Fluorouracil

DRUG NAME: Fluorouracil

SYNONYM(S): 5-FU, 5-Fluorouracil, NSC-19893

COMMON TRADE NAME

eneric available, ADRUCIL(r), EFUDEX(r) CREAM : g

CLASSIFICATION:

antimetabolite, cytotoxic

Special pediatric considerations are noted when applicable, otherwise adult provisions apply.

MECHANISM OF ACTION

:

Fluorouracil is an analog of the pyrimidine uracil and thus acts as a pyrimidine antagonist.2 There are three possible mechanisms of action.3 First, the fluorouracil metabolite fluorodeoxyuridine monophosphate (FdUMP) competes with uracil to bind with thymidylate synthetase (TS) and the folate cofactor.4 This results in decreased thymidine production and therefore decreased DNA synthesis and repair, and ultimately decreased cell proliferation.

Leucovorin (formyltetrahydrofolate, formyl-FH4) enhances fluorouracil by stabilizing the binding of FdUMP to TS. Second, the fluorouracil metabolite fluorodeoxyuridine triphosphate (FdUTP) is incorporated into DNA thus interfering with DNA replication.3 Finally, the fluorouracil metabolite fluorouridine-5-triphosphate (FUTP) is incorporated into RNA in place of uridine triphosphate (UTP), producing a fraudulent RNA and interfering with RNA processing and protein synthesis.5 Fluorouracil is cell-cycle specific (S-phase).4

PHARMACOKINETICS:

Interpatient variability variations in dihydropyrimidine dehydrogenase (DPD) activity result in differences in toxicity 6 (refer to the Dihydropyrimidine dehydrogenase (DPD) deficiency paragraph following the Side Effect table for more information)
Oral Absorption erratic; 28-100%
Distribution approximately 22% of total body water; penetrates extracellular fluid and third space fluids (e.g., malignant effusions and ascitic fluid)
cross blood brain barrier? yes
volume of distribution 7 8-11 L/m 2
plasma protein binding 8 10%
Metabolism activated in target cells; 80% degraded in liver by DPD 7
active metabolite(s) FdUMP, FUTP, and FdUTP
inactive metabolite(s) dihydrofluorouracil
Excretion 60-80% excreted as respiratory CO 2 ; 2-3% by biliary system
urine <10% as intact drug 7
terminal half life IV bolus: 8-14 min (see also nonlinear pharmacokinetics in clearance below)
clearance IV bolus: 350-850 mL/min/m 2 ; dependent on dose, schedule, and route of administration; nonlinear pharmacokinetics due to saturable degradation 7 ; interference with fluorouracil degradation markedly prolongs its half-life 7 continuous infusion: clearance increases
Ethnicity DPD deficiency: caucasian (3-5%); African-American 0.1% 9

Adapted from standard references10,11 unless specified otherwise.

BC Cancer Agency Cancer Drug Manual(c) Page 1 of 11 Fluorouracil Developed: September 1994

Revised: June 2006 Limited revision: May 2007

Fluorouracil

USES:

Primary uses: Other uses:
*Actinic keratoses (topical fluorouracil) 12 Cervical cancer 5
*Bladder cancer Esophageal cancer 5
*Breast cancer Renal cell cancer 5
*Colorectal cancer Skin cancer, Bowen's disease (topical fluorouracil) 13
*Gastric cancer Skin cancer, squamous cell (topical fluorouracil) 13
*Head and neck cancer
*Ovarian cancer
*Pancreatic cancer
*Prostate cancer
*Skin cancer, basal cell (topical fluorouracil) 12

*Health Canada approved indication

SPECIAL PRECAUTIONS:

Contraindicated in patients who have a history of hypersensitivity to fluorouracil or any component of the formulation.11 Relatively contraindicated in patients who have a known hypersensitivity to capecitabine.14

Dihydropyrimidine dehydrogenase (DPD) deficiency may result in life-threatening or fatal toxicity in patients receiving fluorouracil via parenteral or topical administration.7 For more information refer to the Dihydropyrimidine dehydrogenase (DPD) deficiency paragraph following the Side Effect table.

Nonlinear pharmacokinetics result in unpredictable plasma concentrations and toxicity at high doses.7 Elderly patients are at increased risk for developing toxicities, likely due to decreased bone marrow reserve.7 Female patients are at increased risk for developing toxicities.7,15,16

Use with caution in patients who are receiving radiation or who have received high-dose pelvic radiation and in patients previously treated with alkylating agents.11 These patients may have bone marrow suppression.

Carcinogenicity: Not yet studied.4

Mutagenicity: Fluorouracil has been shown to be mutagenic in some bacterial strains.4 It is clastogenic in mammalian in vitro and in vivo chromosome tests.

