5-FU


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5-FU

 
5-fluorouracil; see fluorouracil.

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.

5-FU

Fluorouracil Gynecology A topical cream applied to the cervix and vagina for managing cervical CA Adverse effects Burning, inflammation
References in periodicals archive ?
5-FU significantly increased (P < 0.05) the MPO activity, indicating a pronounced neutrophil accumulation, and also augmented tissue levels of TNF-[alpha] and IL-1[beta] (MPO: 3.5 [+ or -] 0.5 U/mg of tissue; TNF-[alpha]: 1471 [+ or -] 752 pg/mg of tissue; IL-1[beta]: 6870 [+ or -] 2417 pg/mg of tissue) vs the saline group (MPO: 0.9 [+ or -] 0.5; TNF-[alpha]: 0.0 [+ or -] 0.0 pg/mg of tissue; IL-1[beta]: 787.5 [+ or -]356.1 pg/mg of tissue).
Efficacy of 5-FU was confirmed as the viability of 5-FU-treated cells decreased significantly by 30% for IEC-6 cells (p < 0.05; Figures 2A, 3A and 4A) and 50% for Caco-2 cells (p < 0.05; Figures 2B, 3B and 4B).
Swinehart et al.13 used intralesional 5-FU successfully for the treatment of condylomata acuminata.
The nanohydrogel was used in in vitro drug release of 5-FU at different simulated fluids for specific sites such stomach (pH 1.2) and colon (pH 7.4).
Cardiotoxicity is a relevant, important, and underestimated problem in 5-FU treatment.
Moreover, an important characteristic observed at 24 is the presence of few dead cells for AgNPs exposition, indicating the role of the bioextract as a possible cytoprotective agent since it encapsulates the nanoparticles and 5-FU, preventing direct contact with cells, and additionally, the cell cultures remained viable with only the presence of the extract (Figures 6(b)-6(d)).
After synchronization using serum-free RPMI 1640 culture medium, ARPE-19 cells were incubated with 5 mg/mL 5-Fu, 0.02 mg/mL MMC, 2.5 mg/mL BVZ, 5 mg/mL 5-Fu + 2.5 mg/mL BVZ, 0.02 mg/mL MMC + 2.5 mg/mL BVZ, or PBS as the control for 48 h.
Due to its suitable pore size and high density of O donor sites, it could behave as an effective carrier for the 5-Fu capture and release, and a moderate 5-Fu-loading capacity and pH-dependent drug release behavior could be observed.
All experimented doses of 10 to 250 uM 5-FU showed (Fig.
To make our studies reliable and accurate, we used the following inclusion criteria: (1) patients were histologically diagnosed with gastric adenocarcinoma; (2) specimens used to detect the expression level of DPD were obtained by endoscopic biopsy or postoperative samples prior to chemotherapy; (3) the correlation coefficients between the expression level of intratumoral DPD and sensitivity to 5-FU could be found or calculated in the relevant studies; (4) the information on survival was sufficient to calculate HR.
Treatment with 5-FU (Figures 4(b) and 4(c)) or Irinotecan (Figures 4(d) and 4(e)) decreased cell viability of tumor ALI organoids in each patient culture in a dose-dependent manner.
After treatment with 5-Fu, SLPE, or 5-Fu and SLPE, the mean tumor volume was higher on days 10 and 17 than that on day 0.