Fluorouracil 5% Cream 40gm
It is used to treat a precancerous skin problem called actinic keratosis.It is used to treat a type of skin cancer called basal cell carcinoma. Only the 5% strength is for use to treat basal cell carcinoma.
Drug Class
Antineoplastic agent, topical
Pharmacologic Class
Antimetabolite, pyrimidine analog
Pregnancy Category
Category D
FDA Approved
Mar 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Fluorouracil cream is a medication applied to the skin to treat certain types of skin growths, like actinic keratosis (rough, scaly patches caused by sun exposure) and some skin cancers. It works by stopping the growth of abnormal cells. When you use it, the treated skin will likely become red, inflamed, and may even blister or peel. This is a normal part of the treatment process, indicating the medicine is working.
How to Use This Medicine
Using Your Medication Correctly
To use this medication safely and effectively, follow your doctor's instructions and the information provided below.
Apply this medication only to your skin, as directed by your doctor. Do not take it by mouth.
Avoid applying this medication to sensitive areas, including your eyes, eyelids, mouth, or nose, as it may cause irritation or ulcers.
Be careful not to let the medication accumulate in the skin folds around your eyes, nose, or mouth.
If you accidentally get the medication in these areas, rinse them thoroughly with water.
Preparation and Application
1. Wash your hands before and after using the medication, unless your hand is the treated area.
2. Clean the affected area before applying the medication, and make sure it is completely dry.
3. Wait 10 minutes after washing the affected area before applying the medication.
4. Apply a thin layer of the medication to the affected skin and gently rub it in.
Do not cover the treated area with bandages or dressings unless your doctor instructs you to do so.
Avoid applying the medication to cuts, scrapes, eczema, or damaged skin.
Do not apply the medication to healthy skin.
After applying the medication, avoid touching the treated area to someone else's skin.
Storage and Disposal
Store the medication at room temperature, away from freezing temperatures.
Keep the medication in a dry place, avoiding storage in a bathroom.
Store all medications in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, apply it as soon as you remember.
If it is close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not apply two doses at the same time or use extra doses to make up for a missed dose.
To use this medication safely and effectively, follow your doctor's instructions and the information provided below.
Apply this medication only to your skin, as directed by your doctor. Do not take it by mouth.
Avoid applying this medication to sensitive areas, including your eyes, eyelids, mouth, or nose, as it may cause irritation or ulcers.
Be careful not to let the medication accumulate in the skin folds around your eyes, nose, or mouth.
If you accidentally get the medication in these areas, rinse them thoroughly with water.
Preparation and Application
1. Wash your hands before and after using the medication, unless your hand is the treated area.
2. Clean the affected area before applying the medication, and make sure it is completely dry.
3. Wait 10 minutes after washing the affected area before applying the medication.
4. Apply a thin layer of the medication to the affected skin and gently rub it in.
Do not cover the treated area with bandages or dressings unless your doctor instructs you to do so.
Avoid applying the medication to cuts, scrapes, eczema, or damaged skin.
Do not apply the medication to healthy skin.
After applying the medication, avoid touching the treated area to someone else's skin.
Storage and Disposal
Store the medication at room temperature, away from freezing temperatures.
Keep the medication in a dry place, avoiding storage in a bathroom.
Store all medications in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, apply it as soon as you remember.
If it is close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not apply two doses at the same time or use extra doses to make up for a missed dose.
Lifestyle & Tips
- Avoid prolonged exposure to sunlight or artificial UV light (e.g., tanning beds) during and immediately after treatment, as this can worsen skin reactions. Use protective clothing and broad-spectrum sunscreen.
- Apply the cream exactly as directed by your doctor. Do not apply more often or for longer than prescribed.
- Wash hands thoroughly immediately after applying the cream, unless the hands are the treated area.
- Avoid contact with eyes, nose, mouth, and other mucous membranes. If accidental contact occurs, rinse thoroughly with water.
- Do not cover the treated area with occlusive dressings unless specifically instructed by your doctor.