Fertility: The effects of fluorouracil on fertility have not been established.4

Pregnancy11: FDA Pregnancy Category D. There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Breastfeeding is not recommended due to the potential secretion into breast milk.10

SIDE EFFECTS:

The table includes adverse events that presented during drug treatment but may not necessarily have a causal relationship with the drug. Because clinical trials are conducted under very specific conditions, the adverse event rates observed may not reflect the rates observed in clinical practice. Adverse events are generally included if they

were reported in more than 1% of patients in the product monograph or pivotal trials, and/or determined to be clinically important17. When placebo-controlled trials are available, adverse events are included if the incidence is > 5% higher in the treatment group.

BC Cancer Agency Cancer Drug Manual(c) Page 2 of 11 Fluorouracil Developed: September 1994

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Fluorouracil

ORGAN SITE SIDE EFFECT ONSET
Clinically important side effects are in bold, italics I = immediate (onset in hours to days); E = early (days to weeks); D = delayed (weeks to months); L = late (months to years)
allergy/immunology anaphylaxis (rare) 4 I
generalized allergic reactions (rare) 4 I
blood/bone marrow/ febrile neutropenia myelosuppression *: onset: 7-10 days; nadir: 14 days; recovery: 30 days I
cardiovascular (arrhythmia) arrhythmias I
cardiotoxicity * ( < 8%) 18 E
chest pain (< 1%); ranging from mild angina to crushing pain I
CHF (rare) 4 E
hypotension (< 1%) I
constitutional symptoms somnolence (< 1%) I
dermatology/skin extravasation hazard: irritant 11,19,20
For more information on topical application see paragraph after this table.
alopecia (> 10%) E
dermatitis * (>10%) I
dry skin and fissuring (1-10%) E
nail changes (< 1%); banding or loss of nails E
palmar-plantar erythrodysesthesia (PPE) * (<1%) E
photosensitivity (< 1%) I
vein hyperpigmentation (< 1%); proximal to injection sites I
gastrointestinal emetogenic potential 21 : rare (< 10%)
anorexia (> 10%) I
diarrhea * (> 10%) I
esophagitis (>10%) I
heart burn (>10%) I
nausea (< 10%) I
stomatitis * (> 10%) I
epithelial ulceration (1-10%) E
vomiting (< 10%) 21 I
hemorrhage GI bleeding E
hepatic biliary sclerosis 7 E
hepatic toxicity (< 1%) E
neurology acute cerebellar ataxia (< 1%); increased with high doses or intensive regimens E
neurotoxicities * (< 1%) E
ocular/visual excessive lacrimation I

BC Cancer Agency Cancer Drug Manual(c) Page 3 of 11 Fluorouracil Developed: September 1994

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Fluorouracil

ORGAN SITE SIDE EFFECT ONSET
Clinically important side effects are in bold, italics I = immediate (onset in hours to days); E = early (days to weeks); D = delayed (weeks to months); L = late (months to years)
ocular toxicities * E
pain headache (< 1%) I
pulmonary dyspnea (< 1%) I

Adapted from standard references10,11 unless specified otherwise. *Severity varies with route of administration, refer to the following paragraph.

Dosing schedule and toxicity: The spectrum of toxicity associated with fluorouracil treatment varies with dose, schedule, route of administration, and whether the fluorouracil is being used with a biochemical modulator.7 The most commonly seen toxicities when standard doses are administered in the following schedules and routes are:

monthly bolus administration22: myelosuppression can be dose-limiting

daily bolus administration for 5 days22: diarrhea can be dose-limiting; myelosuppression, stomatitis, ocular, and dermatitis7

continuous infusion given over 24 hours to several weeks22: diarrhea, and stomatitis can be dose-limiting; myelosuppression, dermatitis, PPE, neurologic, ocular, and cardiotoxicity11

weekly bolus administration22: diarrhea can be dose-limiting; myelosuppression, stomatitis,7 and ocular23

topical daily7: local inflammation

Oral cryotherapy with bolus doses of fluorouracil: It is recommended that patients receiving bolus fluorouracil undergo 30 minutes of oral cryotherapy to decrease the incidence and severity of fluorouracil-induced stomatitis.24 The incidence can be reduced by 50%.25 Starting 5 minutes before the injection, the patient is asked to place ice chips into their mouth and swish for 30 minutes, replenishing the ice as it melts. This may cause numbness or headaches which subside quickly. This cooling of the oral cavity leads to vasoconstriction resulting in a lower concentration of fluorouracil reaching the oral mucosa.24 Oral cryotherapy is not used for infusional fluorouracil as this would be very inconvenient. It is also not used for bolus fluorouracil administered in combination with oxaliplatin. This is due to the concern with oxaliplatin and cold related laryngo-dysesthesias.17

