fluorouracil topical (Rx)

Brand and Other Names:Efudex, Carac, more...Fluoroplex, Tolak
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

cream

  • 0.5% (Carac)
  • 1% (Fluoroplex)
  • 4% (Tolak)
  • 5% (Efudex)

topical solution

  • 2% (Efudex)
  • 5% (Efudex)

Actinic (Solar) Keratoses

Carac: Apply thin film to affected area qDay for 2-4 wk; healing may not be evident for 1-2 months

Efudex (2% solution): Apply sufficient amount to cover lesions q12hr for 2-4 wk; healing may not be evident for 1-2 months

Fluoroplex: Apply sufficient amount to cover lesions q12hr for 2-6 wk

Tolak (face, ears, or scalp): Apply sufficient amount to cover lesions of affected area(s) qDay for 4 weeks

Superficial Basal Cell Carcinoma

Efudex 5%: Apply sufficient amount of cream or solution to cover lesions q12hr for 3-6 wk; may continue application for up to 10-12 weeks

Not recommended

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Adverse Effects

Frequency Not Defined

Pain

Pruritus

Headache

Insomnia

Irritability

Rash

Photosensitivity

Leukocytosis

Thrombocytopenia

Birth defects

Burning

Inflammation

Miscarriage

Herpes simplex

Allergic contact dermatits

Telangectasia

Hyperpigmentation (rare)

Scarring (rare)

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Warnings

Contraindications

Hypersensitivity to any component

Women who are or may become pregnant

Dihydropyrimidine Dehydrogenase (DPD) deficiency

Cautions

Potential for delayed hypersensitivity reaction to fluorouracil

Occlusive dressings may increase inflammatory reaction in adjacent normal skin

Possibility for increased absorption through inflamed or ulcerated skin

Avoid prolonged exposure to sunlight or other UV irradiation

Superficial BCC treatment only when conventional methods are impractical, since conventional methods have better response rate

Application site adverse reactions (erythema, scaling/dryness, edema, crusting, erosions, stinging/burning, and pruritus) are likely to occur during and for 4 weeks after treatment of actinic keratosis on the face, ears, and/or scalp

Do not apply directly into eyes, nose, mouth, or other mucous membranes because irritation, local inflammation and ulceration can occur

Avoid treatment in periocular area; eye disorders, including corneal reactions have occurred with topical fluorouracil use; avoid accidental transfer of drug into eyes and to periocular area; patients should wash hands well after applying the product; if accidental exposure occurs, seek medical care

Cases of miscarriage and birth defects occurred when pregnant women applied the topical form to mucous membranes; furthermore, fluorouracil interferes with synthesis of deoxyribonucleic acid (DNA), inhibits the formation of ribonucleic acid (RNA), and provokes unbalanced growth and death of cells

Dihydropyrimidine Dehydrogenase Deficiency

  • A large percentage of fluorouracil is catabolized by the DPD enzyme; DPD enzyme deficiency may result in increased availability of fluorouracil to the anabolic pathway, which may lead to increased interference with DNA and RNA synthesis and increased cytotoxic activity and potential toxicities
  • Life-threatening systemic toxicity reported with topical use of fluorouracil in a patient with DPD deficiency; patients should discontinue therapy if symptoms of fluorouracil’s systemic toxicity develop
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Pregnancy & Lactation

Pregnancy

Cases of miscarriage and birth defects (including cleft lip and cleft palate) have been reported when pregnant women were exposed to a topical or parenteral form of the drug; in addition, ventricular septal defect and cases of miscarriage occurred when pregnant women applied a topical fluorouracil product to mucous membranes

Animal data

  • Animal reproduction studies have shown fluorouracil to be teratogenic in mice, rats, and hamsters when given at doses equivalent to the usual human intravenous dose

Lactation

Because many drugs are excreted in human milk and there is some systemic absorption of fluorouracil after topical administration, and because of potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue drug use, taking into account the importance of the drug to the mother

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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Pharmacology

Mechanism of Action

Interferes with synthesis of DNA & to a lesser extent, RNA

Pharmacokinetics

Absorption: Insignificant (~6%)