Available Forms & Alternatives
Available Strengths:
- Fluorouracil 2% Solution 10ml
- Fluorouracil 5% Solution 10ml
- Fluorouracil 50mg/ml Inj, 50ml
- Fluorouracil 5% Cream 40gm
- Fluorouracil 2.5gm/50ml Inj, 1 Vial
- Fluorouracil 500mg/10ml Inj, 10ml
- Fluorouracil 1gm/20ml Inj 20ml
- Fluorouracil 2.5gm/50ml Inj, 50ml
- Fluorouracil 0.5% Cream 30gm
- Fluorouracil 1gm/20ml Inj 20ml
- Fluorouracil 2.5gm/50ml Inj, 50ml
- Fluorouracil 5gm/100ml Inj, 100ml
- Fluorouracil 500mg/10ml Inj 10ml
- Fluorouracil 50mg/ml Inj20ml
Dosing & Administration
Adult Dosing
Standard Dose:
Apply a thin layer to the affected area once or twice daily.
Condition-Specific Dosing:
Actinic Keratosis:
Apply to affected area BID for 2-4 weeks. Complete healing may not be evident for 1-2 months after cessation of therapy.
Superficial Basal Cell Carcinoma:
Apply to affected area BID for 3-6 weeks, up to 12 weeks may be required.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment typically needed due to minimal systemic absorption.
Moderate:
No adjustment typically needed due to minimal systemic absorption.
Severe:
No adjustment typically needed due to minimal systemic absorption.
Dialysis:
Not applicable for topical use; systemic exposure is minimal.
Hepatic Impairment:
Mild:
No adjustment typically needed due to minimal systemic absorption.
Moderate:
No adjustment typically needed due to minimal systemic absorption.
Severe:
No adjustment typically needed due to minimal systemic absorption.
Pharmacology
Mechanism of Action
Fluorouracil is a pyrimidine analog that interferes with DNA and RNA synthesis. It is converted intracellularly to active metabolites, including fluorodeoxyuridine monophosphate (FdUMP) and fluorouridine triphosphate (FUTP). FdUMP inhibits thymidylate synthase, thereby blocking the methylation of deoxyuridylic acid to thymidylic acid, which is essential for DNA synthesis. FUTP is incorporated into RNA, leading to the synthesis of fraudulent RNA and interference with protein synthesis. These actions lead to cell death, particularly in rapidly proliferating cells.
Pharmacokinetics
Absorption:
Bioavailability:
<6% (systemic absorption from topical application)
Tmax:
Not well-defined for topical application; systemic levels are typically very low.
FoodEffect:
Not applicable for topical application.
Distribution:
Vd:
Not clinically relevant for topical application; primarily local distribution.
ProteinBinding:
Not clinically relevant for topical application; minimal systemic binding.
CnssPenetration:
Limited (systemic penetration is minimal, CNS penetration from topical is negligible).
Elimination:
HalfLife:
Not clinically relevant for topical application; systemic half-life is short (10-20 minutes) if absorbed.
Clearance:
Rapid systemic clearance if absorbed.
ExcretionRoute:
Metabolites primarily excreted renally.
Unchanged:
<10% (of systemically absorbed drug)
Pharmacodynamics
OnsetOfAction:
Visible inflammatory response typically begins within 3-5 days of treatment.
PeakEffect:
Peak inflammatory response and lesion erosion usually occur within 2-3 weeks.
DurationOfAction:
Therapeutic effect persists throughout the treatment course; complete healing may take 1-2 months after stopping treatment.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Stomach pain
Bloody diarrhea
Vomiting
Severe diarrhea
Changes in eyesight, eye pain, or severe eye irritation
Mouth irritation or mouth sores
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling very tired or weak
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Itching
Changes in skin color
Scarring
Skin reactions at the application site, including:
+ Burning
+ Dryness
+ Irritation
+ Redness
+ Pain
+ Swelling
* Note: Skin reactions are common and may last for 2 weeks or longer after stopping the medication. If a skin reaction bothers you, contact your doctor.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Stomach pain
Bloody diarrhea
Vomiting
Severe diarrhea
Changes in eyesight, eye pain, or severe eye irritation
Mouth irritation or mouth sores
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling very tired or weak
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Itching
Changes in skin color
Scarring
Skin reactions at the application site, including:
+ Burning
+ Dryness
+ Irritation
+ Redness
+ Pain
+ Swelling
* Note: Skin reactions are common and may last for 2 weeks or longer after stopping the medication. If a skin reaction bothers you, contact your doctor.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe pain or burning that is intolerable.