Acute cerebellar syndrome can rarely occur and is characterized by an acute onset of ataxia, dysmetria, dysarthria, and nystagmus that develops weeks to months after beginning treatment.26 These symptoms usually resolve after discontinuation of fluorouracil.26 Cerebellar syndrome may be partly explained because fluorouracil

crosses the blood-brain barrier, and the highest concentrations are found in the cerebellum.26 Other rarer neurologic side effects include encephalopathy, optic neuropathy, eye movement abnormalities, focal dystonia, cerebrovascular disorders, parkinsonian syndrome, peripheral neuropathy, and seizures.26

Cardiotoxicity18: Fluorouracil has the second highest incidence of chemotherapy induced cardiotoxicity, after the anthracyclines.11 The incidence of fluorouracil induced cardiotoxicity can be as high as 8%.18 Within this group types of cardiotoxicity include27:

electrocardiographic changes, 69%

angina, 48%

myocardial infarction, 23%

acute pulmonary edema, 17%

arrhythmias,16%

elevated cardiac enzymes, 14%

cardiac arrest and pericarditis, 2%

Coronary vasospasm is thought to be the underlying mechanism of this toxicity.18,28 Although most patients who

experience fluorouracil-induced cardiotoxicity have no previous cardiac problems, history of preexisting coronary artery disease is a risk factor. Other risk factors include route of administration (refer to the Dosing schedule and toxicity paragraph following the Side Effect table) and the use of concurrent radiation or anthracyclines.18 Most cases

of fluorouracil-induced cardiotoxicities resolve after termination of fluorouracil infusion and/or administration of nitrates or calcium channel blockers.28 Rechallenging these patients remains controversial. If rechallenged, these

BC Cancer Agency Cancer Drug Manual(c) Page 4 of 11 Fluorouracil Developed: September 1994

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Fluorouracil

patients needs careful observation during drug infusion and may benefit from treatment with calcium channel blockers or nitrates.28

Palmar-plantar erythrodysesthesia (PPE): also called hand-foot skin reaction, may occur in association with the continuous infusion of fluorouracil.19 PPE may gradually disappear over 5-7 days after discontinuance of fluorouracil therapy.4 PPE may be treated with oral pyridoxine 50-150 mg daily29,30; although efficacy has not been well established.4

Dihydropyrimidine dehydrogenase (DPD) deficiency is a rare, inherited disorder of pyrimidine degradation. The frequency of low or deficient DPD activity in predominantly Caucasian and African-American populations is 3-5% and 0.1%, respectively.9 For patients with even a partial DPD deficiency, treatment with fluorouracil can lead to life-

threatening complications. Fluorouracil clearance is dependent on DPD as fluorouracil is enzymatically inactivated to dihydrofluorouracil by DPD.31 There is no evidence of fluorouracil degradation in DPD-deficient patients.32 Toxicities can include severe diarrhea, stomatitis, and myelosuppression.9 Nausea, vomiting, rectal bleeding, volume

depletion, skin changes, and neurologic abnormalities (cerebellar ataxia, changes in cognitive function, changes in the level of consciousness) may also occur.9 Management should include aggressive supportive care with hemodynamic support, parenteral nutrition, antibiotics, and hematopoietic colony stimulating factors.9 Tests for the diagnosis of DPD deficiency are not readily available and as a result most cases are diagnosed long after the

administration of fluorouracil.9

Ocular toxicity: Fluorouracil-induced ocular toxicities result primarily from ocular surface problems, such as excessive lacrimation, blurred vision, photophobia, and eye irritation.22 Excessive lacrimation is the most frequent ocular symptom and can be quite dramatic; it may occur any time during treatment and possibly accompanied with

pruritus and burning.7 Fluorouracil has been found in tear fluid and can cause acute and chronic conjunctivitis

leading to tear duct fibrosis. Ocular toxicities can also include epiphora, blepharitis, conjunctivitis, tear duct stenosis, and sclerosing canaliculitis. Applying ice packs to the eyes before, during, and for 30 minutes after fluorouracil injection may decrease ocular toxicity.22

Topical application leads to the following sequence12: erythema, usually followed by vesiculation, erosion, ulceration, necrosis, and epithelization. The lower frequency and intensity of activity in adjacent normal skin indicates a selective cytotoxic property. The most frequent local reactions are pain, pruritus, hyperpigmentation, and burning at the application site. Other local reactions include dermatitis, scarring, soreness, and tenderness.

