fluorouracil


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fluorouracil

 [floor″o-u´rah-sil]
a uracil analogue that interferes with DNA synthesis; used intrvenously as an antimetaboliteantineoplastic agent for palliative treatment of carcinomas of the breast and gastrointestinal tract; also used topically for treatment of actinic keratoses and superficial basal cell carcinomas. Called also 5-fluorouracil (5-FU).

fluorouracil (5-fluorouracil, 5-FU)

Adrucil, Efudex, Fluoroplex

Pharmacologic class: Antimetabolite

Therapeutic class: Antineoplastic

Pregnancy risk category D

Action

Inhibits DNA and RNA synthesis, leading to death of rapid-growing neoplastic cells. Cell-cycle-S-phase specific.

Availability

Cream: 1%, 5%

Injection: 50 mg/ml in 10-ml ampules and 10-, 20-, and 100-ml vials

Solution: 1%, 2%, 5%

Indications and dosages

Advanced colorectal cancer

Adults: 370 mg/m2 I.V. for 5 days, preceded by leucovorin 200 mg/m2 daily for 5 days; may be repeated q 4 to 5 weeks. No single daily dose should exceed 800 mg.

Colon, rectal, breast, gastric, and pancreatic cancer

Adults: Initially, 12 mg/kg/day I.V. for 4 days; then 6 mg/kg I.V. on days 6, 8, 10, and 12. Maximum dosage is 800 mg/day. For maintenance, start 30 days after last dose. If no toxicity, use dosage from first course. If toxicity occurs, give 10 to 15 mg/kg/week as single dose after toxicity subsides. Don't exceed 1 g/week.

Actinic (solar) keratoses

Adults: 1% solution or cream applied once or twice daily to lesions on head, neck, or chest; 2% to 5% solution or cream may be needed for other areas.

Superficial basal cell carcinoma

Adults: 5% solution or cream applied b.i.d. for 3 to 6 weeks (up to 12 weeks)

Contraindications

• Hypersensitivity to drug or its components
• Bone marrow depression
• Dihydropyrimidine dehydrogenase enzyme deficiency (with topical route)
• Poor nutritional status
• Serious infection
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• renal or hepatic impairment, infections, edema, ascites
• obese patients.

Administration

Consult facility's cancer protocols to ensure correct dosage, administration technique, and cycle length.
• Give antiemetic before fluorouracil, as ordered, to reduce GI upset.
• Know that drug may be given without dilution by direct I.V. injection over 1 to 3 minutes.
• For I.V. infusion, dilute with dextrose 5% in water, sterile water, or normal saline solution in plastic bag (not glass bottle). Infusion may be given over a period of 24 hours or more.

Be aware of the importance of leucovorin rescue with fluorouracil therapy, if prescribed.
• Check infusion site frequently to detect extravasation.
• Use nonmetal applicator or appropriate gloves to apply topical form.
• Avoid applying topical form to mucous membranes or irritated skin.
• Don't use occlusive dressings over topical form.
• Know that pyridoxine may be given with fluorouracil to reduce risk of palmar-plantar erythrodysesthesia (hand-foot syndrome).

Adverse reactions

CNS: confusion, disorientation, euphoria, ataxia, headache, weakness, malaise, acute cerebellar syndrome or dysfunction

CV: angina, myocardial ischemia, thrombophlebitis

EENT: vision changes, photophobia, lacrimation, lacrimal duct stenosis, nystagmus, epistaxis

GI: nausea, vomiting, diarrhea, stomatitis, anorexia, GI ulcer, GI bleeding

Hematologic: anemia, leukopenia, thrombocytopenia

Skin: alopecia, maculopapular rash, melanosis of nails, nail loss, palmar-plantar erythrodysesthesia, photosensitivity, local inflammation reaction (with cream), dermatitis

Other: fever, anaphylaxis

Interactions

Drug-drug.Bone marrow depressants (including other antineoplastics): additive bone marrow depression

Irinotecan: dehydration, neutropenia, sepsis

Leucovorin calcium: increased risk of fluorouracil toxicity

Live-virus vaccines: decreased antibody response to vaccine, increased risk of adverse reactions

Drug-diagnostic tests.Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, lactate dehydrogenase, urinary 5-hydroxyindoleacetic acid: increased levels

Albumin, granulocytes, platelets, red blood cells, white blood cells (WBCs): decreased levels

Drug-behaviors.Sun exposure: increased risk of phototoxicity

Patient monitoring

Watch for signs and symptoms of toxicity, especially stomatitis and diarrhea. If these occur, stop drug and notify prescriber. Note that toxicity may take 1 to 3 weeks to develop.
• Monitor CBC, WBC and platelet counts, and kidney and liver function test results.
• Assess fluid intake and output.
• With long-term use, watch for serious rash on hands and feet. If it occurs, consult prescriber regarding need for pyridoxine.
• Assess for bleeding tendency.
• Monitor blood glucose level in patients at risk for hyperglycemia.

Patient teaching

Emphasize importance of taking leucovorin as prescribed with high-dose therapy.