- Excessive blistering or ulceration beyond the treated area.
- Signs of infection, such as pus, spreading redness, warmth, or fever.
- Allergic reactions like rash, hives, swelling of the face/lips/tongue, or difficulty breathing (rare with topical use).
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a condition called dihydropyrimidine dehydrogenase deficiency.
If you are pregnant or think you might be pregnant. Do not take this medication if you are pregnant.
If you are breastfeeding. You should not breastfeed while taking this medication.
If the patient is a child. This medication is not intended for children and should not be given to them.
This medication can interact with other medications and health conditions. Therefore, it is crucial to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your health problems
Your doctor needs this information to determine if it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a condition called dihydropyrimidine dehydrogenase deficiency.
If you are pregnant or think you might be pregnant. Do not take this medication if you are pregnant.
If you are breastfeeding. You should not breastfeed while taking this medication.
If the patient is a child. This medication is not intended for children and should not be given to them.
This medication can interact with other medications and health conditions. Therefore, it is crucial to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your health problems
Your doctor needs this information to determine if it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
When using this drug to treat basal cell carcinoma, it is crucial to use the 5% strength. If you have been prescribed this medication for basal cell carcinoma but do not have the 5% strength, consult your doctor immediately.
If you have a peanut allergy, discuss this with your doctor before starting treatment.
You may not see the full effects of this medication for a few months. Additionally, your skin may appear worse before it starts to improve.
This medication can increase your risk of sunburn. To minimize this risk, avoid exposure to sunlight, sunlamps, and tanning beds. However, if your doctor recommends it, you can apply a moisturizer or sunscreen 2 hours after applying this medication. Always check with your doctor before using any other skin products or medications.
Patients lacking the enzyme dihydropyrimidine dehydrogenase (DPD) are at a higher risk of experiencing severe and potentially life-threatening side effects. These may include mouth irritation or sores, diarrhea, low white blood cell counts, or nerve problems.
This medication can be toxic and even fatal to pets. To ensure their safety, keep the container and treated skin areas out of their reach. Store the medication in a secure location, and dispose of or thoroughly clean any cloths or applicators used to apply the medication. Avoid getting the medication on your clothing, carpet, or furniture. If a pet ingests the medication, comes into contact with the treated area, or shows signs of illness such as vomiting or seizures after exposure, contact your veterinarian immediately.
There is a risk of harm to the unborn baby if you take this medication during pregnancy. If you become pregnant or suspect you may be pregnant while taking this medication, notify your doctor right away.
To prevent pregnancy during treatment with this medication, use effective birth control methods. Your doctor may also advise you to continue using birth control for a period after your last dose. Discuss your birth control options with your doctor to determine the best approach for your situation.
When using this drug to treat basal cell carcinoma, it is crucial to use the 5% strength. If you have been prescribed this medication for basal cell carcinoma but do not have the 5% strength, consult your doctor immediately.
If you have a peanut allergy, discuss this with your doctor before starting treatment.
You may not see the full effects of this medication for a few months. Additionally, your skin may appear worse before it starts to improve.
This medication can increase your risk of sunburn. To minimize this risk, avoid exposure to sunlight, sunlamps, and tanning beds. However, if your doctor recommends it, you can apply a moisturizer or sunscreen 2 hours after applying this medication. Always check with your doctor before using any other skin products or medications.
Patients lacking the enzyme dihydropyrimidine dehydrogenase (DPD) are at a higher risk of experiencing severe and potentially life-threatening side effects. These may include mouth irritation or sores, diarrhea, low white blood cell counts, or nerve problems.
This medication can be toxic and even fatal to pets. To ensure their safety, keep the container and treated skin areas out of their reach. Store the medication in a secure location, and dispose of or thoroughly clean any cloths or applicators used to apply the medication. Avoid getting the medication on your clothing, carpet, or furniture. If a pet ingests the medication, comes into contact with the treated area, or shows signs of illness such as vomiting or seizures after exposure, contact your veterinarian immediately.