Time to peak: 1 hr

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Administration

Topical Administration

Apply q12hr with nonmetallic applicator, gloved hands or fingertips

If fingertips used, wash hands immediately afterwards

Solution considered more effective than cream for equivalent strength

Complete healing of lesions typically not evident for 1-2 months

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Images

BRAND FORM. UNIT PRICE PILL IMAGE
fluorouracil intravenous
-
500 mg/10 mL vial
fluorouracil intravenous
-
1 gram/20 mL vial
fluorouracil intravenous
-
1 gram/20 mL vial
fluorouracil intravenous
-
5 gram/100 mL vial
fluorouracil intravenous
-
500 mg/10 mL vial
fluorouracil intravenous
-
500 mg/10 mL vial
fluorouracil intravenous
-
5 gram/100 mL vial
fluorouracil intravenous
-
2.5 gram/50 mL vial
fluorouracil intravenous
-
5 gram/100 mL vial
fluorouracil intravenous
-
2.5 gram/50 mL vial
fluorouracil intravenous
-
2.5 gram/50 mL vial
Adrucil intravenous
-
5 gram/100 mL vial
Adrucil intravenous
-
500 mg/10 mL vial
Adrucil intravenous
-
2.5 gram/50 mL vial
fluorouracil topical
-
0.5 % cream
fluorouracil topical
-
5 % cream
fluorouracil topical
-
5 % cream
fluorouracil topical
-
5 % solution
fluorouracil topical
-
2 % solution
fluorouracil topical
-
5 % cream
fluorouracil topical
-
5 % cream
Carac topical
-
0.5 % cream
Efudex topical
-
5 % cream
Fluoroplex topical
-
1 % cream

Copyright © 2010 First DataBank, Inc.

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Patient Handout

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Patient Education
fluorouracil intravenous

FLUOROURACIL - INJECTION

(flewr-oh-YOUR-uh-sill)

COMMON BRAND NAME(S): Adrucil

USES: Fluorouracil is used to treat various types of cancer. It is a chemotherapy drug that is used to slow or stop cancer cell growth.You should be tested for a DPD enzyme deficiency before you start treatment with fluorouracil. Ask your doctor for more details.

HOW TO USE: This medication is usually given by injection into a vein by a health care professional. It may also be given by other methods of injection depending upon your medical condition. The dosage is based on your medical condition, body size, and response to therapy.

SIDE EFFECTS: Nausea, vomiting, loss of appetite, dry/itchy skin, or skin darkening may occur. Nausea and vomiting can be severe. In some cases, drug therapy may be necessary to prevent or relieve nausea and vomiting. Not eating before your treatment may help relieve vomiting. Changes in diet such as eating several small meals or limiting activity may help lessen some of these effects. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.Mild diarrhea is also a common side effect. However, diarrhea can rarely become persistent or severe, causing very serious problems due to dehydration. Tell your doctor right away if you develop: persistent/severe diarrhea, abdominal or stomach pain/cramping, or blood/mucus in your stool.Temporary hair loss may occur. Normal hair growth should return after treatment has ended.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Hand and foot problems sometimes occur with fluorouracil use. You can prevent or reduce these problems by protecting your hands and feet from a great deal of heat or pressure. For example, avoid taking hot baths/showers, handwashing dishes with hot water, taking long walks, and rubbing your hands/feet. Tell your doctor right away if you develop the following symptoms on your hands/feet: redness, peeling skin, blisters, pain, numbness, tingling, or swelling. If you develop these symptoms, consult your doctor for treatment options (e.g., reducing your dose or stopping fluorouracil therapy, applying ice packs to the hands/feet).Tell your doctor right away if you have any serious side effects, including: headache, mental/mood changes (e.g., confusion), vision changes, unusual eye movements, loss of coordination, unusual tiredness.Get medical help right away if any of these rare but very serious side effects occur: easy bruising/bleeding, blood in the urine, black/bloody stools, vomit that looks like coffee grounds, stomach/abdominal pain, chest pain, jaw/left arm pain, fast/slow/irregular heartbeat, mouth sores, sore throat, painful swallowing, heartburn, pain/redness/swelling of the arms/legs.This medication can lower the body's ability to fight an infection. Notify your doctor promptly if you develop any signs of an infection such as fever, chills or persistent sore throat.A very serious allergic reaction to this drug is unlikely, but get medical help right away if it occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.Fluorouracil can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Get medical help right away if you develop a rash.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using fluorouracil, tell your doctor or pharmacist if you are allergic to it; or to flucytosine; or to capecitabine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: poor nutrition, decreased bone marrow function/blood cell disorders (e.g., anemia, leukopenia, thrombocytopenia), a certain enzyme deficiency (dihydropyrimidine dehydrogenase - DPD), a serious infection, liver problems, kidney problems.Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine.Use caution with sharp objects like safety razors or nail cutters and avoid activities such as contact sports to lower the chance of getting cut, bruised or injured.Wash your hands well to prevent the spread of infections.This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Tell your doctor right away if you get sunburned or have skin blisters/redness.This medication is not recommended for use during pregnancy. It may cause harm to an unborn baby. Women of childbearing age and men should use reliable form(s) of birth control during therapy and for some time afterwards. Consult your doctor for more details.It is not known whether this drug passes into breast milk. Because of the potential risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.A product that may interact with this drug is: warfarin.Fluorouracil is very similar to flucytosine and capecitabine. Do not use medications containing flucytosine or capecitabine while using fluorouracil.

OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Laboratory and/or medical tests (e.g., complete blood counts) should be performed to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule.

STORAGE: Consult the product instructions and your pharmacist for storage details. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.