic contact dermatitis, tenderness, scaling, swelling, suppuration, alopecia, photosensitivity, urticaria.
CNS: Insomnia, irritability.
GI: Stomatitis, medicinal taste.
Miscellaneous: Lacrimation, telangiectasia, toxic granulation.
Laboratory Test Alterations:
 Alkaline phosphatase, LDH, serum bilirubin, and serum transaminase.
Overdose Management:
Symptoms: N&V;, diarrhea, GI ulceration, GI bleeding, thrombocytopenia,
agranulocytosis leukopenia.
Treatment: Monitor hematologically for at least 4 weeks.
Drug Interactions:
Leucovorin calcium
toxicity of fluorouracil.
How Supplied:
Cream: 1%, 5%;
Injection: 50 mg/mL;
Solution: 1%, 2%, 5%
Dosage
?IV
Palliative management of selected carcinomas.
Individualize dosage. Initial: 12 mg/kg/day for 4 days, not to exceed 800 mg/day. If no toxicity seen, administer 6 mg/kg on days 6, 8, 10, and 12. Discontinue therapy on day 12 even if there are no toxic symptoms.
Maintenance: Repeat dose of first course q 30 days or when toxicity from initial course of therapy is gone; or, give 10-15 mg/kg/week as a single dose. Do not exceed 1 g/week.
If client is debilitated or is a poor risk: 6 mg/kg/day for 3 days; if no toxicity, give 3 mg/kg on days 5, 7, and 9 (daily dose should not exceed 400 mg).
Metastatic colorectal cancer.
Leucovorin,
IV, 200 mg/m
2/day for 5 days followed by fluorouracil,
IV, 370 mg/m
2/day for 5 days. Repeat q 28 days to maximize response and to prolong survival.
Dukes' stage C colon cancer after surgical resection.
See
Levamisole
[.
]
?Cream, Topical Solution
Actinic or solar keratoses.
Apply 1%-5% cream or solution to cover lesion 1-2 times/day for 2-6 weeks.
Superficial basal cell carcinoma.
Apply 5% cream or solution to cover lesion b.i.d. for 3-6 weeks (up to 10-12 weeks may be required). |