There is a risk of harm to the unborn baby if you take this medication during pregnancy. If you become pregnant or suspect you may be pregnant while taking this medication, notify your doctor right away.
To prevent pregnancy during treatment with this medication, use effective birth control methods. Your doctor may also advise you to continue using birth control for a period after your last dose. Discuss your birth control options with your doctor to determine the best approach for your situation.
Overdose Information
Overdose Symptoms:
- Severe local skin reactions (exaggerated erythema, erosion, ulceration, pain).
- Systemic overdose is highly unlikely with topical application due to minimal absorption, but if significant absorption occurred (e.g., large surface area, broken skin), symptoms could include nausea, vomiting, diarrhea, stomatitis, bone marrow suppression (leukopenia, thrombocytopenia, anemia).
What to Do:
For severe local reactions, discontinue use and seek medical attention. For suspected systemic overdose (extremely rare with topical use), discontinue use, monitor vital signs and blood counts, and provide supportive care. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Monitoring
Baseline Monitoring
Diagnosis confirmation (e.g., biopsy for BCC)
Rationale: To ensure appropriate use for indicated conditions.
Timing: Prior to initiation of therapy.
Baseline skin assessment
Rationale: To document the extent and nature of lesions before treatment.
Timing: Prior to initiation of therapy.
Routine Monitoring
Local skin reactions (erythema, erosion, crusting, pain, burning, itching)
Frequency: Daily during treatment, then periodically until healing.
Target: Expected inflammatory response, but not excessive or signs of infection.
Action Threshold: Severe pain, blistering, signs of infection (pus, fever, spreading redness beyond treated area) warrant medical evaluation.
Photosensitivity
Frequency: Daily during treatment.
Target: Avoidance of direct sun exposure.
Action Threshold: Severe sunburn-like reactions in treated areas.
Symptom Monitoring
- Local irritation
- Pain
- Burning sensation
- Itching
- Crusting
- Erosion
- Ulceration
- Photosensitivity
- Hyperpigmentation
- Hypopigmentation
Special Patient Groups
Pregnancy
Fluorouracil is Pregnancy Category D. It can cause fetal harm when administered to a pregnant woman. Avoid use during pregnancy. If the drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
Trimester-Specific Risks:
First Trimester:
Highest risk of teratogenicity due to organogenesis.
Second Trimester:
Potential for fetal toxicity, though risk of major malformations decreases.
Third Trimester:
Potential for fetal toxicity, including growth restriction or bone marrow suppression.
Lactation
Use with caution. It is not known whether fluorouracil is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from fluorouracil, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Potential for serious adverse effects due to its cytotoxic nature, though systemic absorption from topical application is minimal.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use is generally not recommended.
Geriatric Use
No specific dose adjustments are required for geriatric patients. However, elderly patients may have thinner skin or other comorbidities that could affect skin integrity and healing, requiring careful monitoring of local skin reactions.
Clinical Information
Clinical Pearls
- Patients should be informed that the treated area will look worse before it gets better, with expected inflammatory reactions (redness, crusting, erosion, pain). This is a sign the medication is working.
- Treatment duration varies significantly based on the condition and individual response. Patients should complete the full prescribed course even if lesions appear to resolve earlier.
- Apply with a non-metallic applicator, gloved finger, or thoroughly wash hands immediately after application to prevent spread to unintended areas or other individuals.
- Photosensitivity is a common side effect; strict sun avoidance and use of protective measures are crucial.
- Avoid applying to open wounds, mucous membranes, or near the eyes.
- The 5% cream is generally more potent and causes a more intense reaction than lower concentrations (e.g., 0.5% or 1%).
Alternative Therapies
- Imiquimod cream (for actinic keratosis, superficial BCC)
- Ingenol mebutate gel (for actinic keratosis)
- Diclofenac gel (for actinic keratosis)
- Cryotherapy (liquid nitrogen)
- Photodynamic therapy (PDT)
- Surgical excision
- Curettage and electrodessication
- Laser ablation
Cost & Coverage
Average Cost:
Varies widely, typically $100-$500+ per 40gm tube
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (often covered by most insurance plans with a co-pay)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the substance taken, the amount, and the time it occurred.