Fluorouracil

What is Fluorouracil?

• Fluorouracil is a nucleoside metabolic inhibitor used to treat cancers of the breast, colon, rectum, stomach, and pancreas.
• It is used under the brand names Carac, Tolak, Efudex, and Fluoroplex as a cream to treat actinic keratosis (a skin condition that may become cancer).
• It is also used under the brand name Efudex as a cream to treat basal cell skin cancer that is superficial (not invasive) and cannot be treated with other therapy.
• Fluorouracil is being studied in the treatment of other conditions and types of cancer.

Fluorouracil

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What are the uses of this medicine?

Fluorouracil injection (Adrucil)is used for the treatment of:

• Adenocarcinoma of the Colon and Rectum
• Adenocarcinoma of the Breast
• Gastric Adenocarcinoma
• Pancreatic Adenocarcinoma

• Fluorouracil cream and topical solution (Carac, Tolak, Efudex, and Fluoroplex) are used to treat actinic or solar keratoses (scaly or crusted lesions [skin areas] caused by years of too much exposure to sunlight).

• Fluorouracil cream and topical solution (Efudex)are also used to treat a type of skin cancer called superficial basal cell carcinoma if usual types of treatment cannot be used.

How does this medicine work?

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Fluorouracil mechanism

• Fluorouracil (floo" oh ure' a sil) is a fluoropyrimidine that has antineoplastic action against several solid tumors including breast and colon cancers.
• Fluorouracil is believed to block thymidylate synthase and decrease production of thymidylate, a necessary precursor of DNA.
• This action interferes with the synthesis of DNA, RNA and protein and blocks cell division.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who are or may become pregnant during therapy

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• certain chemotherapy medications such as bendamustine (Treanda), busulfan (Myerlan, Busulfex), carmustine (BiCNU, Gliadel Wafer), cyclophosphamide (Cytoxan), chlorambucil (Leukeran), ifosfamide (Ifex), lomustine (CeeNU), melphalan (Alkeran), procarbazine (Mutalane), or temozolomide (Temodar)
• medications that suppress the immune system such as azathioprine (Imuran), cyclosporine (Neoral, Sandimmune), methotrexate (Rheumatrex), sirolimus (Rapamune), and tacrolimus (Prograf).

Is this medicine FDA approved?

• Fluorouracil was approved for use as an anticancer agent in the United States in 1962 and is currently used as an important component of several anticancer drug regimens.
• Fluorouracil is typically combined with leucovorin (folinic acid) which also inhibits thymidylate synthase, thus enhancing the effects of fluorouracil.

How should this medicine be used?

Recommended dosage: Recommended Dosage for Adenocarcinoma of the Colon and Rectum:

• The recommended dose of fluorouracil, administered in an infusional regimen in combination with leucovorin alone, or in combination with leucovorin and oxaliplatin or irinotecan, is 400 mg/m 2 by intravenous bolus on Day 1, followed by 2400 mg/m 2 to 3000 mg/m 2 intravenously as a continuous infusion over 46 hours every two weeks.
• The recommended dose of fluorouracil, if administered in a bolus dosing regimen in combination with leucovorin, is 500 mg/m 2 by intravenous bolus on Days 1, 8, 15, 22, 29, and 36 in 8-week cycles.

Recommended Dosage for Adenocarcinoma of the Breast:

• The recommended dose of fluorouracil, administered as a component of a cyclophosphamide-based multidrug regimen, is 500 mg/m 2 or 600 mg/m 2 intravenously on Days 1 and 8 every 28 days for 6 cycles.

Recommended Dosage for Gastric Adenocarcinoma:

• The recommended dose of fluorouracil, administered as a component of a platinum-containing multidrug chemotherapy regimen, is 200 mg/m 2 to 1000 mg/m 2 intravenously as a continuous infusion over 24 hours.
• The frequency of dosing in each cycle and the length of each cycle will depend on the dose of fluorouracil and the specific regimen administered.

Recommended Dosage for Pancreatic Adenocarcinoma:

• The recommended dose of fluorouracil, administered as an infusional regimen in combination with leucovorin or as a component of a multidrug chemotherapy regimen that includes leucovorin, is 400 mg/m 2 intravenous bolus on Day 1, followed by 2400 mg/m 2 intravenously as a continuous infusion over 46 hours every two weeks.