Instruct patient to report signs and symptoms of toxicity, particularly stomatitis and diarrhea. Tell him that these may not occur for 1 to 3 weeks.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient to avoid activities that can cause injury. Instruct him to use soft toothbrush and electric razor to avoid gum and skin injury.
• Advise patient to minimize GI upset by eating frequent, small servings of food and drinking adequate fluids.
• Tell patient that drug may cause reversible hair loss.
• Inform patient that he'll undergo regular blood testing during therapy.

Advise female to inform prescriber immediately if she is pregnant. Caution her not to breastfeed.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

fluor·o·u·ra·cil (FU),

(flōr'ō-yū'ră-sil),
A pyrimidine analogue; an antineoplastic effective in the treatment of some carcinomas; the cells of certain neoplasms incorporate uracil into ribonucleic acid more readily than do normal tissue cells.

fluorouracil

/flu·o·ro·ura·cil/ (5-FU) (floor″o-ūr´ah-sil) an antimetabolite activated like uracil, used as a systemic and topical antineoplastic.

fluorouracil

(flo͝or′ō-yo͝or′ə-sĭl, flôr′-)
n.
An antineoplastic agent, C4H3FN2O2, used especially in the treatment of cancers of the skin, breast, and digestive system.

fluorouracil

[floo͡r′ōyoo͡r′əsil]
an antimetabolite antineoplastic.
indications It is prescribed in the treatment of malignant neoplastic disease of the skin, breast, and internal organs.
contraindications Bone marrow depression, infection, poor nutritional status, or known hypersensitivity to this drug prohibits its use.
adverse effects Among the more serious adverse effects are severe depression of the bone marrow and acute GI disturbances, including nausea, vomiting, diarrhea, and stomatitis. Alopecia and dermatitis commonly occur. Effects of topical application include photosensitivity, rash, and scarring.

fluorouracil

5-FU, Efudex® Oncology An antimetabolite that interferes with DNA synthesis, and deprives DNA of functional thymidine; 5-FU is used for bladder CA, for terminal CA and, topically, for actinic keratosis Side effects BM toxicity, mucosal inflammation

flu·o·ro·u·ra·cil

(FU, FUra) (flōr'ō-yū'ră-sil)
An antineoplastic effective in the treatment of some carcinomas.

fluorouracil

A pyrimidine anticancer drug. The drug is on the WHO official list.

Fluorouracil

A cell-killing (cytotoxic) medication that can be applied in cream form to treat cancer of the penis.
Mentioned in: Penile Cancer

flu·o·ro·u·ra·cil

(flōr'ō-yū'ră-sil)
Antineoplastic effective in treatment of some carcinomas.

fluorouracil (topical) (flŏŏr´əyŏŏr´əsil),

n brand names: Efudex, Fluoroplex;
drug class: topical antineoplastic;
action: inhibits synthesis of DNA and RNA in susceptible cells;
uses: keratosis, basal cell carcinoma.
References in periodicals archive ?
Randomized trial comparing epirubicin, cisplatin, and fluorouracil versus fluorouracil, doxorubicin, and methotrexate in advanced esophagogastric cancer.
One course of topical fluorouracil cream reduced the need for localized treatments and the number of actinic keratoses over a mean follow-up of 2.
5% fluorouracil has comparable efficacy, greater tolerability, and lower cost, compared with 5.
Phase III trial comparing 4-day chronomodulated therapy versus 2-day conventional delivery of fluorouracil, leucovorin, and oxaliplatin as first-line chemotherapy of metastatic colorectal cancer.
Irinotecan in combination with fluorouracil in a 48-hour continuous infusion as first-line chemotherapy for elderly patients with metastatic colorectal cancer: a Spanish cooperative group for the treatment of digestive tumors study.
Thierry Andre of Hopital Tenon in Paris, and associates, showed that the addition of oxaliplatin to fluorouracil and leucovorin (FL) adjuvant therapy for stage II or III colon cancer kept 78.
Valeant Pharmaceuticals (NYSE:VRX) today announced that Spear Pharmaceuticals has agreed not to market, sell or ship a generic fluorouracil cream 5% pursuant to a stay in Valeant's legal case against the Food and Drug Administration (FDA).
Clinical benefit with docetaxel plus fluorouracil and cisplatin compared with cisplatin and fluorouracil in a phase III trial of advanced gastric or gastro-esophageal cancer adenocarcinoma: the V-325 Study Group
Patients were treated every three weeks for three cycles with either TPF (Taxotere 75 mg/m2 plus cisplatin 100 mg/m2 and 5-fluorouracil 1000 mg/m2 a day for four days) or PF (intravenous cisplatin 100 mg/m2 followed by 5- fluorouracil 1000 mg/m2 a day for five days), the standard therapy.
5% fluorouracil followed by cryosurgery was more effective than cryosurgery alone in a controlled study.
The combination regimen CapeOX, which is capecitabine (Xeloda, Roche) and oxaliplatin (Eloxatin, sanofi~aventis), was added as an alternate option to the combination of fluorouracil, leucovorin and oxaliplatin (known as FOLFOX).