Insomnia, stomatitis, suppuration, scaling, swelling, irritability, medicinal taste, photosensitivity, and lacrimation have also been reported.33

INTERACTIONS:

AGENT EFFECT MECHANISM MANAGEMENT
cimetidine 34 delayed, moderate, possible; fluorouracil efficacy and toxicity may be increased unknown monitor for fluorouracil toxicity; discontinue cimetidine if necessary
fosphenytoin 34 delayed, moderate, possible; fosphenytoin efficacy and toxicity may be increased inhibition of hydantoin metabolism (CYP2C9) by fluorouracil suspected monitor fosphenytoin plasma levels; observe clinical response when starting or stopping fluorouracil
gemcitabine 35 fluorouracil efficacy and toxicity may be increased unknown some protocols are designed to take advantage of this effect; monitor toxicity closely
leucovorin 22 increased cytotoxic and toxic effects of fluorouracil leucovorin stabilizes the bond to thymidylate synthetase some protocols are designed to take advantage of this effect; monitor toxicity closely

BC Cancer Agency Cancer Drug Manual(c) Page 5 of 11 Fluorouracil Developed: September 1994

Revised: June 2006 Limited revision: May 2007

Fluorouracil

AGENT EFFECT MECHANISM MANAGEMENT
metronidazole 36 fluorouracil efficacy and toxicity may be increased metronidazole may decrease the metabolism of fluorouracil monitor for fluorouracil toxicity
oxaliplatin 37 no influence on fluorouracil pharmacokinetics
phenytoin 34 delayed, moderate, inhibition of hydantoin monitor phenytoin plasma
possible; phenytoin metabolism (CYP2C9) by levels; observe clinical
efficacy and toxicity may fluorouracil suspected response when starting or
be increased stopping fluorouracil
thiazides 34 (e.g., chlorthalidone, hydrochlorothiazide) delayed, moderate, possible; thiazides may prolong fluorouracil- induced leukopenia unknown consider alternative antihypertensive therapy
warfarin 11,34,38 delayed, moderate, documented 39 ; increased effect and toxicity of warfarin possibly protein displacement, inhibition of warfarin metabolism, or inhibition of clotting factor synthesis check baseline INR; monitor weekly INR during, and for one month after, fluorouracil therapy; increase frequency and duration of monitoring if INR unstable; adjust warfarin dose as needed; anticoagulation with LMWH may be considered

SUPPLY AND STORAGE:

Topical33: Supplied as fluorouracil 5% in a vanishing cream base. Non-medicinal ingredients: white petrolatum, stearyl alcohol, propylene glycol, polysorbate 60, and parabens. Store in a dry location at room temperature, away from heat and direct light.

For basic information on the current brand used at the BC Cancer Agency, see Chemotherapy Preparation and Stability Chart in Appendix.

Injection: The Mayne Pharma solution contains the non -medicinal ingredients: sodium hydroxide.12 Product may contain hydrochloric acid as a pH adjuster.12

SOLUTION PREPARATION AND COMPATIBILITY:

For basic information on the current brand used at the BC Cancer Agency, see Chemotherapy Preparation and Stability Chart in Appendix.

Additional information: Slight discolouration does not affect potency or safety.40 Darker yellow discolouration indicates greater decomposition so dark yellow solutions may need to be discarded.40 Crystals that have formed in the solution can be redissolved by warming and shaking.40

Diluted solution for infusion40: The following solutions are compatible with fluorouracil at certain concentrations: D5W; NS; Dextrose 5% in Lactated Ringer's; Dextrose 3.3% in NS 0.3%; Plasmalyte 3G5.

Compatibility of selected drugs 40: The following are compatible with fluorouracil via Y-site injection: bleomycin; cisplatin; cyclophosphamide; doxorubicin; fludarabine; furosemide; gemcitabine; granisetron; heparin;

BC Cancer Agency Cancer Drug Manual(c) Page 6 of 11 Fluorouracil Developed: September 1994

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Fluorouracil

hydrocortisone; leucovorin; mannitol; melphalan; methotrexate; metoclopramide; mitomycin; paclitaxel; piperacillin; potassium chloride; sargramostim; teniposide; thiotepa; vinblastine; vincristine.

Incompatibility of selected drugs 40: The following are incompatible with fluorouracil via Y-site injection: droperidol; filgrastim; ondansetron; vinorelbine.