Administration:

• Fluorouracil injection comes as a solution (liquid) to be given intravenously (into a vein) by a doctor or nurse in a medical facility.
• The length of treatment depends on the types of drugs you are taking, how well your body responds to them, and the type of cancer you have.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• Fluorouracil is available in various sized vials of 50 mg/mL generically and under several brand names including Adrucil and Carac.
• Fluorouracil is also available topically in creams and solutions for therapy of actinic keratoses and basal cell cancers.

This medicine is available in fallowing brand namesː

• Adrucil; Carac; Tolak; Efudex; Fluoroplex

What side effects can this medication cause?

The most common side effects of this medicine include:

• pancytopenia
• gastrointestinal ulceration
• nausea
• vomiting
• anaphylaxis
• generalized allergic reactions
• nystagmus
• headache
• dry skin
• fissuring
• photosensitivity, as manifested by erythema or increased pigmentation of the skin
• vein pigmentation
• lacrimal duct stenosis
• visual changes
• lacrimation
• photophobia
• euphoria
• thrombophlebitis
• epistaxis
• nail changes

What special precautions should I follow?

• Patients with certain homozygous or certain compound heterozygous mutations in the DPD gene that result in complete or near complete absence of Dipyrimidine Dehydrogenase (DPD) activity are at increased risk for acute early-onset of toxicity and severe, life-threatening, or fatal adverse reactions caused by fluorouracil (e.g., mucositis, diarrhea, neutropenia, and neurotoxicity). Withhold or permanently discontinue fluorouracil in patients with evidence of acute early-onset or unusually severe toxicity, which may indicate near complete or total absence of dipyrimidine dehydrogenase (DPD) activity. No fluorouracil dose has been proven safe in patients with absent DPD activity.
• Fluorouracil can cause cardiotoxicity, including angina, myocardial infarction/ischemia, arrhythmia, and heart failure. Withhold fluorouracil for cardiac toxicity.
• Altered mental status, confusion, disorientation, coma, or ataxia with elevated serum ammonia level can occur within 72 hours of initiation of fluorouracil. Withhold fluorouracil and initiate ammonia-lowering therapy.
• Fluorouracil can cause acute cerebellar syndrome, confusion, disorientation, ataxia, or visual disturbances. Withhold fluorouracil for neurologic toxicity.
• Fluorouracil can cause severe diarrhea. Withhold fluorouracil for severe diarrhea until resolved.
• Fluorouracil can cause hand-foot syndrome. If severe, discontinue fluorouracil until resolved or decreased to Grade 1, then resume at a reduced dose.
• Fluorouracil can cause severe and fatal myelosuppression. Withhold fluorouracil until severe myelosuppression resolves, then resume at a reduced dose.
• Fluorouracil can cause severe mucositis. Discontinue fluorouracil until resolved or decreased to Grade 1, then resume at a reduced dose.
• Concurrent administration with warfarin can result in clinically significant increases in coagulation parameters: Closely monitor INR and prothrombin time.
• Fluorouracil can cause fetal harm. Advise females and males of reproductive potential of the potential risk to a fetus.
• Plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Fluorouracil may make your skin sensitive to sunlight.
• Fluorouracil is associated with a low rate of transient serum aminotransferase elevations during therapy and has been implicated in rare cases of clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• nausea
• diarrhea
• vomiting
• fever, chills, sore throat, or other signs of an infection
• unusual bleeding or bruising
• bloody or black, tarry stools
• coughing up or vomiting blood or material that looks like coffee grounds

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Administer uridine triacetate within 96 hours following the end of fluorouracil infusion for management of fluorouracil overdose.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies with fluorouracil in pregnant women.
• Based on its mechanism of action, fluorouracil can cause fetal harm when administered to a pregnant woman.

Can this medicine be used in children?

• The safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredients:

• FLUOROURACIL

Inactive Ingredients:

• WATER
• SODIUM HYDROXIDE

Who manufactures and distributes this medicine?

Manufactured For:

• Accord Healthcare, Inc.,
• Slater Road,
• Suite 210-B, Durham,
• NC, USA.

Manufactured By:

• Intas Pharmaceuticals Limited,
• Ahmedabad , India.

What should I know about storage and disposal of this medication?

• Store at 20°C to 25°C (68°F to 77°F).
• DO NOT FREEZE.
• Protect from light.
• Retain in carton until time of use.
• Fluorouracil is a cytotoxic drug.
• Follow applicable special handling and disposable procedures

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• Dailymed label info on Fluorouracil
• FDA Fluorouracil

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