PARENTERAL ADMINISTRATION:

BCCA administration guideline noted in bold , italics
Subcutaneous not used due to corrosive nature
Intramuscular not used due to corrosive nature
* Direct intravenous over 1-3 minutes
* Intermittent infusion can be used (e.g., dilute in 50 mL and infuse for up to 15 minutes) 11
*Continuous infusion over 24 hours or greater; may be given via an ambulatory infusion device
Intraperitoneal 41 15 mg/kg and 50 mEq sodium bicarbonate to 1000 mL 1.5% dextrose dialysis solution; dwell for 23 hours then drain for one hour
Intrapleural no information found
Intrathecal 2 contraindicated due to neurotoxicity
Intra-arterial 2 hepatic artery
Intravesical 4 portal vein infusion

*Doses prescribed for continuous infusion can be FATAL when given as direct intravenous or intermittent

infusion.

TOPICAL ADMINISTRATION:

The cream is applied twice daily, preferably with a nonmetal applicator or glove. If the cream is applied with fingertips, the hands should be washed immediately afterwards.33 Apply with care near the eyes, mouth and nose. An occlusive dressing is not essential, and may increase the incidence of inflammatory reactions in adjacent normal

skin. Therapy is usually continued until the inflammatory reaction reaches the erosion, necrosis and ulceration stage (2-4 weeks), after which healing occurs over 4-8 weeks. While the patient is undergoing topical 5-FU therapy, consideration can be given to curettage, wound excision and removal of pathological tissue.33 Patients should avoid

prolonged exposure to ultraviolet light while under treatment as the intensity of the reaction may be increased.

DOSAGE GUIDELINES:

Refer to protocol by which patient is being treated. Numerous dosing schedules exist and depend on disease, response and concomitant therapy. Guidelines for dosing also include consideration of absolute neutrophil count (ANC). Dosage may be reduced, delayed or discontinued in patients with bone marrow depression due to cytotoxic/radiation therapy or with other toxicities.

Adults:

Cycle Length:

BCCA usual dose noted in bold, italics

Intravenous: 1 week42,43: 1000 mg/m2 IV over 24 hours for 2 consecutive days starting on day 1

(total dose per cycle 2000 mg/m2) (maximum dose is 5000 mg/48 h)

BC Cancer Agency Cancer Drug Manual(c) Page 7 of 11 Fluorouracil Developed: September 1994

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Fluorouracil

weeks44-48: 400 mg/m2 IV for one dose on day 1 immediately followed by 2400-3000 mg/m2 IV over 46 hours

(total dose per cycle 2800-3400 mg/m2)

weeks49-57: 500-600 mg/m2 IV for one dose on day 1 (total dose per cycle 500-600 mg/m2)

weeks58: 1000 mg/m2IV over 24 hours for 3 consecutive days starting on day 1

(total dose per cycle 3000 mg/m2)

weeks59,60: 425 mg/m2 IV once daily for 5 consecutive days starting on day 1

(total dose per cycle 2125 mg/m2)

4 weeks61,62: when given as a dose-dense regimen with filgrastim (G- CSF) support:

500 mg/m2 IV for one dose on days 1 and 8 (total dose per cycle 1000 mg/m2)

4 weeks63-65: 500-600 mg/m2 IV for one dose on days 1 and 8 (total dose per cycle 1000-1200 mg/m2)

4 weeks66-69: when given as a dose-dense regimen with filgrastim (G- CSF) support:

500 mg/m2 IV for one dose on days 1 and 15 (total dose per cycle 1000 mg/m2)

4 weeks70,71: 1000 mg/m2 IV over 24 hours for 4 consecutive days starting on day 1

(total dose per cycle 4000 mg/m2)

6 weeks72: 400-500 mg/m2 IV on day 1, 8, 15 and 22 (total dose per cycle 1600-2000 mg/m2)

6 weeks73: 1000 mg/m2 IV over 24 hours for 4 consecutive days starting on day 1

(total dose per cycle 4000 mg/m2)

Concurrent radiation74-81: can be used with variable schedules and dosing; specific treatment protocols

must be consulted; see Special Precautions regarding patients who have received high-dose pelvic radiation

Dosage in myelosuppression:

modify according to protocol by which patient is being treated; if no guidelines

available, refer to Appendix 6 "Dosage Modification for Myelosuppression"

Dosage in obesity10: if patient is obese or there has been a spurious weight gain because of edema,

ascites or other form of abnormal fluid retention, the ideal weight or estimated lean body mass should be used

Dosage in renal failure:

no adjustment required

Dosage in hepatic failure11: bilirubin > 86 umol/L omit dose

Dosage in dialysis: hemodialysis: give 1/2 dose8; administer dose following hemodialysis11

BC Cancer Agency Cancer Drug Manual(c) Page 8 of 11 Fluorouracil Developed: September 1994

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Fluorouracil

chronic ambulatory peritoneal dialysis (CAPD): no data8 continuous renal replacement therapy (CRRT): give full dose82

Topical12: apply twice daily x 2-4 weeks. See Topical Administration for more information.

Children:

Intravenous32: 500 mg/m2 IV once or daily x 5 800-1200 mg/m2 IV over 24-120 h

Topical 33: use and dose as determined by physician

REFERENCES:

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  2. Dorr RT, Von-Hoff DD. Cancer chemotherapy handbook. In. second ed. ed. Norwalk, Connecticut: Appleton & Lange; 1994. p. 27-8,123.

  3. van der Wilt CL, Marinelli A, Pinedo HM, et al. The effects of Different Routes of Administration of 5-fluorouracil on Thymidylase Synthase Inhibition in the Rat. Eur J Cancer 1995; 31A(5):754-60.

  4. McEvoy G, editor. American Hospital Formulary Systems Drug Information. Bethesda, MD: American Society of Health System Pharmacists; 2006.

  5. McEvoy G, editor. American Hospital Formulary Systems Drug Information. Bethesda, MD: American Society of Health System Pharmacists; 2005.

  6. van Kuilenburg AB, Muller EW, Haasjes J, et al. Lethal outcome of a patient with a complete dihydropyrimidine dehydrogenase (DPD) deficiency after administration of 5-fluorouracil: frequency of the common IVS14+1G>A mutation causing DPD deficiency. Clin Cancer Res 2001; 7(5):1149-53.

  7. Chabner B, Longo D, editors. Cancer Chemotherapy and Biotherapy Principles and Practice. 3rd edition ed. Philadelphia, PA: Lippincott Williams and Wilkins; 2001.

  8. Aronoff GR, Berns JS, Brier ME, et al. Drug Prescribing in Renal Failure. 4th ed; 1999. p. 74.

  9. Halmos B, Edner JP. Enterotoxicity of chemotherapeutic agents. In: Rose BD, editor. UpToDate. Wellesley, MA; 2006.

  10. Mayne Pharma Canada Inc. Fluorouracil Product Monograph. Montreal Quebec; 2003, date of revision.

  11. Fluorouracil: Drug Information. In: Rose BD, editor. UpToDate. Wellesley, MA; 2006.

  12. Repchinsky C, editor. Compendium of Pharmaceuticals and Specialties. Ottawa, Ontario: Canadian Pharmacists Association; 2005.

  13. Treatment and prognois of cutaneous squamous cell carcinoma. In: Rose BD, editor. UpToDate. Wellesley, MA,: UpToDate; 2006.

  14. Hoffman-La Roche Limited. Xeloda product monograph. Mississauga, Ontario; 31 July, 2002.

  15. Sloan JA, Goldberg RM, Sargent DJ, et al. Women experience greater toxicity with fluorouracil-based chemotherapy for colorectal cancer. J Clin Oncol 2002; 20(6):1491-8.

  16. Chansky K, Benedette J, Macdonald JS. Differences in toxicity between men and women treated with 5-fluorouracil therapy for colorectal cancer. Cancer 2005; 103(6):1165-71.

  17. Sharlene Gill, MD. Personal communication. Medical Oncologist BC Cancer Agency, Vancouver BC; April 2006.

  18. Cerqueira M. Cardiotoxicity in Patients receiving Chemotherapy. In: Rose BD, editor. UpToDate. Wellesley, MA; 2006.

  19. Mayne Pharma Canada Inc. Fluorouracil Product Monograph. Montreal Quebec; 2003,.

  20. Teta JB, O'Connor L. Local Tissue Damage from 5-fluorouracil Extravasation (letter). Oncol Nurs Forum 1984; 11(77).

  21. B.C. Cancer Agency. SCNAUSEA Protocol Summary. Vancouver, British Columbia: BC Cancer Agency; 2005.

  22. Finley RS, Balmer CB. Concepts in Oncology Therapeutics. second ed. Bethesda: American Society of Health-System Pharmacists; 1998.

  23. Petrelli N, Douglass HD, L. H, et al. The modulation of fluorouracil with leucovorin in metastatic colorectal carcinoma: a prospective randomized phase III trail. J Clin Oncol 1991; 7:1419-1426.

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Masci G, Magagnoli M, Zucali PA, et al. Minidose warfarin prophylaxis for catheter-associated thrombosis in cancer patients: can it be safely associated with fluorouracil-based chemotherapy? 2003:736-9, 2003 Feb 15. Camidge R, Reigner B, Cassidy J, et al. Significant Effect of Capecitabine on the Pharmacokinetics and Pharmacodynamics of Warfarin in Patients with Cancer. J Clin Oncol 2005; 23(21 (July 20)):4719-25. Trissel L. Handbook on injectable drugs. 13th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2005. p. 613-22. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for the Chemotherapy of Pseudomyxoma Peritonei using intraperitoneal using Mitomycin and Fluorouracil. Vancouver: BC Cancer Agency; UGIFUIP, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Chemotherapy for Upper Gastrointestinal Tract Cancer (Gastric, Esophageal, Gall Bladder Carcinoma and Cholangiocarcinoma) and Metastatic Anal Cancer using Infusional Fluorouracil and Cisplatin. Vancouver: BC Cancer Agency; GIFUC, 2005. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Combination Chemotherapy for Metastatic Colorectal Adenocarcinoma using Infusional Fluorouracil. Vancouver: BC Cancer Agency; GIFUINF, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Combination Chemotherapy for Metastatic Colorectal Cancer using Irinotecan, Fluorouracil and Folic Acid (Leucovorin). Vancouver: BC Cancer Agency; GIFOLFIRI, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Adjuvant Combination Chemotherapy for Stage III Colon Cancer using Oxaliplatin, 5-Fuorouracil and Folic Acid (Leucovorin). Vancouver: BC Cancer Agency; UGIAJFOLFOX, 2005. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Combination Chemotherapy for Metastatic Colorectal Cancer using Irinotecan, Fluorouracil, Folic Acid (Leucovorin) and Bevacizumab. Vancouver: BC Cancer Agency; UGIFFIRB, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Combination Chemotherapy for Metastatic Colorectal Cancer using Oxaliplatin, 5-Fluorouracil and Folic Acid (Leucovorin) and Bevacizumab. Vancouver: BC Cancer Agency; UGIFFOXB, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Combination Chemotherapy for Metastatic Colorectal Cancer using Oxaliplatin, 5-Fuorouracil and Folic Acid (Leucovorin). Vancouver: BC Cancer Agency; UGIFOLFOX, 2005. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Breast Cancer using Cyclophosphamide, Doxorubicin and Fuorouracil. Vancouver: BC Cancer Agency; BRAJCAF, 2004. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Premenopausal High Risk Breast Cancer using Cyclophosphamide, Methotrexate and Fluorouracil. Vancouver: BC Cancer Agency; BRAJCMF, 1999. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Breast Cancer using Cyclophosphamide, Epirubicin and Fuorouracil. Vancouver: BC Cancer Agency; BRAJFEC, 2005. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Breast Cancer using Fluorouracil, Cyclophosphamide and Docetaxel. Vancouver: BC Cancer Agency; UBRAJFECD, 2006. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Palliative Therapy for Metastatic Breast Cancer using Cyclophosphamide, Doxorubicin and Fluorouracil. Vancouver: BC Cancer Agency; BRAVCAF, 2004. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Palliative Therapy for Advanced Breast Cancer using Cyclophosphamide, Methotrexate and Fuorouracil. Vancouver: BC Cancer Agency; BRAVCMF, 2004. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Inflammatory Breast Cancer using Cyclophosphamide, Doxorubicin and Fuorouracil. Vancouver: BC Cancer Agency; BRINFCAF, 2004.

BC Cancer Agency Cancer Drug Manual(c) Page 10 of 11 Fluorouracil Developed: September 1994

Revised: June 2006 Limited revision: May 2007

Fluorouracil

BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Inflammatory Breast Cancer using Cyclophosphamide, Epirubicin and Fuorouracil. Vancouver: BC Cancer Agency; BRINFCEF, 2005. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Locally Advanced Breast Cancer using Cyclophosphamide, Doxorubicin, Fuorouracil. Vancouver: BC Cancer Agency; BRLA2, 2004. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Therapy of Pancreatic Endocrine Tumours using Carmustine and Fluorouracil. Vancouver: BC Cancer Agency; GIENDO1, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Stage III and High Risk Stage II Colon Cancer using Leucovorin and Fluorouracil. Vancouver: BC Cancer Agency; GIFFAD, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Resected Pancreatic Cancer using Leucovorin and Fluorouracil. Vancouver: BC Cancer Agency; GIPAJFF, 2006. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Breast Cancer using Oral Cyclophosphamide, Doxorubicin, Fuorouracil. Vancouver: BC Cancer Agency; BRAJCAFPO, 2004. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Breast Cancer using Cyclophosphamide, Epirubicin and Fuorouracil. Vancouver: BC Cancer Agency; BRAJCEF, 2005. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Premenopausal High-Risk Breast Cancer using (oral) Cyclophosphamide, Methotrexate and Fuorouracil. Vancouver: BC Cancer Agency; BRAJCMFPO, 1999. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Palliative Therapy for Advanced Breast Cancer using Cyclophosphamide (oral), Methotrexate and Fuorouracil. Vancouver: BC Cancer Agency; BRAVCMFPO, 2004. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Locally Advanced Breast Cancer using Cyclophosphamide, Epirubicin and Fuorouracil. Vancouver: BC Cancer Agency; BRLACEF, 2005. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Breast Cancer using Cyclophosphamide, Doxorubicin, Fuorouracil and Filgrastim (G-CSF). Vancouver: BC Cancer Agency; BRAJCAF-G, 2004. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Adjuvant Therapy for Breast Cancer using Cyclophosphamide, Epirubicin, Fluorouracil and Filgrastim (G-CSF). Vancouver: BC Cancer Agency; BRAJCEFG, 2005. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Inflammatory Breast Cancer using Cyclophosphamide, Doxorubicin, Fuorouracil and Filgrastim (G-CSF). Vancouver: BC Cancer Agency; BRINFCEFG, 2005. BC Cancer Agency Breast Tumour Group. BCCA Protocol summary for Inflammatory Breast Cancer using Cyclophosphamide, Epirubicin, Fluorouracil and Filgrastim (G-CSF). Vancouver: BC Cancer Agency; BRLACEFG, 2005. BC Cancer Agency Genitourinary Tumour Group. BCCA Protocol summary for Combined Modality Therapy for Squamous Cell Cancer of the Genitourinary System Using Fluorouracil and Cisplatin. Vancouver: BC Cancer Agency; GUFUP, 2005. BC Cancer Agency Head and neck Tumour Group. BCCA Protocol summary for Advanced Head and Neck Cancer using Cisplatin and Fluorouracil. Vancouver: BC Cancer Agency; HNFUP, 2005. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Palliative Chemotherapy for Metastatic Colorectal Cancer using Irinotecan, Fluorouracil and Folinic Acid (Leucovorin). Vancouver: BC Cancer Agency; UGIIRFUFA, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Advanced Colorectal Cancer using Leucovorin and Fluorouracil. Vancouver: BC Cancer Agency; GIFUFA, 2006. BC Cancer Agency Head and neck Tumour Group. BCCA Protocol summary for Combined Chemotherapy (Carboplatin and Fluorouracil) and Radiation Treatment for Locally Advanced Squamous Cell Carcinoma of the Head and Neck. Vancouver: BC Cancer Agency; HNCMT, 2001. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Combined Modality Adjuvant Therapy for Completely Resected Gastric Adenocarcinoma using Fluorouracil and Folinic Acid (Leucovorin) and Radiation Therapy. Vancouver: BC Cancer Agency; GIGAI, 2006. BC Cancer Agency Head and neck Tumour Group. BCCA Protocol summary for Combined Modality therapy for Advanced Head and Neck Cancer using Mitomycin, Fluorouracil and Spit Course Radiation Therapy. Vancouver: BC Cancer Agency; HNFUA, 2005. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Combined Modality Adjuvant Therapy for High Risk Rectal Carcinoma using Fluorouracil, Leucovorin and Radiation Therapy. Vancouver: BC Cancer Agency; GIFUR2, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Combined Modality Adjuvant Therapy for High Risk Rectal Carcinoma using Fluorouracil, Folinic Acid (Leucovorin) and Radiation Therapy. Vancouver: BC Cancer Agency; GIFUR3, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Combined Modality Therapy for Locally Advanced Esophageal Cancer using Cisplatin Infusional Fluororuracil and Radiation Therapy. Vancouver: BC Cancer Agency; GIEFUP, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Pre-Operative Concurrent Chemotherapy and Radiotherapy and Post Operative Chemotherapy for Locally Advanced (Borderline Resectable or Unresectable) Rectal Adenocarcinoma (Interm Version). Vancouver: BC Cancer Agency; GIRLAIFF, 2006. BC Cancer Agency Gastrointestinal Tumour Group. BCCA Protocol summary for Curative Combined Modality Therapy for Carcinoma of the Anal Canal using Mitomycin, Infusional Fluorouracil and Radiation Therapy. Vancouver: BC Cancer Agency; GIFUA, 2005. Aronoff GR, Brier ME, Berns JS, et al. The Renal Drug Book. 2006. Available from http://www.kdp- baptist.louisville.edu/renalbook/expand.asp?ID=1436. Accessed April 20, 2006.

BC Cancer Agency Cancer Drug Manual(c) Page 11 of 11 Fluorouracil Developed: September 1994

Revised: June 2006 Limited revision: May 2007